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Allosteric drugs and mutations: chances, challenges, and necessity.
Current Opinion in Structural Biology ( IF 6.1 ) Pub Date : 2020-02-12 , DOI: 10.1016/j.sbi.2020.01.010
Enrico Guarnera 1 , Igor N Berezovsky 2
Affiliation  

Allosteric drugs have become an indispensable toolbox of rapidly developing precision medicine, having already established reputation of advantages over traditional medicines. Allosteric mechanisms are also widely involved in the action of SNPs and latent cancer drivers, and can be used in fine and specific tuning of biologics, providing a great potential in diagnostics and therapy. We discuss here major targets for prospected allosteric medicines, currently available allosteric compounds, and drug-candidates at different stages of research and (pre)clinical trials. We describe our computational model of the comprehensive allosteric control of protein activity, outlining the ways of implementing it in pharmacological applications. Finally, we formulate outstanding questions and discuss feasible directions in the work on allosteric drugs and mutations.

中文翻译:

变构药物和突变:机会、挑战和必要性。

变构药物已成为精准医疗快速发展不可或缺的工具箱,已经确立了优于传统药物的声誉。变构机制也广泛参与 SNP 和潜在癌症驱动因素的作用,可用于生物制剂的精细和特异性调整,在诊断和治疗方面具有巨大潜力。我们在这里讨论了预期变构药物的主要目标、目前可用的变构化合物以及处于不同研究和(预)临床试验阶段的候选药物。我们描述了我们的蛋白质活性综合变构控制的计算模型,概述了在药理学应用中实现它的方法。最后,
更新日期:2020-02-12
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