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靶向生存素的肽抑制剂的计算与实验发现及其在癌症治疗中的潜力

Computational and experimental discovery of peptide inhibitors targeting survivin for therapeutic potential in cancer.

作者信息

Ahmadi Seyedeh Fatemeh, Arab Seyed Shahriar, Samadikhah Hamidreza

机构信息

Department of Biology, CT.C. Islamic Azad University, Tehran, Iran.

Center for Molecular Medicine, Georgia University, Athens, USA.

出版信息

Sci Rep. 2025 Aug 20;15(1):30599. doi: 10.1038/s41598-025-13110-3.

DOI:10.1038/s41598-025-13110-3
PMID:40835666
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12368056/
Abstract

Evidence indicates that the survivin protein is overexpressed in various types of cancer. Survivin belongs to the inhibitors of apoptosis proteins (IAPs) family, which plays a crucial role in preventing apoptosis and regulating the cell cycle. This protein has a multifaceted function in the cell cycle, particularly in regulating mitosis and cytokinesis. Survivin binds to XIAP, enhancing its stability, and interactively inhibiting caspase-9 activity. Additionally, survivin inhibits apoptosis by inactivating the Smac/DIABLO factor. In this study, we investigated the dual role of peptides in disrupting cell division and inducing apoptosis. Specifically, we designed anti-cancer peptides derived from the Borealin protein. Through single-point mutations, we developed several peptide variants and evaluated their efficacy using bioinformatics approaches, including molecular docking and molecular dynamics simulations. Based on these analyses, we identified P2 and P3 peptides as candidates with the highest binding affinities. Subsequently, the P3 was synthesized for experimental validation. By targeting key mechanisms involved in cancer cell survival and proliferation, P3 demonstrates significant potential as a novel anti-cancer agent with reduced side effects. These findings mark an important step forward in the development of more effective cancer therapies.

摘要

有证据表明,生存素蛋白在多种类型的癌症中过度表达。生存素属于凋亡抑制蛋白(IAPs)家族,在防止细胞凋亡和调节细胞周期中起关键作用。这种蛋白在细胞周期中具有多方面功能,特别是在调节有丝分裂和胞质分裂方面。生存素与XIAP结合,增强其稳定性,并交互抑制半胱天冬酶-9的活性。此外,生存素通过使Smac/DIABLO因子失活来抑制细胞凋亡。在本研究中,我们研究了肽在破坏细胞分裂和诱导细胞凋亡中的双重作用。具体而言,我们设计了源自Borealin蛋白的抗癌肽。通过单点突变,我们开发了几种肽变体,并使用生物信息学方法评估其功效,包括分子对接和分子动力学模拟。基于这些分析,我们确定P2和P3肽为具有最高结合亲和力的候选物。随后,合成了P3肽用于实验验证。通过靶向癌细胞存活和增殖所涉及的关键机制,P3作为一种新型抗癌药物,具有显著潜力且副作用减少。这些发现标志着在开发更有效的癌症治疗方法方面向前迈出了重要一步。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5440/12368056/014fed138e2c/41598_2025_13110_Fig8_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5440/12368056/43a275caa671/41598_2025_13110_Fig1a_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5440/12368056/894064291559/41598_2025_13110_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5440/12368056/5255c5bbaaf5/41598_2025_13110_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5440/12368056/8c37ceaf9628/41598_2025_13110_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5440/12368056/9ca87d8aa598/41598_2025_13110_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5440/12368056/ebedcb4446e6/41598_2025_13110_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5440/12368056/3557ebb63617/41598_2025_13110_Fig7_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5440/12368056/014fed138e2c/41598_2025_13110_Fig8_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5440/12368056/43a275caa671/41598_2025_13110_Fig1a_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5440/12368056/894064291559/41598_2025_13110_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5440/12368056/5255c5bbaaf5/41598_2025_13110_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5440/12368056/8c37ceaf9628/41598_2025_13110_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5440/12368056/9ca87d8aa598/41598_2025_13110_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5440/12368056/ebedcb4446e6/41598_2025_13110_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5440/12368056/3557ebb63617/41598_2025_13110_Fig7_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5440/12368056/014fed138e2c/41598_2025_13110_Fig8_HTML.jpg

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本文引用的文献

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2
Survivin as a Therapeutic Target for the Treatment of Human Cancer.生存素作为治疗人类癌症的治疗靶点。
Cancers (Basel). 2024 Apr 27;16(9):1705. doi: 10.3390/cancers16091705.
3
Computational design of anti-cancer peptides tailored to target specific tumor markers.针对特定肿瘤标志物量身定制的抗癌肽的计算设计。
BMC Chem. 2024 Feb 22;18(1):39. doi: 10.1186/s13065-024-01143-0.
4
Molecular dynamics simulation as a promising approach for computational study of liquid crystal-based aptasensors.分子动力学模拟作为一种用于基于液晶的适配体传感器计算研究的有前景的方法。
J Biomol Struct Dyn. 2024 Feb 12:1-13. doi: 10.1080/07391102.2024.2315326.
5
Three Rounds of Stability-Guided Optimization and Systematical Evaluation of Oncolytic Peptide LTX-315.三轮稳定性导向优化及溶瘤肽 LTX-315 的系统评价。
J Med Chem. 2024 Mar 14;67(5):3885-3908. doi: 10.1021/acs.jmedchem.3c02232. Epub 2024 Jan 26.
6
Development of therapeutic monoclonal antibodies against DKK1 peptide-HLA-A2 complex to treat human cancers.针对 DKK1 肽-HLA-A2 复合物的治疗性单克隆抗体的开发,用于治疗人类癌症。
J Immunother Cancer. 2024 Jan 24;12(1):e008145. doi: 10.1136/jitc-2023-008145.
7
Overview of role of survivin in cancer: expression, regulation, functions, and its potential as a therapeutic target.Survivin 在癌症中的作用概述:表达、调控、功能及其作为治疗靶点的潜力。
J Drug Target. 2024 Dec;32(3):223-240. doi: 10.1080/1061186X.2024.2309563. Epub 2024 Feb 1.
8
Structure based docking and biological evaluation towards exploring potential anti-cancerous and apoptotic activity of 6-Gingerol against human prostate carcinoma cells.基于结构的对接和生物评估探索 6-姜酚对人前列腺癌细胞的潜在抗癌和促凋亡活性。
BMC Complement Med Ther. 2024 Jan 2;24(1):8. doi: 10.1186/s12906-023-04269-1.
9
Targeting survivin for cancer therapy: Strategies, small molecule inhibitors and vaccine based therapeutics in development.针对癌症治疗的生存素:开发中的策略、小分子抑制剂和疫苗治疗。
Life Sci. 2023 Dec 15;335:122260. doi: 10.1016/j.lfs.2023.122260. Epub 2023 Nov 12.
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Molecules. 2023 Oct 19;28(20):7165. doi: 10.3390/molecules28207165.