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Structure-based Druggability Assessment of Anti-virulence Targets from Pseudomonas aeruginosa

机译：铜绿假单胞菌的抗毒力靶标基于结构的可解性评估

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摘要

Antimicrobial Resistance (AMR) represents a serious threat to health and the global economy.However, interest in antibacterial drug development has decreased substantially in recent decades.Meanwhile, anti-virulence drug development has emerged as an attractive alternative to fight AMR.Although several macromolecular targets have been explored for this goal, their druggability is a vital piece of information that has been overlooked.This review explores this subject by showing how structure-based freely available in silico tools, such as PockDrug and FTMap, might be useful for designing novel inhibitors of the pyocyanin biosynthesis pathway and improving the potency/selectivity of compounds that target the Pseudomonas aeruginosa quorum sensing mechanism.The information provided by hotspot analysis, along with binding site features, reveals novel druggable targets (PhzA and PhzS) that remain largely unexplored.However, it also highlights that In silico druggability prediction tools have several limitations that might be overcome in the near future.Meanwhile, anti-virulence drug targets should be assessed by complementary methods, such as the combined use of FTMap/PockDrug, once the consensus druggability classification reduces the risk of wasting resources on undruggable proteins.
机译：耐药性（AMR）代表健康和全球economy.However，在抗菌药物研发的兴趣在最近decades.Meanwhile大幅下降的严重威胁，抗毒性药物开发已成为一个有吸引力的替代打AMR.Although几个大分子目标已探索了这个目标，他们的成药是信息的重要一块已经overlooked.This回顾探讨这一主题展示了如何基于结构的，在硅片工具，如PockDrug和FTMap免费提供的，可能是设计新的有用的绿脓素的生物合成途径和改善靶向由热点分析提供的铜绿假单胞菌群体感应机制等的信息，与结合位点的特征沿化合物的效力/选择性的抑制剂，表明基本上还未新颖成药目标（PhzA和PhzS）。然而，它也强调了在硅片成药预测工具有可能在不久的future.Meanwhile克服的局限性，抗毒性的药物靶点应该互补的方法，如组合使用FTMap / PockDrug的评估，一旦达成共识成药分类减少了undruggable蛋白质资源浪费的风险。

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