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Covalent Inhibition in Drug Discovery.
ChemMedChem ( IF 3.6 ) Pub Date : 2019-03-26 , DOI: 10.1002/cmdc.201900107 Avick Kumar Ghosh 1 , Indranil Samanta 1 , Anushree Mondal 1 , Wenshe Ray Liu 1
ChemMedChem ( IF 3.6 ) Pub Date : 2019-03-26 , DOI: 10.1002/cmdc.201900107 Avick Kumar Ghosh 1 , Indranil Samanta 1 , Anushree Mondal 1 , Wenshe Ray Liu 1
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Although covalent inhibitors have been used as therapeutics for more than a century, there has been general resistance in the pharmaceutical industry against their further development due to safety concerns. This inclination has recently been reverted after the development of a wide variety of covalent inhibitors to address human health conditions along with the US Food and Drug Administration (FDA) approval of several covalent therapeutics for use in humans. Along with this exciting resurrection of an old drug discovery concept, this review surveys enzymes that can be targeted by covalent inhibitors for the treatment of human diseases. We focus on protein kinases, RAS proteins, and a few other enzymes that have been studied extensively as targets for covalent inhibition, with the aim to address challenges in designing effective covalent drugs and to provide suggestions in the area that have yet to be explored.
中文翻译：
药物发现中的共价抑制。
尽管共价抑制剂已经用作治疗剂已有一个多世纪的历史了，但出于安全考虑，制药行业普遍反对其进一步发展。在开发出多种共价抑制剂以解决人类健康问题之后，这种倾向最近得到了纠正，同时美国食品药品监督管理局（FDA）批准了几种用于人体的共价疗法。伴随着对旧药物发现概念的令人兴奋的复活，本综述探讨了可被共价抑制剂靶向治疗人类疾病的酶。我们专注于蛋白激酶，RAS蛋白和其他一些已被广泛研究为共价抑制靶标的酶，
更新日期：2019-03-26
中文翻译：
药物发现中的共价抑制。
尽管共价抑制剂已经用作治疗剂已有一个多世纪的历史了，但出于安全考虑，制药行业普遍反对其进一步发展。在开发出多种共价抑制剂以解决人类健康问题之后，这种倾向最近得到了纠正，同时美国食品药品监督管理局（FDA）批准了几种用于人体的共价疗法。伴随着对旧药物发现概念的令人兴奋的复活，本综述探讨了可被共价抑制剂靶向治疗人类疾病的酶。我们专注于蛋白激酶，RAS蛋白和其他一些已被广泛研究为共价抑制靶标的酶，
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