Inhibitors of JmjC-containing histone demethylases by Wright, M, Kawamura, A, Brennan, PE

Recent progress in histone demethylase inhibitors by McAllister, T, England, KS, Hopkinson, R, Brennan, PE, Kawamura, A, Schofield, CJ

Development of selective ADAMTS-5 peptide substrates to monitor proteinase activity by Fowkes, MM, Troeberg, L, Brennan, PE, Vincent, TL, Meldal, M, Lim, NH

Regulation of inositol 5-phosphatase activity by the C2 domain of SHIP1 and SHIP2 by Bradshaw, WJ, Kennedy, EC, Moreira, T, Smith, LA, Chalk, R, Katis, VL, Benesch, JLP, Brennan, PE, Murphy, EJ, Gileadi, O

Discovery and development strategies for SARS-CoV-2 NSP3 macrodomain inhibitors by Schuller, M, Zarganis-Tzitzikas, T, Bennett, J, De Cesco, S, Fearon, D, von Delft, F, Fedorov, O, Brennan, PE, Ahel, I

A phenotypic high-content, high-throughput screen identifies inhibitors of NLRP3 inflammasome activation by Nizami, S, Millar, V, Arunasalam, K, Zarganes-Tzitzikas, T, Brough, D, Tresadern, G, Brennan, PE, Davis, JB, Ebner, D, Di Daniel, E

Fragment screening reveals starting points for rational design of galactokinase 1 inhibitors to treat classic galactosemia by Mackinnon, SR, Krojer, T, Foster, WR, Diaz-Saez, L, Tang, M, Huber, KVM, von Delft, F, Lai, K, Brennan, PE, Arruda Bezerra, G, Yue, WW

Structural premise of selective deubiquitinase USP30 inhibition by small-molecule benzosulfonamides by O’Brien, DP, Jones, HBL, Guenther, F, Murphy, EJ, England, KS, Vendrell, I, Anderson, M, Brennan, PE, Davis, JB, Pinto-Fernández, A, Turnbull, AP, Kessler, BM

Synthesis of meta-substituted arene bioisosteres from [3.1.1]propellane by Frank, N, Nugent, J, Shire, BR, Pickford, HD, Rabe, P, Sterling, AJ, Zarganes-Tzitzikas, T, Grimes, T, Thompson, AL, Smith, RC, Schofield, CJ, Brennan, PE, Duarte, F, Anderson, EA

Alzheimer’s disease drug discovery: targeting Dickkopf-1 induction of the Wnt-PCP non-canonical pathway by Johanssen, T, Wren, SP, Woffindale, C, Priestley, R, De Cesco, S, Ehebauer, MT, Dixon-Clarke, S, Katsouri, L, England, K, Bennet, JM, Fedorov, O, Brennan, PE, Di Daniel, E, Davis, JB

An activity-based probe targeting non-catalytic, highly conserved amino acid residues within bromodomains by D'Ascenzio, M, Pugh, KM, Konietzny, R, Berridge, G, Tallant, C, Hashem, S, Monteiro, O, Thomas, JR, Schirle, M, Knapp, S, Marsden, B, Fedorov, O, Bountra, C, Kessler, BM, Brennan, PE

Inhibition of the SUV4-20 H1 histone methyltransferase increases frataxin expression in Friedreich's ataxia patient cells by Vilema Enriquez, MG, Quinlan, R, Kilfeather, P, Mazzone, R, Saqlain, S, Del Molino Del Barrio, I, Donato, A, Corda, G, Li, F, Vedadi, M, Németh, AH, Brennan, PE, Wade-Martins, R

Inhibition of histone H3K27 demethylases inactivates brachyury (TBXT) and promotes chordoma cell death by Cottone, L, Cribbs, AP, Khandelwal, G, Wells, G, Ligammari, L, Philpott, M, Tumber, A, Lombard, P, Hookway, ES, Szommer, T, Johansson, C, Brennan, PE, Pillay, N, Jenner, RG, Oppermann, U, Flanagan, AM

The structural basis of fatty acid elongation by the ELOVL elongases by Nie, L, Pascoa, TC, Pike, ACW, Bushell, SR, Quigley, A, Ruda, GF, Chu, A, Cole, V, Speedman, D, Moreira, T, Shrestha, L, Mukhopadhyay, SMM, Burgess-Brown, NA, Love, JD, Brennan, PE, Carpenter, EP

Structural dynamics of the ubiquitin specific protease UPS30 in complex with a cyanopyrrolidine-containing covalent inhibitor by O’Brien, DP, Jones, HBL, Shi, Y, Guenther, F, Vendrell, I, Viner, R, Brennan, PE, Mead, E, Zarganes-Tzitzikas, T, Davis, JB, Pinto-Fernández, A, England, KS, Murphy, EJ, Turnbull, AP, Kessler, BM

Discovery of a highly selective cell-active inhibitor of the histone lysine demethylases KDM2/7 by Gerken, PA, Wolstenhulme, JR, Tumber, AM, Hatch, SB, Zhang, Y, Müller, S, Chandler, SA, Mair, B, Li, F, Nijman, SMB, Konietzny, R, Szommer, T, Yapp, C, Fedorov, O, Benesch, JLP, Vedadi, M, Kessler, BM, Kawamura, A, Brennan, PE, Smith, MD

Unexpected Noncovalent Off-Target Activity of Clinical BTK Inhibitors Leads to Discovery of a Dual NUDT5/14 Antagonist by Balıkçı, E, Marques, AMC, Bauer, LG, Seupel, R, Bennett, J, Raux, B, Buchan, K, Simelis, K, Singh, U, Rogers, C, Ward, J, Cheng, C, Szommer, T, Schützenhofer, K, Elkins, JM, Sloman, DL, Ahel, I, Fedorov, O, Brennan, PE, Huber, KVM

ALK2 inhibitors display beneficial effects in preclinical models of ACVR1 mutant diffuse intrinsic pontine glioma by Carvalho, D, Taylor, KR, Olaciregui, NG, Molinari, V, Clarke, M, Mackay, A, Ruddle, R, Henley, A, Valenti, M, Hayes, A, Brandon, ADH, Eccles, SA, Raynaud, F, Boudhar, A, Monje, M, Popov, S, Moore, AS, Mora, J, Cruz, O, Vinci, M, Brennan, PE, Bullock, AN, Carcaboso, AM, Jones, C

Identification of a chemical probe for family VIII bromodomains through optimization of a fragment hit by Gerstenberger, BS, Trzupek, JD, Tallant, C, Fedorov, O, Filippakopoulos, P, Brennan, PE, Fedele, V, Martin, S, Picaud, S, Rogers, C, Parikh, M, Taylor, A, Samas, B, O'Mahony, A, Berg, E, Pallares, G, Torrey, AD, Treiber, DK, Samardjiev, IJ, Nasipak, BT, Padilla-Benavides, T, Wu, Q, Imbalzano, AN, Nickerson, JA, Bunnage, ME, Müller, S, Knapp, S, Owen, DR

Selective targeting of bromodomains of the bromodomain-PHD fingers family impairs osteoclast differentiation by Meier, JC, Tallant, C, Fedorov, O, Witwicka, H, Hwang, SY, van Stiphout, RG, Lambert, JP, Rogers, C, Yapp, C, Gerstenberger, BS, Fedele, V, Savitsky, P, Heidenreich, D, Daniels, DL, Owen, DR, Fish, PV, Igoe, NM, Bayle, ED, Haendler, B, Oppermann, UCT, Buffa, F, Brennan, PE, Müller, S, Gingras, AC, Odgren, PR, Birnbaum, MJ, Knapp, S