Opher Gileadi

2024

Characterization of covalent inhibitors that disrupt the interaction between the tandem SH2 domains of SYK and FCER1G phospho-ITAM.

Bashore FM, Katis VL, Du Y, Sikdar A, Wang D, Bradshaw WJ, Rygiel KA, Leisner TM, Chalk R, Mishra S, Williams CA, Gileadi O, Brennan PE, Wiley JC, Gockley J, Cary GA, Carter GW, Young JE, Pearce KH, Fu H, Axtman AD
PLoS One. 13.04.2024 19(2):e0293548. doi: 10.1371/journal.pone.0293548
PMID: 38359047

2023

Open science discovery of potent noncovalent SARS-CoV-2 main protease inhibitors.

Boby ML, Fearon D, Ferla M, Filep M, Koekemoer L, Robinson MC, Chodera JD, Lee AA, London N, von Delft A, von Delft F, Achdout H, Aimon A, Alonzi DS, Arbon R, Aschenbrenner JC, Balcomb BH, Bar-David E, Barr H, Ben-Shmuel A, Bennett J, Bilenko VA, Borden B, Boulet P, Bowman GR, Brewitz L, Brun J, Bvnbs S, Calmiano M, Carbery A, Carney DW, Cattermole E, Chang E, Chernyshenko E, Clyde A, Coffland JE, Cohen G, Cole JC, Contini A, Cox L, Croll TI, Cvitkovic M, De Jonghe S, Dias A, Donckers K, Dotson DL, Douangamath A, Duberstein S, Dudgeon T, Dunnett LE, Eastman P, Erez N, Eyermann CJ, Fairhead M, Fate G, Fedorov O, Fernandes RS, Ferrins L, Foster R, Foster H, Fraisse L, Gabizon R, García-Sastre A, Gawriljuk VO, Gehrtz P, Gileadi C, Giroud C, Glass WG, Glen RC, Glinert I, Godoy AS, Gorichko M, Gorrie-Stone T, Griffen EJ, Haneef A, Hassell Hart S, Heer J, Henry M, Hill M, Horrell S, Huang QYJ, Huliak VD, Hurley MFD, Israely T, Jajack A, Jansen J, Jnoff E, Jochmans D, John T, Kaminow B, Kang L, Kantsadi AL, Kenny PW, Kiappes JL, Kinakh SO, Kovar B, Krojer T, La VNT, Laghnimi-Hahn S, Lefker BA, Levy H, Lithgo RM, Logvinenko IG, Lukacik P, Macdonald HB, MacLean EM, Makower LL, Malla TR, Marples PG, Matviiuk T, McCorkindale W, McGovern BL, Melamed S, Melnykov KP, Michurin O, Miesen P, Mikolajek H, Milne BF, Minh D, Morris A, Morris GM, Morwitzer MJ, Moustakas D, Mowbray CE, Nakamura AM, Neto JB, Neyts J, Nguyen L, Noske GD, Oleinikovas V, Oliva G, Overheul GJ, Owen CD, Pai R, Pan J, Paran N, Payne AM, Perry B, Pingle M, Pinjari J, Politi B, Powell A, Pšenák V, Pulido I, Puni R, Rangel VL, Reddi RN, Rees P, Reid SP, Reid L, Resnick E, Ripka EG, Robinson RP, Rodriguez-Guerra J, Rosales R, Rufa DA, Saar K, Saikatendu KS, Salah E, Schaller D, Scheen J, Schiffer CA, Schofield CJ, Shafeev M, Shaikh A, Shaqra AM, Shi J, Shurrush K, Singh S, Sittner A, Sjö P, Skyner R, Smalley A, Smeets B, Smilova MD, Solmesky LJ, Spencer J, Strain-Damerell C, Swamy V, Tamir H, Taylor JC, Tennant RE, Thompson W, Thompson A, Tomásio S, Tomlinson CWE, Tsurupa IS, Tumber A, Vakonakis I, van Rij RP, Vangeel L, Varghese FS, Vaschetto M, Vitner EB, Voelz V, Volkamer A, Walsh MA, Ward W, Weatherall C, Weiss S, White KM, Wild CF, Witt KD, Wittmann M, Wright N, Yahalom-Ronen Y, Yilmaz NK, Zaidmann D, Zhang I, Zidane H, Zitzmann N, Zvornicanin SN
Science. 10.11.2023 382(6671):eabo7201. doi: 10.1126/science.abo7201
PMID: 37943932

Discovery of FERM domain protein-protein interaction inhibitors for MSN and CD44 as a potential therapeutic approach for Alzheimer's disease.

Du Y, Bradshaw WJ, Leisner TM, Annor-Gyamfi JK, Qian K, Bashore FM, Sikdar A, Nwogbo FO, Ivanov AA, Frye SV, Gileadi O, Brennan PE, Levey AI, Axtman AD, Pearce KH, Fu H, Katis VL
J Biol Chem. 20.10.2023 105382. doi: 10.1016/j.jbc.2023.105382
PMID: 37866628

Open drug discovery in Alzheimer's disease.

Axtman AD, Brennan PE, Frappier-Brinton T, Betarbet R, Carter GW, Fu H, Gileadi O, Greenwood AK, Leal K, Longo FM, Mangravite LM, Edwards AM, Levey AI
Alzheimers Dement (N Y). 22.05.2023 9(2):e12394. doi: 10.1002/trc2.12394
PMID: 37215505

2021

FOXN1 forms higher-order nuclear condensates displaced by mutations causing immunodeficiency.

Rota IA, Handel AE, Maio S, Klein F, Dhalla F, Deadman ME, Cheuk S, Newman JA, Michaels YS, Zuklys S, Prevot N, Hublitz P, Charles PD, Gkazi AS, Adamopoulou E, Qasim W, Davies EG, Hanson I, Pagnamenta AT, Camps C, Dreau HM, White A, James K, Fischer R, Gileadi O, Taylor JC, Fulga T, Lagerholm BC, Anderson G, Sezgin E, Holländer GA
Sci Adv. 03.12.2021 7(49):eabj9247. doi: 10.1126/sciadv.abj9247
PMID: 34860543

Structure, mechanism and crystallographic fragment screening of the SARS-CoV-2 NSP13 helicase.

Newman JA, Douangamath A, Yadzani S, Yosaatmadja Y, Aimon A, Brandão-Neto J, Dunnett L, Gorrie-Stone T, Skyner R, Fearon D, Schapira M, von Delft F, Gileadi O
Nat Commun. 11.08.2021 12(1):4848. doi: 10.1038/s41467-021-25166-6
PMID: 34381037

2020

Structure of the helicase core of Werner helicase, a key target in microsatellite instability cancers.

Newman JA, Gavard AE, Lieb S, Ravichandran MC, Hauer K, Werni P, Geist L, Böttcher J, Engen JR, Rumpel K, Samwer M, Petronczki M, Gileadi O
Life Sci Alliance. 18.11.2020 4(1):. doi: 10.26508/lsa.202000795
PMID: 33199508

Screening and Production of Recombinant Human Proteins: Protein Production in Insect Cells.

Mahajan P, Strain-Damerell C, Mukhopadhyay S, Fernandez-Cid A, Gileadi O, Burgess-Brown NA
Methods Mol Biol. 31.10.2020 2199:67-94. doi: 10.1007/978-1-0716-0892-0_5
PMID: 33125645

Screening and Production of Recombinant Human Proteins: Protein Production in E. coli.

Burgess-Brown NA, Mahajan P, Strain-Damerell C, Fernandez-Cid A, Gileadi O, Gräslund S
Methods Mol Biol. 31.10.2020 2199:45-66. doi: 10.1007/978-1-0716-0892-0_4
PMID: 33125644

Screening and Production of Recombinant Human Proteins: Ligation-Independent Cloning.

Strain-Damerell C, Mahajan P, Fernandez-Cid A, Gileadi O, Burgess-Brown NA
Methods Mol Biol. 31.10.2020 2199:23-43. doi: 10.1007/978-1-0716-0892-0_3
PMID: 33125643

RecQ helicases in DNA repair and cancer targets.

Newman JA, Gileadi O
Essays Biochem. 26.10.2020 64(5):819-830. doi: 10.1042/EBC20200012
PMID: 33095241

The SNM1A DNA repair nuclease.

Baddock HT, Yosaatmadja Y, Newman JA, Schofield CJ, Gileadi O, McHugh PJ
DNA Repair (Amst.). 31.07.2020 95:102941. doi: 10.1016/j.dnarep.2020.102941
PMID: 32866775

STAG1 vulnerabilities for exploiting cohesin synthetic lethality in STAG2-deficient cancers

van der Lelij P, Newman JA, Lieb S, Jude J, Katis V, Hoffmann T, Hinterndorfer M, Bader G, Kraut N, Pearson MA, Peters JM, Zuber J, Gileadi O, Petronczki M
Life science alliance. 30.06.2020 3:-. doi: 10.26508/lsa.202000725
PMID: 32467316

STAG1 vulnerabilities for exploiting cohesin synthetic lethality in STAG2-deficient cancers.

van der Lelij P, Newman JA, Lieb S, Jude J, Katis V, Hoffmann T, Hinterndorfer M, Bader G, Kraut N, Pearson MA, Peters JM, Zuber J, Gileadi O, Petronczki M
Life Sci Alliance. 30.05.2020 3(7):. doi: 10.26508/lsa.202000725
PMID: 32467316

SGC-AAK1-1: A Chemical Probe Targeting AAK1 and BMP2K.

Wells C, Couñago RM, Limas JC, Almeida TL, Cook JG, Drewry DH, Elkins JM, Gileadi O, Kapadia NR, Lorente-Macias A, Pickett JE, Riemen A, Ruela-de-Sousa RR, Willson TM, Zhang C, Zuercher WJ, Zutshi R, Axtman AD
ACS Med Chem Lett. 12.03.2020 11(3):340-345. doi: 10.1021/acsmedchemlett.9b00399
PMID: 32184967

2019

The crystal structure of human forkhead box N1 in complex with DNA reveals the structural basis for forkhead box family specificity.

Newman JA, Aitkenhead H, Gavard AE, Rota IA, Handel AE, Hollander GA, Gileadi O
J. Biol. Chem.. 30.12.2019 . doi: 10.1074/jbc.RA119.010365
PMID: 31914405

Binding and structural analyses of potent inhibitors of the human Ca2+/calmodulin dependent protein kinase kinase 2 (CAMKK2) identified from a collection of commercially-available kinase inhibitors.

Profeta GS, Dos Reis CV, Santiago ADS, Godoi PHC, Fala AM, Wells CI, Sartori R, Salmazo APT, Ramos PZ, Massirer KB, Elkins JM, Drewry DH, Gileadi O, Couñago RM
Sci Rep. 11.11.2019 9(1):16452. doi: 10.1038/s41598-019-52795-1
PMID: 31712618

Binding and structural analyses of potent inhibitors of the human Ca<sup>2+</sup>/calmodulin dependent protein kinase kinase 2 (CAMKK2) identified from a collection of commercially-available kinase inhibitors

Profeta GS, Dos Reis CV, Santiago ADS, Godoi PHC, Fala AM, Wells CI, Sartori R, Salmazo APT, Ramos PZ, Massirer KB, Elkins JM, Drewry DH, Gileadi O, Couñago RM
Scientific reports. 11.11.2019 9:16452-. doi: 10.1038/s41598-019-52795-1
PMID: 31712618

SGC-AAK1-1: A Chemical Probe Targeting AAK1 and BMP2K

Wells C, Couñago RM, Limas JC, Almeida TL, Cook JG, Drewry DH, Elkins JM, Gileadi O, Kapadia NR, Lorente-Macias A, Pickett JE, Riemen A, Ruela-De-Sousa RR, Willson TM, Zhang C, Zuercher WJ, Zutshi R, Axtman AD
ACS Medicinal Chemistry Letters. 29.10.2019 . doi: 10.1021/acsmedchemlett.9b00399
PMID:

The C-Terminal Domains SnRK2 Box and ABA Box Have a Role in Sugarcane SnRK2s Auto-Activation and Activity.

Righetto GL, Sriranganadane D, Halabelian L, Chiodi CG, Elkins JM, Massirer KB, Gileadi O, Menossi M, Couñago RM
Front Plant Sci. 18.10.2019 10:1105. doi: 10.3389/fpls.2019.01105
PMID: 31620147

Implementation of an antibody characterization procedure and application to the major ALS/FTD disease gene C9ORF72.

Laflamme C, McKeever PM, Kumar R, Schwartz J, Kolahdouzan M, Chen CX, You Z, Benaliouad F, Gileadi O, McBride HM, Durcan TM, Edwards AM, Healy LM, Robertson J, McPherson PS
Elife. 15.10.2019 8:. doi: 10.7554/eLife.48363
PMID: 31612854

A Chemical Probe for Tudor Domain Protein Spindlin1 to Investigate Chromatin Function.

Fagan V, Johansson C, Gileadi C, Monteiro O, Dunford JE, Nibhani R, Philpott M, Malzahn J, Wells G, Farham R, Cribbs A, Halidi N, Li F, Chau I, Greschik H, Velupillai S, Allali-Hassani A, Bennett JM, Christott T, Giroud C, Lewis AM, Huber KVM, Athanasou N, Bountra C, Jung M, Schüle R, Vedadi M, Arrowsmith CH, Xiong Y, Jin J, Fedorov O, Farnie G, Brennan PE, Oppermann UCT
J. Med. Chem.. 24.09.2019 . doi: 10.1021/acs.jmedchem.9b00562
PMID: 31550156

A Chemical Probe for Tudor Domain Protein Spindlin1 to Investigate Chromatin Function

Fagan V, Johansson C, Gileadi C, Monteiro O, Dunford JE, Nibhani R, Philpott M, Malzahn J, Wells G, Farham R, Cribbs A, Halidi N, Li F, Chau I, Greschik H, Velupillai S, Allali-Hassani A, Bennett JM, Christott T, Giroud C, Lewis AM, Huber KVM, Athanasou N, Bountra C, Jung M, Schüle R, Vedadi M, Arrowsmith CH, Xiong Y, Jin J, Fedorov O, Farnie G, Brennan PE, Oppermann UCT
Journal of Medicinal Chemistry. 23.09.2019 62:9008-9025. doi: 10.1021/acs.jmedchem.9b00562
PMID: 31550156

The C-Terminal Domains SnRK2 Box and ABA Box Have a Role in Sugarcane SnRK2s Auto-Activation and Activity

Righetto GL, Sriranganadane D, Halabelian L, Chiodi CG, Elkins JM, Massirer KB, Gileadi O, Menossi M, Couñago RM
Frontiers in Plant Science. 16.09.2019 10:1105-. doi: 10.3389/fpls.2019.01105
PMID: 31620147

Development of Pyridine-based Inhibitors for the Human Vaccinia-related Kinases 1 and 2.

Serafim RAM, de Souza Gama FH, Dutra LA, Dos Reis CV, Vasconcelos SNS, da Silva Santiago A, Takarada JE, Di Pillo F, Azevedo H, Mascarello A, Elkins JM, Massirer KB, Gileadi O, Guimarães CRW, Couñago RM
ACS Med Chem Lett. 12.09.2019 10(9):1266-1271. doi: 10.1021/acsmedchemlett.9b00082
PMID: 31531195

Development of Pyridine-based Inhibitors for the Human Vaccinia-related Kinases 1 and 2

Serafim RAM, De Souza Gama FH, Dutra LA, Dos Reis CV, Vasconcelos SNS, Da Silva Santiago A, Takarada JE, Di Pillo F, Azevedo H, Mascarello A, Elkins JM, Massirer KB, Gileadi O, Guimarães CRW, Couñago RM
ACS Medicinal Chemistry Letters. 12.09.2019 10:1266-1271. doi: 10.1021/acsmedchemlett.9b00082
PMID: 31531195

A Chemical Probe Targeting AAK1 and BMP2K

Wells C, Counago R, Limas J, Almeida T, Cook J, Drewry D, Elkins J, Gileadi O, Kapadia N, Lorente-Macías Á, Pickett J, Riemen A, R. Ruela-de-Sousa R, Willson T, Zhang C, Zuercher W, Zutshi R, Axtman A
. 03.09.2019 . doi: 10.26434/chemrxiv.9756785.v1
PMID:

A Ubiquitin-Binding Domain that Binds a Structural Fold Distinct from that of Ubiquitin

Lim M, Newman JA, Williams HL, Masino L, Aitkenhead H, Gravard AE, Gileadi O, Svejstrup JQ
Structure. 06.08.2019 27:1316-1325.e6. doi: 10.1016/j.str.2019.05.003
PMID: 31204252

Streamlining the production of proteins for structural biology.

Owens RJ, Gileadi O
Biophys Rev. 27.06.2019 . doi: 10.1007/s12551-019-00565-8
PMID: 31250316

Streamlining the production of proteins for structural biology

Owens RJ, Gileadi O
Biophysical Reviews. 27.06.2019 11:533-534. doi: 10.1007/s12551-019-00565-8
PMID: 31250316

Insights into the full-length SRPK2 structure and its hydrodynamic behavior.

de Almeida Alves Barbosa É, Seraphim TV, Gandin CA, Teixeira LF, da Silva RAG, Righetto GL, Goncalves KA, de Souza Vasconcellos R, de Almeida Lamêgo MR, Júnior AS, Fietto JLR, Kobarg J, Gileadi C, Massirer KB, Borges JC, de Oliveira Neto M, Bressan GC
Int. J. Biol. Macromol.. 20.06.2019 . doi: 10.1016/j.ijbiomac.2019.06.135
PMID: 31229549

A Ubiquitin-Binding Domain that Binds a Structural Fold Distinct from that of Ubiquitin.

Lim M, Newman JA, Williams HL, Masino L, Aitkenhead H, Gravard AE, Gileadi O, Svejstrup JQ
Structure. 28.05.2019 . doi: 10.1016/j.str.2019.05.003
PMID: 31204252

Role of protein structure in variant annotation: structural insight of mutations causing 6-pyruvoyl-tetrahydropterin synthase deficiency

Muniz JRC, Szeto NW-S, Frise R, Lee WH, Wang X-S, Thöny B, Himmelreich N, Blau N, Hsiao K-J, Liu T-T, Gileadi O, Oppermann U, Von Delft F, Yue WW, Tang NL-S
Pathology. 01.04.2019 51:274-280. doi: 10.1016/j.pathol.2018.11.011
PMID: 30853107

Role of protein structure in variant annotation: structural insight of mutations causing 6-pyruvoyl-tetrahydropterin synthase deficiency.

Muniz JRC, Szeto NW, Frise R, Lee WH, Wang XS, Thöny B, Himmelreich N, Blau N, Hsiao KJ, Liu TT, Gileadi O, Oppermann U, Von Delft F, Yue WW, Tang NL
Pathology. 07.03.2019 . doi: 10.1016/j.pathol.2018.11.011
PMID: 30853107

WNT Activates the AAK1 Kinase to Promote Clathrin-Mediated Endocytosis of LRP6 and Establish a Negative Feedback Loop.

Agajanian MJ, Walker MP, Axtman AD, Ruela-de-Sousa RR, Serafin DS, Rabinowitz AD, Graham DM, Ryan MB, Tamir T, Nakamichi Y, Gammons MV, Bennett JM, Couñago RM, Drewry DH, Elkins JM, Gileadi C, Gileadi O, Godoi PH, Kapadia N, Müller S, Santiago AS, Sorrell FJ, Wells CI, Fedorov O, Willson TM, Zuercher WJ, Major MB
Cell Rep. 02.01.2019 26(1):79-93.e8. doi: 10.1016/j.celrep.2018.12.023
PMID: 30605688

2018

Discovery of a Selective Inhibitor for the YEATS Domains of ENL/AF9.

Christott T, Bennett J, Coxon C, Monteiro O, Giroud C, Beke V, Felce SL, Gamble V, Gileadi C, Poda G, Al-Awar R, Farnie G, Fedorov O
SLAS Discov. 25.10.2018 2472555218809904. doi: 10.1177/2472555218809904
PMID: 30359161

Discovery of an MLLT1/3 YEATS Domain Chemical Probe.

Moustakim M, Christott T, Monteiro OP, Bennett J, Giroud C, Ward J, Rogers CM, Smith P, Panagakou I, Saez LD, Felce SL, Gamble V, Gileadi C, Halidi N, Heidenreich D, Chaikuad A, Knapp S, Huber KVM, Farnie G, Heer J, Manevski N, Poda G, Al-Awar R, Dixon DJ, Fedorov O, Brennan P
Angew. Chem. Int. Ed. Engl.. 05.10.2018 . doi: 10.1002/anie.201810617
PMID: 30288907

Structural Analysis of Inhibitor Binding to CAMKK1 Identifies Features Necessary for Design of Specific Inhibitors.

Santiago ADS, Couñago RM, Ramos PZ, Godoi PHC, Massirer KB, Gileadi O, Elkins JM
Sci Rep. 04.10.2018 8(1):14800. doi: 10.1038/s41598-018-33043-4
PMID: 30287839

Structural Analysis of Inhibitor Binding to CAMKK1 Identifies Features Necessary for Design of Specific Inhibitors

Santiago, ADS; Couñago, R; Zonzini Ramos, P; Godoi, PHC; Massirer, KB; Gileadi, O; Elkins, J;
Scientific Reports. 4.10.2018 :-. doi: 10.1101/292797
PMID: 30287839

The structural basis for forkhead box family specificity revealed by the crystal structure of human FOXN1 in complex with DNA

Newman, J; Aitkenhead, H; Gavard, A; Rota, I; Handel, A; Hollander, G; Gileadi, O;
. 26.9.2018 :-. doi: 10.1101/428011
PMID:

Structural Analysis of Inhibitor Binding to CAMKK1 Identifies Features Necessary for Design of Specific Inhibitors

Santiago, ADS; Couñago, R; Zonzini Ramos, P; Godoi, PHC; Massirer, KB; Gileadi, O; Elkins, J;
. 31.3.2018 :-. doi: 10.1101/292797
PMID:

Tryptophan-Mediated Interactions between Tristetraprolin and the CNOT9 Subunit Are Required for CCR4-NOT Deadenylase Complex Recruitment.

Bulbrook, D; Brazier, H; Mahajan, P; Kliszczak, M; Fedorov, O; Marchese, FP; Aubareda, A; Chalk, R; Picaud, S; Strain-Damerell, C; Filippakopoulos, P; Gileadi, O; Clark, AR; Yue, WW; Burgess-Brown, NA; Dean, JLE;
Journal of Molecular Biology. 01.3.2018 430:722-736. doi: 10.1016/j.jmb.2017.12.018
PMID: 29291391

2017

The SGC beyond structural genomics: redefining the role of 3D structures by coupling genomic stratification with fragment-based discovery.

Bradley AR, Echalier A, Fairhead M, Strain-Damerell C, Brennan P, Bullock AN, Burgess-Brown NA, Carpenter EP, Gileadi O, Marsden BD, Lee WH, Yue W, Bountra C, von Delft F
Essays Biochem.. 08.11.2017 61(5):495-503. doi: 10.1042/EBC20170051
PMID: 29118096

Structural characterization of human Vaccinia-Related Kinases (VRK) bound to small-molecule inhibitors identifies different P-loop conformations.

Couñago RM, Allerston CK, Savitsky P, Azevedo H, Godoi PH, Wells CI, Mascarello A, de Souza Gama FH, Massirer KB, Zuercher WJ, Guimarães CRW, Gileadi O
Sci Rep. 08.08.2017 7(1):7501. doi: 10.1038/s41598-017-07755-y
PMID: 28790404

Progress towards a public chemogenomic set for protein kinases and a call for contributions.

Drewry DH, Wells CI, Andrews DM, Angell R, Al-Ali H, Axtman AD, Capuzzi SJ, Elkins JM, Ettmayer P, Frederiksen M, Gileadi O, Gray N, Hooper A, Knapp S, Laufer S, Luecking U, Michaelides M, Müller S, Muratov E, Denny RA, Saikatendu KS, Treiber DK, Zuercher WJ, Willson TM
PLoS ONE. 03.08.2017 12(8):e0181585. doi: 10.1371/journal.pone.0181585
PMID: 28767711

Structural Characterization of Maize SIRK1 Kinase Domain Reveals an Unusual Architecture of the Activation Segment.

Aquino B, Couñago RM, Verza N, Ferreira LM, Massirer KB, Gileadi O, Arruda P
Front Plant Sci. 13.06.2017 8:852. doi: 10.3389/fpls.2017.00852
PMID: 28603531

Recombinant Protein Expression in E. coli : A Historical Perspective.

Gileadi O
Methods Mol. Biol.. 05.05.2017 1586:3-10. doi: 10.1007/978-1-4939-6887-9_1
PMID: 28470595

Virtual fragment screening and linking discovers Jumonji histone demethylase inhibitors

Korczynska, M; Le, D; Siklos, M; Younger, N; Gregori-Puigjane, E; Tumber, A; Krojer, T; Velupillai, S; Gileadi, C; Nowak, R; Iwasa, E; Pollock, S; Torres, IO; Oppermann, U; Shoichet, B; Fujimori, D;
ACS National Meeting Book of Abstracts. 2.4.2017 253:-. doi:
PMID:

Conformational Plasticity of the MAGE-A3 Protein as a Therapeutic Strategy in Multiple Myeloma

Osman, R; Cho, HJ; Gileadi, O;
Biophysical Journal. 3.2.2017 112:340A-340A. doi: 10.1016/j.bpj.2016.11.1840
PMID:

Insights into the RecQ helicase mechanism revealed by the structure of the helicase domain of human RECQL5.

Newman JA, Aitkenhead H, Savitsky P, Gileadi O
Nucleic Acids Res.. 18.01.2017 . doi: 10.1093/nar/gkw1362
PMID: 28100692

2016

Metalloprotease SPRTN/DVC1 Orchestrates Replication-Coupled DNA-Protein Crosslink Repair.

Vaz B, Popovic M, Newman JA, Fielden J, Aitkenhead H, Halder S, Singh AN, Vendrell I, Fischer R, Torrecilla I, Drobnitzky N, Freire R, Amor DJ, Lockhart PJ, Kessler BM, McKenna GW, Gileadi O, Ramadan K
Mol. Cell. 17.11.2016 64(4):704-719. doi: 10.1016/j.molcel.2016.09.032
PMID: 27871366

Structural analysis of human KDM5B guides histone demethylase inhibitor development.

Johansson C, Velupillai S, Tumber A, Szykowska A, Hookway ES, Nowak RP, Strain-Damerell C, Gileadi C, Philpott M, Burgess-Brown N, Wu N, Kopec J, Nuzzi A, Steuber H, Egner U, Badock V, Munro S, LaThangue NB, Westaway S, Brown J, Athanasou N, Prinjha R, Brennan PE, Oppermann U
Nat. Chem. Biol.. 23.05.2016 . doi: 10.1038/nchembio.2087
PMID: 27214403

Structural analysis of human KDM5B guides histone demethylase inhibitor development

Johansson, C; Velupillai, S; Tumber, A; Szykowska, A; Hookway, ES; Nowak, RP; Strain-Damerell, C; Gileadi, C; Philpott, M; Burgess-Brown, N; Wu, N; Kopec, J; Nuzzi, A; Steuber, H; Egner, U; Badock, V; Munro, S; LaThangue, NB; Westaway, S; Brown, J; Athanasou, N; Prinjha, R; Brennan, PE; Oppermann, U;
Nature Chemical Biology. 01.7.2016 12:539-545. doi: 10.1038/nchembio.2087
PMID: 27214403

Cephalosporins inhibit human metallo β-lactamase fold DNA repair nucleases SNM1A and SNM1B/apollo.

Lee SY, Brem J, Pettinati I, Claridge TD, Gileadi O, Schofield CJ, McHugh PJ
Chem. Commun. (Camb.). 28.04.2016 . doi: 10.1039/c6cc00529b
PMID: 27121860

Structures of Two Melanoma-Associated Antigens Suggest Allosteric Regulation of Effector Binding.

Newman JA, Cooper CD, Roos AK, Aitkenhead H, Oppermann UC, Cho HJ, Osman R, Gileadi O
PLoS ONE. 24.02.2016 11(2):e0148762. doi: 10.1371/journal.pone.0148762
PMID: 26910052

Conformational Plasticity of the MAGE-A3 Protein as a Therapeutic Strategy in Multiple Myeloma

Osman, R; Cho, HJ; Mei, AH; Newman, JA; Gileadi, O;
Biophysical Journal. 16.2.2016 110:535A-535A. doi: 10.1016/j.bpj.2015.11.2862
PMID:

Identification of LACTB2, a metallo-β-lactamase protein, as a human mitochondrial endoribonuclease.

Levy S, Allerston CK, Liveanu V, Habib MR, Gileadi O, Schuster G
Nucleic Acids Res.. 29.01.2016 . doi: 10.1093/nar/gkw050
PMID: 26826708

EXD2 promotes homologous recombination by facilitating DNA end resection.

Broderick R, Nieminuszczy J, Baddock HT, Deshpande RA, Gileadi O, Paull TT, McHugh PJ, Niedzwiedz W
Nat. Cell Biol.. 25.01.2016 . doi: 10.1038/ncb3303
PMID: 26807646

8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors.

Bavetsias V, Lanigan RM, Ruda GF, Atrash B, McLaughlin MG, Tumber A, Mok NY, Le Bihan YV, Dempster S, Boxall KJ, Jeganathan F, Hatch SB, Savitsky P, Velupillai S, Krojer T, England KS, Sejberg J, Thai C, Donovan A, Pal A, Scozzafava G, Bennett JM, Kawamura A, Johansson C, Szykowska A, Gileadi C, Burgess-Brown NA, von Delft F, Oppermann U, Walters Z, Shipley J, Raynaud FI, Westaway SM, Prinjha RK, Fedorov O, Burke R, Schofield CJ, Westwood IM, Bountra C, Müller S, van Montfort RL, Brennan PE, Blagg J
J. Med. Chem.. 07.01.2016 . doi: 10.1021/acs.jmedchem.5b01635
PMID: 26741168

2015

Docking and Linking of Fragments To Discover Jumonji Histone Demethylase Inhibitors.

Korczynska M, Le DD, Younger N, Gregori-Puigjané E, Tumber A, Krojer T, Velupillai S, Gileadi C, Nowak RP, Iwasa E, Pollock SB, Ortiz Torres I, Oppermann U, Shoichet BK, Fujimori DG
J. Med. Chem.. 23.12.2015 . doi: 10.1021/acs.jmedchem.5b01527
PMID: 26699912

Structure of the Helicase Domain of DNA Polymerase Theta Reveals a Possible Role in the Microhomology-Mediated End-Joining Pathway.

Newman JA, Cooper CD, Aitkenhead H, Gileadi O
Structure. 01.12.2015 23(12):2319-30. doi: 10.1016/j.str.2015.10.014
PMID: 26636256

The structures of the SNM1A and SNM1B/Apollo nuclease domains reveal a potential basis for their distinct DNA processing activities.

Allerston CK, Lee SY, Newman JA, Schofield CJ, McHugh PJ, Gileadi O
Nucleic Acids Res.. 17.11.2015 . doi: 10.1093/nar/gkv1256
PMID: 26582912

Structural basis of metallo-β-lactamase inhibition by captopril stereoisomers.

Brem J, van Berkel SS, Zollman D, Lee SY, Gileadi O, McHugh PJ, Walsh TR, McDonough MA, Schofield CJ
Antimicrob. Agents Chemother.. 19.10.2015 . doi: 10.1128/AAC.01335-15
PMID: 26482303

CSB interacts with SNM1A and promotes DNA interstrand crosslink processing

Iyama, T; Lee, SY; Berquist, BR; Gileadi, O; Bohr, VA; Seidman, MM; McHugh, PJ; Wilson, DM;
Nucleic Acids Research. 1.9.2015 43:247-258. doi: 10.1093/nar/gku1279
PMID:

Crystal structure of the Bloom's syndrome helicase indicates a role for the HRDC domain in conformational changes.

Newman JA, Savitsky P, Allerston CK, Bizard AH, Özer Ö, Sarlós K, Liu Y, Pardon E, Steyaert J, Hickson ID, Gileadi O
Nucleic Acids Res.. 21.04.2015 . doi: 10.1093/nar/gkv373
PMID: 25901030

Structures of the Ets Domains of Transcription Factors ETV1, ETV4, ETV5 and FEV: Determinants of DNA Binding and Redox Regulation by Disulfide bond formation.

Cooper CD, Newman JA, Aitkenhead H, Allerston CK, Gileadi O
J. Biol. Chem.. 12.04.2015 . doi: 10.1074/jbc.M115.646737
PMID: 25866208

Structures of the Ets Protein DNA-binding Domains of Transcription Factors Etv1, Etv4, Etv5, and Fev: DETERMINANTS OF DNA BINDING AND REDOX REGULATION BY DISULFIDE BOND FORMATION.

Cooper, CDO; Newman, JA; Aitkenhead, H; Allerston, CK; Gileadi, O;
Journal of Biological Chemistry. 01.5.2015 290:13692-13709. doi: 10.1074/jbc.M115.646737
PMID: 25866208

Human RECQ1 helicase-driven DNA unwinding, annealing, and branch migration: Insights from DNA complex structures.

Pike AC, Gomathinayagam S, Swuec P, Berti M, Zhang Y, Schnecke C, Marino F, von Delft F, Renault L, Costa A, Gileadi O, Vindigni A
Proc. Natl. Acad. Sci. U.S.A.. 23.03.2015 . doi: 10.1073/pnas.1417594112
PMID: 25831490

Preclinical target validation using patient-derived cells.

Edwards AM, Arrowsmith CH, Bountra C, Bunnage ME, Feldmann M, Knight JC, Patel DD, Prinos P, Taylor MD, Sundström M, Barker P, Barsyte D, Bengtson MH, Bell C, Bowness P, Boycott KM, Buser-Doepner C, Carpenter CL, Carr AJ, Clark K, Das AM, Dhanak D, Dirks P, Ellis J, Fantin VR, Flores C, Fon EA, Frail DE, Gileadi O, O'Hagan RC, Howe T, Isaac JT, Jabado N, Jakobsson PJ, Klareskog L, Knapp S, Lee WH, Lima-Fernandes E, Lundberg IE, Marshall J, Massirer KB, MacKenzie AE, Maruyama T, Mueller-Fahrnow A, Muthuswamy S, Nanchahal J, O'Brien C, Oppermann U, Ostermann N, Petrecca K, Pollock BG, Poupon V, Prinjha RK, Rosenberg SH, Rouleau G, Skingle M, Slutsky AS, Smith GA, Verhelle D, Widmer H, Young LT
Nat Rev Drug Discov. 20.02.2015 14(3):149-50. doi: 10.1038/nrd4565
PMID: 25722227

Structural insights into the autoregulation and cooperativity of the human transcription factor Ets-2.

Newman, JA; Cooper, CDO; Aitkenhead, H; Gileadi, O;
Journal of Biological Chemistry. 01.3.2015 290:8539-8549. doi: 10.1074/jbc.M114.619270
PMID: 25670864

Structural Insights into the Auto-regulation and Cooperativity of the Human Transcription Factor Ets-2.

Newman JA, Cooper CD, Aitkenhead H, Gileadi O
J. Biol. Chem.. 10.02.2015 . doi: 10.1074/jbc.M114.619270
PMID: 25670864

2014

CSB interacts with SNM1A and promotes DNA interstrand crosslink processing.

Iyama T, Lee SY, Berquist BR, Gileadi O, Bohr VA, Seidman MM, McHugh PJ, Wilson DM
Nucleic Acids Res.. 10.12.2014 . doi: 10.1093/nar/gku1279
PMID: 25505141

Mechanistic insight into the interaction of BLM helicase with intra-strand G-quadruplex structures.

Chatterjee S, Zagelbaum J, Savitsky P, Sturzenegger A, Huttner D, Janscak P, Hickson ID, Gileadi O, Rothenberg E
Nat Commun. 25.11.2014 5:5556. doi: 10.1038/ncomms6556
PMID: 25418155

Human UTY(KDM6C) is a male-specific N-methyl lysyl demethylase.

Walport LJ,Hopkinson RJ,Vollmar M,Madden SK,Gileadi C,Oppermann U,Schofield CJ,Johansson C.
The Journal of biological chemistry. 27/06/2014 289(26):18302-18313. doi: http://dx.doi.org/10.1074/jbc.M114.555052
PMID: 24798337

Human UTY(KDM6C) is a Male-Specific N{epsilon}-Methyl Lysyl-Demethylase.

Walport LJ, Hopkinson RJ, Vollmar M, Madden SK, Gileadi C, Oppermann U, Schofield CJ, Johansson C
J. Biol. Chem.. 05.05.2014 . doi: 10.1074/jbc.M114.555052
PMID: 24798337

Human UTY(KDM6C) is a male-specific Nϵ-methyl lysyl demethylase.

Walport, LJ; Hopkinson, RJ; Vollmar, M; Madden, SK; Gileadi, C; Oppermann, U; Schofield, CJ; Johansson, C;
Journal of Biological Chemistry. 01.6.2014 289:18302-18313. doi: 10.1074/jbc.M114.555052
PMID: 24798337

The roles of Jumonji-type oxygenases in human disease.

Johansson C, Tumber A, Che K, Cain P, Nowak R, Gileadi C, Oppermann U
Epigenomics. 04.03.2014 6(1):89-120. doi: 10.2217/epi.13.79
PMID: 24579949

Structures of soluble guanylate cyclase: implications for regulatory mechanisms and drug development.

Gileadi O
Biochem. Soc. Trans.. 01.02.2014 42(1):108-13. doi: 10.1042/BST20130228
PMID: 24450636

Recent advances in the structural molecular biology of Ets transcription factors: interactions, interfaces and inhibition.

Cooper CD, Newman JA, Gileadi O
Biochem. Soc. Trans.. 01.02.2014 42(1):130-8. doi: 10.1042/BST20130227
PMID: 24450640

2013

Medium-Throughput Production of Recombinant Human Proteins: Protein Production in E. coli.

Burgess-Brown NA, Mahajan P, Strain-Damerell C, Gileadi O, Gräslund S
Methods Mol. Biol.. 10.11.2013 1091:73-94. doi: 10.1007/978-1-62703-691-7_5
PMID: 24203325

Medium-throughput production of recombinant human proteins: ligation-independent cloning.

Strain-Damerell C, Mahajan P, Gileadi O, Burgess-Brown NA
Methods Mol. Biol.. 10.11.2013 1091:55-72. doi: 10.1007/978-1-62703-691-7_4
PMID: 24203324

Medium-throughput production of recombinant human proteins: protein production in insect cells.

Mahajan P, Strain-Damerell C, Gileadi O, Burgess-Brown NA
Methods Mol. Biol.. 10.11.2013 1091:95-121. doi: 10.1007/978-1-62703-691-7_6
PMID: 24203326

Synthesis and SAR studies of 5-(pyridin-4-yl)-1,3,4-thiadiazol-2-amine derivatives as potent inhibitors of Bloom helicase

Rosenthal, AS; Dexheimer, TS; Jadhav, A; Simeonov, A; Maloney, DJ; Gileadi, O; Nguyen, GH; Hickson, ID; Chu, WK;
Bioorganic and Medicinal Chemistry Letters. 01.01.2013 :-. doi: 10.1016/j.bmcl.2013.08.025
PMID: 24012121

Synthesis and SAR studies of 5-(pyridin-4-yl)-1,3,4-thiadiazol-2-amine derivatives as potent inhibitors of Bloom helicase.

Rosenthal AS, Dexheimer TS, Gileadi O, Nguyen GH, Chu WK, Hickson ID, Jadhav A, Simeonov A, Maloney DJ
Bioorg. Med. Chem. Lett.. 13.08.2013 . doi: 10.1016/j.bmcl.2013.08.025
PMID: 24012121

Crystal Structures of Malonyl-Coenzyme A Decarboxylase Provide Insights into Its Catalytic Mechanism and Disease-Causing Mutations.

Froese DS, Forouhar F, Tran TH, Vollmar M, Kim YS, Lew S, Neely H, Seetharaman J, Shen Y, Xiao R, Acton TB, Everett JK, Cannone G, Puranik S, Savitsky P, Krojer T, Pilka ES, Kiyani W, Lee WH, Marsden BD, von Delft F, Allerston CK, Spagnolo L, Gileadi O, Montelione GT, Oppermann U, Yue WW, Tong L
Structure. 18.06.2013 . doi: 10.1016/j.str.2013.05.001
PMID: 23791943

Structures of ABCB10, a human ATP-binding cassette transporter in apo- and nucleotide-bound states.

Shintre CA, Pike AC, Li Q, Kim JI, Barr AJ, Goubin S, Shrestha L, Yang J, Berridge G, Ross J, Stansfeld PJ, Sansom MS, Edwards AM, Bountra C, Marsden BD, von Delft F, Bullock AN, Gileadi O, Burgess-Brown NA, Carpenter EP
Proc. Natl. Acad. Sci. U.S.A.. 11.06.2013 110(24):9710-5. doi: 10.1073/pnas.1217042110
PMID: 23716676

Homozygous mutations in a predicted endonuclease cause Congenital Dyserythropoietic Anemia Type I.

Babbs C, Roberts NA, Sanchez-Pulido L, McGowan SJ, Ahmed MR, Brown JM, Sabry MA, Bentley DR, McVean GA, Donnelly P, Gileadi O, Ponting CP, Higgs DR, Buckle VJ
Haematologica. 28.05.2013 . doi: 10.3324/haematol.2013.089490
PMID: 23716552

Homozygous mutations in a predicted endonuclease are a novel cause of congenital dyserythropoietic anemia type I.

Babbs, C; Roberts, NA; Sanchez-Pulido, L; McGowan, SJ; Ahmed, MR; Brown, JM; Sabry, MA; WGS500 Consortium, ; Bentley, DR; McVean, GA; Donnelly, P; Gileadi, O; Ponting, CP; Higgs, DR; Buckle, VJ;
Haematologica. 01.9.2013 98:1383-1387. doi: 10.3324/haematol.2013.089490
PMID: 23716552

Structural Basis for Cul3 Protein Assembly with the BTB-Kelch Family of E3 Ubiquitin Ligases.

Canning P, Cooper CD, Krojer T, Murray JW, Pike AC, Chaikuad A, Keates T, Thangaratnarajah C, Hojzan V, Marsden BD, Gileadi O, Knapp S, von Delft F, Bullock AN
J. Biol. Chem.. 15.03.2013 288(11):7803-14. doi: 10.1074/jbc.M112.437996
PMID: 23349464

Crystal Structures of the Catalytic Domain of Human Soluble Guanylate Cyclase

Allerston, CK; von Delft, F; Gileadi, O;
PLoS ONE. 7.3.2013 8:-. doi: 10.1371/journal.pone.0057644
PMID: 23505436

Crystal structures of the catalytic domain of human soluble guanylate cyclase.

Allerston CK, von Delft F, Gileadi O
PLoS ONE. 07.03.2013 8(3):e57644. doi: 10.1371/journal.pone.0057644
PMID: 23505436

A small molecule inhibitor of the BLM helicase modulates chromosome stability in human cells.

Nguyen GH, Dexheimer TS, Rosenthal AS, Chu WK, Singh DK, Mosedale G, Bachrati CZ, Schultz L, Sakurai M, Savitsky P, Abu M, McHugh PJ, Bohr VA, Harris CC, Jadhav A, Gileadi O, Maloney DJ, Simeonov A, Hickson ID
Chem. Biol.. 24.01.2013 20(1):55-62. doi: 10.1016/j.chembiol.2012.10.016
PMID: 23352139

2012

Mutations in multidomain protein MEGF8 identify a Carpenter syndrome subtype associated with defective lateralization.

Twigg SR, Lloyd D, Jenkins D, Elçioglu NE, Cooper CD, Al-Sannaa N, Annagür A, Gillessen-Kaesbach G, Hüning I, Knight SJ, Goodship JA, Keavney BD, Beales PL, Gileadi O, McGowan SJ, Wilkie AO
Am. J. Hum. Genet.. 02.11.2012 91(5):897-905. doi: 10.1016/j.ajhg.2012.08.027
PMID: 23063620

Mutations in multidomain protein MEGF8 identify a carpenter syndrome subtype associated with defective lateralization

Twigg, SRF; Lloyd, D; Jenkins, D; Elçioglu, NE; Cooper, CDO; Al-Sannaa, N; Annagür, A; Gillessen-Kaesbach, G; Hüning, I; Knight, SJL; Goodship, JA; Keavney, BD; Beales, PL; Gileadi, O; McGowan, SJ; Wilkie, AOM;
American Journal of Human Genetics. 2.11.2012 91:897-905. doi: 10.1016/j.ajhg.2012.08.027
PMID:

A Small Molecule Inhibitor of the BLM Helicase That Modulates Chromosome Stability in Human Cells

Dexheimer, TS; Nguyen, GH; Rosenthal, AS; Bohr, VA; Harris, CC; Jadhav, A; Gileadi, O; Maloney, DJ; Simeonov, A; Hickson, ID;
European Journal of Cancer. 01.11.2012 48:85-85. doi: 10.1016/S0959-8049(12)72074-9
PMID:

The PHD and chromo domains regulate the ATPase activity of the human chromatin remodeler CHD4.

Watson AA, Mahajan P, Mertens HD, Deery MJ, Zhang W, Pham P, Du X, Bartke T, Zhang W, Edlich C, Berridge G, Chen Y, Burgess-Brown NA, Kouzarides T, Wiechens N, Owen-Hughes T, Svergun DI, Gileadi O, Laue ED
J. Mol. Biol.. 07.09.2012 422(1):3-17. doi: 10.1016/j.jmb.2012.04.031
PMID: 22575888

Characterization of the human SNM1A and SNM1B/Apollo DNA repair exonucleases.

Sengerová B, Allerston CK, Abu M, Lee SY, Hartley J, Kiakos K, Schofield CJ, Hartley JA, Gileadi O, McHugh PJ
J. Biol. Chem.. 27.07.2012 287(31):26254-67. doi: 10.1074/jbc.M112.367243
PMID: 22692201

Plant growth regulator daminozide is a selective inhibitor of human KDM2/7 histone demethylases.

Rose NR, Woon EC, Tumber A, Walport LJ, Chowdhury R, Li XS, King ON, Lejeune C, Ng SS, Krojer T, Chan MC, Rydzik AM, Hopkinson RJ, Che KH, Daniel M, Strain-Damerell C, Gileadi C, Kochan G, Leung IK, Dunford J, Yeoh KK, Ratcliffe PJ, Burgess-Brown N, von Delft F, Muller S, Marsden B, Brennan PE, McDonough MA, Oppermann U, Klose RJ, Schofield CJ, Kawamura A
J. Med. Chem.. 26.07.2012 55(14):6639-43. doi: 10.1021/jm300677j
PMID: 22724510

Expressing the human proteome for affinity proteomics: optimising expression of soluble protein domains and in vivo biotinylation.

Keates T, Cooper CD, Savitsky P, Allerston CK, Phillips C, Hammarström M, Daga N, Berridge G, Mahajan P, Burgess-Brown NA, Müller S, Gräslund S, Gileadi O
N Biotechnol. 15.06.2012 29(5):515-25. doi: 10.1016/j.nbt.2011.10.007
PMID: 22027370

Structural and functional insights into the DNA replication factor Cdc45 reveal an evolutionary relationship to the DHH family of phosphoesterases.

Krastanova I, Sannino V, Amenitsch H, Gileadi O, Pisani FM, Onesti S
J. Biol. Chem.. 03.02.2012 287(6):4121-8. doi: 10.1074/jbc.M111.285395
PMID: 22147708

2011

Structural and evolutionary basis for the dual substrate selectivity of human KDM4 histone demethylase family.

Hillringhaus L, Yue WW, Rose NR, Ng SS, Gileadi C, Loenarz C, Bello SH, Bray JE, Schofield CJ, Oppermann U
J. Biol. Chem.. 02.12.2011 286(48):41616-25. doi: 10.1074/jbc.M111.283689
PMID: 21914792

Human SNM1A and XPF-ERCC1 collaborate to initiate DNA interstrand cross-link repair.

Wang AT, Sengerová B, Cattell E, Inagawa T, Hartley JM, Kiakos K, Burgess-Brown NA, Swift LP, Enzlin JH, Schofield CJ, Gileadi O, Hartley JA, McHugh PJ
Genes Dev.. 01.09.2011 25(17):1859-70. doi: 10.1101/gad.15699211
PMID: 21896658

Human SNM1a and XPF-ERCC1 collaborate to initiate DNA interstrand cross-link repair

Wang, AT; Sengerová, B; Cattell, E; Inagawa, T; Hartley, JM; Kiakos, K; Burgess-Brown, NA; Swift, LP; Enzlin, JH; Schofield, CJ; Gileadi, O; Hartley, JA; McHugh, PJ;
Genes and Development. 1.9.2011 25:1859-1870. doi: 10.1101/gad.15699211
PMID:

Identification of macrodomain proteins as novel O-acetyl-ADP-ribose deacetylases.

Chen D, Vollmar M, Rossi MN, Phillips C, Kraehenbuehl R, Slade D, Mehrotra PV, von Delft F, Crosthwaite SK, Gileadi O, Denu JM, Ahel I
J. Biol. Chem.. 15.04.2011 286(15):13261-71. doi: 10.1074/jbc.M110.206771
PMID: 21257746

Structural basis of fumarate hydratase deficiency.

Picaud S, Kavanagh KL, Yue WW, Lee WH, Muller-Knapp S, Gileadi O, Sacchettini J, Oppermann U
J. Inherit. Metab. Dis.. 29.03.2011 34(3):671-6. doi: 10.1007/s10545-011-9294-8
PMID: 21445611

High-performance liquid chromatography separation and intact mass analysis of detergent-solubilized integral membrane proteins.

Berridge G, Chalk R, D'Avanzo N, Dong L, Doyle D, Kim JI, Xia X, Burgess-Brown N, Deriso A, Carpenter EP, Gileadi O
Anal. Biochem.. 15.03.2011 410(2):272-80. doi: 10.1016/j.ab.2010.11.008
PMID: 21093405

DELINEATING THE MITOCHONDRIAL VITAMIN B12 PATHWAY THROUGH STRUCTURAL AND INTERACTION STUDIES

Froese, DS; Kochan, G; Muniz, JRC; Chaikuad, A; Wu, X; Gileadi, C; Ugochukwu, E; Krysztofinska, E; Gravel, RA; Oppermann, U; Yue, WW;
Journal of Inherited Metabolic Disease. 01.01.2011 34:S119-S119. doi:
PMID:

2010

Structures of the human GTPase MMAA and vitamin B12-dependent methylmalonyl-CoA mutase and insight into their complex formation.

Froese DS, Kochan G, Muniz JR, Wu X, Gileadi C, Ugochukwu E, Krysztofinska E, Gravel RA, Oppermann U, Yue WW
J. Biol. Chem.. 03.12.2010 285(49):38204-13. doi: 10.1074/jbc.M110.177717
PMID: 20876572

High-performance liquid chromatography separation and intact mass analysis of detergent-solubilized integral membrane proteins

Berridge, G; Chalk, R; Burgess-Brown, NA; Carpenter, EP; Gileadi, O;
Analytical Biochemistry. 17.11.2010 :-. doi: 10.1016/j.ab.2010.11.008
PMID:

A prominent β-hairpin structure in the winged-helix domain of RECQ1 is required for DNA unwinding and oligomer formation.

Lucic B, Zhang Y, King O, Mendoza-Maldonado R, Berti M, Niesen FH, Burgess-Brown NA, Pike AC, Cooper CD, Gileadi O, Vindigni A
Nucleic Acids Res.. 08.11.2010 39(5):1703-17. doi: 10.1093/nar/gkq1031
PMID: 21059676

Isolated short CTG/CAG DNA slip-outs are repaired efficiently by hMutSbeta, but clustered slip-outs are poorly repaired.

Panigrahi GB, Slean MM, Simard JP, Gileadi O, Pearson CE
Proc. Natl. Acad. Sci. U.S.A.. 13.07.2010 107(28):12593-8. doi: 10.1073/pnas.0909087107
PMID: 20571119

High-throughput production of human proteins for crystallization: the SGC experience.

Savitsky P, Bray J, Cooper CD, Marsden BD, Mahajan P, Burgess-Brown NA, Gileadi O
J. Struct. Biol.. 10.06.2010 172(1):3-13. doi: 10.1016/j.jsb.2010.06.008
PMID: 20541610

Unusual binding interactions in PDZ domain crystal structures help explain binding mechanisms.

Elkins, JM; Gileadi, C; Shrestha, L; Phillips, C; Wang, J; Muniz, JRC; Doyle, DA;
Protein Science. 01.4.2010 19:731-741. doi: 10.1002/pro.349
PMID: 20120020

Probing the structural basis of RecQ helicase function.

Vindigni A, Marino F, Gileadi O
Biophys. Chem.. 20.03.2010 149(3):67-77. doi: 10.1016/j.bpc.2010.03.012
PMID: 20392558

2009

Structure of the human RECQ1 helicase reveals a putative strand-separation pin.

Pike AC, Shrestha B, Popuri V, Burgess-Brown N, Muzzolini L, Costantini S, Vindigni A, Gileadi O
Proc. Natl. Acad. Sci. U.S.A.. 27.01.2009 106(4):1039-44. doi: 10.1073/pnas.0806908106
PMID: 19151156

2008

High throughput production of recombinant human proteins for crystallography.

Gileadi O, Burgess-Brown NA, Colebrook SM, Berridge G, Savitsky P, Smee CE, Loppnau P, Johansson C, Salah E, Pantic NH
Methods Mol. Biol.. 11.06.2008 426:221-46. doi: 10.1007/978-1-60327-058-8_14
PMID: 18542867

Structural diversity in the RGS domain and its interaction with heterotrimeric G protein alpha-subunits.

Soundararajan, M; Willard, FS; Kimple, AJ; Turnbull, AP; Ball, LJ; Schoch, GA; Gileadi, C; Fedorov, OY; Dowler, EF; Higman, VA; Hutsell, SQ; Sundström, M; Doyle, DA; Siderovski, DP;
Proceedings of the National Academy of Sciences. 23.4.2008 105:6457-6462. doi: 10.1073/pnas.0801508105
PMID: 18434541

Baculovirus expression vector system: an emerging host for high-throughput eukaryotic protein expression.

Shrestha B, Smee C, Gileadi O
Methods Mol. Biol.. 29.03.2008 439:269-89. doi: 10.1007/978-1-59745-188-8_19
PMID: 18370110

Protein production and purification.

Gräslund S, Nordlund P, Weigelt J, Hallberg BM, Bray J, Gileadi O, Knapp S, Oppermann U, Arrowsmith C, Hui R, Ming J, dhe-Paganon S, Park HW, Savchenko A, Yee A, Edwards A, Vincentelli R, Cambillau C, Kim R, Kim SH, Rao Z, Shi Y, Terwilliger TC, Kim CY, Hung LW, Waldo GS, Peleg Y, Albeck S, Unger T, Dym O, Prilusky J, Sussman JL, Stevens RC, Lesley SA, Wilson IA, Joachimiak A, Collart F, Dementieva I, Donnelly MI, Eschenfeldt WH, Kim Y, Stols L, Wu R, Zhou M, Burley SK, Emtage JS, Sauder JM, Thompson D, Bain K, Luz J, Gheyi T, Zhang F, Atwell S, Almo SC, Bonanno JB, Fiser A, Swaminathan S, Studier FW, Chance MR, Sali A, Acton TB, Xiao R, Zhao L, Ma LC, Hunt JF, Tong L, Cunningham K, Inouye M, Anderson S, Janjua H, Shastry R, Ho CK, Wang D, Wang H, Jiang M, Montelione GT, Stuart DI, Owens RJ, Daenke S, Schütz A, Heinemann U, Yokoyama S, Büssow K, Gunsalus KC
Nat. Methods. 01.02.2008 5(2):135-46. doi: 10.1038/nmeth.f.202
PMID: 18235434

Codon optimization can improve expression of human genes in Escherichia coli: A multi-gene study.

Burgess-Brown NA, Sharma S, Sobott F, Loenarz C, Oppermann U, Gileadi O
Protein Expr. Purif.. 26.01.2008 59(1):94-102. doi: 10.1016/j.pep.2008.01.008
PMID: 18289875

Baculovirus expression vector system: An emerging host for high-throughput eukaryotic protein expression

Shrestha, B; Smee, C; Gileadi, O;
Methods in Molecular Biology. 1.1.2008 439:269-289. doi: 10.1007/978-1-59745-188-8_19
PMID:

2007

The scientific impact of the Structural Genomics Consortium: a protein family and ligand-centered approach to medically-relevant human proteins.

Gileadi O, Knapp S, Lee WH, Marsden BD, Müller S, Niesen FH, Kavanagh KL, Ball LJ, von Delft F, Doyle DA, Oppermann UC, Sundström M
J. Struct. Funct. Genomics. 12.10.2007 8(2-3):107-19. doi: 10.1007/s10969-007-9027-2
PMID: 17932789

Crystal structures of histone demethylase JMJD2A reveal basis for substrate specificity.

Ng SS, Kavanagh KL, McDonough MA, Butler D, Pilka ES, Lienard BM, Bray JE, Savitsky P, Gileadi O, von Delft F, Rose NR, Offer J, Scheinost JC, Borowski T, Sundstrom M, Schofield CJ, Oppermann U
Nature. 05.07.2007 448(7149):87-91. doi: 10.1038/nature05971
PMID: 17589501

Structure of PICK1 and other PDZ domains obtained with the help of self-binding C-terminal extensions.

Elkins, JM; Papagrigoriou, E; Berridge, G; Yang, X; Phillips, C; Gileadi, C; Savitsky, P; Doyle, DA;
Protein Science. 01.4.2007 16:683-694. doi:
PMID: 17384233

Reversible sequestration of active site cysteines in a 2Fe-2S-bridged dimer provides a mechanism for glutaredoxin 2 regulation in human mitochondria.

Johansson C, Kavanagh KL, Gileadi O, Oppermann U
J. Biol. Chem.. 02.02.2007 282(5):3077-82. doi: 10.1074/jbc.M608179200
PMID: 17121859

2006

Direct observation of RuvAB-catalyzed branch migration of single Holliday junctions (vol 101, pg 11605, 2004)

Amit, R; Gileadi, O; Stavans, J;
Proceedings of the National Academy of Sciences. 15.8.2006 103:12654-12654. doi:
PMID:

Erratum: Direct observation of RuvAB-catalyzed branch migration of single Holliday junctions (Proceedings of the National Academy of Sciences of the United States of America (August 10, 2004) 101, 32 (11605-11616): 10.1073/pnas.0404332101)

Amit, R; Gileadi, O; Stavans, J;
Proceedings of the National Academy of Sciences. 15.8.2006 103:12654-. doi: 10.1073/pnas.0605122103
PMID:

2005

The structural genomics consortium: High-output structure determination

Gileadi, O; Colebrook, S; Burgess, N; Berridge, G; Haroniti, A; Shrestha, B; Smee, C; Sundstrom, M;
FASEB Journal. 4.3.2005 19:A315-A315. doi:
PMID:

2004

Direct observation of RuvAB-catalyzed branch migration of single Holliday junctions.

Amit, R; Gileadi, O; Stavans, J;
Proceedings of the National Academy of Sciences. 10.8.2004 101:11605-11610. doi: 10.1073/pnas.0404332101
PMID: 15292509

Electron microscopy of wet tissues: a case study in renal pathology.

Nyska, A; Cummings, CA; Vainshtein, A; Nadler, J; Ezov, N; Grunfeld, Y; Gileadi, O; Behar, V;
Toxicologic Pathology. 01.5.2004 32:357-363. doi: 10.1080/01926230490431772
PMID: 15204979

Fat cell precursors from different human fat depots are distinct: Morphological and gene expression profiles

Kirkland, J; Tchkonia, T; Frampton, G; Lenberg, M; Giorgadze, N; Sabban, A; Pirtskhalava, T; Cartwright, M; Gerry, N; Forse, A; Thomou, T; Gileadi, O;
International Journal of Obesity. 01.5.2004 28:S99-S99. doi:
PMID:

Scanning electron microscopy of cells and tissues under fully hydrated conditions.

Thiberge, S; Nechushtan, A; Sprinzak, D; Gileadi, O; Behar, V; Zik, O; Chowers, Y; Michaeli, S; Schlessinger, J; Moses, E;
Proceedings of the National Academy of Sciences. 9.3.2004 101:3346-3351. doi: 10.1073/pnas.0400088101
PMID: 14988502

A novel method for "Wet" SEM.

Barshack, I; Kopolovic, J; Chowers, Y; Gileadi, O; Vainshtein, A; Zik, O; Behar, V;
Ultrastructural Pathology. 01.1.2004 28:29-31. doi:
PMID: 14967596

2003

Squid sperm to clam eggs: imaging wet samples in a scanning electron microscope.

Gileadi, O; Sabban, A;
Biological Bulletin. 01.10.2003 205:177-179. doi: 10.2307/1543239
PMID: 14583516

Electron microscopy of wet cells and tissues

Gileadi, O; Behar, V; Ezer, S; Horowitz, M; Nechushtan, A; Sabban, A; Sprinzak, D; Vainshtein, A; Zik, O;
FASEB Journal. 17.3.2003 17:A1080-A1080. doi:
PMID:

Scanning electron microscopy of wet biological specimens

Gileadi, O; Behar, V; Ezer, S; Horowitz, M; Nechushtan, A; Sabban, A; Sprinzak, D; Vainshtein, A; Zik, O;
Microscopy and Microanalysis. 30.10.2003 9:486-487. doi:
PMID:

2002

Mutations in the RING domain of TFB3, a subunit of yeast transcription factor IIH, reveal a role in cell cycle progression.

Jona, G; Livi, LL; Gileadi, O;
Journal of Biological Chemistry. 18.10.2002 277:39409-39416. doi: 10.1074/jbc.M202733200
PMID: 12176978

Compaction of single DNA molecules by histone-like binding protein HU.

Schnurr, B; Amit, R; Oppenheim, AB; Gileadi, O; Stavans, J;
Biophysical Journal. 01.1.2002 82:51A-51A. doi:
PMID:

2001

Objective-type dark-field illumination for scattering from microbeads.

Braslavsky, I; Amit, R; Jaffar Ali, BM; Gileadi, O; Oppenheim, A; Stavans, J;
Applied Optics. 1.11.2001 40:5650-5657. doi:
PMID: 18364854

Compaction of single DNA molecules induced by binding of integration host factor (IHF).

Ali, BM; Amit, R; Braslavsky, I; Oppenheim, AB; Gileadi, O; Stavans, J;
Proceedings of the National Academy of Sciences. 11.9.2001 98:10658-10663. doi: 10.1073/pnas.181029198
PMID: 11535804

Involvement of yeast carboxy-terminal domain kinase I (CTDK-I) in transcription elongation in vivo.

Jona, G; Wittschieben, BO; Svejstrup, JQ; Gileadi, O;
Gene. 4.4.2001 267:31-36. doi:
PMID: 11311553

Autophosphorylation restrains the apoptotic activity of DRP-1 kinase by controlling dimerization and calmodulin binding.

Shani, G; Henis-Korenblit, S; Jona, G; Gileadi, O; Eisenstein, M; Ziv, T; Admon, A; Kimchi, A;
EMBO Journal. 1.3.2001 20:1099-1113. doi: 10.1093/emboj/20.5.1099
PMID: 11230133

2000

Distinct regions of MAT1 regulate cdk7 kinase and TFIIH transcription activities.

Busso, D; Keriel, A; Sandrock, B; Poterszman, A; Gileadi, O; Egly, JM;
Journal of Biological Chemistry. 28.7.2000 275:22815-22823. doi: 10.1074/jbc.M002578200
PMID: 10801852

Glucose starvation induces a drastic reduction in the rates of both transcription and degradation of mRNA in yeast.

Jona, G; Choder, M; Gileadi, O;
BBA - Biochimica et Biophysica Acta. 25.4.2000 1491:37-48. doi:
PMID: 10760568

Rad25p, a DNA helicase subunit of yeast transcription factor TFIIH, is required for promoter escape in vivo.

Ostapenko, D; Gileadi, O;
Gene. 7.3.2000 245:109-117. doi:
PMID: 10713451

Subunit interactions in yeast transcription/repair factor TFIIH. Requirement for Tfb3 subunit in nucleotide excision repair.

Feaver, WJ; Huang, W; Gileadi, O; Myers, L; Gustafsson, CM; Kornberg, RD; Friedberg, EC;
Journal of Biological Chemistry. 25.2.2000 275:5941-5946. doi:
PMID: 10681587

Erratum: Cak1 is required for Kin28 phosphorylation and activation in vivo (Molecular and Cellular Biology (1999) 19:12 (6365-6373))

Espinoza, FH; Farrell, A; Nourse, JL; Chamberlin, HM; Gileadi, O; Morgan, DO;
Molecular and Cellular Biology. 1.1.2000 20:1898-. doi: 10.1128/MCB.20.5.1898-1898.2000
PMID:

1999

An unusual eukaryotic protein phosphatase required for transcription by RNA polymerase II and CTD dephosphorylation in S. cerevisiae.

Kobor, MS; Archambault, J; Lester, W; Holstege, FC; Gileadi, O; Jansma, DB; Jennings, EG; Kouyoumdjian, F; Davidson, AR; Young, RA; Greenblatt, J;
Molecular Cell. 01.7.1999 4:55-62. doi:
PMID: 10445027

1998

Cak1 is required for Kin28 phosphorylation and activation in vivo.

Espinoza, FH; Farrell, A; Nourse, JL; Chamberlin, HM; Gileadi, O; Morgan, DO;
Molecular and Cellular Biology. 01.11.1998 18:6365-6373. doi:
PMID: 9774652

Analysis of the Ac promoter: structure and regulation.

Fridlender, M; Sitrit, Y; Shaul, O; Gileadi, O; Levy, AA;
Molecular and General Genetics MGG. 01.5.1998 258:306-314. doi:
PMID: 9645437

1995

Partial truncation of the yeast RNA polymerase II carboxyl-terminal domain preferentially reduces expression of glycolytic genes.

Meisels, E; Gileadi, O; Corden, JL;
Journal of Biological Chemistry. 29.12.1995 270:31255-31261. doi:
PMID: 8537392

1994

Yeast TFIIE. Cloning, expression, and homology to vertebrate proteins.

Feaver, WJ; Henry, NL; Bushnell, DA; Sayre, MH; Brickner, JH; Gileadi, O; Kornberg, RD;
Journal of Biological Chemistry. 4.11.1994 269:27549-27553. doi:
PMID: 7961670

1993

CHARACTERIZATION OF YEAST RNA POLYMERASE-II TRANSCRIPTION FACTOR-B AND CTD KINASE

FEAVER, WJ; GILEADI, O; KORNBERG, RD;
Journal of Cellular Biochemistry. 9.1.1993 :71-71. doi:
PMID:

YEAST RNA POLYMERASE-II TRANSCRIPTION - STRUCTURE, MECHANISM AND REGULATION

KORNBERG, RD; CHASMAN, DI; DARST, SA; DAVID, P; EDWARDS, AM; FEAVER, WJ; FLANAGAN, PM; GILEADI, O; HENRY, NL; KELLEHER, RJ; LI, Y; LORCH, Y; MEREDITH, G; POGLITSCH, C; SAYRE, MH; TSCHOCHNER, H;
Journal of Cellular Biochemistry. 9.1.1993 :55-55. doi:
PMID:

1992

Identification of human satellite DNA sequences associated with chemically resistant nonhistone polypeptide adducts.

Pfütz, M; Gileadi, O; Werner, D;
Chromosoma. 01.10.1992 101:609-617. doi:
PMID: 1424985

Cloning of a subunit of yeast RNA polymerase II transcription factor b and CTD kinase.

Gileadi, O; Feaver, WJ; Kornberg, RD;
Science. 4.9.1992 257:1389-1392. doi:
PMID: 1445600

Transcription of the H19 gene in differentiating cytotrophoblasts from human placenta.

Rachmilewitz, J; Gileadi, O; Eldar-Geva, T; Schneider, T; de-Groot, N; Hochberg, A;
Molecular Reproduction and Development. 01.7.1992 32:196-202. doi: 10.1002/mrd.1080320303
PMID: 1497869

YEAST RNA POLYMERASE-II TRANSCRIPTION - ENZYMATIC-ACTIVITIES OF GENERAL INITIATION-FACTORS, 3-D STRUCTURES OF INITIATION-FACTORS AND RNA-POLYMERASE, AND MECHANISM OF TRANSCRIPTIONAL ACTIVATION

KORNBERG, R; CHASMAN, D; DARST, S; EDWARDS, A; FEAVER, W; FLANAGAN, P; GILEADI, O; HINDS, D; KELLEHER, R; MEREDITH, G; LI, Y; LORCH, Y; PARK, B; SAYRE, M; TSCHOCHNER, H;
FASEB Journal. 1.1.1992 6:A274-A274. doi:
PMID: