靶向周期蛋白依赖性激酶11:一种发现天然抗癌化合物的计算方法。

IF 3.9 2区 化学 Q2 CHEMISTRY, APPLIED
Suruchi Bhambri, Prakash C Jha
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引用次数: 0

摘要

癌症是全球主要的死亡原因,由于对化疗和放疗等传统疗法的耐药性,给治疗带来了相当大的挑战。细胞周期蛋白依赖性激酶11 (Cyclin-dependent kinase 11, CDK11)在细胞周期调控和转录中起着关键作用,在多种癌症中过表达,并与不良预后有关。本研究的重点是使用计算药物发现方法识别CDK11的潜在抑制剂。采用药效团建模、虚拟筛选、分子对接、ADMET预测、分子动力学模拟、结合自由能分析等技术筛选大型天然产物数据库。验证了三种药效团模型,从而鉴定出几种具有比参考抑制剂更强结合亲和力的有希望的化合物。ADMET分析显示了良好的药物样特性,而分子动力学模拟证实了顶级候选药物与CDK11的稳定性和良好的相互作用。结合自由能进一步计算表明,UNPD29888具有最强的结合亲和力。总之,基于计算预测,鉴定的化合物显示出作为CDK11抑制剂的潜力,表明它们未来通过靶向CDK11在癌症治疗中的应用。这些计算结果鼓励进一步的实验验证作为抗癌剂。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Targeting cyclin-dependent kinase 11: a computational approach for natural anti-cancer compound discovery.

Cancer, a leading global cause of death, presents considerable treatment challenges due to resistance to conventional therapies like chemotherapy and radiotherapy. Cyclin-dependent kinase 11 (CDK11), which plays a pivotal role in cell cycle regulation and transcription, is overexpressed in various cancers and is linked to poor prognosis. This study focused on identifying potential inhibitors of CDK11 using computational drug discovery methods. Techniques such as pharmacophore modeling, virtual screening, molecular docking, ADMET predictions, molecular dynamics simulations, and binding free energy analysis were applied to screen a large natural product database. Three pharmacophore models were validated, leading to the identification of several promising compounds with stronger binding affinities than the reference inhibitor. ADMET profiling indicated favorable drug-like properties, while molecular dynamics simulations confirmed the stability and favorable interactions of top candidates with CDK11. Binding free energy calculations further revealed that UNPD29888 exhibited the strongest binding affinity. In conclusion, the identified compound shows potential as a CDK11 inhibitor based on computational predictions, suggesting their future application in cancer treatment by targeting CDK11. These computational findings encourage further experimental validation as anti-cancer agents.

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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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