4LH5

Dual inhibition of HIV-1 replication by Integrase-LEDGF allosteric inhibitors is predominant at post-integration stage during virus production rather than at integration

4LH5 の概要

• エントリーDOI: 10.2210/pdb4lh5/pdb
• 関連するPDBエントリー: 1BHL 4LH4
• 分子名称: Integrase, (2S)-tert-butoxy[4-(3,4-dihydro-2H-chromen-6-yl)-2-methylquinolin-3-yl]ethanoic acid, MAGNESIUM ION, ... (4 entities in total)
• 機能のキーワード: transferase-transferase inhibitor complex, transferase/transferase inhibitor
• 由来する生物種: Human immunodeficiency virus 1
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 20569.44

構造登録者

Ruff, M.,Levy, N.,Eiler, S. (登録日: 2013-06-30, 公開日: 2013-12-25, 最終更新日: 2024-11-20)

主引用文献

Le Rouzic, E.,Bonnard, D.,Chasset, S.,Bruneau, J.M.,Chevreuil, F.,Le Strat, F.,Nguyen, J.,Beauvoir, R.,Amadori, C.,Brias, J.,Vomscheid, S.,Eiler, S.,Levy, N.,Delelis, O.,Deprez, E.,Saib, A.,Zamborlini, A.,Emiliani, S.,Ruff, M.,Ledoussal, B.,Moreau, F.,Benarous, R.
Dual inhibition of HIV-1 replication by integrase-LEDGF allosteric inhibitors is predominant at the post-integration stage.
Retrovirology, 10:144-144, 2013

PubMed Abstract: LEDGF/p75 (LEDGF) is the main cellular cofactor of HIV-1 integrase (IN). It acts as a tethering factor for IN, and targets the integration of HIV in actively transcribed gene regions of chromatin. A recently developed class of IN allosteric inhibitors can inhibit the LEDGF-IN interaction.

PubMed: 24261564
DOI: 10.1186/1742-4690-10-144

実験手法

X-RAY DIFFRACTION (2.19 Å)