scholarly journals Lack of Pharmacokinetic Interaction Between the HIV‐1 Maturation Inhibitor GSK3640254 and Combination Oral Contraceptives in Healthy Women

2021 ◽  
Author(s):  
Teodora Pene Dumitrescu ◽  
Thomas J. Greene ◽  
Samit R. Joshi ◽  
Jianfeng Xu ◽  
Mark Johnson ◽  
...  
Keyword(s):  
Oral Contraceptives ◽  
Pharmacokinetic Interaction ◽  
Healthy Women ◽  
Maturation Inhibitor ◽  
Hiv 1

Increased frequency of mind wandering in healthy women using oral contraceptives

2019 ◽  
Vol 101 ◽  
pp. 121-127 ◽  
Author(s):  
Catherine Raymond ◽  
Marie-France Marin ◽  
Robert-Paul Juster ◽  
Sarah Leclaire ◽  
Olivier Bourdon ◽  
...  
Keyword(s):  
Oral Contraceptives ◽  
Mind Wandering ◽  
Healthy Women

Ex vivo analysis of HIV-1 co-receptors at the endocervical mucosa of women using oral contraceptives

2004 ◽  
Vol 111 (12) ◽  
pp. 1468-1470 ◽  
Author(s):  
Manyu Prakash ◽  
Steve Patterson ◽  
Frances Gotch ◽  
Moses S. Kapembwa
Keyword(s):  
Oral Contraceptives ◽  
Ex Vivo ◽  
Hiv 1

scholarly journals Influence of female hormonal fluctuation on maximum occlusal force

2011 ◽  
Vol 22 (6) ◽  
pp. 497-501
Author(s):  
Thaís Marques Simek Vega Gonçalves ◽  
Lucíola Maria Rodrigues de Vasconcelos ◽  
Wander José da Silva ◽  
Altair Antoninha Del Bel Cury ◽  
Renata Cunha Matheus Rodrigues Garcia
Keyword(s):  
Menstrual Cycle ◽  
Test Data ◽  
Oral Contraceptives ◽  
Occlusal Force ◽  
Menstrual Cycles ◽  
Healthy Women ◽  
Hormonal Fluctuations ◽  
One Way Anova ◽  
Molar Region ◽  
Hormonal Levels

Hormonal fluctuations during the menstrual cycle may influence on muscular tensions and probably alter occlusal force. The aim of this study was to evaluate whether hormonal levels affect maximum occlusal force (MOF) of healthy women throughout the different phases of the menstrual cycle. Sixty complete dentate subjects who were not under use of oral contraceptives were selected to participate in this study. MOF was bilaterally evaluated on the molar region, during 3 complete menstrual cycles, using 5.65 mm-wide sensors. Measurements were carried out during each of the following menstrual cycle phases: menstrual, follicular, periovulatory and luteal, presumed by ovulation test. Data were analyzed by one-way ANOVA and Tukey-Kramer test (p<0.05). Comparisons among menstrual cycle phases showed no differences on MOF (p=0.27). Under the conditions of this study, it may be concluded that hormonal fluctuations during the menstrual cycle do not affect MOF of a sample of healthy women.

scholarly journals The HIV-1 maturation inhibitor, EP39, interferes with the dynamic helix-coil equilibrium of the CA-SP1 junction of Gag

2020 ◽  
Vol 204 ◽  
pp. 112634
Author(s):  
Xiaowei Chen ◽  
Pascale Coric ◽  
Valery Larue ◽  
Serge Turcaud ◽  
Xiao Wang ◽  
...  
Keyword(s):  
Maturation Inhibitor ◽  
Hiv 1

scholarly journals Identification and Characterization of BMS-955176, a Second-Generation HIV-1 Maturation Inhibitor with Improved Potency, Antiviral Spectrum, and Gag Polymorphic Coverage

2016 ◽  
Vol 60 (7) ◽  
pp. 3956-3969 ◽  
Author(s):  
Beata Nowicka-Sans ◽  
Tricia Protack ◽  
Zeyu Lin ◽  
Zhufang Li ◽  
Sharon Zhang ◽  
...  
Keyword(s):  
Human Serum ◽  
Second Generation ◽  
Mononuclear Cells ◽  
Integrase Inhibitor ◽  
Wild Type Virus ◽  
Peripheral Blood Mononuclear ◽  
Subtype B ◽  
Maturation Inhibitor ◽  
Hiv 1

ABSTRACTBMS-955176 is a second-generation human immunodeficiency virus type 1 (HIV-1) maturation inhibitor (MI). A first-generation MI, bevirimat, showed clinical efficacy in early-phase studies, but ∼50% of subjects had viruses with reduced susceptibility associated with naturally occurring polymorphisms in Gag near the site of MI action. MI potency was optimized using a panel of engineered reporter viruses containing site-directed polymorphic changes in Gag that reduce susceptibility to bevirimat (including V362I, V370A/M/Δ, and T371A/Δ), leading incrementally to the identification of BMS-955176. BMS-955176 exhibits potent activity (50% effective concentration [EC50], 3.9 ± 3.4 nM [mean ± standard deviation]) toward a library (n= 87) ofgag/prrecombinant viruses representing 96.5% of subtype B polymorphic Gag diversity near the CA/SP1 cleavage site. BMS-955176 exhibited a median EC50of 21 nM toward a library of subtype B clinical isolates assayed in peripheral blood mononuclear cells (PBMCs). Potent activity was maintained against a panel of reverse transcriptase, protease, and integrase inhibitor-resistant viruses, with EC50s similar to those for the wild-type virus. A 5.4-fold reduction in EC50occurred in the presence of 40% human serum plus 27 mg/ml of human serum albumin (HSA), which corresponded well to anin vitromeasurement of 86% human serum binding. Time-of-addition and pseudotype reporter virus studies confirm a mechanism of action for the compound that occurs late in the virus replication cycle. BMS-955176 inhibits HIV-1 protease cleavage at the CA/SP1 junction within Gag in virus-like particles (VLPs) and in HIV-1-infected cells, and it binds reversibly and with high affinity to assembled Gag in purified HIV-1 VLPs. Finally,in vitrocombination studies showed no antagonistic interactions with representative antiretrovirals (ARVs) of other mechanistic classes. In conclusion, BMS-955176 is a second-generation MI with potentin vitroanti-HIV-1 activity and a greatly improved preclinical profile compared to that of bevirimat.

scholarly journals In Vitro Resistance to the Human Immunodeficiency Virus Type 1 Maturation Inhibitor PA-457 (Bevirimat)

2006 ◽  
Vol 80 (22) ◽  
pp. 10957-10971 ◽  
Author(s):  
Catherine S. Adamson ◽  
Sherimay D. Ablan ◽  
Ioana Boeras ◽  
Ritu Goila-Gaur ◽  
Ferri Soheilian ◽  
...  
Keyword(s):  
Human Immunodeficiency Virus ◽  
Human Immunodeficiency Virus Type ◽  
Virus Type ◽  
Single Amino Acid ◽  
Compensatory Mutation ◽  
C Terminus ◽  
Immunodeficiency Virus ◽  
Maturation Inhibitor ◽  
Hiv 1

ABSTRACT 3-O-(3′,3′-dimethylsuccinyl)betulinic acid (PA-457 or bevirimat) potently inhibits human immunodeficiency virus type 1 (HIV-1) maturation by blocking a late step in the Gag processing pathway, specifically the cleavage of SP1 from the C terminus of capsid (CA). To gain insights into the mechanism(s) by which HIV-1 could evolve resistance to PA-457 and to evaluate the likelihood of such resistance arising in PA-457-treated patients, we sought to identify and characterize a broad spectrum of HIV-1 variants capable of conferring resistance to this compound. Numerous independent rounds of selection repeatedly identified six single-amino-acid substitutions that independently confer PA-457 resistance: three at or near the C terminus of CA (CA-H226Y, -L231F, and -L231M) and three at the first and third residues of SP1 (SP1-A1V, -A3T, and -A3V). We determined that mutations CA-H226Y, CA-L231F, CA-L231M, and SP1-A1V do not impose a significant replication defect on HIV-1 in culture. In contrast, mutations SP1-A3V and -A3T severely impaired virus replication and inhibited virion core condensation. The replication defect imposed by SP1-A3V was reversed by a second-site compensatory mutation in CA (CA-G225S). Intriguingly, high concentrations of PA-457 enhanced the maturation of SP1 residue 3 mutants. The different phenotypes associated with mutations that confer PA-457 resistance suggest the existence of multiple mechanisms by which HIV-1 can evolve resistance to this maturation inhibitor. These findings have implications for the ongoing development of PA-457 to treat HIV-1 infection in vivo.

scholarly journals Determinants of activity of the HIV-1 maturation inhibitor PA-457

Virology ◽  
2006 ◽  
Vol 356 (1-2) ◽  
pp. 217-224 ◽  
Author(s):  
Feng Li ◽  
Dorian Zoumplis ◽  
Claudia Matallana ◽  
Nicole R. Kilgore ◽  
Mary Reddick ◽  
...  
Keyword(s):  
Maturation Inhibitor ◽  
Hiv 1
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