抗艾滋病药物新靶标及其小分子抑制剂的研究进展

Progress on AIDS drug targets and small molecule inhibitors

抗艾滋病药物的长期使用导致严重的耐药性和药物不良反应,以及难以根治等问题,迫使人们不断研发新的抗艾滋病药物。随着HIV-1致病机制和生物学特征的深入研究以及药物发现筛选技术的快速发展,新一代抗艾滋病药物靶标及其抑制剂被陆续发现,为艾滋病的治疗方案提供了新的选择。本综述精选近几年最具代表性的研究实例,从药物化学的视角总结了抗艾滋病药物新靶标及其小分子抑制剂的前沿进展。

The difficulty to eradicate the HIV-1, off-target effects together with the rapid emergence of multidrug-resistant strains have created an urgent need for more potent and less toxic therapies against other targets of HIV virus. From the point of view of medicinal chemistry, we summarizes and discusses current endeavours towards the discovery and development of novel inhibitors with various scaffolds or distinct mechanisms of action, and also provides examples illustrating new methodologies in medicinal chemistry that contribute to the identification of novel antiretroviral agents.