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Learning from the past for TB drug discovery in the future.
Mikušová K, Ekins S. Mikušová K, et al. 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.
DprE1 Is a Vulnerable Tuberculosis Drug Target Due to Its Cell Wall Localization.
Brecik M, Centárová I, Mukherjee R, Kolly GS, Huszár S, Bobovská A, Kilacsková E, Mokošová V, Svetlíková Z, Šarkan M, Neres J, Korduláková J, Cole ST, Mikušová K. Brecik M, et al. Among authors: mikusova k. ACS Chem Biol. 2015 Jul 17;10(7):1631-6. doi: 10.1021/acschembio.5b00237. Epub 2015 Apr 29. ACS Chem Biol. 2015. PMID: 25906160
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: mikusova k. 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.
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: mikusova k. 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
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: mikusova k. Sci Rep. 2018 Feb 16;8(1):3187. doi: 10.1038/s41598-018-21614-4. Sci Rep. 2018. PMID: 29453370 Free PMC article.
The EU approved antimalarial pyronaridine shows antitubercular activity and synergy with rifampicin, targeting RNA polymerase.
Mori G, Orena BS, Franch C, Mitchenall LA, Godbole AA, Rodrigues L, Aguilar-Pérez C, Zemanová J, Huszár S, Forbak M, Lane TR, Sabbah M, Deboosere N, Frita R, Vandeputte A, Hoffmann E, Russo R, Connell N, Veilleux C, Jha RK, Kumar P, Freundlich JS, Brodin P, Aínsa JA, Nagaraja V, Maxwell A, Mikušová K, Pasca MR, Ekins S. Mori G, et al. Among authors: mikusova k. Tuberculosis (Edinb). 2018 Sep;112:98-109. doi: 10.1016/j.tube.2018.08.004. Epub 2018 Aug 11. Tuberculosis (Edinb). 2018. PMID: 30205975
Identification of a small molecule with activity against drug-resistant and persistent tuberculosis.
Wang F, Sambandan D, Halder R, Wang J, Batt SM, Weinrick B, Ahmad I, Yang P, Zhang Y, Kim J, Hassani M, Huszar S, Trefzer C, Ma Z, Kaneko T, Mdluli KE, Franzblau S, Chatterjee AK, Johnsson K, Mikusova K, Besra GS, Fütterer K, Robbins SH, Barnes SW, Walker JR, Jacobs WR Jr, Schultz PG. Wang F, et al. Among authors: mikusova k. Proc Natl Acad Sci U S A. 2013 Jul 2;110(27):E2510-7. doi: 10.1073/pnas.1309171110. Epub 2013 Jun 17. Proc Natl Acad Sci U S A. 2013. PMID: 23776209 Free PMC article.
Lead selection and characterization of antitubercular compounds using the Nested Chemical Library.
Sipos A, Pató J, Székely R, Hartkoorn RC, Kékesi L, Őrfi L, Szántai-Kis C, Mikušová K, Svetlíková Z, Korduláková J, Nagaraja V, Godbole AA, Bush N, Collin F, Maxwell A, Cole ST, Kéri G. Sipos A, et al. Among authors: mikusova k. Tuberculosis (Edinb). 2015 Jun;95 Suppl 1:S200-6. doi: 10.1016/j.tube.2015.02.028. Epub 2015 Feb 28. Tuberculosis (Edinb). 2015. PMID: 25801335
63 results