Dutta Anirudha, Chowdhury Antarika, Roy Parijat, Bhowmik Priyanka
Department of Biological Sciences, Adamas University, Barrackpore-Barasat Road, 24 Parganas North, Jagannathpur, Kolkata, West Bengal, India.
Protein J. 2025 Aug 19. doi: 10.1007/s10930-025-10284-7.
Bacterial antimicrobial resistance is a great public health threat worldwide, a situation that is much escalated by the rapid propagation of Extended Spectrum β-lactamase (ESBL) enzymes. These can hydrolyze and inactivate a broad range of β-lactams, including third-generation cephalosporins, penicillin, and aztreonam and are known to be associated with various bacterial infections, ranging from uncomplicated urinary tract infections to life-threatening sepsis.Variation is the essential raw material of Darwinian evolution and the accumulation of mutations plays one of the most important roles in it. Sequential acquisition of spontaneous mutations followed by successive rounds of selection can be attributed as one of the major reasons for the rapid diversification of ESBL enzymes. The ESBLs are excellent examples of 'microevolution' that led to 'gain-of-function' with an extended substrate spectrum. However, acquiring newer phenotypes sometimes comes with fitness costs and different mutational pathways interact with each other, triggering both additive and non-additive fitness to generate a rugged fitness landscape, that influences the path a strain must follow to adapt and evolve under selection pressure. Therefore, it is important to understand the role of mutations in the emergence of these enzyme variants. This review focuses on the understanding of different facades of mutational pathways that lead to the adaptive evolution of ESBL phenotype. The structural and mechanistic basis of the extension of the substrate spectrum by mutations are also discussed.
细菌的抗菌耐药性是全球范围内对公众健康的重大威胁,超广谱β-内酰胺酶(ESBL)的迅速传播使这种情况更加严重。这些酶能够水解并使多种β-内酰胺类药物失活,包括第三代头孢菌素、青霉素和氨曲南,并且已知与各种细菌感染有关,从不复杂的尿路感染到危及生命的败血症。变异是达尔文进化的基本原材料,突变的积累在其中起着最重要的作用之一。自发突变的连续获得以及随后连续几轮的选择可被视为ESBL酶快速多样化的主要原因之一。ESBL是“微进化”的绝佳例子,它导致了底物谱扩展的“功能获得”。然而,获得新表型有时会伴随着适应性代价,不同的突变途径相互作用,引发累加和非累加适应性,从而产生崎岖的适应性景观,这会影响菌株在选择压力下适应和进化必须遵循的路径。因此,了解突变在这些酶变体出现中的作用很重要。本综述着重于理解导致ESBL表型适应性进化的突变途径的不同方面。还讨论了通过突变扩展底物谱的结构和机制基础。