| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 2082536 | Drug Discovery Today: Technologies | 2012 | 8 Pages |
Abstract
Integrase (IN) is the last of the three Human Immunodeficiency Virus-1 (HIV-1) enzymes to be targeted by antiretroviral therapy. At present, a single integration inhibitor (raltegravir) has been approved for clinical use. Rapid emergence of drug resistance warrants development of novel inhibitors. Fortunately, the past few years have brought forth a tremendous increase in the understanding of the molecular and structural biology of integration. We discuss recent discoveries as well as novel opportunities for structure-based design in the quest for novel IN inhibitors.
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Authors
Jonas Demeulemeester, Frauke Christ, Marc De Maeyer, Zeger Debyser,