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Page 1
Overcoming Preclinical Safety Obstacles to Discover (S)-N-((1,2,3,5,6,7-Hexahydro-s-indacen-4-yl)carbamoyl)-6-(methylamino)-6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine-3-sulfonamide (GDC-2394): A Potent and Selective NLRP3 Inhibitor.
McBride C, Trzoss L, Povero D, Lazic M, Ambrus-Aikelin G, Santini A, Pranadinata R, Bain G, Stansfield R, Stafford JA, Veal J, Takahashi R, Ly J, Chen S, Liu L, Nespi M, Blake R, Katewa A, Kleinheinz T, Sujatha-Bhaskar S, Ramamoorthi N, Sims J, McKenzie B, Chen M, Ultsch M, Johnson M, Murray J, Ciferri C, Staben ST, Townsend MJ, Stivala CE. McBride C, et al. Among authors: nespi m. J Med Chem. 2022 Nov 10;65(21):14721-14739. doi: 10.1021/acs.jmedchem.2c01250. Epub 2022 Oct 24. J Med Chem. 2022. PMID: 36279149
Discovery of Selective Tertiary Amide Inhibitors of Cyclin-Dependent Kinase 2 (CDK2).
Zeng M, Grandner JM, Bryan MC, Verma V, Larouche-Gauthier R, Leclerc JP, Zhao L, Haghshenas P, Aubert-Nicol S, Yadav A, Ashley M, Chen JZ, Durk M, Samy KE, Nespi M, Levy E, Merrick K, Moffat JG, Murray J, Oh A, Orr C, Segal E, Sims J, Sneeringer C, Prangley M, Vartanian S, Magnuson S, Parr BT. Zeng M, et al. Among authors: nespi m. ACS Med Chem Lett. 2023 Aug 24;14(9):1179-1187. doi: 10.1021/acsmedchemlett.3c00142. eCollection 2023 Sep 14. ACS Med Chem Lett. 2023. PMID: 37736184 Free PMC article.
Association of Combination of Conformation-Specific KIT Inhibitors With Clinical Benefit in Patients With Refractory Gastrointestinal Stromal Tumors: A Phase 1b/2a Nonrandomized Clinical Trial.
Wagner AJ, Severson PL, Shields AF, Patnaik A, Chugh R, Tinoco G, Wu G, Nespi M, Lin J, Zhang Y, Ewing T, Habets G, Burton EA, Matusow B, Tsai J, Tsang G, Shellooe R, Carias H, Chan K, Rezaei H, Sanftner L, Marimuthu A, Spevak W, Ibrahim PN, Inokuchi K, Alcantar O, Michelson G, Tsiatis AC, Zhang C, Bollag G, Trent JC, Tap WD. Wagner AJ, et al. Among authors: nespi m. JAMA Oncol. 2021 Sep 1;7(9):1343-1350. doi: 10.1001/jamaoncol.2021.2086. JAMA Oncol. 2021. PMID: 34236401 Free PMC article. Clinical Trial.
Sustained microglial depletion with CSF1R inhibitor impairs parenchymal plaque development in an Alzheimer's disease model.
Spangenberg E, Severson PL, Hohsfield LA, Crapser J, Zhang J, Burton EA, Zhang Y, Spevak W, Lin J, Phan NY, Habets G, Rymar A, Tsang G, Walters J, Nespi M, Singh P, Broome S, Ibrahim P, Zhang C, Bollag G, West BL, Green KN. Spangenberg E, et al. Among authors: nespi m. Nat Commun. 2019 Aug 21;10(1):3758. doi: 10.1038/s41467-019-11674-z. Nat Commun. 2019. PMID: 31434879 Free PMC article.
PLX9486 shows anti-tumor efficacy in patient-derived, tyrosine kinase inhibitor-resistant KIT-mutant xenograft models of gastrointestinal stromal tumors.
Gebreyohannes YK, Burton EA, Wozniak A, Matusow B, Habets G, Wellens J, Cornillie J, Lin J, Nespi M, Wu G, Zhang C, Bollag G, Debiec-Rychter M, Sciot R, Schöffski P. Gebreyohannes YK, et al. Among authors: nespi m. Clin Exp Med. 2019 May;19(2):201-210. doi: 10.1007/s10238-018-0541-2. Epub 2018 Dec 6. Clin Exp Med. 2019. PMID: 30523507
BRD4 Profiling Identifies Critical Chronic Lymphocytic Leukemia Oncogenic Circuits and Reveals Sensitivity to PLX51107, a Novel Structurally Distinct BET Inhibitor.
Ozer HG, El-Gamal D, Powell B, Hing ZA, Blachly JS, Harrington B, Mitchell S, Grieselhuber NR, Williams K, Lai TH, Alinari L, Baiocchi RA, Brinton L, Baskin E, Cannon M, Beaver L, Goettl VM, Lucas DM, Woyach JA, Sampath D, Lehman AM, Yu L, Zhang J, Ma Y, Zhang Y, Spevak W, Shi S, Severson P, Shellooe R, Carias H, Tsang G, Dong K, Ewing T, Marimuthu A, Tantoy C, Walters J, Sanftner L, Rezaei H, Nespi M, Matusow B, Habets G, Ibrahim P, Zhang C, Mathé EA, Bollag G, Byrd JC, Lapalombella R. Ozer HG, et al. Among authors: nespi m. Cancer Discov. 2018 Apr;8(4):458-477. doi: 10.1158/2159-8290.CD-17-0902. Epub 2018 Jan 31. Cancer Discov. 2018. PMID: 29386193 Free PMC article.
RAF inhibitors that evade paradoxical MAPK pathway activation.
Zhang C, Spevak W, Zhang Y, Burton EA, Ma Y, Habets G, Zhang J, Lin J, Ewing T, Matusow B, Tsang G, Marimuthu A, Cho H, Wu G, Wang W, Fong D, Nguyen H, Shi S, Womack P, Nespi M, Shellooe R, Carias H, Powell B, Light E, Sanftner L, Walters J, Tsai J, West BL, Visor G, Rezaei H, Lin PS, Nolop K, Ibrahim PN, Hirth P, Bollag G. Zhang C, et al. Among authors: nespi m. Nature. 2015 Oct 22;526(7574):583-6. doi: 10.1038/nature14982. Epub 2015 Oct 14. Nature. 2015. PMID: 26466569
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