Zhang Chengfeng, Li Benteng, Li Jiamei, Zhang Haihong, Wu Yuqing
State Key Laboratory for Supramolecular Structure and Materials, College of Chemistry, Jilin University, No. 2699 Qianjin Street, Changchun 130012, China.
Institute of Theoretical Chemistry, College of Chemistry, Jilin University, No. 2 Liutiao Road, Changchun 130023, China.
Int J Mol Sci. 2025 Jun 17;26(12):5819. doi: 10.3390/ijms26125819.
The HIV-1 capsid has emerged as a highly attractive drug target due to its highly conserved sequence and critical role in the viral life cycle. By disrupting interactions between capsid proteins and impairing the proper assembly or disassembly of the capsid, the inhibitors can effectively suppress HIV-1 replication and infection. Based on this mechanism, numerous small-molecule agents targeting the HIV-1 capsid protein have been developed to date. In this review, we report the latest advances in such inhibitors and delve into their molecular mechanisms of action. We find a focus on small molecules modulating capsid stability and their assembly/disassembly. Hopefully this study will further enhance the understanding of HIV-1 inhibition mechanisms, facilitating the future exploration of novel capsid inhibitors.
由于HIV-1衣壳具有高度保守的序列以及在病毒生命周期中的关键作用，它已成为极具吸引力的药物靶点。通过破坏衣壳蛋白之间的相互作用并损害衣壳的正确组装或拆卸，抑制剂可有效抑制HIV-1的复制和感染。基于这一机制，迄今为止已开发出许多靶向HIV-1衣壳蛋白的小分子药物。在本综述中，我们报告了此类抑制剂的最新进展，并深入探讨了它们的分子作用机制。我们发现研究重点在于调节衣壳稳定性及其组装/拆卸的小分子。希望这项研究将进一步加深对HIV-1抑制机制的理解，促进未来新型衣壳抑制剂的探索。
