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CPSF3-dependent pre-mRNA processing as a druggable node in AML and Ewing's sarcoma.
Ross NT, Lohmann F, Carbonneau S, Fazal A, Weihofen WA, Gleim S, Salcius M, Sigoillot F, Henault M, Carl SH, Rodríguez-Molina JB, Miller HR, Brittain SM, Murphy J, Zambrowski M, Boynton G, Wang Y, Chen A, Molind GJ, Wilbertz JH, Artus-Revel CG, Jia M, Akinjiyan FA, Turner J, Knehr J, Carbone W, Schuierer S, Reece-Hoyes JS, Xie K, Saran C, Williams ET, Roma G, Spencer M, Jenkins J, George EL, Thomas JR, Michaud G, Schirle M, Tallarico J, Passmore LA, Chao JA, Beckwith REJ. Ross NT, et al. Among authors: weihofen wa. Nat Chem Biol. 2020 Jan;16(1):50-59. doi: 10.1038/s41589-019-0424-1. Epub 2019 Dec 9. Nat Chem Biol. 2020. PMID: 31819276 Free PMC article.
Discovery of a ZIP7 inhibitor from a Notch pathway screen.
Nolin E, Gans S, Llamas L, Bandyopadhyay S, Brittain SM, Bernasconi-Elias P, Carter KP, Loureiro JJ, Thomas JR, Schirle M, Yang Y, Guo N, Roma G, Schuierer S, Beibel M, Lindeman A, Sigoillot F, Chen A, Xie KX, Ho S, Reece-Hoyes J, Weihofen WA, Tyskiewicz K, Hoepfner D, McDonald RI, Guthrie N, Dogra A, Guo H, Shao J, Ding J, Canham SM, Boynton G, George EL, Kang ZB, Antczak C, Porter JA, Wallace O, Tallarico JA, Palmer AE, Jenkins JL, Jain RK, Bushell SM, Fryer CJ. Nolin E, et al. Among authors: weihofen wa. Nat Chem Biol. 2019 Feb;15(2):179-188. doi: 10.1038/s41589-018-0200-7. Epub 2019 Jan 14. Nat Chem Biol. 2019. PMID: 30643281 Free PMC article.
Author Correction: CPSF3-dependent pre-mRNA processing as a druggable node in AML and Ewing's sarcoma.
Ross NT, Lohmann F, Carbonneau S, Fazal A, Weihofen WA, Gleim S, Salcius M, Sigoillot F, Henault M, Carl SH, Rodríguez-Molina JB, Miller HR, Brittain SM, Murphy J, Zambrowski M, Boynton G, Wang Y, Chen A, Molind GJ, Wilbertz JH, Artus-Revel CG, Jia M, Akinjiyan FA, Turner J, Knehr J, Carbone W, Schuierer S, Reece-Hoyes JS, Xie K, Saran C, Williams ET, Roma G, Spencer M, Jenkins J, George EL, Thomas JR, Michaud G, Schirle M, Tallarico J, Passmore LA, Chao JA, Beckwith REJ. Ross NT, et al. Among authors: weihofen wa. Nat Chem Biol. 2020 Apr;16(4):479. doi: 10.1038/s41589-020-0508-y. Nat Chem Biol. 2020. PMID: 32139909
Structure based design of nicotinamide phosphoribosyltransferase (NAMPT) inhibitors from a phenotypic screen.
Palacios DS, Meredith E, Kawanami T, Adams C, Chen X, Darsigny V, Geno E, Palermo M, Baird D, Boynton G, Busby SA, George EL, Guy C, Hewett J, Tierney L, Thigale S, Weihofen W, Wang L, White N, Yin M, Argikar UA. Palacios DS, et al. Bioorg Med Chem Lett. 2018 Feb 1;28(3):365-370. doi: 10.1016/j.bmcl.2017.12.037. Epub 2017 Dec 18. Bioorg Med Chem Lett. 2018. PMID: 29275937
Scaffold Morphing Identifies 3-Pyridyl Azetidine Ureas as Inhibitors of Nicotinamide Phosphoribosyltransferase (NAMPT).
Palacios DS, Meredith EL, Kawanami T, Adams CM, Chen X, Darsigny V, Palermo M, Baird D, George EL, Guy C, Hewett J, Tierney L, Thigale S, Wang L, Weihofen WA. Palacios DS, et al. Among authors: weihofen wa. ACS Med Chem Lett. 2019 Oct 10;10(11):1524-1529. doi: 10.1021/acsmedchemlett.9b00325. eCollection 2019 Nov 14. ACS Med Chem Lett. 2019. PMID: 31749905 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: weihofen wa. 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
Enzymatic blockade of the ubiquitin-proteasome pathway.
Ernst R, Claessen JH, Mueller B, Sanyal S, Spooner E, van der Veen AG, Kirak O, Schlieker CD, Weihofen WA, Ploegh HL. Ernst R, et al. Among authors: weihofen wa. PLoS Biol. 2011 Mar;8(3):e1000605. doi: 10.1371/journal.pbio.1000605. Epub 2011 Mar 29. PLoS Biol. 2011. PMID: 21468303 Free PMC article.
25 results