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Conformational-Design-Driven Discovery of EZM0414: A Selective, Potent SETD2 Inhibitor for Clinical Studies.
Alford JS, Lampe JW, Brach D, Chesworth R, Cosmopoulos K, Duncan KW, Eckley ST, Kutok JL, Raimondi A, Riera TV, Shook B, Tang C, Totman J, Farrow NA. Alford JS, et al. Among authors: farrow na. ACS Med Chem Lett. 2022 Jun 7;13(7):1137-1143. doi: 10.1021/acsmedchemlett.2c00167. eCollection 2022 Jul 14. ACS Med Chem Lett. 2022. PMID: 35859865 Free PMC article.
Discovery of a First-in-Class Inhibitor of the Histone Methyltransferase SETD2 Suitable for Preclinical Studies.
Lampe JW, Alford JS, Boriak-Sjodin PA, Brach D, Cosmopoulos K, Duncan KW, Eckley ST, Foley MA, Harvey DM, Motwani V, Munchhof MJ, Raimondi A, Riera TV, Tang C, Thomenius MJ, Totman J, Farrow NA. Lampe JW, et al. Among authors: farrow na. ACS Med Chem Lett. 2021 Aug 24;12(10):1539-1545. doi: 10.1021/acsmedchemlett.1c00272. eCollection 2021 Oct 14. ACS Med Chem Lett. 2021. PMID: 34671445 Free PMC article.
Indole Inhibitors of MMP-13 for Arthritic Disorders.
Taylor SJ, Abeywardane A, Liang S, Xiong Z, Proudfoot JR, Farmer BS, Gao DA, Heim-Riether A, Smith-Keenan LL, Muegge I, Yu Y, Zhang Q, Souza D, Panzenbeck M, Goldberg D, Hill-Drzewi M, Margarit M, Collins B, Li JX, Zuvela-Jelaska L, Li J, Farrow NA. Taylor SJ, et al. Among authors: farrow na. ACS Omega. 2021 Jul 19;6(29):18635-18650. doi: 10.1021/acsomega.1c01320. eCollection 2021 Jul 27. ACS Omega. 2021. PMID: 34337203 Free PMC article.
Structural studies unravel the active conformation of apo RORγt nuclear receptor and a common inverse agonism of two diverse classes of RORγt inhibitors.
Li X, Anderson M, Collin D, Muegge I, Wan J, Brennan D, Kugler S, Terenzio D, Kennedy C, Lin S, Labadia ME, Cook B, Hughes R, Farrow NA. Li X, et al. Among authors: farrow na. J Biol Chem. 2017 Jul 14;292(28):11618-11630. doi: 10.1074/jbc.M117.789024. Epub 2017 May 25. J Biol Chem. 2017. PMID: 28546429 Free PMC article.
Crystal structure of human GDF11.
Padyana AK, Vaidialingam B, Hayes DB, Gupta P, Franti M, Farrow NA. Padyana AK, et al. Among authors: farrow na. Acta Crystallogr F Struct Biol Commun. 2016 Mar;72(Pt 3):160-4. doi: 10.1107/S2053230X16001588. Epub 2016 Feb 16. Acta Crystallogr F Struct Biol Commun. 2016. PMID: 26919518 Free PMC article.
Correction to Fragment-Based Discovery of Indole Inhibitors of Matrix Metalloproteinase-13.
Taylor SJ, Abeywardane A, Liang S, Muegge I, Padyana AK, Xiong Z, Hill-Drzewi M, Farmer B, Li X, Collins B, Li JX, Heim-Riether A, Proudfoot J, Zhang Q, Goldberg D, Zuvela-Jelaska L, Zaher H, Li J, Farrow NA. Taylor SJ, et al. Among authors: farrow na. J Med Chem. 2015 Aug 13;58(15):6318. doi: 10.1021/acs.jmedchem.5b00962. Epub 2015 Jul 27. J Med Chem. 2015. PMID: 26214135 No abstract available.
Fragment-based discovery of indole inhibitors of matrix metalloproteinase-13.
Taylor SJ, Abeywardane A, Liang S, Muegge I, Padyana AK, Xiong Z, Hill-Drzewi M, Farmer B, Li X, Collins B, Li JX, Heim-Riether A, Proudfoot J, Zhang Q, Goldberg D, Zuvela-Jelaska L, Zaher H, Li J, Farrow NA. Taylor SJ, et al. Among authors: farrow na. J Med Chem. 2011 Dec 8;54(23):8174-87. doi: 10.1021/jm201129m. Epub 2011 Nov 9. J Med Chem. 2011. PMID: 22017539
40 results