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Mini-Reviews in Organic Chemistry


ISSN (Print): 1570-193X
ISSN (Online): 1875-6298

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

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

Volume 9, Issue 1, 2012

Page: [20 - 26] Pages: 7

DOI: 10.2174/157019312799080080

Price: $65


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.

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

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