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A multitarget approach to drug discovery inhibiting Mycobacterium tuberculosis PyrG and PanK.
Chiarelli LR, Mori G, Orena BS, Esposito M, Lane T, de Jesus Lopes Ribeiro AL, Degiacomi G, Zemanová J, Szádocka S, Huszár S, Palčeková Z, Manfredi M, Gosetti F, Lelièvre J, Ballell L, Kazakova E, Makarov V, Marengo E, Mikusova K, Cole ST, Riccardi G, Ekins S, Pasca MR. Chiarelli LR, et al. Among authors: ekins s. Sci Rep. 2018 Feb 16;8(1):3187. doi: 10.1038/s41598-018-21614-4. Sci Rep. 2018. PMID: 29453370 Free PMC article.
Thiophenecarboxamide Derivatives Activated by EthA Kill Mycobacterium tuberculosis by Inhibiting the CTP Synthetase PyrG.
Mori G, Chiarelli LR, Esposito M, Makarov V, Bellinzoni M, Hartkoorn RC, Degiacomi G, Boldrin F, Ekins S, de Jesus Lopes Ribeiro AL, Marino LB, Centárová I, Svetlíková Z, Blaško J, Kazakova E, Lepioshkin A, Barilone N, Zanoni G, Porta A, Fondi M, Fani R, Baulard AR, Mikušová K, Alzari PM, Manganelli R, de Carvalho LP, Riccardi G, Cole ST, Pasca MR. Mori G, et al. Among authors: ekins s. Chem Biol. 2015 Jul 23;22(7):917-27. doi: 10.1016/j.chembiol.2015.05.016. Epub 2015 Jun 18. Chem Biol. 2015. PMID: 26097035 Free PMC article.
Learning from the past for TB drug discovery in the future.
Mikušová K, Ekins S. Mikušová K, et al. Among authors: ekins s. Drug Discov Today. 2017 Mar;22(3):534-545. doi: 10.1016/j.drudis.2016.09.025. Epub 2016 Oct 4. Drug Discov Today. 2017. PMID: 27717850 Free PMC article. Review.
A Phenotypic Based Target Screening Approach Delivers New Antitubercular CTP Synthetase Inhibitors.
Esposito M, Szadocka S, Degiacomi G, Orena BS, Mori G, Piano V, Boldrin F, Zemanová J, Huszár S, Barros D, Ekins S, Lelièvre J, Manganelli R, Mattevi A, Pasca MR, Riccardi G, Ballell L, Mikušová K, Chiarelli LR. Esposito M, et al. Among authors: ekins s. ACS Infect Dis. 2017 Jun 9;3(6):428-437. doi: 10.1021/acsinfecdis.7b00006. Epub 2017 May 11. ACS Infect Dis. 2017. PMID: 28475832
371 results