Computational dissection of membrane transport at a microscopic level

T Jiang, PC Wen, N Trebesch, Z Zhao, S Pant… - Trends in biochemical …, 2020 - cell.com
Membrane transporters are key gatekeeper proteins at cellular membranes that closely
control the traffic of materials. Their function relies on structural rearrangements of varying …

[HTML][HTML] Study Models of Drug–Drug Interactions Involving P-Glycoprotein: The Potential Benefit of P-Glycoprotein Modulation at the Kidney and Intestinal Levels

J Veiga-Matos, AI Morales, M Prieto, F Remião, R Silva - Molecules, 2023 - mdpi.com
P-glycoprotein (P-gp) is a crucial membrane transporter situated on the cell's apical surface,
being responsible for eliminating xenobiotics and endobiotics. P-gp modulators are …

[HTML][HTML] Knockout of ABC transporters by CRISPR/Cas9 contributes to reliable and accurate transporter substrate identification for drug discovery

D Feng, G Zhong, Q Zuo, Y Wan, W Xu, C He… - Frontiers in …, 2022 - frontiersin.org
It is essential to explore the relationship between drugs and transporters in the process of
drug development. Strong background signals in nonhuman MDCK or LLC-PK1 cells and …

[HTML][HTML] Use of simulated vaginal and menstrual fluids to model in vivo discolouration of silicone elastomer vaginal rings

CF McCoy, P Spence, YHD Bashi, DJ Murphy… - International Journal of …, 2021 - Elsevier
Vaginal rings releasing antiretrovirals–either alone or in combination with contraceptive
progestins–are being developed for prevention of human immunodeficiency virus (HIV) …

Acyclic nucleosides via allylic amination of 2-methylidenetrimethylene carbonate with N-heteroaromatics

KX Huang, ZY Chen, FY Lai, YX Yu, MC Zhang - Tetrahedron, 2024 - Elsevier
A highly efficient Pd-catalyzed allylic amination reaction using N-heteroaromatics to react
with 2-methylidenetrimethylene carbonate was achieved (24 examples, up to 95% yield, up …

Influence of plasticizers on the pH-dependent drug release and cellular interactions of hydroxypropyl methylcellulose/zein vaginal anti-HIV films containing tenofovir

F Notario-Pérez, R Cazorla-Luna… - …, 2021 - ACS Publications
Vaginal films featuring the pH-dependent release of tenofovir (TFV) were developed for the
prevention of sexual transmission of human immunodeficiency syndrome (HIV). Films based …

In Vivo Modulation of Cervicovaginal Drug Transporters and Tissue Distribution by Film-Released Tenofovir and Darunavir for Topical Prevention of HIV-1

K Hijazi, F Iannelli, AM Cuppone… - Molecular …, 2020 - ACS Publications
Clinical trials have demonstrated partial protection against HIV-1 infection by vaginal
microbicide formulations based on antiretroviral (ARV) drugs. Improved formulations that will …

[HTML][HTML] Transport and Permeation Properties of Dapivirine: Understanding Potential Drug-Drug Interactions

R Zheng, GR Valicherla, J Zhang, J Nuttall, P Silvera… - Pharmaceutics, 2022 - mdpi.com
The dapivirine (DPV) vaginal ring was developed by the nonprofit International Partnership
for Microbicides (IPM) for reducing the risk of HIV infection. A clinical study (IPM 028) …

[HTML][HTML] The Pre-clinical Toolbox of Pharmacokinetics and Pharmacodynamics: in vitro and ex vivo Models

C Herrera - Frontiers in pharmacology, 2019 - frontiersin.org
Prevention strategies against sexual transmission of human immunodeficiency virus (HIV)
are essential to curb the rate of new infections. In the absence of a correlate of protection …

[HTML][HTML] Comprehensive Study of Antiretroviral Drug Permeability at the Cervicovaginal Mucosa via an In Vitro Model

C Carserides, K Smith, M Zinicola, A Kumar… - Pharmaceutics, 2022 - mdpi.com
Modulation of drug transporter activity at mucosal sites of HIV-1 transmission may be
exploited to optimize retention of therapeutic antiretroviral drug concentrations at target …