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.
Keywords: Coiled-coil, docking simulation, gp41, heptad repeat, HIV, membrane fusion, quantitative structure-activity relationship, smallmolecule inhibitors, HAART, drug targets, bioavailability
Mini-Reviews in Organic Chemistry
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:
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.
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Cite this article as:
Kawashita Norihito, Tian Yu-Shi, Chandimal de Silva U., Okamoto Kousuke and Takagi Tatsuya, Recent Advances in the Development of Small-Molecule Compounds Targeting HIV- 1 gp41 as Membrane Fusion Inhibitors, Mini-Reviews in Organic Chemistry 2012; 9 (1) . https://dx.doi.org/10.2174/157019312799080080
DOI https://dx.doi.org/10.2174/157019312799080080 |
Print ISSN 1570-193X |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6298 |
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