Publications

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Displaying 51 - 100 of 1788

2020

June 2020

Epigenetic switch-induced viral mimicry evasion in chemotherapy resistant breast cancer.
Deblois G, Madani Tonekaboni SA, Grillo G, Martinez C, Kao YI, Tai F, Ettayebi I, Fortier AM, Savage P, Fedor AN, Liu X, Guilhamon P, Lima-Fernandes E, Murison A, Kuasne H, Ba-Alawi W, Cescon DW, Arrowsmith CH, De Carvalho DD, Haibe-Kains B, Locasale JW, Park M, Lupien M
Cancer Discov . doi: 10.1158/2159-8290.CD-19-1493
Publication date: June 16, 2020
PMID: 32546577
Tuning transcription factor availability through acetylation-mediated genomic redistribution
GODING C
Molecular Cell 79:472-487.e10 . doi: 10.1016/j.molcel.2020.05.025
Publication date: June 10, 2020
PMID: 32531202
Recognition of nonproline N-terminal residues by the Pro/N-degron pathway.
Dong C, Chen SJ, Melnykov A, Weirich S, Sun K, Jeltsch A, Varshavsky A, Min J
Proc. Natl. Acad. Sci. U.S.A. . doi: 10.1073/pnas.2007085117
Publication date: June 8, 2020
PMID: 32513738
Human aminolevulinate synthase structure reveals a eukaryotic-specific autoinhibitory loop regulating substrate binding and product release
Bailey HJ, Bezerra GA, Marcero JR, Padhi S, Foster WR, Rembeza E, Roy A, Bishop DF, Desnick RJ, Bulusu G, Dailey HA, Yue WW
Nature Communications 11:2813- . doi: 10.1038/s41467-020-16586-x
Publication date: June 3, 2020
PMID: 32499479
Quantifying CDK inhibitor selectivity in live cells
Wells CI, Vasta JD, Corona CR, Wilkinson J, Zimprich CA, Ingold MR, Pickett JE, Drewry DH, Pugh KM, Schwinn MK, Hwang B, Zegzouti H, Huber KVM, Cong M, Meisenheimer PL, Willson TM, Robers MB
Nature Communications 11:2743- . doi: 10.1038/s41467-020-16559-0
Publication date: June 1, 2020
PMID: 32488087

May 2020

Preclinical drug studies in MEN1-related neuroendocrine neoplasms (MEN1-NENs)
Grozinsky-Glasberg S, Lines KE, Avniel-Polak S, Bountra C, Thakker RV
Endocrine-related cancer 27:R345-R355 . doi: 10.1530/ERC-20-0127
Publication date: May 31, 2020
PMID: 32590358
Structural Basis for the Binding Selectivity of Human CDY Chromodomains.
Dong C, Liu Y, Lyu TJ, Beldar S, Lamb KN, Tempel W, Li Y, Li Z, James LI, Qin S, Wang Y, Min J
Cell Chem Biol . doi: 10.1016/j.chembiol.2020.05.007
Publication date: May 26, 2020
PMID: 32470319
Crystallographic and electrophilic fragment screening of the SARS-CoV-2 main protease
KROJER T, Douangamath A, Fearon D, Gehrtz P, Lukacik P, Owen CD, Resnick E, Strain-Damerell C, Aimon A, Ábrányi-Balogh P, Brandaõ-Neto J, Carbery A, Davison G, Dias A, Downes TD, Dunnett L, FAIRHEAD M, Firth JD, Jones P, Keely A, Keserü GM, Klein HF, Martin MP, Noble MEM, O’Brien P, Powell A, Reddi R, Skyner R, Snee M, Waring MJ, Wild C, London N, VON DELFT F, Walsh ME
biorxiv . doi: 10.1101/2020.05.27.118117
Publication date: May 26, 2020
PMID:
Metabolic Regulation of the Epigenome Drives Lethal Infantile Ependymoma.
Michealraj KA, Kumar SA, Kim LJY, Cavalli FMG, Przelicki D, Wojcik JB, Delaidelli A, Bajic A, Saulnier O, MacLeod G, Vellanki RN, Vladoiu MC, Guilhamon P, Ong W, Lee JJY, Jiang Y, Holgado BL, Rasnitsyn A, Malik AA, Tsai R, Richman CM, Juraschka K, Haapasalo J, Wang EY, De Antonellis P, Suzuki H, Farooq H, Balin P, Kharas K, Van Ommeren R, Sirbu O, Rastan A, Krumholtz SL, Ly M, Ahmadi M, Deblois G, Srikanthan D, Luu B, Loukides J, Wu X, Garzia L, Ramaswamy V, Kanshin E, Sánchez-Osuna M, El-Hamamy I, Coutinho FJ, Prinos P, Singh S, Donovan LK, Daniels C, Schramek D, Tyers M, Weiss S, Stein LD, Lupien M, Wouters BG, Garcia BA, Arrowsmith CH, Sorensen PH, Angers S, Jabado N, Dirks PB, Mack SC, Agnihotri S, Rich JN, Taylor MD
Cell . doi: 10.1016/j.cell.2020.04.047
Publication date: May 20, 2020
PMID: 32445698
Receptor-interacting protein kinase 2 (RIPK2) and nucleotide-binding oligomerization domain (NOD) cell signaling inhibitors based on a 3,5-diphenyl-2-aminopyridine scaffold
Suebsuwong C, Dai B, Pinkas DM, Duddupudi AL, Li L, Bufton JC, Schlicher L, Gyrd-Hansen M, Hu M, Bullock AN, Degterev A, Cuny GD
European Journal of Medicinal Chemistry 200:112417- . doi: 10.1016/j.ejmech.2020.112417
Publication date: May 14, 2020
PMID: 32505849
Pharmacological inhibition of PRMT7 links arginine monomethylation to the cellular stress response.
Szewczyk MM, Ishikawa Y, Organ S, Sakai N, Li F, Halabelian L, Ackloo S, Couzens AL, Eram M, Dilworth D, Fukushi H, Harding R, Dela Seña CC, Sugo T, Hayashi K, McLeod D, Zepeda C, Aman A, Sánchez-Osuna M, Bonneil E, Takagi S, Al-Awar R, Tyers M, Richard S, Takizawa M, Gingras AC, Arrowsmith CH, Vedadi M, Brown PJ, Nara H, Barsyte-Lovejoy D
Nat Commun 11(1):2396 . doi: 10.1038/s41467-020-16271-z
Publication date: May 14, 2020
PMID: 32409666
Targeting ALK2: An Open Science Approach to Developing Therapeutics for the Treatment of Diffuse Intrinsic Pontine Glioma.
Ensan D, Smil D, Zepeda-Velázquez CA, Panagopoulos D, Wong JF, Williams EP, Adamson R, Bullock AN, Kiyota T, Aman A, Roberts OG, Edwards AM, O'Meara JA, Isaac MB, Al-Awar R
J. Med. Chem. . doi: 10.1021/acs.jmedchem.0c00395
Publication date: May 5, 2020
PMID: 32369358
Discovery of a First-in-class Protein Arginine Methyltransferase 6 (PRMT6) Covalent Inhibitor.
Shen Y, Li F, Szewczyk MM, Halabelian L, Park KS, Chau I, Dong A, Zeng H, Chen H, Meng F, Barsyte-Lovejoy D, Arrowsmith CH, Brown P, Liu J, Vedadi M, Jin J
J. Med. Chem. . doi: 10.1021/acs.jmedchem.0c00406
Publication date: May 5, 2020
PMID: 32367723

April 2020

A lower X-gate in TASK channels traps inhibitors within the vestibule
RODSTROM K, Kiper A, Zhang W, Rinne S, PIKE A, Goldstein M, Conrad L, Delbeck M, Hahn M, Meier H, Platzk M, Quigley A, Speedman D, SHRESTHA L, Mukhopadhyay S, BURGESS-BROWN N, TUCKER S, Mueller T, Decher N, CARPENTER E
Nature 582:443-447 . doi: 10.1038/s41586-020-2250-8
Publication date: April 28, 2020
PMID: 32499642
Telomere dysfunction cooperates with epigenetic alterations to impair murine embryonic stem cell fate commitment.
Criqui M, Qamra A, Chu TW, Sharma M, Tsao J, Henry DA, Barsyte-Lovejoy D, Arrowsmith CH, Winegarden N, Lupien M, Harrington L
Elife 9: . doi: 10.7554/eLife.47333
Publication date: April 16, 2020
PMID: 32297856
Targeting der kleinen GTPasen über ihre regulatorischen Proteine
Gray JL, Delft F, Brennan PE
Angewandte Chemie 132:6402-6428 . doi: 10.1002/ange.201900585
Publication date: April 15, 2020
PMID:
Development of 2-(4-pyridyl)-benzimidazoles as PKN2 chemical tools to probe cancer
Scott F, Fala AM, Pennicott LE, Reuillon TD, Massirer KB, Elkins JM, Ward SE
Bioorganic and Medicinal Chemistry Letters 30:127040- . doi: 10.1016/j.bmcl.2020.127040
Publication date: April 14, 2020
PMID: 32085971
The RESOLUTE consortium: unlocking SLC transporters for drug discovery.
Superti-Furga G, Lackner D, Wiedmer T, Ingles-Prieto A, Barbosa B, Girardi E, Goldmann U, Gürtl B, Klavins K, Klimek C, Lindinger S, Liñeiro-Retes E, Müller AC, Onstein S, Redinger G, Reil D, Sedlyarov V, Wolf G, Crawford M, Everley R, Hepworth D, Liu S, Noell S, Piotrowski M, Stanton R, Zhang H, Corallino S, Faedo A, Insidioso M, Maresca G, Redaelli L, Sassone F, Scarabottolo L, Stucchi M, Tarroni P, Tremolada S, Batoulis H, Becker A, Bender E, Chang YN, Ehrmann A, Müller-Fahrnow A, Pütter V, Zindel D, Hamilton B, Lenter M, Santacruz D, Viollet C, Whitehurst C, Johnsson K, Leippe P, Baumgarten B, Chang L, Ibig Y, Pfeifer M, Reinhardt J, Schönbett J, Selzer P, Seuwen K, Bettembourg C, Biton B, Czech J, de Foucauld H, Didier M, Licher T, Mikol V, Pommereau A, Puech F, Yaligara V, Edwards A, Bongers BJ, Heitman LH, IJzerman AP, Sijben HJ, van Westen GJP, Grixti J, Kell DB, Mughal F, Swainston N, Wright-Muelas M, Bohstedt T, Burgess-Brown N, Carpenter L, Dürr K, Hansen J, Scacioc A, Banci G, Colas C, Digles D, Ecker G, Füzi B, Gamsjäger V, Grandits M, Martini R, Troger F, Altermatt P, Doucerain C, Dürrenberger F, Manolova V, Steck AL, Sundström H, Wilhelm M, Steppan CM
Nat Rev Drug Discov . doi: 10.1038/d41573-020-00056-6
Publication date: April 7, 2020
PMID: 32265506
Hotspots API: A Python Package for the Detection of Small Molecule Binding Hotspots and Application to Structure-Based Drug Design
Curran PR, Radoux CJ, Smilova MD, Sykes RA, Higueruelo AP, Bradley AR, Marsden BD, Spring DR, Blundell TL, Leach AR, Pitt WR, Cole JC
Journal of chemical information and modeling 60:1911-1916 . doi: 10.1021/acs.jcim.9b00996
Publication date: April 1, 2020
PMID: 32207937

March 2020

Structural Basis for EPC1-Mediated Recruitment of MBTD1 into the NuA4/TIP60 Acetyltransferase Complex.
Zhang H, Devoucoux M, Song X, Li L, Ayaz G, Cheng H, Tempel W, Dong C, Loppnau P, Côté J, Min J
Cell Rep 30(12):3996-4002.e4 . doi: 10.1016/j.celrep.2020.03.003
Publication date: March 24, 2020
PMID: 32209463
Quantifying Target Occupancy of Small Molecules within Living Cells
Robers MB, Friedman-Ohana R, Huber KVM, Huber KVM, Kilpatrick L, Kilpatrick L, Vasta JD, Berger BT, Chaudhry C, Hill S, Hill S, Müller S, Müller S, Knapp S, Knapp S, Knapp S, Knapp S, Wood KV, Wood KV
Annual Review of Biochemistry 89:557-581 . doi: 10.1146/annurev-biochem-011420-092302
Publication date: March 24, 2020
PMID: 32208767
A Highly Selective Chemical Probe for Activin Receptor-like Kinases ALK4 and ALK5
Hanke T, Wong JF, Berger B-T, Abdi I, Berger LM, Tesch R, Tredup C, Bullock AN, Müller S, Knapp S
ACS Chemical Biology 15:862-870 . doi: 10.1021/acschembio.0c00076
Publication date: March 20, 2020
PMID: 32176847
Importance of Quantifying Drug-Target Engagement in Cells
Stefaniak J, Huber KVM
ACS Medicinal Chemistry Letters 11:403-406 . doi: 10.1021/acsmedchemlett.9b00570
Publication date: March 6, 2020
PMID: 32292539
Mutant ACVR1 Arrests Glial Cell Differentiation to Drive Tumorigenesis in Pediatric Gliomas
Fortin J, Tian R, Zarrabi I, Hill G, Williams E, Sanchez-Duffhues G, Thorikay M, Ramachandran P, Siddaway R, Wong JF, Wu A, Apuzzo LN, Haight J, You-Ten A, Snow BE, Wakeham A, Goldhamer DJ, Schramek D, Bullock AN, Dijke PT, Hawkins C, Mak TW
Cancer Cell 37:308-323.e12 . doi: 10.1016/j.ccell.2020.02.002
Publication date: March 5, 2020
PMID: 32142668
Crystal structure of the catalytic D2 domain of the AAA+ ATPase p97 reveals a putative helical split-washer-type mechanism for substrate unfolding
Stach L, Morgan RM, Makhlouf L, Douangamath A, von Delft F, Zhang X, Freemont PS
FEBS Letters 594:933-943 . doi: 10.1002/1873-3468.13667
Publication date: March 1, 2020
PMID: 31701538
Effects of epigenetic pathway inhibitors on corticotroph tumour AtT20 cells
LINES K, FILIPPAKOPOULOS P, STEVENSON M, Lockstone H, WRIGHT B, BUCK D, BOUNTRA C, THAKKER RV
Endocrine-Related Cancer 27:163-174 . doi: 10.1530/ERC-19-0448
Publication date: March 1, 2020
PMID: 31935194

February 2020

Re-evaluating the mechanism of action of α,β-unsaturated carbonyl DUB inhibitors b-AP15 and VLX1570: a paradigmatic example of unspecific protein crosslinking with Michael acceptor motif-containing drugs
WARD JA, PINTO FERNANDEZ A, Cornelissen L, BONHAM S, DIAZ SAEZ L, Riant O, HUBER KVM, KESSLER BM, Feron O, Tate EW
Journal of Medicinal Chemistry 63:3756-3762 . doi: 10.1021/acs.jmedchem.0c00144
Publication date: February 28, 2020
PMID:
Structure-based view of the druggable genome.
Wang J, Yazdani S, Han A, Schapira M
Drug Discov. Today . doi: 10.1016/j.drudis.2020.02.006
Publication date: February 19, 2020
PMID: 32084498
MichelaNglo: sculpting protein views on web pages without coding
Ferla MP, Pagnamenta AT, Damerell D, Taylor JC, Marsden BD
Bioinformatics 36:3268-3270 . doi: 10.1093/bioinformatics/btaa104
Publication date: February 15, 2020
PMID: 32061125
2019

December 2019

Human MettL3-MettL14 complex is a sequence-specific DNA adenine methyltransferase active on single-strand and unpaired DNA in vitro.
Woodcock CB, Yu D, Hajian T, Li J, Huang Y, Dai N, Corrêa IR, Wu T, Vedadi M, Zhang X, Cheng X
Cell Discov 5:63 . doi: 10.1038/s41421-019-0136-4
Publication date: December 31, 2019
PMID: 31885874
Discovery of a chemical probe for PRDM9.
Allali-Hassani A, Szewczyk MM, Ivanochko D, Organ SL, Bok J, Ho JSY, Gay FPH, Li F, Blazer L, Eram MS, Halabelian L, Dilworth D, Luciani GM, Lima-Fernandes E, Wu Q, Loppnau P, Palmer N, Talib SZA, Brown PJ, Schapira M, Kaldis P, O'Hagan RC, Guccione E, Barsyte-Lovejoy D, Arrowsmith CH, Sanders JM, Kattar SD, Bennett DJ, Nicholson B, Vedadi M
Nat Commun 10(1):5759 . doi: 10.1038/s41467-019-13652-x
Publication date: December 17, 2019
PMID: 31848333
Synthesis and Biological Investigation of (+)-JD1, an Organometallic BET Bromodomain Inhibitor
Hassell-Hart S, Runcie A, Krojer T, Doyle J, Lineham E, Ocasio CA, Neto BAD, Fedorov O, Marsh G, Maple H, Felix R, Banks R, Ciulli A, Picaud S, Filippakopoulos P, Von Delft F, Brennan P, Stewart HJS, Chevassut TJ, Walker M, Austin C, Morley S, Spencer J
Organometallics . doi: 10.1021/acs.organomet.9b00750
Publication date: December 17, 2019
PMID:
Methyltransferase Inhibitors: Competing with, or Exploiting the Bound Cofactor.
Ferreira de Freitas R, Ivanochko D, Schapira M
Molecules 24(24): . doi: 10.3390/molecules24244492
Publication date: December 8, 2019
PMID: 31817960
Structural consequences of BMPR2 kinase domain mutations causing pulmonary arterial hypertension
BULLOCK A, Chaikuad A, Thangaratnarajah C, VON DELFT F
Scientific Reports 9:18351- . doi: 10.1038/s41598-019-54830-7
Publication date: December 4, 2019
PMID: 31797984
Chemical Probes for Protein Arginine Methyltransferases.
Ming Li AS, Li F, Eram MS, Bolotokova A, Dela Seña CC, Vedadi M
Methods . doi: 10.1016/j.ymeth.2019.11.017
Publication date: December 3, 2019
PMID: 31809836
Lipid Interactions of a Ciliary Membrane TRP Channel: Simulation and Structural Studies of Polycystin-2 (PC2)
WANG Q, COREY RA, Hedger G, Aryal P, GRIEBEN M, NASRALLAH C, Baronina A, PIKE A, Shi J, CARPENTER EP, SANSOM MSP
Structure 28:169-184.e5 . doi: 10.1016/j.str.2019.11.005
Publication date: December 2, 2019
PMID: 31806353

November 2019

Synthetic Peptides as Therapeutic Agents: Lessons Learned From Evolutionary Ancient Peptides and Their Transit Across Blood-Brain Barriers.
Lovejoy DA, Hogg DW, Dodsworth TL, Jurado FR, Read CC, D'Aquila AL, Barsyte-Lovejoy D
Front Endocrinol (Lausanne) 10:730 . doi: 10.3389/fendo.2019.00730
Publication date: November 30, 2019
PMID: 31781029
Structural Insights into Interaction Mechanisms of Alternative Piperazine-urea YEATS Domain Binders in MLLT1
Ni X, Heidenreich D, Christott T, Bennett J, Moustakim M, Brennan PE, Fedorov O, Knapp S, Chaikuad A
ACS Medicinal Chemistry Letters 10:1661-1666 . doi: 10.1021/acsmedchemlett.9b00460
Publication date: November 25, 2019
PMID: 31857843
Janus kinase inhibition for autoinflammation in patients with DNASE2 deficiency
Hong Y, Capitani M, Murphy C, Pandey S, Cavounidis A, Takeshita H, Nanthapisal S, Yasuda T, Bader-Meunier B, McCreary D, Omoyinmi E, Rao A, Booth C, Gilmour K, Sebire N, Shah N, Klein N, Bullock AN, Eleftheriou D, Uhlig HH, Brogan P
Journal of Allergy and Clinical Immunology 145:701-705.e8 . doi: 10.1016/j.jaci.2019.11.020
Publication date: November 24, 2019
PMID: 31775019
HMCES Functions in the Alternative End-Joining Pathway of the DNA DSB Repair during Class Switch Recombination in B Cells.
Shukla V, Halabelian L, Balagere S, Samaniego-Castruita D, Feldman DE, Arrowsmith CH, Rao A, Aravind L
Mol. Cell . doi: 10.1016/j.molcel.2019.10.031
Publication date: November 15, 2019
PMID: 31806351
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 9:16452- . doi: 10.1038/s41598-019-52795-1
Publication date: November 11, 2019
PMID: 31712618
Emerging tools to investigate bromodomain functions
Kougnassoukou Tchara PE, Filippakopoulos P, Lambert JP
Methods . doi: 10.1016/j.ymeth.2019.11.003
Publication date: November 11, 2019
PMID: 31726225
Towards the Development of an In vivo Chemical Probe for Cyclin G Associated Kinase (GAK)
Asquith CRM, Bennett JM, Su L, Laitinen T, Elkins JM, Pickett JE, Wells CI, Li Z, Willson TM, Zuercher WJ
Molecules (Basel, Switzerland) 24:- . doi: 10.3390/molecules24224016
Publication date: November 6, 2019
PMID: 31698822
Multiple direct interactions of TBP with the MYC oncoprotein.
Wei Y, Resetca D, Li Z, Johansson-Åkhe I, Ahlner A, Helander S, Wallenhammar A, Morad V, Raught B, Wallner B, Kokubo T, Tong Y, Penn LZ, Sunnerhagen M
Nat. Struct. Mol. Biol. . doi: 10.1038/s41594-019-0321-z
Publication date: November 4, 2019
PMID: 31686052
Microenvironmental IL1β promotes breast cancer metastatic colonisation in the bone via activation of Wnt signalling
eyres R, clarke R, FARNIE G
Nature Communications 10:5016- . doi: 10.1038/s41467-019-12807-0
Publication date: November 1, 2019
PMID: 31676788
Design and Analysis of the 4-Anilinoquin(az)oline Kinase Inhibition Profiles of GAK/SLK/STK10 Using Quantitative Structure-Activity Relationships
Asquith CRM, Laitinen T, Bennett JM, Wells CI, Elkins JM, Zuercher WJ, Tizzard GJ, Poso A
ChemMedChem 15:26-49 . doi: 10.1002/cmdc.201900521
Publication date: November 1, 2019
PMID: 31675459

October 2019

Targeted protein degradation: expanding the toolbox.
Schapira M, Calabrese MF, Bullock AN, Crews CM
Nat Rev Drug Discov . doi: 10.1038/s41573-019-0047-y
Publication date: October 30, 2019
PMID: 31666732
Targeted protein degradation: expanding the toolbox
Schapira M, Calabrese MF, Bullock AN, Crews CM
Nature Reviews Drug Discovery 18:949-963 . doi: 10.1038/s41573-019-0047-y
Publication date: October 30, 2019
PMID: 31666732
Discovery of small molecule antagonists of the USP5 zinc finger ubiquitin-binding domain.
Mann MK, Franzoni I, de Freitas RF, Tempel W, Houliston S, Smith L, Vedadi M, Arrowsmith CH, Harding RJ, Schapira M
J. Med. Chem. . doi: 10.1021/acs.jmedchem.9b00988
Publication date: October 30, 2019
PMID: 31663737
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 . doi: 10.1021/acsmedchemlett.9b00399
Publication date: October 29, 2019
PMID:

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