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A TRIM21-based bioPROTAC highlights the therapeutic benefit of HuR degradation.
Fletcher A, Clift D, de Vries E, Martinez Cuesta S, Malcolm T, Meghini F, Chaerkady R, Wang J, Chiang A, Weng SHS, Tart J, Wong E, Donohoe G, Rawlins P, Gordon E, Taylor JD, James L, Hunt J. Fletcher A, et al. Among authors: rawlins p. Nat Commun. 2023 Nov 4;14(1):7093. doi: 10.1038/s41467-023-42546-2. Nat Commun. 2023. PMID: 37925433 Free PMC article.
Design of rigid protein-protein interaction inhibitors enables targeting of undruggable Mcl-1.
Hargreaves D, Carbajo RJ, Bodnarchuk MS, Embrey K, Rawlins PB, Packer M, Degorce SL, Hird AW, Johannes JW, Chiarparin E, Schade M. Hargreaves D, et al. Among authors: rawlins pb. Proc Natl Acad Sci U S A. 2023 May 23;120(21):e2221967120. doi: 10.1073/pnas.2221967120. Epub 2023 May 15. Proc Natl Acad Sci U S A. 2023. PMID: 37186857 Free PMC article.
Fragment screening at AstraZeneca: developing the next generation biophysics fragment set.
Lucas SCC, Börjesson U, Bostock MJ, Cuff J, Edfeldt F, Embrey KJ, Eriksson PO, Gohlke A, Gunnarson A, Lainchbury M, Milbradt AG, Moore R, Rawlins PB, Sinclair I, Stubbs C, Storer RI. Lucas SCC, et al. Among authors: rawlins pb. RSC Med Chem. 2022 Jul 4;13(9):1052-1057. doi: 10.1039/d2md00154c. eCollection 2022 Sep 21. RSC Med Chem. 2022. PMID: 36324499 Free PMC article.
Pharmacological inhibition of MERTK induces in vivo retinal degeneration: a multimodal imaging ocular safety assessment.
Hamm G, Maglennon G, Williamson B, Macdonald R, Doherty A, Jones S, Harris J, Blades J, Harmer AR, Barton P, Rawlins PB, Smith P, Winter-Holt J, McMurray L, Johansson J, Fitzpatrick P, McCoull W, Coen M. Hamm G, et al. Among authors: rawlins pb. Arch Toxicol. 2022 Feb;96(2):613-624. doi: 10.1007/s00204-021-03197-8. Epub 2022 Jan 1. Arch Toxicol. 2022. PMID: 34973110 Free PMC article.
Diverse, Potent, and Efficacious Inhibitors That Target the EED Subunit of the Polycomb Repressive Complex 2 Methyltransferase.
Bagal SK, Gregson C, O' Donovan DH, Pike KG, Bloecher A, Barton P, Borodovsky A, Code E, Fillery SM, Hsu JH, Kawatkar SP, Li C, Longmire D, Nai Y, Nash SC, Pike A, Robinson J, Read JA, Rawlins PB, Shen M, Tang J, Wang P, Woods H, Williamson B. Bagal SK, et al. Among authors: rawlins pb. J Med Chem. 2021 Dec 9;64(23):17146-17183. doi: 10.1021/acs.jmedchem.1c01161. Epub 2021 Nov 22. J Med Chem. 2021. PMID: 34807608
Optimization of an Imidazo[1,2-a]pyridine Series to Afford Highly Selective Type I1/2 Dual Mer/Axl Kinase Inhibitors with In Vivo Efficacy.
McCoull W, Boyd S, Brown MR, Coen M, Collingwood O, Davies NL, Doherty A, Fairley G, Goldberg K, Hardaker E, He G, Hennessy EJ, Hopcroft P, Hodgson G, Jackson A, Jiang X, Karmokar A, Lainé AL, Lindsay N, Mao Y, Markandu R, McMurray L, McLean N, Mooney L, Musgrove H, Nissink JWM, Pflug A, Reddy VP, Rawlins PB, Rivers E, Schimpl M, Smith GF, Tentarelli S, Travers J, Troup RI, Walton J, Wang C, Wilkinson S, Williamson B, Winter-Holt J, Yang D, Zheng Y, Zhu Q, Smith PD. McCoull W, et al. Among authors: rawlins pb. J Med Chem. 2021 Sep 23;64(18):13524-13539. doi: 10.1021/acs.jmedchem.1c00920. Epub 2021 Sep 3. J Med Chem. 2021. PMID: 34478292
Free energy perturbation in the design of EED ligands as inhibitors of polycomb repressive complex 2 (PRC2) methyltransferase.
O' Donovan DH, Gregson C, Packer MJ, Greenwood R, Pike KG, Kawatkar S, Bloecher A, Robinson J, Read J, Code E, Hsu JH, Shen M, Woods H, Barton P, Fillery S, Williamson B, Rawlins PB, Bagal SK. O' Donovan DH, et al. Among authors: rawlins pb. Bioorg Med Chem Lett. 2021 May 1;39:127904. doi: 10.1016/j.bmcl.2021.127904. Epub 2021 Mar 6. Bioorg Med Chem Lett. 2021. PMID: 33684441
63 results