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Targeting Protein Folding: A Novel Approach for the Treatment of Pathogenic Bacteria.
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2020-08-13 , DOI: 10.1021/acs.jmedchem.0c00911 Nicolas J Scheuplein 1 , Nicole M Bzdyl 2 , Emily A Kibble 2, 3 , Theresa Lohr 1 , Ulrike Holzgrabe 1 , Mitali Sarkar-Tyson 2
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2020-08-13 , DOI: 10.1021/acs.jmedchem.0c00911 Nicolas J Scheuplein 1 , Nicole M Bzdyl 2 , Emily A Kibble 2, 3 , Theresa Lohr 1 , Ulrike Holzgrabe 1 , Mitali Sarkar-Tyson 2
Affiliation
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Infectious diseases are a major cause of morbidity and mortality worldwide, exacerbated by increasing antibiotic resistance in many bacterial species. The development of drugs with new modes of action is essential. A leading strategy is antivirulence, with the aim to target bacterial proteins that are important in disease causation and progression but do not affect growth, resulting in reduced selective pressure for resistance. Immunophilins, a superfamily of peptidyl-prolyl cis–trans isomerase (PPIase) enzymes have been shown to be important for virulence in a broad-spectrum of pathogenic bacteria. This Perspective will provide an overview of the recent advances made in understanding the role of each immunophilin family, cyclophilins, FK506 binding proteins (FKBPs), and parvulins in bacteria. Inhibitor design and medicinal chemistry strategies for development of novel drugs against bacterial FKBPs will be discussed. Furthermore, drugs against human cyclophilins and parvulins will be reviewed in their current indication as antiviral and anticancer therapies.
中文翻译：
靶向蛋白质折叠：一种治疗病原细菌的新方法。
传染病是全球发病率和死亡率的主要原因，许多细菌物种对抗生素的抗药性不断加剧。开发具有新作用方式的药物至关重要。领先的策略是抗病毒，其目标是靶向对疾病致病和进展很重要但不影响生长的细菌蛋白质，从而降低抗药性的选择性压力。免疫因子，一个家族的肽基脯氨酰顺-反式异构酶（PPIase）酶已被证明对广谱致病细菌的毒力很重要。本观点将概述在理解每个亲免蛋白家族，亲环蛋白，FK506结合蛋白（FKBPs）和小白蛋白在细菌中的作用方面的最新进展。将讨论针对细菌FKBPs的新药开发的抑制剂设计和药物化学策略。此外，针对人类亲环蛋白和小白蛋白的药物将以其目前的适应症作为抗病毒和抗癌疗法进行审查。
更新日期：2020-08-13
中文翻译：
靶向蛋白质折叠：一种治疗病原细菌的新方法。
传染病是全球发病率和死亡率的主要原因，许多细菌物种对抗生素的抗药性不断加剧。开发具有新作用方式的药物至关重要。领先的策略是抗病毒，其目标是靶向对疾病致病和进展很重要但不影响生长的细菌蛋白质，从而降低抗药性的选择性压力。免疫因子，一个家族的肽基脯氨酰顺-反式异构酶（PPIase）酶已被证明对广谱致病细菌的毒力很重要。本观点将概述在理解每个亲免蛋白家族，亲环蛋白，FK506结合蛋白（FKBPs）和小白蛋白在细菌中的作用方面的最新进展。将讨论针对细菌FKBPs的新药开发的抑制剂设计和药物化学策略。此外，针对人类亲环蛋白和小白蛋白的药物将以其目前的适应症作为抗病毒和抗癌疗法进行审查。
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