Publications

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Displaying 251 - 300 of 2157

2020

January 2020

In Depth Analysis of Kinase Cross Screening Data to Identify CAMKK2 Inhibitory Scaffolds.
O'Byrne SN, Scott JW, Pilotte JR, Santiago ADS, Langendorf CG, Oakhill JS, Eduful BJ, Couñago RM, Wells CI, Zuercher WJ, Willson TM, Drewry DH
Molecules 25(2): . doi: 10.3390/molecules25020325
Publication date: January 13, 2020
PMID: 31941153
Overcoming Fungal Echinocandin Resistance through Inhibition of the Non-essential Stress Kinase Yck2.
Caplan T, Lorente-Macías Á, Stogios PJ, Evdokimova E, Hyde S, Wellington MA, Liston S, Iyer KR, Puumala E, Shekhar-Guturja T, Robbins N, Savchenko A, Krysan DJ, Whitesell L, Zuercher WJ, Cowen LE
Cell Chem Biol . doi: 10.1016/j.chembiol.2019.12.008
Publication date: January 6, 2020
PMID: 31924499
Effects of epigenetic pathway inhibitors on corticotroph tumour AtT20 cells.
Lines KE, Filippakopoulos P, Stevenson M, Muller S, Lockstone HE, Wright B, Knapp S, Buck D, Bountra C, Thakker RV
Endocr. Relat. Cancer . doi: 10.1530/ERC-19-0448
Publication date: January 1, 2020
PMID: 31935194
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
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. . doi: 10.1074/jbc.RA119.010365
Publication date: December 30, 2019
PMID: 31914405
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:
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
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 Med Chem Lett 10(12):1661-1666 . doi: 10.1021/acsmedchemlett.9b00460
Publication date: December 12, 2019
PMID: 31857843
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.
Chaikuad A, Thangaratnarajah C, von Delft F, Bullock AN
Sci Rep 9(1):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
Development of Macrocycle Kinase Inhibitors for ALK2 Using Fibrodysplasia Ossificans Progressiva-Derived Endothelial Cells.
Sánchez-Duffhues G, Williams E, Benderitter P, Orlova V, van Wijhe M, Garcia de Vinuesa A, Kerr G, Caradec J, Lodder K, de Boer HC, Goumans MJ, Eekhoff EMW, Morales-Piga A, Bachiller-Corral J, Koolwijk P, Bullock AN, Hoflack J, Ten Dijke P
JBMR Plus 3(11):e10230 . doi: 10.1002/jbm4.10230
Publication date: November 27, 2019
PMID: 31768489
Lipid Interactions of a Ciliary Membrane TRP Channel: Simulation and Structural Studies of Polycystin-2.
Wang Q, Corey RA, Hedger G, Aryal P, Grieben M, Nasrallah C, Baronina A, Pike ACW, Shi J, Carpenter EP, Sansom MSP
Structure . doi: 10.1016/j.str.2019.11.005
Publication date: November 27, 2019
PMID: 31806353
The fungal metabolite chaetocin is a sensitizer for pro-apoptotic therapies in glioblastoma.
Ozyerli-Goknar E, Sur-Erdem I, Seker F, Cingöz A, Kayabolen A, Kahya-Yesil Z, Uyulur F, Gezen M, Tolay N, Erman B, Gönen M, Dunford J, Oppermann U, Bagci-Onder T
Cell Death Dis 10(12):894 . doi: 10.1038/s41419-019-2107-y
Publication date: November 26, 2019
PMID: 31772153
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
Janus kinase inhibition for autoinflammation in 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
J. Allergy Clin. Immunol. . doi: 10.1016/j.jaci.2019.11.020
Publication date: November 24, 2019
PMID: 31775019
An epigenetic screening determines BET proteins as targets to suppress self-renewal and tumorigenicity in canine mammary cancer cells.
Xavier PLP, Cordeiro YG, Alexandre PA, Pires PRL, Saranholi BH, Silva ER, Müller S, Fukumasu H
Sci Rep 9(1):17363 . doi: 10.1038/s41598-019-53915-7
Publication date: November 22, 2019
PMID: 31758045
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
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
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 9(1):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
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
A fast iterative synthetic approach towards the identification of novel highly selective p38 MAP kinase inhibitors.
Röhm S, Berger BT, Schröder M, Chaikuad A, Winkel R, Hekking KFW, Benningshof JJC, Mueller G, Tesch R, Kudolo M, Forster M, Laufer SA, Knapp S
J. Med. Chem. . doi: 10.1021/acs.jmedchem.9b01227
Publication date: November 8, 2019
PMID: 31702918
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 24(22): . doi: 10.3390/molecules24224016
Publication date: November 6, 2019
PMID: 31698822
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
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
Design and analysis of the 4-anilino-quin(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 G, Poso A
ChemMedChem . doi: 10.1002/cmdc.201900521
Publication date: November 1, 2019
PMID: 31675459
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

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:
A chemical probe of CARM1 alters epigenetic plasticity against breast cancer cell invasion.
Cai XC, Zhang T, Kim EJ, Jiang M, Wang K, Wang J, Chen S, Zhang N, Wu H, Li F, Dela Seña CC, Zeng H, Vivcharuk V, Niu X, Zheng W, Lee JP, Chen Y, Barsyte D, Szewczyk M, Hajian T, Ibáñez G, Dong A, Dombrovski L, Zhang Z, Deng H, Min J, Arrowsmith CH, Mazutis L, Shi L, Vedadi M, Brown PJ, Xiang J, Qin LX, Xu W, Luo M
Elife 8: . doi: 10.7554/eLife.47110
Publication date: October 28, 2019
PMID: 31657716
Aspartate/asparagine-β-hydroxylase crystal structures reveal an unexpected epidermal growth factor-like domain substrate disulfide pattern.
Pfeffer I, Brewitz L, Krojer T, Jensen SA, Kochan GT, Kershaw NJ, Hewitson KS, McNeill LA, Kramer H, Münzel M, Hopkinson RJ, Oppermann U, Handford PA, McDonough MA, Schofield CJ
Nat Commun 10(1):4910 . doi: 10.1038/s41467-019-12711-7
Publication date: October 28, 2019
PMID: 31659163
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 J, Pinto-Fernandez A, Cornelissen L, BONHAM S, DIAZ SAEZ L, Riant O, HUBER K, KESSLER B, Feron O, Tate E
ChemRxiv . doi:
Publication date: October 24, 2019
PMID:
A structure-guided molecular chaperone approach for restoring the transcriptional activity of the p53 cancer mutant Y220C.
Bauer MR, Jones RN, Tareque RK, Springett B, Dingler FA, Verduci L, Patel KJ, Fersht AR, Joerger AC, Spencer J
Future Med Chem 11(19):2491-2504 . doi: 10.4155/fmc-2019-0181
Publication date: October 22, 2019
PMID: 31633398
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 10:1105 . doi: 10.3389/fpls.2019.01105
Publication date: October 18, 2019
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 8: . doi: 10.7554/eLife.48363
Publication date: October 15, 2019
PMID: 31612854
Structural basis for the recognition of non-methylated DNA by the CXXC domain.
Liu K, Min J
J. Mol. Biol. . doi: 10.1016/j.jmb.2019.09.025
Publication date: October 15, 2019
PMID: 31626811
Lessons from LIMK1 enzymology and their impact on inhibitor design.
Salah E, Chatterjee D, Beltrami A, Tumber A, Preuss F, Canning P, Chaikuad A, Knaus P, Knapp S, Bullock AN, Mathea S
Biochem. J. . doi: 10.1042/BCJ20190517
Publication date: October 14, 2019
PMID: 31652302
Quinazoline-based anti-virulence compounds selectively target Salmonella PhoP/PhoQ signal transduction system.
Carabajal MA, Asquith CRM, Laitinen T, Tizzard GJ, Yim L, Rial A, Chabalgoity JA, Zuercher WJ, García Véscovi E
Antimicrob. Agents Chemother. . doi: 10.1128/AAC.01744-19
Publication date: October 14, 2019
PMID: 31611347
Lessons from LIMK1 enzymology and their impact on inhibitor design
Salah E, Chatterjee D, Beltrami A, Tumber A, Preuss F, Canning P, Chaikuad A, Knaus P, Knapp S, Bullock AN, Mathea S
Biochemical Journal 476:3197-3209 . doi: 10.1042/bcj20190517
Publication date: October 13, 2019
PMID: 31652302
Development of macrocycle kinase inhibitors for ALK2 using Fibrodysplasia ossificans progressiva-derived endothelial cells
BULLOCK A, WILLIAMS E, KERR G
JBMR Plus 3:e10230- . doi: 10.1002/jbm4.10230
Publication date: October 6, 2019
PMID: 31768489
Targeting non-bromodomain chromatin readers.
Arrowsmith CH, Schapira M
Nat. Struct. Mol. Biol. 26(10):863-869 . doi: 10.1038/s41594-019-0290-2
Publication date: October 5, 2019
PMID: 31582844
SuCOS is Better than RMSD for Evaluating Fragment Elaboration and Docking Poses
Leung S, Bodkin M, von Delft F, Brennan P, Morris G
ChemRxiv . doi: 10.26434/chemrxiv.8100203.v1
Publication date: October 4, 2019
PMID:
Cryo-EM structures of the human glutamine transporter SLC1A5 (ASCT2) in the outward-facing conformation.
Yu X, Plotnikova O, Bonin PD, Subashi TA, McLellan TJ, Dumlao D, Che Y, Dong YY, Carpenter EP, West GM, Qiu X, Culp JS, Han S
Elife 8: . doi: 10.7554/eLife.48120
Publication date: October 3, 2019
PMID: 31580259

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