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A Phenotypic Screen Identifies a Compound Series That Induces Differentiation of Acute Myeloid Leukemia Cells In Vitro and Shows Antitumor Effects In Vivo.
Josa-Culleré L, Madden KS, Cogswell TJ, Jackson TR, Carter TS, Zhang D, Trevitt G, Davies SG, Vyas P, Wynne GM, Milne TA, Russell AJ. Josa-Culleré L, et al. Among authors: trevitt g. J Med Chem. 2021 Nov 11;64(21):15608-15628. doi: 10.1021/acs.jmedchem.1c00574. Epub 2021 Oct 21. J Med Chem. 2021. PMID: 34672555 Free article.
Discovery of IACS-9779 and IACS-70465 as Potent Inhibitors Targeting Indoleamine 2,3-Dioxygenase 1 (IDO1) Apoenzyme.
Hamilton MM, Mseeh F, McAfoos TJ, Leonard PG, Reyna NJ, Harris AL, Xu A, Han M, Soth MJ, Czako B, Theroff JP, Mandal PK, Burke JP, Virgin-Downey B, Petrocchi A, Pfaffinger D, Rogers NE, Parker CA, Yu SS, Jiang Y, Krapp S, Lammens A, Trevitt G, Tremblay MR, Mikule K, Wilcoxen K, Cross JB, Jones P, Marszalek JR, Lewis RT. Hamilton MM, et al. Among authors: trevitt g. J Med Chem. 2021 Aug 12;64(15):11302-11329. doi: 10.1021/acs.jmedchem.1c00679. Epub 2021 Jul 22. J Med Chem. 2021. PMID: 34292726
Tetrahydroisoquinoline amide substituted phenyl pyrazoles as selective Bcl-2 inhibitors.
Porter J, Payne A, de Candole B, Ford D, Hutchinson B, Trevitt G, Turner J, Edwards C, Watkins C, Whitcombe I, Davis J, Stubberfield C. Porter J, et al. Among authors: trevitt g. Bioorg Med Chem Lett. 2009 Jan 1;19(1):230-3. doi: 10.1016/j.bmcl.2008.10.113. Epub 2008 Oct 31. Bioorg Med Chem Lett. 2009. PMID: 19027294
Atropisomeric small molecule Bcl-2 ligands: determination of bioactive conformation.
Porter J, Payne A, Whitcombe I, de Candole B, Ford D, Garlish R, Hold A, Hutchinson B, Trevitt G, Turner J, Edwards C, Watkins C, Davis J, Stubberfield C. Porter J, et al. Among authors: trevitt g. Bioorg Med Chem Lett. 2009 Mar 15;19(6):1767-72. doi: 10.1016/j.bmcl.2009.01.071. Epub 2009 Jan 27. Bioorg Med Chem Lett. 2009. PMID: 19217289
Repurposing isoxazoline veterinary drugs for control of vector-borne human diseases.
Miglianico M, Eldering M, Slater H, Ferguson N, Ambrose P, Lees RS, Koolen KMJ, Pruzinova K, Jancarova M, Volf P, Koenraadt CJM, Duerr HP, Trevitt G, Yang B, Chatterjee AK, Wisler J, Sturm A, Bousema T, Sauerwein RW, Schultz PG, Tremblay MS, Dechering KJ. Miglianico M, et al. Among authors: trevitt g. Proc Natl Acad Sci U S A. 2018 Jul 17;115(29):E6920-E6926. doi: 10.1073/pnas.1801338115. Epub 2018 Jul 2. Proc Natl Acad Sci U S A. 2018. PMID: 29967151 Free PMC article.
Antimalarial pantothenamide metabolites target acetyl-coenzyme A biosynthesis in Plasmodium falciparum.
Schalkwijk J, Allman EL, Jansen PAM, de Vries LE, Verhoef JMJ, Jackowski S, Botman PNM, Beuckens-Schortinghuis CA, Koolen KMJ, Bolscher JM, Vos MW, Miller K, Reeves SA, Pett H, Trevitt G, Wittlin S, Scheurer C, Sax S, Fischli C, Angulo-Barturen I, Jiménez-Diaz MB, Josling G, Kooij TWA, Bonnert R, Campo B, Blaauw RH, Rutjes FPJT, Sauerwein RW, Llinás M, Hermkens PHH, Dechering KJ. Schalkwijk J, et al. Among authors: trevitt g. Sci Transl Med. 2019 Sep 18;11(510):eaas9917. doi: 10.1126/scitranslmed.aas9917. Sci Transl Med. 2019. PMID: 31534021
Preclinical characterization and target validation of the antimalarial pantothenamide MMV693183.
de Vries LE, Jansen PAM, Barcelo C, Munro J, Verhoef JMJ, Pasaje CFA, Rubiano K, Striepen J, Abla N, Berning L, Bolscher JM, Demarta-Gatsi C, Henderson RWM, Huijs T, Koolen KMJ, Tumwebaze PK, Yeo T, Aguiar ACC, Angulo-Barturen I, Churchyard A, Baum J, Fernández BC, Fuchs A, Gamo FJ, Guido RVC, Jiménez-Diaz MB, Pereira DB, Rochford R, Roesch C, Sanz LM, Trevitt G, Witkowski B, Wittlin S, Cooper RA, Rosenthal PJ, Sauerwein RW, Schalkwijk J, Hermkens PHH, Bonnert RV, Campo B, Fidock DA, Llinás M, Niles JC, Kooij TWA, Dechering KJ. de Vries LE, et al. Among authors: trevitt g. Nat Commun. 2022 Apr 20;13(1):2158. doi: 10.1038/s41467-022-29688-5. Nat Commun. 2022. PMID: 35444200 Free PMC article.
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