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Page 1
The Tuberculosis Drug Accelerator at year 10: what have we learned?
Aldridge BB, Barros-Aguirre D, Barry CE 3rd, Bates RH, Berthel SJ, Boshoff HI, Chibale K, Chu XJ, Cooper CB, Dartois V, Duncan K, Fotouhi N, Gusovsky F, Hipskind PA, Kempf DJ, Lelièvre J, Lenaerts AJ, McNamara CW, Mizrahi V, Nathan C, Olsen DB, Parish T, Petrassi HM, Pym A, Rhee KY, Robertson GT, Rock JM, Rubin EJ, Russell B, Russell DG, Sacchettini JC, Schnappinger D, Schrimpf M, Upton AM, Warner P, Wyatt PG, Yuan Y. Aldridge BB, et al. Among authors: gusovsky f. Nat Med. 2021 Aug;27(8):1333-1337. doi: 10.1038/s41591-021-01442-2. Nat Med. 2021. PMID: 34226736 Free PMC article.
Allosteric inhibitors of Mycobacterium tuberculosis tryptophan synthase.
Michalska K, Chang C, Maltseva NI, Jedrzejczak R, Robertson GT, Gusovsky F, McCarren P, Schreiber SL, Nag PP, Joachimiak A. Michalska K, et al. Among authors: gusovsky f. Protein Sci. 2020 Mar;29(3):779-788. doi: 10.1002/pro.3825. Epub 2020 Jan 20. Protein Sci. 2020. PMID: 31930594 Free PMC article.
Diversity-oriented synthesis yields novel multistage antimalarial inhibitors.
Kato N, Comer E, Sakata-Kato T, Sharma A, Sharma M, Maetani M, Bastien J, Brancucci NM, Bittker JA, Corey V, Clarke D, Derbyshire ER, Dornan GL, Duffy S, Eckley S, Itoe MA, Koolen KM, Lewis TA, Lui PS, Lukens AK, Lund E, March S, Meibalan E, Meier BC, McPhail JA, Mitasev B, Moss EL, Sayes M, Van Gessel Y, Wawer MJ, Yoshinaga T, Zeeman AM, Avery VM, Bhatia SN, Burke JE, Catteruccia F, Clardy JC, Clemons PA, Dechering KJ, Duvall JR, Foley MA, Gusovsky F, Kocken CH, Marti M, Morningstar ML, Munoz B, Neafsey DE, Sharma A, Winzeler EA, Wirth DF, Scherer CA, Schreiber SL. Kato N, et al. Among authors: gusovsky f. Nature. 2016 Oct 20;538(7625):344-349. doi: 10.1038/nature19804. Epub 2016 Sep 7. Nature. 2016. PMID: 27602946 Free PMC article.
Discovery of a potent, metabolically stabilized resorcylic lactone as an anti-inflammatory lead.
Du H, Matsushima T, Spyvee M, Goto M, Shirota H, Gusovsky F, Chiba K, Kotake M, Yoneda N, Eguchi Y, DiPietro L, Harmange JC, Gilbert S, Li XY, Davis H, Jiang Y, Zhang Z, Pelletier R, Wong N, Sakurai H, Yang H, Ito-Igarashi H, Kimura A, Kuboi Y, Mizui Y, Tanaka I, Ikemori-Kawada M, Kawakami Y, Inoue A, Kawai T, Kishi Y, Wang Y. Du H, et al. Among authors: gusovsky f. Bioorg Med Chem Lett. 2009 Nov 1;19(21):6196-9. doi: 10.1016/j.bmcl.2009.08.096. Epub 2009 Sep 3. Bioorg Med Chem Lett. 2009. PMID: 19783437
Discovery of an in vitro and in vivo potent resorcylic lactone analog of LL-Z1640-2 as anti-inflammatory lead, II.
Shen Y, Du H, Kotake M, Matsushima T, Goto M, Shirota H, Gusovsky F, Li X, Jiang Y, Schiller S, Spyvee M, Davis H, Zhang Z, Pelletier R, Ikemori-Kawada M, Kawakami Y, Inoue A, Wang Y. Shen Y, et al. Among authors: gusovsky f. Bioorg Med Chem Lett. 2010 May 15;20(10):3047-9. doi: 10.1016/j.bmcl.2010.03.119. Epub 2010 Apr 9. Bioorg Med Chem Lett. 2010. PMID: 20427182
Discovery of anti-inflammatory clinical candidate E6201, inspired from resorcylic lactone LL-Z1640-2, III.
Shen Y, Boivin R, Yoneda N, Du H, Schiller S, Matsushima T, Goto M, Shirota H, Gusovsky F, Lemelin C, Jiang Y, Zhang Z, Pelletier R, Ikemori-Kawada M, Kawakami Y, Inoue A, Schnaderbeck M, Wang Y. Shen Y, et al. Among authors: gusovsky f. Bioorg Med Chem Lett. 2010 May 15;20(10):3155-7. doi: 10.1016/j.bmcl.2010.03.087. Epub 2010 Mar 30. Bioorg Med Chem Lett. 2010. PMID: 20399648
Safety, tolerability, pharmacokinetics, and antimalarial efficacy of a novel Plasmodium falciparum ATP4 inhibitor SJ733: a first-in-human and induced blood-stage malaria phase 1a/b trial.
Gaur AH, McCarthy JS, Panetta JC, Dallas RH, Woodford J, Tang L, Smith AM, Stewart TB, Branum KC, Freeman BB 3rd, Patel ND, John E, Chalon S, Ost S, Heine RN, Richardson JL, Christensen R, Flynn PM, Van Gessel Y, Mitasev B, Möhrle JJ, Gusovsky F, Bebrevska L, Guy RK. Gaur AH, et al. Among authors: gusovsky f. Lancet Infect Dis. 2020 Aug;20(8):964-975. doi: 10.1016/S1473-3099(19)30611-5. Epub 2020 Apr 8. Lancet Infect Dis. 2020. PMID: 32275867 Clinical Trial.
The TLR4 antagonist Eritoran protects mice from lethal influenza infection.
Shirey KA, Lai W, Scott AJ, Lipsky M, Mistry P, Pletneva LM, Karp CL, McAlees J, Gioannini TL, Weiss J, Chen WH, Ernst RK, Rossignol DP, Gusovsky F, Blanco JC, Vogel SN. Shirey KA, et al. Among authors: gusovsky f. Nature. 2013 May 23;497(7450):498-502. doi: 10.1038/nature12118. Epub 2013 May 1. Nature. 2013. PMID: 23636320 Free PMC article.
E6201 [(3S,4R,5Z,8S,9S,11E)-14-(ethylamino)-8, 9,16-trihydroxy-3,4-dimethyl-3,4,9,19-tetrahydro-1H-2-benzoxacyclotetradecine-1,7(8H)-dione], a novel kinase inhibitor of mitogen-activated protein kinase/extracellular signal-regulated kinase kinase (MEK)-1 and MEK kinase-1: in vitro characterization of its anti-inflammatory and antihyperproliferative activities.
Goto M, Chow J, Muramoto K, Chiba K, Yamamoto S, Fujita M, Obaishi H, Tai K, Mizui Y, Tanaka I, Young D, Yang H, Wang YJ, Shirota H, Gusovsky F. Goto M, et al. Among authors: gusovsky f. J Pharmacol Exp Ther. 2009 Nov;331(2):485-95. doi: 10.1124/jpet.109.156554. Epub 2009 Aug 14. J Pharmacol Exp Ther. 2009. PMID: 19684251
E6201, a novel kinase inhibitor of mitogen-activated protein kinase/extracellular signal-regulated kinase kinase-1 and mitogen-activated protein kinase/extracellular signal-regulated kinase kinase kinase-1: in vivo effects on cutaneous inflammatory responses by topical administration.
Muramoto K, Goto M, Inoue Y, Ishii N, Chiba K, Kuboi Y, Omae T, Wang YJ, Gusovsky F, Shirota H. Muramoto K, et al. Among authors: gusovsky f. J Pharmacol Exp Ther. 2010 Oct;335(1):23-31. doi: 10.1124/jpet.110.168583. Epub 2010 Jul 13. J Pharmacol Exp Ther. 2010. PMID: 20627998
100 results