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Page 1
Evolution of Novartis' Small Molecule Screening Deck Design.
Schuffenhauer A, Schneider N, Hintermann S, Auld D, Blank J, Cotesta S, Engeloch C, Fechner N, Gaul C, Giovannoni J, Jansen J, Joslin J, Krastel P, Lounkine E, Manchester J, Monovich LG, Pelliccioli AP, Schwarze M, Shultz MD, Stiefl N, Baeschlin DK. Schuffenhauer A, et al. Among authors: shultz md. J Med Chem. 2020 Dec 10;63(23):14425-14447. doi: 10.1021/acs.jmedchem.0c01332. Epub 2020 Nov 3. J Med Chem. 2020. PMID: 33140646 Review.
Allosteric Inhibition of SHP2: Identification of a Potent, Selective, and Orally Efficacious Phosphatase Inhibitor.
Garcia Fortanet J, Chen CH, Chen YN, Chen Z, Deng Z, Firestone B, Fekkes P, Fodor M, Fortin PD, Fridrich C, Grunenfelder D, Ho S, Kang ZB, Karki R, Kato M, Keen N, LaBonte LR, Larrow J, Lenoir F, Liu G, Liu S, Lombardo F, Majumdar D, Meyer MJ, Palermo M, Perez L, Pu M, Ramsey T, Sellers WR, Shultz MD, Stams T, Towler C, Wang P, Williams SL, Zhang JH, LaMarche MJ. Garcia Fortanet J, et al. Among authors: shultz md. J Med Chem. 2016 Sep 8;59(17):7773-82. doi: 10.1021/acs.jmedchem.6b00680. Epub 2016 Jul 12. J Med Chem. 2016. PMID: 27347692
The design, synthesis and structure-activity relationships of novel isoindoline-based histone deacetylase inhibitors.
Shultz M, Fan J, Chen C, Cho YS, Davis N, Bickford S, Buteau K, Cao X, Holmqvist M, Hsu M, Jiang L, Liu G, Lu Q, Patel C, Suresh JR, Selvaraj M, Urban L, Wang P, Yan-Neale Y, Whitehead L, Zhang H, Zhou L, Atadja P. Shultz M, et al. Bioorg Med Chem Lett. 2011 Aug 15;21(16):4909-12. doi: 10.1016/j.bmcl.2011.06.015. Bioorg Med Chem Lett. 2011. PMID: 21742496
Human HDAC isoform selectivity achieved via exploitation of the acetate release channel with structurally unique small molecule inhibitors.
Whitehead L, Dobler MR, Radetich B, Zhu Y, Atadja PW, Claiborne T, Grob JE, McRiner A, Pancost MR, Patnaik A, Shao W, Shultz M, Tichkule R, Tommasi RA, Vash B, Wang P, Stams T. Whitehead L, et al. Bioorg Med Chem. 2011 Aug 1;19(15):4626-34. doi: 10.1016/j.bmc.2011.06.030. Epub 2011 Jun 15. Bioorg Med Chem. 2011. PMID: 21723733
Structure-Guided Design of EED Binders Allosterically Inhibiting the Epigenetic Polycomb Repressive Complex 2 (PRC2) Methyltransferase.
Lingel A, Sendzik M, Huang Y, Shultz MD, Cantwell J, Dillon MP, Fu X, Fuller J, Gabriel T, Gu J, Jiang X, Li L, Liang F, McKenna M, Qi W, Rao W, Sheng X, Shu W, Sutton J, Taft B, Wang L, Zeng J, Zhang H, Zhang M, Zhao K, Lindvall M, Bussiere DE. Lingel A, et al. Among authors: shultz md. J Med Chem. 2017 Jan 12;60(1):415-427. doi: 10.1021/acs.jmedchem.6b01473. Epub 2017 Jan 3. J Med Chem. 2017. PMID: 27992714
Optimization of the in vitro cardiac safety of hydroxamate-based histone deacetylase inhibitors.
Shultz MD, Cao X, Chen CH, Cho YS, Davis NR, Eckman J, Fan J, Fekete A, Firestone B, Flynn J, Green J, Growney JD, Holmqvist M, Hsu M, Jansson D, Jiang L, Kwon P, Liu G, Lombardo F, Lu Q, Majumdar D, Meta C, Perez L, Pu M, Ramsey T, Remiszewski S, Skolnik S, Traebert M, Urban L, Uttamsingh V, Wang P, Whitebread S, Whitehead L, Yan-Neale Y, Yao YM, Zhou L, Atadja P. Shultz MD, et al. J Med Chem. 2011 Jul 14;54(13):4752-72. doi: 10.1021/jm200388e. Epub 2011 Jun 17. J Med Chem. 2011. PMID: 21650221
47 results