Inhibition of HIV-1 by non-nucleoside reverse transcriptase inhibitors via an induced fit mechanism-Importance of slow dissociation and relaxation rates for antiviral efficacy.
本研究考察非核苷逆转录酶抑制剂(NNRTIs)缓慢解离对抗HIV-1疗效的重要性。作者采用表面等离子共振(SPR)生物传感器技术,分析一系列NNRTIs与野生型及耐药突变体HIV-1逆转录酶(RT)的相互作用,并在MT-4细胞和外周血单个核细胞(PBMC)中测定抗病毒效应。由于解离极慢且机制复杂,速率常数无法定量,故用模拟传感器图进...