Development of HIV entry inhibitors targeted to the coiled-coil regions ofgp41

The discoveries that synthetic peptides corresponding to the N- and C-termi nal heptad repeat (HR) regions of gp41 have potent anti-HIV activity opened a new avenue to identification of small molecule HIV entry inhibitors targ eted to the HIV gp41 coiled-coil regions. Based on the structural informati on of the HIV gp41 core, three distinct approaches to develop small molecul e anti-HIV agents have been reported. Each of these approaches has specific advantages, which will have complementary effects on the design of new str ategies for identification of more potent HIV entry inhibitors. It is expec ted that novel antiviral drugs targeted to the HIV gp41 coiled-coil regions will be developed in the near future for the chemotherapy and/or prophylax is of HIV infection and AIDS. (C) 2000 Academic Press.