Basavapathruni Aravind, Anderson Karen S
Yale University School of Medicine, Department of Pharmacology, New Haven, CT 06520-8066, USA.
FASEB J. 2007 Dec;21(14):3795-808. doi: 10.1096/fj.07-8697rev. Epub 2007 Jul 17.
The HIV/AIDS pandemic has existed for >25 years. Extensive work globally has provided avenues to combat viral infection, but the disease continues to rage on in the human population and infected approximately 4 million people in 2006 alone. In this review, we provide a brief history of HIV/AIDS, followed by analysis of one therapeutic target of HIV-1: its reverse transcriptase (RT). We discuss the biochemical characterization of RT in order to place emphasis on possible avenues of inhibition, which now includes both nucleoside and non-nucleoside modalities. Therapies against RT remain a cornerstone of anti-HIV treatment, but the virus eventually resists inhibition through the selection of drug-resistant RT mutations. Current inhibitors and associated resistance are discussed, with the hopes that new therapeutics can be developed against RT.
艾滋病毒/艾滋病大流行已存在超过25年。全球范围内的大量工作为抗击病毒感染提供了途径，但该疾病仍在人类群体中肆虐，仅在2006年就感染了约400万人。在本综述中，我们简要介绍了艾滋病毒/艾滋病的历史，随后分析了HIV-1的一个治疗靶点：其逆转录酶（RT）。我们讨论了RT的生化特性，以强调可能的抑制途径，目前这包括核苷类和非核苷类方式。针对RT的疗法仍然是抗艾滋病毒治疗的基石，但病毒最终会通过选择耐药性RT突变来抵抗抑制。本文讨论了当前的抑制剂及相关耐药性，希望能够开发出针对RT的新疗法。
