Bacheler Lee T.
Experimental Station, DuPont Pharmaceuticals Company, Wilmington, DE, USA
Drug Resist Updat. 1999 Feb;2(1):56-67. doi: 10.1054/drup.1998.0064.
Non-nucleoside reverse transcriptase inhibitors (NNRTIs) are a structurally diverse group of compounds which function as inhibitors of HIV-1 replication in vitro and in vivo. Viral resistance is mediated through alterations in the amino acids which form the allosteric site on the HIV-1 reverse transcriptase to which NNRTIs bind. The rapid emergence of resistant viruses has limited the utility of NNRTI monotherapy; however, recent clinical studies have shown that potent NNRTIs can contribute to profound suppression of HIV replication when used in combination therapy. An understanding of the development of resistance to NNRTIs is critical to the effective use of this class of antiretroviral agents. Copyright 1999 Harcourt Publishers Ltd.
非核苷类逆转录酶抑制剂（NNRTIs）是一类结构多样的化合物，在体外和体内均发挥HIV-1复制抑制剂的作用。病毒耐药性是通过构成HIV-1逆转录酶变构位点（NNRTIs与之结合）的氨基酸改变介导的。耐药病毒的迅速出现限制了NNRTI单一疗法的应用；然而，最近的临床研究表明，强效NNRTIs在联合治疗中使用时可显著抑制HIV复制。了解对NNRTIs的耐药性发展对于有效使用这类抗逆转录病毒药物至关重要。版权所有1999年哈考特出版有限公司。
