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Page 1
Inhibitors of histone acetyltransferases KAT6A/B induce senescence and arrest tumour growth.
Baell JB, Leaver DJ, Hermans SJ, Kelly GL, Brennan MS, Downer NL, Nguyen N, Wichmann J, McRae HM, Yang Y, Cleary B, Lagiakos HR, Mieruszynski S, Pacini G, Vanyai HK, Bergamasco MI, May RE, Davey BK, Morgan KJ, Sealey AJ, Wang B, Zamudio N, Wilcox S, Garnham AL, Sheikh BN, Aubrey BJ, Doggett K, Chung MC, de Silva M, Bentley J, Pilling P, Hattarki M, Dolezal O, Dennis ML, Falk H, Ren B, Charman SA, White KL, Rautela J, Newbold A, Hawkins ED, Johnstone RW, Huntington ND, Peat TS, Heath JK, Strasser A, Parker MW, Smyth GK, Street IP, Monahan BJ, Voss AK, Thomas T. Baell JB, et al. Among authors: parker mw. Nature. 2018 Aug;560(7717):253-257. doi: 10.1038/s41586-018-0387-5. Epub 2018 Aug 1. Nature. 2018. PMID: 30069049
A RIPK2 inhibitor delays NOD signalling events yet prevents inflammatory cytokine production.
Nachbur U, Stafford CA, Bankovacki A, Zhan Y, Lindqvist LM, Fiil BK, Khakham Y, Ko HJ, Sandow JJ, Falk H, Holien JK, Chau D, Hildebrand J, Vince JE, Sharp PP, Webb AI, Jackman KA, Mühlen S, Kennedy CL, Lowes KN, Murphy JM, Gyrd-Hansen M, Parker MW, Hartland EL, Lew AM, Huang DC, Lessene G, Silke J. Nachbur U, et al. Among authors: parker mw. Nat Commun. 2015 Mar 17;6:6442. doi: 10.1038/ncomms7442. Nat Commun. 2015. PMID: 25778803 Free article.
Discovery and SAR of novel pyrazolo[1,5-a]pyrimidines as inhibitors of CDK9.
Phillipson LJ, Segal DH, Nero TL, Parker MW, Wan SS, de Silva M, Guthridge MA, Wei AH, Burns CJ. Phillipson LJ, et al. Among authors: parker mw. Bioorg Med Chem. 2015 Oct 1;23(19):6280-96. doi: 10.1016/j.bmc.2015.08.035. Epub 2015 Aug 28. Bioorg Med Chem. 2015. PMID: 26349627
Transitional changes in the CRP structure lead to the exposure of proinflammatory binding sites.
Braig D, Nero TL, Koch HG, Kaiser B, Wang X, Thiele JR, Morton CJ, Zeller J, Kiefer J, Potempa LA, Mellett NA, Miles LA, Du XJ, Meikle PJ, Huber-Lang M, Stark GB, Parker MW, Peter K, Eisenhardt SU. Braig D, et al. Among authors: parker mw. Nat Commun. 2017 Jan 23;8:14188. doi: 10.1038/ncomms14188. Nat Commun. 2017. PMID: 28112148 Free PMC article.
Structural Determinants for Small-Molecule Activation of Skeletal Muscle AMPK α2β2γ1 by the Glucose Importagog SC4.
Ngoei KRW, Langendorf CG, Ling NXY, Hoque A, Varghese S, Camerino MA, Walker SR, Bozikis YE, Dite TA, Ovens AJ, Smiles WJ, Jacobs R, Huang H, Parker MW, Scott JW, Rider MH, Foitzik RC, Kemp BE, Baell JB, Oakhill JS. Ngoei KRW, et al. Among authors: parker mw. Cell Chem Biol. 2018 Jun 21;25(6):728-737.e9. doi: 10.1016/j.chembiol.2018.03.008. Epub 2018 Apr 12. Cell Chem Biol. 2018. PMID: 29657085 Free article.
Discovery of Benzoylsulfonohydrazides as Potent Inhibitors of the Histone Acetyltransferase KAT6A.
Leaver DJ, Cleary B, Nguyen N, Priebbenow DL, Lagiakos HR, Sanchez J, Xue L, Huang F, Sun Y, Mujumdar P, Mudududdla R, Varghese S, Teguh S, Charman SA, White KL, Katneni K, Cuellar M, Strasser JM, Dahlin JL, Walters MA, Street IP, Monahan BJ, Jarman KE, Sabroux HJ, Falk H, Chung MC, Hermans SJ, Parker MW, Thomas T, Baell JB. Leaver DJ, et al. Among authors: parker mw. J Med Chem. 2019 Aug 8;62(15):7146-7159. doi: 10.1021/acs.jmedchem.9b00665. Epub 2019 Jul 17. J Med Chem. 2019. PMID: 31256587
489 results