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119 results

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Page 1
Potent, Selective, and Orally Bioavailable Inhibitors of VPS34 Provide Chemical Tools to Modulate Autophagy in Vivo.
Honda A, Harrington E, Cornella-Taracido I, Furet P, Knapp MS, Glick M, Triantafellow E, Dowdle WE, Wiedershain D, Maniara W, Moore C, Finan PM, Hamann LG, Firestone B, Murphy LO, Keaney EP. Honda A, et al. Among authors: knapp ms. ACS Med Chem Lett. 2015 Nov 13;7(1):72-6. doi: 10.1021/acsmedchemlett.5b00335. eCollection 2016 Jan 14. ACS Med Chem Lett. 2015. PMID: 26819669 Free PMC article.
Identification and structure-activity relationship of 2-morpholino 6-(3-hydroxyphenyl) pyrimidines, a class of potent and selective PI3 kinase inhibitors.
Pecchi S, Renhowe PA, Taylor C, Kaufman S, Merritt H, Wiesmann M, Shoemaker KR, Knapp MS, Ornelas E, Hendrickson TF, Fantl W, Voliva CF. Pecchi S, et al. Among authors: knapp ms. Bioorg Med Chem Lett. 2010 Dec 1;20(23):6895-8. doi: 10.1016/j.bmcl.2010.10.021. Epub 2010 Oct 13. Bioorg Med Chem Lett. 2010. PMID: 21035331
Structure guided optimization of a fragment hit to imidazopyridine inhibitors of PI3K.
Pecchi S, Ni ZJ, Han W, Smith A, Lan J, Burger M, Merritt H, Wiesmann M, Chan J, Kaufman S, Knapp MS, Janssen J, Huh K, Voliva CF. Pecchi S, et al. Among authors: knapp ms. Bioorg Med Chem Lett. 2013 Aug 15;23(16):4652-6. doi: 10.1016/j.bmcl.2013.06.010. Epub 2013 Jun 12. Bioorg Med Chem Lett. 2013. PMID: 23820386
Synthesis and in Vitro and in Vivo Evaluation of Phosphoinositide-3-kinase Inhibitors.
Burger MT, Knapp M, Wagman A, Ni ZJ, Hendrickson T, Atallah G, Zhang Y, Frazier K, Verhagen J, Pfister K, Ng S, Smith A, Bartulis S, Merrit H, Weismann M, Xin X, Haznedar J, Voliva CF, Iwanowicz E, Pecchi S. Burger MT, et al. ACS Med Chem Lett. 2010 Oct 13;2(1):34-8. doi: 10.1021/ml1001932. eCollection 2011 Jan 13. ACS Med Chem Lett. 2010. PMID: 24900252 Free PMC article.
Identification of NVP-BKM120 as a Potent, Selective, Orally Bioavailable Class I PI3 Kinase Inhibitor for Treating Cancer.
Burger MT, Pecchi S, Wagman A, Ni ZJ, Knapp M, Hendrickson T, Atallah G, Pfister K, Zhang Y, Bartulis S, Frazier K, Ng S, Smith A, Verhagen J, Haznedar J, Huh K, Iwanowicz E, Xin X, Menezes D, Merritt H, Lee I, Wiesmann M, Kaufman S, Crawford K, Chin M, Bussiere D, Shoemaker K, Zaror I, Maira SM, Voliva CF. Burger MT, et al. ACS Med Chem Lett. 2011 Aug 26;2(10):774-9. doi: 10.1021/ml200156t. eCollection 2011 Oct 13. ACS Med Chem Lett. 2011. PMID: 24900266 Free PMC article.
Potent nonimmunosuppressive cyclophilin inhibitors with improved pharmaceutical properties and decreased transporter inhibition.
Fu J, Tjandra M, Becker C, Bednarczyk D, Capparelli M, Elling R, Hanna I, Fujimoto R, Furegati M, Karur S, Kasprzyk T, Knapp M, Leung K, Li X, Lu P, Mergo W, Miault C, Ng S, Parker D, Peng Y, Roggo S, Rivkin A, Simmons RL, Wang M, Wiedmann B, Weiss AH, Xiao L, Xie L, Xu W, Yifru A, Yang S, Zhou B, Sweeney ZK. Fu J, et al. J Med Chem. 2014 Oct 23;57(20):8503-16. doi: 10.1021/jm500862r. Epub 2014 Oct 13. J Med Chem. 2014. PMID: 25310383
Selective VPS34 inhibitor blocks autophagy and uncovers a role for NCOA4 in ferritin degradation and iron homeostasis in vivo.
Dowdle WE, Nyfeler B, Nagel J, Elling RA, Liu S, Triantafellow E, Menon S, Wang Z, Honda A, Pardee G, Cantwell J, Luu C, Cornella-Taracido I, Harrington E, Fekkes P, Lei H, Fang Q, Digan ME, Burdick D, Powers AF, Helliwell SB, D'Aquin S, Bastien J, Wang H, Wiederschain D, Kuerth J, Bergman P, Schwalb D, Thomas J, Ugwonali S, Harbinski F, Tallarico J, Wilson CJ, Myer VE, Porter JA, Bussiere DE, Finan PM, Labow MA, Mao X, Hamann LG, Manning BD, Valdez RA, Nicholson T, Schirle M, Knapp MS, Keaney EP, Murphy LO. Dowdle WE, et al. Among authors: knapp ms. Nat Cell Biol. 2014 Nov;16(11):1069-79. doi: 10.1038/ncb3053. Epub 2014 Oct 19. Nat Cell Biol. 2014. PMID: 25327288
Structure-Based Drug Design of Novel, Potent, and Selective Azabenzimidazoles (ABI) as ATR Inhibitors.
Barsanti PA, Pan Y, Lu Y, Jain R, Cox M, Aversa RJ, Dillon MP, Elling R, Hu C, Jin X, Knapp M, Lan J, Ramurthy S, Rudewicz P, Setti L, Subramanian S, Mathur M, Taricani L, Thomas G, Xiao L, Yue Q. Barsanti PA, et al. ACS Med Chem Lett. 2014 Oct 30;6(1):42-6. doi: 10.1021/ml500352s. eCollection 2015 Jan 8. ACS Med Chem Lett. 2014. PMID: 25589928 Free PMC article.
119 results