HIV-1 integrase: The next target for AIDS therapy?

Pathologie Biologie

Volumn 49, Issue 3, 2001, Pages 237-246

  D'Angelo, J ^a   Mouscadet, J F ^b   Desmaele D ^a   Zouhiri, F ^c   Leh, H ^c  

^a CNRS   (France)

^b INSTITUT GUSTAVE ROUSSY   (France)

^c BioAlliance Pharma   (France)

Author keywords

AIDS; Antiviral agents; Enzyme inhibitors; HIV; Virus integration

Indexed keywords

ASPARTIC ACID; GLUTAMIC ACID; GLUTAMINE; INTEGRASE; INTEGRASE INHIBITOR; LYSINE; MAGNESIUM; MANGANESE; METAL ION; PROTEINASE INHIBITOR; RNA DIRECTED DNA POLYMERASE; STYRYLQUINOLINE; UNCLASSIFIED DRUG; VIRUS DNA; VIRUS ENZYME;

ACQUIRED IMMUNE DEFICIENCY SYNDROME; ANTIVIRAL ACTIVITY; CATALYSIS; CRYSTAL STRUCTURE; DNA INTEGRATION; DRUG MECHANISM; DRUG POTENCY; DRUG STRUCTURE; DRUG TARGETING; HUMAN IMMUNODEFICIENCY VIRUS 1; REVIEW; VIRUS REPLICATION;

ACQUIRED IMMUNODEFICIENCY SYNDROME; ANIMALS; ANTI-HIV AGENTS; BINDING SITES; CELL LINE; CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; ENZYME INHIBITORS; HIV INTEGRASE; HIV-1; HUMANS; MACROMOLECULAR SUBSTANCES; MOLECULAR STRUCTURE; PROTEIN CONFORMATION; PROTEIN STRUCTURE, TERTIARY; QUINOLINES; RATS; RECOMBINANT PROTEINS; VIRUS INTEGRATION;

EID: 0035045365     PISSN: 03698114     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0369-8114(01)00135-3     Document Type: Short Survey

References (42)

1. Declining morbidity and mortality among patients with advanced human immunodeficiency virus infection. HIV outpatient study investigators
2. The decay of the latent reservoir of replication-competent HIV-1 is inversely correlated with the extent of residual viral replication during prolonged anti-retroviral therapy
3. Latent infection of CD4+ T cells provides a mechanism for lifelong persistence of HIV-1, even in patients on effective combination therapy
4. Mode of interaction of G-quartets with the integrase of human immunodeficiency virus type 1
5. Retroviral DNA integration: Structure of an integration intermediate
6. Retroviral integration: Structure of the initial covalent product and its precursor, and a role for the viral IN protein
7. Integration
8. Retroviral integrases and their cousins
9. Five-stranded beta-sheet sandwiched with two alpha-helices: A structural link between restriction endonucleases EcoRI and EcoRV
10. Inhibitors of human immunodeficiency virus integrase
11. 2+-dependent activities of recombinant human immunodeficiency virus type I integrase
12. Oligomeric states of the HIV-I integrase as measured by time-resolved fluorescence anisotropy
13. Effect of topoisomerase inhibitors on the in vitro HIV DNA integration reaction
14. Alternate strand DNA triple helix-mediated inhibition of HIV-1 U5 long terminal repeat integration in vitro
15. Inhibitory effect of the polyanionic drug suramin in the in vitro HIV DNA integration reaction
16. Inhibition of HIV-1 integration protein by aurintricarboxylic acid monomers, monomer analogs, and polymer fractions
17. Inhibition of human immunodeficiency virus integrase by bis-catechols
18. Inhibition of HIV-1 integrase by flavones caffeic acid phenethyl ester (CAPE) and related compounds
19. Inhibition of human immunodeficiency virus type-1 integrase by curcumin
20. Effects of tyrphostins, protein kinase inhibitors, on human immunodeficiency virus type 1 integrase
21. Arctigenin as a lead structure for inhibitors of human immunodeficiency virus type-1 integrase
22. Coumarin-based inhibitors of HIV integrase
23. Cosalane analogues with enhanced potencies as inhibitors of HIV-1 protease and integrase
24. Potent inhibitors of human immunodeficiency virus type I integrase: Identification of a novel four-point pharmacophore and tetracyclines as novel inhibitors
25. Hydrazide-containing inhibitors of HIV-1 integrase
26. Depsides and depsidones as inhibitors of HIV-1 integrase: Discovery of novel inhibitors through 3D database searching
27. Diarylsulfones, a novel class of human immunodeficiency virus type 1 integrase inhibitors
28. Stucture-activity relationships: Analogues of the dicaffeoylquinic and dicaffeoyltartaric acids as potent inhibitors of human immunodeficiency virus type 1 integrase and replication
29. Structure of the HIV-1 integrase catalytic domain complexed with an inhibitor: A platform for antiviral drug design
30. Inhibitors of strand transfer that prevent integration and inhibit HIV-1 replication in cells
31. Styryl-quinoline derivatives: A new class of potent HIV-1-integrase inhibitors that block HIV-1 replication in CEM cells
32. Structure-activity relationships and binding mode of styrylquinolines as potent inhibitors of HIV-1 integrase and replication of HIV-1 in cell culture
33. Crystal structure of the catalytic domain of HIV-1 integrase: Similarity to other polynucleotidyl transferases
34. The catalytic domain of human immunodeficiency virus integrase: Ordered active site in the F185H mutant
35. Three new structures of the core domain of HIV-1 integrase: An active site that binds magnesium
36. A structural basis for metal ion mutagenicity and nucleotide selectivity in human DNA polymerase β
37. Structural basis for the 3′-5′exonuclease activity of Escherichia coli DNA polymerase I: A two metal ion mechanism
38. Similarities in the HIV-1 and ASV integrase active sites upon metal cofactor binding
39. Stucture of the catalytic domain of avian sarcoma virus integrase with a bound HIV-1 integrase-targeted inhibitor
40. Identification of a nucleotide binding site in HIV-1 integrase
41. Modeling of the inhibition of retroviral integrases by styrylquinoline derivatives
42. Resistance to the anti-human immunodeficiency virus type 1 compound L-chicoric acid results from a single mutation at amino acid 140 of integrase