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New Insights into the Mechanism of Action of the Thienopyrimidine Antitubercular Prodrug TP053.
Chiarelli LR, Salina EG, Mori G, Azhikina T, Riabova O, Lepioshkin A, Grigorov A, Forbak M, Madacki J, Orena BS, Manfredi M, Gosetti F, Buzzi A, Degiacomi G, Sammartino JC, Marengo E, Korduláková J, Riccardi G, Mikušová K, Makarov V, Pasca MR. Chiarelli LR, et al. ACS Infect Dis. 2020 Feb 14;6(2):313-323. doi: 10.1021/acsinfecdis.9b00388. Epub 2019 Dec 2. ACS Infect Dis. 2020. PMID: 31729215
Biological and structural characterization of the Mycobacterium smegmatis nitroreductase NfnB, and its role in benzothiazinone resistance.
Manina G, Bellinzoni M, Pasca MR, Neres J, Milano A, Ribeiro AL, Buroni S, Skovierová H, Dianišková P, Mikušová K, Marák J, Makarov V, Giganti D, Haouz A, Lucarelli AP, Degiacomi G, Piazza A, Chiarelli LR, De Rossi E, Salina E, Cole ST, Alzari PM, Riccardi G. Manina G, et al. Among authors: chiarelli lr. Mol Microbiol. 2010 Sep;77(5):1172-85. doi: 10.1111/j.1365-2958.2010.07277.x. Mol Microbiol. 2010. PMID: 20624223 Free article.
Analogous mechanisms of resistance to benzothiazinones and dinitrobenzamides in Mycobacterium smegmatis.
Ribeiro AL, Degiacomi G, Ewann F, Buroni S, Incandela ML, Chiarelli LR, Mori G, Kim J, Contreras-Dominguez M, Park YS, Han SJ, Brodin P, Valentini G, Rizzi M, Riccardi G, Pasca MR. Ribeiro AL, et al. Among authors: chiarelli lr. PLoS One. 2011;6(11):e26675. doi: 10.1371/journal.pone.0026675. Epub 2011 Nov 1. PLoS One. 2011. PMID: 22069462 Free PMC article.
Structural basis for benzothiazinone-mediated killing of Mycobacterium tuberculosis.
Neres J, Pojer F, Molteni E, Chiarelli LR, Dhar N, Boy-Röttger S, Buroni S, Fullam E, Degiacomi G, Lucarelli AP, Read RJ, Zanoni G, Edmondson DE, De Rossi E, Pasca MR, McKinney JD, Dyson PJ, Riccardi G, Mattevi A, Cole ST, Binda C. Neres J, et al. Among authors: chiarelli lr. Sci Transl Med. 2012 Sep 5;4(150):150ra121. doi: 10.1126/scitranslmed.3004395. Sci Transl Med. 2012. PMID: 22956199 Free PMC article.
Mechanism of action of 5-nitrothiophenes against Mycobacterium tuberculosis.
Hartkoorn RC, Ryabova OB, Chiarelli LR, Riccardi G, Makarov V, Cole ST. Hartkoorn RC, et al. Among authors: chiarelli lr. Antimicrob Agents Chemother. 2014 May;58(5):2944-7. doi: 10.1128/AAC.02693-13. Epub 2014 Feb 18. Antimicrob Agents Chemother. 2014. PMID: 24550336 Free PMC article.
4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.
Naik M, Humnabadkar V, Tantry SJ, Panda M, Narayan A, Guptha S, Panduga V, Manjrekar P, Jena LK, Koushik K, Shanbhag G, Jatheendranath S, Manjunatha MR, Gorai G, Bathula C, Rudrapatna S, Achar V, Sharma S, Ambady A, Hegde N, Mahadevaswamy J, Kaur P, Sambandamurthy VK, Awasthy D, Narayan C, Ravishankar S, Madhavapeddi P, Reddy J, Prabhakar K, Saralaya R, Chatterji M, Whiteaker J, McLaughlin B, Chiarelli LR, Riccardi G, Pasca MR, Binda C, Neres J, Dhar N, Signorino-Gelo F, McKinney JD, Ramachandran V, Shandil R, Tommasi R, Iyer PS, Narayanan S, Hosagrahara V, Kavanagh S, Dinesh N, Ghorpade SR. Naik M, et al. Among authors: chiarelli lr. J Med Chem. 2014 Jun 26;57(12):5419-34. doi: 10.1021/jm5005978. Epub 2014 Jun 11. J Med Chem. 2014. PMID: 24871036
Rv2466c mediates the activation of TP053 to kill replicating and non-replicating Mycobacterium tuberculosis.
Albesa-Jové D, Chiarelli LR, Makarov V, Pasca MR, Urresti S, Mori G, Salina E, Vocat A, Comino N, Mohorko E, Ryabova S, Pfieiffer B, Lopes Ribeiro AL, Rodrigo-Unzueta A, Tersa M, Zanoni G, Buroni S, Altmann KH, Hartkoorn RC, Glockshuber R, Cole ST, Riccardi G, Guerin ME. Albesa-Jové D, et al. Among authors: chiarelli lr. ACS Chem Biol. 2014 Jul 18;9(7):1567-75. doi: 10.1021/cb500149m. Epub 2014 Jun 13. ACS Chem Biol. 2014. PMID: 24877756 Free article.
2-Carboxyquinoxalines kill mycobacterium tuberculosis through noncovalent inhibition of DprE1.
Neres J, Hartkoorn RC, Chiarelli LR, Gadupudi R, Pasca MR, Mori G, Venturelli A, Savina S, Makarov V, Kolly GS, Molteni E, Binda C, Dhar N, Ferrari S, Brodin P, Delorme V, Landry V, de Jesus Lopes Ribeiro AL, Farina D, Saxena P, Pojer F, Carta A, Luciani R, Porta A, Zanoni G, De Rossi E, Costi MP, Riccardi G, Cole ST. Neres J, et al. Among authors: chiarelli lr. ACS Chem Biol. 2015 Mar 20;10(3):705-14. doi: 10.1021/cb5007163. Epub 2014 Dec 9. ACS Chem Biol. 2015. PMID: 25427196
100 results