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Page 1
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
Successful Strategies for Mitigation of a Preclinical Signal for Phototoxicity in a DGAT1 Inhibitor.
Harrison TJ, Bauer D, Berdichevsky A, Chen X, Duvadie R, Hoogheem B, Hatsis P, Liu Q, Mao J, Miduturu V, Rocheford E, Zecri F, Zessis R, Zheng R, Zhu Q, Streeper R, Patel SJ. Harrison TJ, et al. Among authors: zessis r. 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.
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
Identification and characterization of human GDF15 knockouts.
Gurtan AM, Khalid S, Koch C, Khan MZ, Lamarche LB, Splawski I, Dolan E, Carrion AM, Zessis R, Clement ME, Chen Z, Lindsley LD, Chiu YH, Streeper RS, Denning DP, Goldfine AB, Doyon B, Abbasi A, Harrow JL, Tsunoyama K, Asaumi M, Kou I, Shuldiner AR, Rodriguez-Flores JL, Rasheed A, Jahanzaib M, Mian MR, Liaqat MB, Raza SS, Sultana R, Jalal A, Saeed MH, Abbas S, Memon FR, Ishaq M, Dominy JE, Saleheen D. Gurtan AM, et al. Among authors: zessis r. Nat Metab. 2024 Oct;6(10):1913-1921. doi: 10.1038/s42255-024-01135-3. Epub 2024 Sep 26. Nat Metab. 2024. PMID: 39327531