Affiliation: Johnson and Johnson Pharmaceutical Research and Development
- Novel HIV-1 reverse transcriptase inhibitorsDirk Jochmans
Tibotec BVBA, Gen De Wittelaan L 11B 3, 2800 Mechelen, Belgium
Virus Res 134:171-85. 2008..This promising research provides much optimism that RT inhibitors will continue to evolve with subsequent clinical benefit...
- Indolopyridones inhibit human immunodeficiency virus reverse transcriptase with a novel mechanism of actionDirk Jochmans
Tibotec BVBA, Generaal de Wittelaan L 11B 3, 2800 Mechelen, Belgium
J Virol 80:12283-92. 2006..In conclusion, this class of indolopyridones can occupy the nucleotide binding site of HIV RT by forming a stable ternary complex whose stability is mainly dependent on the nature of the primer 3' end...
- Resistance mutations in human immunodeficiency virus type 1 integrase selected with elvitegravir confer reduced susceptibility to a wide range of integrase inhibitorsOlivia Goethals
Tibotec BVBA, Mechelen, Belgium
J Virol 82:10366-74. 2008..These data broaden the understanding of antiviral resistance against integrase inhibitors and may give insight facilitating the discovery of second-generation compounds...
- TMC125 displays a high genetic barrier to the development of resistance: evidence from in vitro selection experimentsJohan Vingerhoets
Tibotec, Mechelen, Belgium
J Virol 79:12773-82. 2005..These results demonstrate that TMC125 has a unique profile of activity against NNRTI-resistant virus and possesses a high genetic barrier to the development of resistance in vitro...
- TMC114, a novel human immunodeficiency virus type 1 protease inhibitor active against protease inhibitor-resistant viruses, including a broad range of clinical isolatesSandra De Meyer
Tibotec, Gen De Wittelaan L 11B 3, B2800 Mechelen, Belgium
Antimicrob Agents Chemother 49:2314-21. 2005..Combinations with ritonavir, nelfinavir, and amprenavir showed some evidence of synergy. These results suggest that TMC114 is a potential candidate for the treatment of both naive and PI-experienced patients with HIV...
- Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agentRoger G Ptak
Southern Research Institute, Frederick, Maryland 21701, USA
Antimicrob Agents Chemother 52:1302-17. 2008..Thus, Debio-025 seems to interfere with the function of CypA during the progression/completion of HIV-1 reverse transcription...
- MAPPIT (MAmmalian Protein-Protein Interaction Trap) as a tool to study HIV reverse transcriptase dimerization in intact human cellsEls Pattyn
Department of Medical Protein Research, VIB, A Baertsoenkaai 3, 9000 Ghent, Belgium
J Virol Methods 153:7-15. 2008..These results show that MAPPIT can be used as a novel screening tool for anti-HIV compounds in intact human cells...