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The small-molecule SMARt751 reverses Mycobacterium tuberculosis resistance to ethionamide in acute and chronic mouse models of tuberculosis.
Flipo M, Frita R, Bourotte M, Martínez-Martínez MS, Boesche M, Boyle GW, Derimanov G, Drewes G, Gamallo P, Ghidelli-Disse S, Gresham S, Jiménez E, de Mercado J, Pérez-Herrán E, Porras-De Francisco E, Rullas J, Casado P, Leroux F, Piveteau C, Kiass M, Mathys V, Soetaert K, Megalizzi V, Tanina A, Wintjens R, Antoine R, Brodin P, Delorme V, Moune M, Djaout K, Slupek S, Kemmer C, Gitzinger M, Ballell L, Mendoza-Losana A, Lociuro S, Deprez B, Barros-Aguirre D, Remuiñán MJ, Willand N, Baulard AR. Flipo M, et al. Among authors: drewes g. Sci Transl Med. 2022 May 4;14(643):eaaz6280. doi: 10.1126/scitranslmed.aaz6280. Epub 2022 May 4. Sci Transl Med. 2022. PMID: 35507672
Biochemical Screening of Five Protein Kinases from Plasmodium falciparum against 14,000 Cell-Active Compounds.
Crowther GJ, Hillesland HK, Keyloun KR, Reid MC, Lafuente-Monasterio MJ, Ghidelli-Disse S, Leonard SE, He P, Jones JC, Krahn MM, Mo JS, Dasari KS, Fox AM, Boesche M, El Bakkouri M, Rivas KL, Leroy D, Hui R, Drewes G, Maly DJ, Van Voorhis WC, Ojo KK. Crowther GJ, et al. Among authors: drewes g. PLoS One. 2016 Mar 2;11(3):e0149996. doi: 10.1371/journal.pone.0149996. eCollection 2016. PLoS One. 2016. PMID: 26934697 Free PMC article.
THPP target assignment reveals EchA6 as an essential fatty acid shuttle in mycobacteria.
Cox JA, Abrahams KA, Alemparte C, Ghidelli-Disse S, Rullas J, Angulo-Barturen I, Singh A, Gurcha SS, Nataraj V, Bethell S, Remuiñán MJ, Encinas L, Jervis PJ, Cammack NC, Bhatt A, Kruse U, Bantscheff M, Fütterer K, Barros D, Ballell L, Drewes G, Besra GS. Cox JA, et al. Among authors: drewes g. Nat Microbiol. 2016 Jan 18;1:15006. doi: 10.1038/nmicrobiol.2015.6. Nat Microbiol. 2016. PMID: 27571973
Identification of KasA as the cellular target of an anti-tubercular scaffold.
Abrahams KA, Chung CW, Ghidelli-Disse S, Rullas J, Rebollo-López MJ, Gurcha SS, Cox JA, Mendoza A, Jiménez-Navarro E, Martínez-Martínez MS, Neu M, Shillings A, Homes P, Argyrou A, Casanueva R, Loman NJ, Moynihan PJ, Lelièvre J, Selenski C, Axtman M, Kremer L, Bantscheff M, Angulo-Barturen I, Izquierdo MC, Cammack NC, Drewes G, Ballell L, Barros D, Besra GS, Bates RH. Abrahams KA, et al. Among authors: drewes g. Nat Commun. 2016 Sep 1;7:12581. doi: 10.1038/ncomms12581. Nat Commun. 2016. PMID: 27581223 Free PMC article.
Essential but Not Vulnerable: Indazole Sulfonamides Targeting Inosine Monophosphate Dehydrogenase as Potential Leads against Mycobacterium tuberculosis.
Park Y, Pacitto A, Bayliss T, Cleghorn LA, Wang Z, Hartman T, Arora K, Ioerger TR, Sacchettini J, Rizzi M, Donini S, Blundell TL, Ascher DB, Rhee K, Breda A, Zhou N, Dartois V, Jonnala SR, Via LE, Mizrahi V, Epemolu O, Stojanovski L, Simeons F, Osuna-Cabello M, Ellis L, MacKenzie CJ, Smith AR, Davis SH, Murugesan D, Buchanan KI, Turner PA, Huggett M, Zuccotto F, Rebollo-Lopez MJ, Lafuente-Monasterio MJ, Sanz O, Diaz GS, Lelièvre J, Ballell L, Selenski C, Axtman M, Ghidelli-Disse S, Pflaumer H, Bösche M, Drewes G, Freiberg GM, Kurnick MD, Srikumaran M, Kempf DJ, Green SR, Ray PC, Read K, Wyatt P, Barry CE 3rd, Boshoff HI. Park Y, et al. Among authors: drewes g. ACS Infect Dis. 2017 Jan 13;3(1):18-33. doi: 10.1021/acsinfecdis.6b00103. Epub 2016 Oct 17. ACS Infect Dis. 2017. PMID: 27704782 Free PMC article.
Antimalarial efficacy of MMV390048, an inhibitor of Plasmodium phosphatidylinositol 4-kinase.
Paquet T, Le Manach C, Cabrera DG, Younis Y, Henrich PP, Abraham TS, Lee MCS, Basak R, Ghidelli-Disse S, Lafuente-Monasterio MJ, Bantscheff M, Ruecker A, Blagborough AM, Zakutansky SE, Zeeman AM, White KL, Shackleford DM, Mannila J, Morizzi J, Scheurer C, Angulo-Barturen I, Martínez MS, Ferrer S, Sanz LM, Gamo FJ, Reader J, Botha M, Dechering KJ, Sauerwein RW, Tungtaeng A, Vanachayangkul P, Lim CS, Burrows J, Witty MJ, Marsh KC, Bodenreider C, Rochford R, Solapure SM, Jiménez-Díaz MB, Wittlin S, Charman SA, Donini C, Campo B, Birkholtz LM, Hanson KK, Drewes G, Kocken CHM, Delves MJ, Leroy D, Fidock DA, Waterson D, Street LJ, Chibale K. Paquet T, et al. Among authors: drewes g. Sci Transl Med. 2017 Apr 26;9(387):eaad9735. doi: 10.1126/scitranslmed.aad9735. Sci Transl Med. 2017. PMID: 28446690 Free PMC article.
The Discovery of Novel Antimalarial Aminoxadiazoles as a Promising Nonendoperoxide Scaffold.
Sandoval E, Lafuente-Monasterio MJ, Almela MJ, Castañeda P, Jiménez Díaz MB, Martínez-Martínez MS, Vidal J, Angulo-Barturen Í, Bamborough P, Burrows J, Cammack N, Chaparro MJ, Coterón JM, de Cozar C, Crespo B, Díaz B, Drewes G, Fernández E, Ferrer-Bazaga S, Fraile MT, Gamo FJ, Ghidelli-Disse S, Gómez R, Haselden J, Huss S, León ML, de Mercado J, Macdonald SJF, Martín Hernando JI, Prats S, Puente M, Rodríguez A, de la Rosa JC, Rueda L, Selenski C, Willis P, Wilson DM, Witty M, Calderón F. Sandoval E, et al. Among authors: drewes g. J Med Chem. 2017 Aug 24;60(16):6880-6896. doi: 10.1021/acs.jmedchem.6b01441. Epub 2017 Aug 14. J Med Chem. 2017. PMID: 28806082
Novel Antitubercular 6-Dialkylaminopyrimidine Carboxamides from Phenotypic Whole-Cell High Throughput Screening of a SoftFocus Library: Structure-Activity Relationship and Target Identification Studies.
Wilson CR, Gessner RK, Moosa A, Seldon R, Warner DF, Mizrahi V, Soares de Melo C, Simelane SB, Nchinda A, Abay E, Taylor D, Njoroge M, Brunschwig C, Lawrence N, Boshoff HIM, Barry CE 3rd, Sirgel FA, van Helden P, Harris CJ, Gordon R, Ghidelli-Disse S, Pflaumer H, Boesche M, Drewes G, Sanz O, Santos G, Rebollo-Lopez MJ, Urones B, Selenski C, Lafuente-Monasterio MJ, Axtman M, Lelièvre J, Ballell L, Mueller R, Street LJ, Ghorpade SR, Chibale K. Wilson CR, et al. Among authors: drewes g. J Med Chem. 2017 Dec 28;60(24):10118-10134. doi: 10.1021/acs.jmedchem.7b01347. Epub 2017 Dec 7. J Med Chem. 2017. PMID: 29148755 Free PMC article.
Cyclin-dependent kinase 12 is a drug target for visceral leishmaniasis.
Wyllie S, Thomas M, Patterson S, Crouch S, De Rycker M, Lowe R, Gresham S, Urbaniak MD, Otto TD, Stojanovski L, Simeons FRC, Manthri S, MacLean LM, Zuccotto F, Homeyer N, Pflaumer H, Boesche M, Sastry L, Connolly P, Albrecht S, Berriman M, Drewes G, Gray DW, Ghidelli-Disse S, Dixon S, Fiandor JM, Wyatt PG, Ferguson MAJ, Fairlamb AH, Miles TJ, Read KD, Gilbert IH. Wyllie S, et al. Among authors: drewes g. Nature. 2018 Aug;560(7717):192-197. doi: 10.1038/s41586-018-0356-z. Epub 2018 Jul 25. Nature. 2018. PMID: 30046105 Free PMC article.
115 results