通过计算方法优化抗体抑制CD47- SIRPα的稳定性和有效性。

IF 3.9 2区 化学 Q2 CHEMISTRY, APPLIED Molecular Diversity Pub Date : 2025-01-20 DOI:10.1007/s11030-024-11037-x
Kapil Laddha, M Elizabeth Sobhia
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引用次数: 0

摘要

CD47是一种细胞表面蛋白,作为一种“不要吃我”的信号,在与SIRPα相互作用时阻止免疫细胞吞噬健康细胞。癌细胞利用这一机制通过过表达CD47来逃避免疫破坏。阻断CD47与其受体SIRPα之间的相互作用是一种很有前景的治疗策略。靶向这些表面蛋白与小分子之间的相互作用是相当具有挑战性的,另一方面,抗体提供了潜力。然而,抗原(CD47)和抗体(B6H12.2)之间的相互作用在这种情况下起着至关重要的作用,通过突变相互作用残基来增加亲和力可能会影响抗体对抗原的倾向性和有效性。因此,本研究的重点是设计与野生型相比对抗原具有更高亲和力和稳定性的抗体。残差扫描计算突变抗体的相互作用残基和疏水残基,并评估亲和力。计算方法包括抗原-抗体对接研究和分子动力学模拟,以评估这些修饰抗体的亲和力、稳定性和治疗潜力。
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Optimizing antibody stability and efficacy in CD47- SIRPα inhibition via computational approaches.

CD47, a cell surface protein, serves as a "don't eat me" signal that prevents immune cells from engulfing healthy cells upon its interaction with SIRPα. Cancer cells exploit this mechanism by overexpressing CD47 to evade immune destruction. Blocking the interaction between CD47 and its receptor, SIRPα, is a promising therapeutic strategy. Targeting the interactions between these surface proteins with small molecules is quite challenging, and on the other hand, antibodies offer potential. However, the interactions between antigen (CD47) and antibody (B6H12.2) play a crucial role in this scenario, and increasing the affinity by mutating the interacting residues might impact the inclination and effectiveness of the antibody towards antigen. Thus, this study focuses on designing antibodies with increased affinity and stability towards the antigen compared to the wild-type. Residual scanning calculations were performed to mutate the interacting as well as the hydrophobic residues of the antibody and affinity was assessed. Computational approaches, including antigen-antibody docking studies and molecular dynamics simulations, were employed to evaluate the affinity, stability and therapeutic potential of these modified antibodies.

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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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