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Page 1
Identification of Purines and 7-Deazapurines as Potent and Selective Type I Inhibitors of Troponin I-Interacting Kinase (TNNI3K).
Lawhorn BG, Philp J, Zhao Y, Louer C, Hammond M, Cheung M, Fries H, Graves AP, Shewchuk L, Wang L, Cottom JE, Qi H, Zhao H, Totoritis R, Zhang G, Schwartz B, Li H, Sweitzer S, Holt DA, Gatto GJ Jr, Kallander LS. Lawhorn BG, et al. Among authors: graves ap. J Med Chem. 2015 Sep 24;58(18):7431-48. doi: 10.1021/acs.jmedchem.5b00931. Epub 2015 Sep 10. J Med Chem. 2015. PMID: 26355916
Inhibition of the cardiomyocyte-specific kinase TNNI3K limits oxidative stress, injury, and adverse remodeling in the ischemic heart.
Vagnozzi RJ, Gatto GJ Jr, Kallander LS, Hoffman NE, Mallilankaraman K, Ballard VL, Lawhorn BG, Stoy P, Philp J, Graves AP, Naito Y, Lepore JJ, Gao E, Madesh M, Force T. Vagnozzi RJ, et al. Among authors: graves ap. Sci Transl Med. 2013 Oct 16;5(207):207ra141. doi: 10.1126/scitranslmed.3006479. Sci Transl Med. 2013. PMID: 24132636 Free PMC article.
Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2.
Verma SK, Tian X, LaFrance LV, Duquenne C, Suarez DP, Newlander KA, Romeril SP, Burgess JL, Grant SW, Brackley JA, Graves AP, Scherzer DA, Shu A, Thompson C, Ott HM, Aller GS, Machutta CA, Diaz E, Jiang Y, Johnson NW, Knight SD, Kruger RG, McCabe MT, Dhanak D, Tummino PJ, Creasy CL, Miller WH. Verma SK, et al. Among authors: graves ap. ACS Med Chem Lett. 2012 Oct 19;3(12):1091-6. doi: 10.1021/ml3003346. eCollection 2012 Dec 13. ACS Med Chem Lett. 2012. PMID: 24900432 Free PMC article.
GSK114: A selective inhibitor for elucidating the biological role of TNNI3K.
Lawhorn BG, Philp J, Graves AP, Shewchuk L, Holt DA, Gatto GJ Jr, Kallander LS. Lawhorn BG, et al. Among authors: graves ap. Bioorg Med Chem Lett. 2016 Jul 15;26(14):3355-3358. doi: 10.1016/j.bmcl.2016.05.033. Epub 2016 May 14. Bioorg Med Chem Lett. 2016. PMID: 27246618
A High-Throughput Dose-Response Cellular Thermal Shift Assay for Rapid Screening of Drug Target Engagement in Living Cells, Exemplified Using SMYD3 and IDO1.
McNulty DE, Bonnette WG, Qi H, Wang L, Ho TF, Waszkiewicz A, Kallal LA, Nagarajan RP, Stern M, Quinn AM, Creasy CL, Su DS, Graves AP, Annan RS, Sweitzer SM, Holbert MA. McNulty DE, et al. Among authors: graves ap. SLAS Discov. 2018 Jan;23(1):34-46. doi: 10.1177/2472555217732014. Epub 2017 Sep 28. SLAS Discov. 2018. PMID: 28957646 Free article.
Discovery of a crystalline sulforaphane analog with good solid-state stability and engagement of the Nrf2 pathway in vitro and in vivo.
Boehm J, Davis R, Murar CE, Li T, McCleland B, Dong S, Yan H, Kerns J, Moody CJ, Wilson AJ, Graves AP, Mentzer M, Qi H, Yonchuk J, Kou JP, Foley J, Sanchez Y, Podolin PL, Bolognese B, Booth-Genthe C, Galop M, Wolfe L, Carr R, Callahan JF. Boehm J, et al. Among authors: graves ap. Bioorg Med Chem. 2019 Feb 15;27(4):579-588. doi: 10.1016/j.bmc.2018.12.026. Epub 2018 Dec 21. Bioorg Med Chem. 2019. PMID: 30626555
Discovery of Isoxazole Amides as Potent and Selective SMYD3 Inhibitors.
Su DS, Qu J, Schulz M, Blackledge CW, Yu H, Zeng J, Burgess J, Reif A, Stern M, Nagarajan R, Pappalardi MB, Wong K, Graves AP, Bonnette W, Wang L, Elkins P, Knapp-Reed B, Carson JD, McHugh C, Mohammad H, Kruger R, Luengo J, Heerding DA, Creasy CL. Su DS, et al. Among authors: graves ap. ACS Med Chem Lett. 2019 Dec 27;11(2):133-140. doi: 10.1021/acsmedchemlett.9b00493. eCollection 2020 Feb 13. ACS Med Chem Lett. 2019. PMID: 32071679 Free PMC article.
27 results