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基于结构的FDA批准药物筛选鉴定出潜在的组蛋白去乙酰化酶3重新利用抑制剂:分子对接和分子动力学模拟方法。

Structure-based screening of FDA-approved drugs identifies potential histone deacetylase 3 repurposed inhibitor: molecular docking and molecular dynamic simulation approaches.

作者信息

Shamsi Anas, Khan Mohd Shahnawaz, Yadav Dharmendra Kumar, Shahwan Moyad

机构信息

Center for Medical and Bio-Allied Health Sciences Research, Ajman University, Ajman, United Arab Emirates.

Department of Biochemistry, College of Science, King Saud University, Riyadh, Saudi Arabia.

出版信息

Front Pharmacol. 2024 Jun 28;15:1424175. doi: 10.3389/fphar.2024.1424175. eCollection 2024.

DOI:10.3389/fphar.2024.1424175
PMID:39005934
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11239971/
Abstract

Histone deacetylase 3 (HDAC3) is a member of the histone deacetylase family that has emerged as a crucial target in the quest for novel therapeutic interventions against various complex diseases, including cancer. The repositioning of FDA-approved drugs presents a promising avenue for the rapid discovery of potential HDAC3 inhibitors. In this study, we performed a structure-based virtual screening of FDA-approved drugs obtained from DrugBank. Candidate hits were selected based on their binding affinities and interactions with HDAC3. These promising hits were then subjected to a comprehensive assessment of their biological properties and drug profiles. Our investigation identified two FDA-approved drugs, Imatinib and Carpipramine, characterized by their exceptional affinity and specificity for the binding pocket of HDAC3. These molecules demonstrated a strong preference for HDAC3 binding site and formed interactions with functionally significant residues within the active site pocket. To gain deeper insights into the binding dynamics, structural stability, and interaction mechanisms, we performed molecular dynamics (MD) simulations spanning 300 nanoseconds (ns). The results of MD simulations indicated that Imatinib and Carpipramine stabilized the structure of HDAC3 and induced fewer conformational changes. Taken together, the findings from this study suggest that Imatinib and Carpipramine may offer significant therapeutic potential for treating complex diseases, especially cancer.

摘要

组蛋白去乙酰化酶3(HDAC3)是组蛋白去乙酰化酶家族的成员,在寻求针对包括癌症在内的各种复杂疾病的新型治疗干预措施中,已成为一个关键靶点。重新定位美国食品药品监督管理局(FDA)批准的药物为快速发现潜在的HDAC3抑制剂提供了一条有前景的途径。在本研究中,我们对从DrugBank获得的FDA批准药物进行了基于结构的虚拟筛选。根据候选药物与HDAC3的结合亲和力和相互作用来选择命中药物。然后对这些有前景的命中药物进行其生物学特性和药物概况的全面评估。我们的研究鉴定出两种FDA批准的药物,伊马替尼和卡比咪嗪,它们对HDAC3的结合口袋具有特殊的亲和力和特异性。这些分子对HDAC3结合位点表现出强烈的偏好,并与活性位点口袋内功能重要的残基形成相互作用。为了更深入地了解结合动力学、结构稳定性和相互作用机制,我们进行了长达300纳秒(ns)的分子动力学(MD)模拟。MD模拟结果表明,伊马替尼和卡比咪嗪稳定了HDAC3的结构,并诱导较少的构象变化。综上所述,本研究结果表明,伊马替尼和卡比咪嗪可能为治疗复杂疾病,尤其是癌症,提供显著的治疗潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a683/11239971/7af4f51855be/fphar-15-1424175-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a683/11239971/5c41da8177e5/fphar-15-1424175-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a683/11239971/bf2f66e145d4/fphar-15-1424175-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a683/11239971/8f1b4096d46d/fphar-15-1424175-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a683/11239971/98bcd5d6987e/fphar-15-1424175-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a683/11239971/bf3f36525c25/fphar-15-1424175-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a683/11239971/7d4e72061636/fphar-15-1424175-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a683/11239971/849b220c4197/fphar-15-1424175-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a683/11239971/0ef570faf1a3/fphar-15-1424175-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a683/11239971/7af4f51855be/fphar-15-1424175-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a683/11239971/5c41da8177e5/fphar-15-1424175-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a683/11239971/bf2f66e145d4/fphar-15-1424175-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a683/11239971/8f1b4096d46d/fphar-15-1424175-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a683/11239971/98bcd5d6987e/fphar-15-1424175-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a683/11239971/bf3f36525c25/fphar-15-1424175-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a683/11239971/7d4e72061636/fphar-15-1424175-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a683/11239971/849b220c4197/fphar-15-1424175-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a683/11239971/0ef570faf1a3/fphar-15-1424175-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a683/11239971/7af4f51855be/fphar-15-1424175-g009.jpg

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