Recent progress and structural insights of potential Hsp90 inhibitors as anticancer agents.

IF 3.9 2区 化学 Q2 CHEMISTRY, APPLIED
Aastha Singh, Subhadip Maity, Priya Devi, Aman Rai, Vivek Asati
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引用次数: 0

Abstract

Hsp90, or heat shock protein 90, a well-preserved molecular chaperone that is essential for the coordination of numerous biological pathways and cellular processes. Hsp90 is a molecular chaperone, which promises a target for cancer treatment. Hsp90 inhibitors are a class of drugs that have been extensively studied in preclinical models and demonstrated promise in treating a variety of illnesses, particularly cancer. Hsp90 inhibitors, however, have been encountered a number of challenges during the clinical development process, such as low efficacy, toxicity, and drug resistance. This literature survey emphasizes the importance of HSP90 inhibitors incorporating diverse heterocyclic rings, such as pyrazole, indole, pyrimidine, triazole, and thioquinazoline, which have exhibited promising anticancer activity. This review covers several parameters, including kinetic investigation, binding interactions, IC50 value, structure-activity relationship, and molecular docking studies of the most potent compound. There are several heterocyclic small molecules under investigation in clinical studies, such as AUY922, SNX-5422, STA-9090, and others. This review also contained a patent of HSP90 inhibitors, which showed greater effectiveness. Therefore, the main objective of this paper is to summarize all recent developments in the creation of anticancer medications that target HSP90 inhibitors in order to treat anticancer disease.

Hsp90抑制剂作为抗癌药物的最新进展和结构见解。
热休克蛋白90是一种保存完好的分子伴侣,对许多生物途径和细胞过程的协调至关重要。Hsp90是一种分子伴侣,有望成为癌症治疗的靶点。热休克蛋白90抑制剂是一类在临床前模型中被广泛研究的药物,在治疗各种疾病,特别是癌症方面表现出了希望。然而,Hsp90抑制剂在临床开发过程中遇到了一些挑战,如低疗效、毒性和耐药。本文献综述强调了含有不同杂环的HSP90抑制剂的重要性,如吡唑、吲哚、嘧啶、三唑和硫代喹唑啉,它们已显示出有希望的抗癌活性。本文综述了最有效化合物的动力学研究、结合作用、IC50值、构效关系和分子对接研究等参数。有几种杂环小分子正在临床研究中,如AUY922、SNX-5422、STA-9090等。这篇综述还包含了一项HSP90抑制剂的专利,它显示出更大的有效性。因此,本文的主要目的是总结所有针对HSP90抑制剂的抗癌药物的最新进展,以治疗抗癌疾病。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
Molecular Diversity
Molecular Diversity 化学-化学综合
CiteScore
7.30
自引率
7.90%
发文量
219
审稿时长
2.7 months
期刊介绍: Molecular Diversity is a new publication forum for the rapid publication of refereed papers dedicated to describing the development, application and theory of molecular diversity and combinatorial chemistry in basic and applied research and drug discovery. The journal publishes both short and full papers, perspectives, news and reviews dealing with all aspects of the generation of molecular diversity, application of diversity for screening against alternative targets of all types (biological, biophysical, technological), analysis of results obtained and their application in various scientific disciplines/approaches including: combinatorial chemistry and parallel synthesis; small molecule libraries; microwave synthesis; flow synthesis; fluorous synthesis; diversity oriented synthesis (DOS); nanoreactors; click chemistry; multiplex technologies; fragment- and ligand-based design; structure/function/SAR; computational chemistry and molecular design; chemoinformatics; screening techniques and screening interfaces; analytical and purification methods; robotics, automation and miniaturization; targeted libraries; display libraries; peptides and peptoids; proteins; oligonucleotides; carbohydrates; natural diversity; new methods of library formulation and deconvolution; directed evolution, origin of life and recombination; search techniques, landscapes, random chemistry and more;
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