Small molecule CCR5 antagonists in clinical trials and their drug resistances:research advances / 国际药学研究杂志

ABSTRACT

C-C chemokine receptor 5 (CCR5), one of the major co-receptors of HIV-1, can mediate the fusion of HIV-1 to cell membranes. CCR5 antagonists can bind to CCR5 and cause conformational changes in CCR5, thus blocking HIV-1 infection. Several small molecule CCR5 antagonists with strong activity and good tolerance have been screened and entered the clinical trials. With the widespread use of CCR5 antagonists, drug resistance has gradually emerged. There are many reports about of drug-related failure in vivo and in vitro. Therefore, this review summarizes the mechanism of CCR5-mediated HIV-1 infection, the research progress in maraviroc and other CCR5 antagonists which have entered clinical trials and their drug resistance.