Rossini Nicolas de Oliveira, Dias Marcio Vinicius Bertacine
Universidade de São Paulo, Instituto de Ciências Biomédicas, Departamento de Microbiologia, São Paulo, SP, Brazil.
University of Warwick, Department of Chemistry, Coventry, United Kingdom.
Genet Mol Biol. 2023 Jan 23;46(1 Suppl 2):e20220261. doi: 10.1590/1678-4685-GMB-2022-0261. eCollection 2023.
Genetically antimicrobial resistance in Mycobacterium tuberculosis is currently one of the most important aspects of tuberculosis, considering that there are emerging resistant strains for almost every known drug used for its treatment. There are multiple antimicrobials used for tuberculosis treatment, and the most effective ones are the first-line drugs, which include isoniazid, pyrazinamide, rifampicin, and ethambutol. In this context, understanding the mechanisms of action and resistance of these molecules is essential for proposing new therapies and strategies of treatment. Additionally, understanding how and where mutations arise conferring a resistance profile to the bacteria and their effect on bacterial metabolism is an important requisite to be taken in producing safer and less susceptible drugs to the emergence of resistance. In this review, we summarize the most recent literature regarding novel mutations reported between 2017 and 2022 and the advances in the molecular mechanisms of action and resistance against first-line drugs used in tuberculosis treatment, highlighting recent findings in pyrazinamide resistance involving PanD and, additionally, resistance-conferring mutations for novel drugs such as bedaquiline, pretomanid, delamanid and linezolid.
鉴于用于治疗结核病的几乎每种已知药物都出现了耐药菌株,结核分枝杆菌的基因抗药性目前是结核病最重要的方面之一。有多种抗菌药物用于结核病治疗,其中最有效的是一线药物,包括异烟肼、吡嗪酰胺、利福平和乙胺丁醇。在这种情况下,了解这些分子的作用机制和耐药性对于提出新的治疗方法和策略至关重要。此外,了解赋予细菌耐药谱的突变如何以及在何处产生及其对细菌代谢的影响,是生产更安全、更不易产生耐药性的药物时需要考虑的重要必要条件。在本综述中,我们总结了2017年至2022年间报道的关于新突变的最新文献,以及结核病治疗中一线药物的作用和耐药分子机制的进展,重点介绍了涉及PanD的吡嗪酰胺耐药性的最新发现,以及贝达喹啉、普瑞玛尼、德拉马尼和利奈唑胺等新药的耐药性突变。