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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: falk h. Nature. 2018 Aug;560(7717):253-257. doi: 10.1038/s41586-018-0387-5. Epub 2018 Aug 1. Nature. 2018. PMID: 30069049
Characterization of the novel broad-spectrum kinase inhibitor CTx-0294885 as an affinity reagent for mass spectrometry-based kinome profiling.
Zhang L, Holmes IP, Hochgräfe F, Walker SR, Ali NA, Humphrey ES, Wu J, de Silva M, Kersten WJ, Connor T, Falk H, Allan L, Street IP, Bentley JD, Pilling PA, Monahan BJ, Peat TS, Daly RJ. Zhang L, et al. Among authors: falk h. J Proteome Res. 2013 Jul 5;12(7):3104-16. doi: 10.1021/pr3008495. Epub 2013 Jun 25. J Proteome Res. 2013. PMID: 23692254
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: falk h. Nat Commun. 2015 Mar 17;6:6442. doi: 10.1038/ncomms7442. Nat Commun. 2015. PMID: 25778803 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: falk h. 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
Regulation of PRMT5-MDM4 axis is critical in the response to CDK4/6 inhibitors in melanoma.
AbuHammad S, Cullinane C, Martin C, Bacolas Z, Ward T, Chen H, Slater A, Ardley K, Kirby L, Chan KT, Brajanovski N, Smith LK, Rao AD, Lelliott EJ, Kleinschmidt M, Vergara IA, Papenfuss AT, Lau P, Ghosh P, Haupt S, Haupt Y, Sanij E, Poortinga G, Pearson RB, Falk H, Curtis DJ, Stupple P, Devlin M, Street I, Davies MA, McArthur GA, Sheppard KE. AbuHammad S, et al. Among authors: falk h. Proc Natl Acad Sci U S A. 2019 Sep 3;116(36):17990-18000. doi: 10.1073/pnas.1901323116. Epub 2019 Aug 22. Proc Natl Acad Sci U S A. 2019. PMID: 31439820 Free PMC article.
HBO1 is required for the maintenance of leukaemia stem cells.
MacPherson L, Anokye J, Yeung MM, Lam EYN, Chan YC, Weng CF, Yeh P, Knezevic K, Butler MS, Hoegl A, Chan KL, Burr ML, Gearing LJ, Willson T, Liu J, Choi J, Yang Y, Bilardi RA, Falk H, Nguyen N, Stupple PA, Peat TS, Zhang M, de Silva M, Carrasco-Pozo C, Avery VM, Khoo PS, Dolezal O, Dennis ML, Nuttall S, Surjadi R, Newman J, Ren B, Leaver DJ, Sun Y, Baell JB, Dovey O, Vassiliou GS, Grebien F, Dawson SJ, Street IP, Monahan BJ, Burns CJ, Choudhary C, Blewitt ME, Voss AK, Thomas T, Dawson MA. MacPherson L, et al. Among authors: falk h. Nature. 2020 Jan;577(7789):266-270. doi: 10.1038/s41586-019-1835-6. Epub 2019 Dec 11. Nature. 2020. PMID: 31827282
Discovery of Acylsulfonohydrazide-Derived Inhibitors of the Lysine Acetyltransferase, KAT6A, as Potent Senescence-Inducing Anti-Cancer Agents.
Priebbenow DL, Leaver DJ, Nguyen N, Cleary B, Lagiakos HR, Sanchez J, Xue L, Huang F, Sun Y, Mujumdar P, Mudududdla R, Varghese S, Teguh S, Charman SA, White KL, Shackleford DM, Katneni K, Cuellar M, Strasser JM, Dahlin JL, Walters MA, Street IP, Monahan BJ, Jarman KE, Jousset Sabroux H, Falk H, Chung MC, Hermans SJ, Downer NL, Parker MW, Voss AK, Thomas T, Baell JB. Priebbenow DL, et al. Among authors: falk h. J Med Chem. 2020 May 14;63(9):4655-4684. doi: 10.1021/acs.jmedchem.9b02071. Epub 2020 Mar 19. J Med Chem. 2020. PMID: 32118427
447 results