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Successful Strategies for Mitigation of a Preclinical Signal for Phototoxicity in a DGAT1 Inhibitor.
ACS Med Chem Lett. 2019 Jun 20;10(8):1128-1133. doi: 10.1021/acsmedchemlett.9b00117. eCollection 2019 Aug 8.
ACS Med Chem Lett. 2019.
PMID: 31413796
Free PMC article.
Structure-Based Design and Preclinical Characterization of Selective and Orally Bioavailable Factor XIa Inhibitors: Demonstrating the Power of an Integrated S1 Protease Family Approach.
Lorthiois E, Roache J, Barnes-Seeman D, Altmann E, Hassiepen U, Turner G, Duvadie R, Hornak V, Karki RG, Schiering N, Weihofen WA, Perruccio F, Calhoun A, Fazal T, Dedic D, Durand C, Dussauge S, Fettis K, Tritsch F, Dentel C, Druet A, Liu D, Kirman L, Lachal J, Namoto K, Bevan D, Mo R, Monnet G, Muller L, Zessis R, Huang X, Lindsley L, Currie T, Chiu YH, Fridrich C, Delgado P, Wang S, Hollis-Symynkywicz M, Berghausen J, Williams E, Liu H, Liang G, Kim H, Hoffmann P, Hein A, Ramage P, D'Arcy A, Harlfinger S, Renatus M, Ruedisser S, Feldman D, Elliott J, Sedrani R, Maibaum J, Adams CM.
Lorthiois E, et al. Among authors: zessis r.
J Med Chem. 2020 Aug 13;63(15):8088-8113. doi: 10.1021/acs.jmedchem.0c00279. Epub 2020 Jul 21.
J Med Chem. 2020.
PMID: 32551603
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A Phenotypic Screen Identifies Calcium Overload as a Key Mechanism of β-Cell Glucolipotoxicity.
Vogel J, Yin J, Su L, Wang SX, Zessis R, Fowler S, Chiu CH, Wilson AC, Chen A, Zecri F, Turner G, Smith TM, DeChristopher B, Xing H, Rothman DM, Cai X, Berdichevsky A.
Vogel J, et al. Among authors: zessis r.
Diabetes. 2020 May;69(5):1032-1041. doi: 10.2337/db19-0813. Epub 2020 Feb 20.
Diabetes. 2020.
PMID: 32079579
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2-Aminopyrazolo[1,5-a]pyrimidines as potent and selective inhibitors of JAK2.
Ledeboer MW, Pierce AC, Duffy JP, Gao H, Messersmith D, Salituro FG, Nanthakumar S, Come J, Zuccola HJ, Swenson L, Shlyakter D, Mahajan S, Hoock T, Fan B, Tsai WJ, Kolaczkowski E, Carrier S, Hogan JK, Zessis R, Pazhanisamy S, Bennani YL.
Ledeboer MW, et al. Among authors: zessis r.
Bioorg Med Chem Lett. 2009 Dec 1;19(23):6529-33. doi: 10.1016/j.bmcl.2009.10.053. Epub 2009 Oct 24.
Bioorg Med Chem Lett. 2009.
PMID: 19857967
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