Recent Advances in the Development of Small-Molecule Compounds Targeting HIV- 1 gp41 as Membrane Fusion Inhibitors

Title: Recent Advances in the Development of Small-Molecule Compounds Targeting HIV- 1 gp41 as Membrane Fusion Inhibitors

VOLUME: 9 ISSUE: 1

Author(s):Norihito Kawashita, Yu-Shi Tian, U. Chandimal de Silva, Kousuke Okamoto and Tatsuya Takagi

Affiliation:Graduate School of Pharmaceutical Sciences, Osaka University, 1-6 Yamadaoka, Suita, Osaka, 565-0871, Japan.

Keywords:Coiled-coil, docking simulation, gp41, heptad repeat, HIV, membrane fusion, quantitative structure-activity relationship, smallmolecule inhibitors, HAART, drug targets, bioavailability

Abstract: Over the past few years, remarkable progress has been made in the development of human immunodeficiency virus (HIV) membrane fusion inhibitors. The focus has been on peptide inhibitors, which were developed by mimicking HIV sequences; however, these types of inhibitors generally lack oral bioavailability and are expensive. Therefore, development of small-molecule inhibitors has gained importance and recently progressed. This paper reviews the rapid advancements in the development of small-molecule HIV inhibitors over the last decade.