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Profile of a Highly Selective Quaternized Pyrrolidine Betaine αvβ6 Integrin Inhibitor-(3S)-3-(3-(3,5-Dimethyl-1H-pyrazol-1-yl)phenyl)-4-((1S and 1R,3R)-1-methyl-3-(2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl)pyrrolidin-1-ium-1-yl)butanoate Synthesized by Stereoselective Methylation.
Barrett TN, Taylor JA, Barker D, Procopiou PA, Thompson JDF, Barrett J, Le J, Lynn SM, Pogany P, Pratley C, Pritchard JM, Roper JA, Rowedder JE, Slack RJ, Vitulli G, Macdonald SJF, Kerr WJ. Barrett TN, et al. Among authors: kerr wj. J Med Chem. 2019 Aug 22;62(16):7543-7556. doi: 10.1021/acs.jmedchem.9b00819. Epub 2019 Aug 5. J Med Chem. 2019. PMID: 31381331 Free article.
Design, synthesis and antibacterial properties of pyrimido[4,5-b]indol-8-amine inhibitors of DNA gyrase.
McGarry DH, Cooper IR, Walker R, Warrilow CE, Pichowicz M, Ratcliffe AJ, Salisbury AM, Savage VJ, Moyo E, Maclean J, Smith A, Charrier C, Stokes NR, Lindsay DM, Kerr WJ. McGarry DH, et al. Among authors: kerr wj. Bioorg Med Chem Lett. 2018 Sep 15;28(17):2998-3003. doi: 10.1016/j.bmcl.2018.05.049. Epub 2018 May 26. Bioorg Med Chem Lett. 2018. PMID: 30122228 Free article.
Structure-Based Design of a Bromodomain and Extraterminal Domain (BET) Inhibitor Selective for the N-Terminal Bromodomains That Retains an Anti-inflammatory and Antiproliferative Phenotype.
Wellaway CR, Bamborough P, Bernard SG, Chung CW, Craggs PD, Cutler L, Demont EH, Evans JP, Gordon L, Karamshi B, Lewis AJ, Lindon MJ, Mitchell DJ, Rioja I, Soden PE, Taylor S, Watson RJ, Willis R, Woolven JM, Wyspiańska BS, Kerr WJ, Prinjha RK. Wellaway CR, et al. Among authors: kerr wj. J Med Chem. 2020 Sep 10;63(17):9020-9044. doi: 10.1021/acs.jmedchem.0c00566. Epub 2020 Aug 3. J Med Chem. 2020. PMID: 32787145 Free article.
Structure-Guided Design of a Domain-Selective Bromodomain and Extra Terminal N-Terminal Bromodomain Chemical Probe.
Bradley E, Fusani L, Chung CW, Craggs PD, Demont EH, Humphreys PG, Mitchell DJ, Phillipou A, Rioja I, Shah RR, Wellaway CR, Prinjha RK, Palmer DS, Kerr WJ, Reid M, Wall ID, Cookson R. Bradley E, et al. Among authors: kerr wj. J Med Chem. 2023 Dec 14;66(23):15728-15749. doi: 10.1021/acs.jmedchem.3c00906. Epub 2023 Nov 15. J Med Chem. 2023. PMID: 37967462 Free PMC article.
Discovery of novel irreversible inhibitors of interleukin (IL)-2-inducible tyrosine kinase (Itk) by targeting cysteine 442 in the ATP pocket.
Harling JD, Deakin AM, Campos S, Grimley R, Chaudry L, Nye C, Polyakova O, Bessant CM, Barton N, Somers D, Barrett J, Graves RH, Hanns L, Kerr WJ, Solari R. Harling JD, et al. Among authors: kerr wj. J Biol Chem. 2013 Sep 27;288(39):28195-206. doi: 10.1074/jbc.M113.474114. Epub 2013 Aug 9. J Biol Chem. 2013. PMID: 23935099 Free PMC article.
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