Publications
137 results found
Maertens G, Cherepanov P, Debyser Z, et al., 2004, Identification and characterization of a functional nuclear localization signal in the HIV-1 integrase interactor LEDGF/p75, JOURNAL OF BIOLOGICAL CHEMISTRY, Vol: 279, Pages: 33421-33429, ISSN: 0021-9258
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- Citations: 82
van Griensven J, Zhan XJ, Van Maele B, et al., 2004, Expression of HIV-1 integrase in CEM cells inhibits HIV-1 replication, JOURNAL OF GENE MEDICINE, Vol: 6, Pages: 268-277, ISSN: 1099-498X
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- Citations: 1
Maertens G, Cherepanov P, Pluymers W, et al., 2003, LEDGF/p75 is essential for nuclear and chromosomal targeting of HIV-1 integrase in human cells, JOURNAL OF BIOLOGICAL CHEMISTRY, Vol: 278, Pages: 33528-33539, ISSN: 0021-9258
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- Citations: 403
Cherepanov P, Maertens G, Proost P, et al., 2003, HIV-1 integrase forms stable tetramers and associates with LEDGF/p75 protein in human cells, JOURNAL OF BIOLOGICAL CHEMISTRY, Vol: 278, Pages: 372-381, ISSN: 0021-9258
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- Citations: 549
Fikkert V, Cherepanov P, van Laethem K, et al., 2002, <i>env</i> chimeric virus technology for evaluating human immunodeficiency virus susceptibility to entry inhibitors, ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, Vol: 46, Pages: 3954-3962, ISSN: 0066-4804
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- Citations: 36
Pannecouque C, Pluymers W, Van Maele N, et al., 2002, New class of HIV integrase inhibitors that block viral replication in cell culture, CURRENT BIOLOGY, Vol: 12, Pages: 1169-1177, ISSN: 0960-9822
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- Citations: 98
Debyser Z, Cherepanov P, Van Maele B, et al., 2002, In search of authentic inhibitors of HIV-1 integration., Antivir Chem Chemother, Vol: 13, Pages: 1-15, ISSN: 0956-3202
Current strategies for the treatment of HIV infection are based on cocktails of drugs that target the viral reverse transcriptase or protease enzymes. At present, the clinical benefit of this combination therapy for HIV-infected patients is considerable, although it is not clear how long this effect will last taking into account the emergence of multiple drug-resistant viral strains. Addition of new anti-HIV drugs targeting additional steps of the viral replication cycle may increase the potency of inhibition and prevent resistance development. During HIV replication, integration of the viral genome into the cellular chromosome is an essential step catalysed by the viral integrase. Although HIV integrase is an attractive target for antiviral therapy, so far all research efforts have led to the identification of only one series of compounds that selectively inhibit the integration step during HIV replication, namely the diketo acids. In this review we try to address the question why it has proven so difficult to find potent and selective integrase inhibitors. We point to potential pitfalls in defining an inhibitor as an authentic integrase inhibitor, and propose new strategies and technologies for the discovery of authentic HIV integration inhibitors.
Debyser Z, Cherepanov P, Pluymers W, et al., 2001, Assays for the evaluation of HIV-1 integrase inhibitors., Methods Mol Biol, Vol: 160, Pages: 139-155, ISSN: 1064-3745
Baekelandt V, Claeys A, Cherepanov P, et al., 2000, DNA-dependent protein kinase is not required for efficient lentivirus integration, JOURNAL OF VIROLOGY, Vol: 74, Pages: 11278-11285, ISSN: 0022-538X
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- Citations: 80
Cherepanov P, Pluymers W, Claeys A, et al., 2000, High-level expression of active HIV-1 integrase from a synthetic gene in human cells, FASEB JOURNAL, Vol: 14, Pages: 1389-1399, ISSN: 0892-6638
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- Citations: 56
Ostendorf T, Cherepanov P, de Vries J, et al., 1999, Characterization of a <i>dam</i> mutant of <i>Serratia marcescens</i> and nucleotide sequence of the <i>dam</i> region, JOURNAL OF BACTERIOLOGY, Vol: 181, Pages: 3880-3885, ISSN: 0021-9193
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- Citations: 17
Pluymers W, Cherepanov P, Schols D, et al., 1999, Nuclear localization of human immunodeficiency virus type 1 integrase expressed as a fusion protein with green fluorescent protein, VIROLOGY, Vol: 258, Pages: 327-332, ISSN: 0042-6822
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- Citations: 64
Cherepanov P, Surratt D, Toelen J, et al., 1999, Activity of recombinant HIV-1 integrase on mini-HIV DNA, NUCLEIC ACIDS RESEARCH, Vol: 27, Pages: 2202-2210, ISSN: 0305-1048
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- Citations: 40
Esté JA, Cabrera C, Schols D, et al., 1998, Human immunodeficiency virus glycoprotein gp120 as the primary target for the antiviral action of AR177 (Zintevir), MOLECULAR PHARMACOLOGY, Vol: 53, Pages: 340-345, ISSN: 0026-895X
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- Citations: 114
Cherepanov P, Este JA, Rando RF, et al., 1997, Mode of interaction of G-quartets with the integrase of human immunodeficiency virus type 1, MOLECULAR PHARMACOLOGY, Vol: 52, Pages: 771-780, ISSN: 0026-895X
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- Citations: 84
Witvrouw M, Balzarini J, Pannecouque C, et al., 1997, SRR-SB3, a disulfide-containing macrolide that inhibits a late stage of the replicative cycle of human immunodeficiency virus, ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, Vol: 41, Pages: 262-268, ISSN: 0066-4804
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- Citations: 39
CHEREPANOV PP, WACKERNAGEL W, 1995, GENE DISRUPTION IN ESCHERICHIA-COLI - TCR AND KM(R) CASSETTES WITH THE OPTION OF FLP-CATALYZED EXCISION OF THE ANTIBIOTIC-RESISTANCE DETERMINANT, GENE, Vol: 158, Pages: 9-14, ISSN: 0378-1119
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- Citations: 1397
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