Results 31 to 40 of about 71,892 (273)

Comparative biochemical analysis of HIV-1 subtype B and C integrase enzymes

Retrovirology, 2009
Background Integrase inhibitors are currently being incorporated into highly active antiretroviral therapy (HAART). Due to high HIV variability, integrase inhibitor efficacy must be evaluated against a range of integrase enzymes from different subtypes ...
Kuhl Björn D, Donahue Daniel A, Faltenbacher Verena H, Sloan Richard D, Bar-Magen Tamara, Oliveira Maureen, Xu Hongtao, Wainberg Mark A   +7 more
doaj   +1 more source

Emergence of the G118R Pan-Integrase Resistance Mutation as a Result of Low Compliance to a Dolutegravir-Based cART

Infectious Disease Reports, 2022
HIV-1 resistance towards integrase inhibitors is a potential threat of the success of HIV-1 combination treatment. G118R is a rare drug resistance mutation conferring pan-integrase resistance.
Helene Mens, Lasse Fjordside, Jannik Fonager, Jan Gerstoft   +3 more
doaj   +1 more source

Clinical Extrapolation of the Effects of Dolutegravir and Other HIV Integrase Inhibitors on Folate Transport Pathways

Drug Metabolism And Disposition, 2019
Preliminary analysis of ongoing birth surveillance study identified evidence of potential increased risk for neural tube defects (NTDs) in newborns associated with exposure to dolutegravir at the time of conception. Folate deficiency is a common cause of
M. Zamek-Gliszczynski, Xuexiang Zhang, Jennypher Mudunuru, Yewei Du, Jian-Lu Chen, Kunal S. Taskar, Jane Huang, Yong Huang, E. Romach   +8 more
semanticscholar   +1 more source

Absence of Resistance Mutations in the Integrase Coding Region among ART-Experienced Patients in the Republic of the Congo

Microorganisms, 2021
Background: HIV infects around one hundred thousand patients in the Republic of the Congo. Approximately 25% of them receive an antiretroviral treatment; current first-line regimens include two NRTIs and one NNRTI, reverse transcriptase inhibitors ...
Ferdinand Emaniel Brel Got, Patricia Recordon-Pinson, Ghislain Loubano-Voumbi, Dagene Ebourombi, Marie-Lise Blondot, Mathieu Metifiot, Gontran Ondzotto, Marie-Line Andreola   +7 more
doaj   +1 more source

Docking Studies on HIV Integrase Inhibitors Based On Potential Ligand Binding Sites [PDF]

International Journal on Bioinformatics & Biosciences, vol. 2, pp. 21-29, 2012, 2012
HIV integrase is a 32 kDa protein produced from the C-terminal portion of the Pol gene product, and is an attractive target for new anti-HIV drugs. Integrase is an enzyme produced by a retrovirus (such as HIV) that enables its genetic material to be integrated into the DNA of the infected cell.
arxiv   +1 more source

Reduced efficacy of HIV-1 integrase inhibitors in patients with drug resistance mutations in reverse transcriptase

Nature Communications, 2020
Little is known about the impact of pretreatment drug resistance (PDR) on the efficacy of second generation integrase inhibitors. We sequenced pretreatment plasma specimens from the ADVANCE trial (NCT03122262).
M. Siedner, Michelle A. Moorhouse, Bryony Simmons, Túlio de Oliveira, R. Lessells, J. Giandhari, S. Kemp, B. Chimukangara, Godspower Akpomiemie, Celicia M. Serenata, W. Venter, A. Hill, Ravindra K. Gupta   +12 more
semanticscholar   +1 more source

Integrase Inhibitor Resistance Mechanisms and Structural Characteristics in Antiretroviral Therapy-Experienced, Integrase Inhibitor-Naive Adults with HIV-1 Infection Treated with Dolutegravir plus Two Nucleoside Reverse Transcriptase Inhibitors in the DAWNING Study

Antimicrobial Agents and Chemotherapy, 2021
At week 48 in the phase IIIb DAWNING study, the integrase strand transfer inhibitor (INSTI) dolutegravir plus 2 nucleoside reverse transcriptase inhibitors demonstrated superiority to ritonavir-boosted lopinavir in achieving virologic suppression in ...
M. Underwood, Joseph H Horton, Keith Nangle, J. Hopking, Kimberly Smith, M. Aboud, B. Wynne, Jörg Sievers, E. Stewart, Ruolan Wang   +9 more
semanticscholar   +1 more source

Authentic HIV-1 Integrase Inhibitors [PDF]

Future Medicinal Chemistry, 2010
HIV-1 integrase (IN) is indispensable for HIV-1 replication and has become a validated target for developing anti-AIDS agents. In two decades of development of IN inhibition-based anti-HIV therapeutics, a significant number of compounds were identified as IN inhibitors, but only some of them showed antiviral activity.
Terrence R. Burke, Christophe Marchand, Chenzhong Liao, Yves Pommier, Marc C. Nicklaus   +4 more
openaire   +3 more sources

Quantum-Chemistry based design of halobenzene derivatives with augmented affinities for the HIV-1 viral G4/C16 base-pair [PDF]

Front. Chem., 2020, 8, 440, 2019
The HIV-1 integrase (IN) is a major target for the design of novel anti-HIV inhibitors. Among these, three inhibitors which embody a halobenzene ring derivative (HR) in their structures are presently used in clinics. High-resolution X-ray crystallography of the complexes of the IN-viral DNA transient complex bound to each of the three inhibitors showed
arxiv   +1 more source

Synthesis of an Atropisomeric HIV Integrase Inhibitor [PDF]

Synfacts, 2015
Philip Kocieński
openalex   +3 more sources