ArticleAntimicrobial agents and chemotherapy2009
Reverse transcriptase inhibitors as potential colorectal microbicides.
Article in Antimicrobial agents and chemotherapy, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 43 papers.
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Who cites it
43 citing papers in PubMed.
- Pharmacokinetic/pharmacodynamic investigation of raltegravir with or without lamivudine in the context of HIV-1 pre-exposure prophylaxis (PrEP).The Journal of antimicrobial chemotherapy · 2021Trial
- Heterogeneous antiretroviral drug distribution and HIV/SHIV detection in the gut of three species.Science translational medicine · 2019Trial
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- Microbial remodeling of gut tryptophan metabolism and indole-3-lactate production regulate epithelial barrier repair and viral suppression in human and simian immunodeficiency virus infections.Mucosal immunology · 2025Article
- Mucosal Responses to Zika Virus Infection in Cynomolgus Macaques.Pathogens (Basel, Switzerland) · 2022Article
- TheiScience · 2022Article
- Pre-Clinical Evaluation of Tenofovir and Tenofovir Alafenamide for HIV-1 Pre-Exposure Prophylaxis in Foreskin Tissue.Pharmaceutics · 2022Article
- Ex Vivo Evaluation of Mucosal Responses to Vaccination with ALVAC and AIDSVAX of Non-Human Primates.Vaccines · 2022Article
- Pre-clinical evaluation of antiproteases as potential candidates for HIV-1 pre-exposure prophylaxis.Frontiers in reproductive health · 2022Article
- Peptide Amphiphilic-Based Supramolecular Structures with Anti-HIV-1 Activity.Bioconjugate chemistry · 2021Article
- Article
- Human Organotypic Models for Anti-infective Research.Current topics in microbiology and immunology · 2021Article
- Efficacy of silk fibroin biomaterial vehicle for in vivo mucosal delivery of Griffithsin and protection against HIV and SHIV infection ex vivo.Journal of the International AIDS Society · 2020Article
- Importance of structure-based studies for the design of a novel HIV-1 inhibitor peptide.Scientific reports · 2020Article
- Sustained release silk fibroin discs: Antibody and protein delivery for HIV prevention.Journal of controlled release : official journal of the Controlled Release Society · 2019Article
- The Pre-clinical Toolbox of Pharmacokinetics and Pharmacodynamics:Frontiers in pharmacology · 2019Review
- A novel preventive strategy against HIV-1 infection: combinatorial use of inhibitors targeting the nucleocapsid and fusion proteins.Emerging microbes & infections · 2017Article
- Oligonucleotide-Lipid Conjugates Forming G-Quadruplex Structures Are Potent and Pangenotypic Hepatitis C Virus Entry InhibitorsAntimicrobial agents and chemotherapy · 2017Article
- Stabilization and Sustained Release of HIV Inhibitors by Encapsulation in Silk Fibroin Disks.ACS biomaterials science & engineering · 2017Article
Corrections and comments
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Authors and funding
5 authors.
Funding
Abstract
We investigated whether reverse transcriptase (RT) inhibitors (RTI) can be combined to inhibit human immunodeficiency virus type 1 (HIV-1) infection of colorectal tissue ex vivo as part of a strategy to develop an effective rectal microbicide. The nucleotide RTI (NRTI) PMPA (tenofovir) and two nonnucleoside RTI (NNRTI), UC-781 and TMC120 (dapivirine), were evaluated. Each compound inhibited the replication of the HIV isolates tested in TZM-bl cells, peripheral blood mononuclear cells, and colorectal explants. Dual combinations of the three compounds, either NRTI-NNRTI or NNRTI-NNRTI combinations, were more active than any of the individual compounds in both cellular and tissue models. Combinations were key to inhibiting infection by NRTI- and NNRTI-resistant isolates in all models tested. Moreover, we found that the replication capacities of HIV-1 isolates in colorectal explants were affected by single point mutations in RT that confer resistance to RTI. These data demonstrate that colorectal explants can be used to screen compounds for potential efficacy as part of a combination microbicide and to determine the mucosal fitness of RTI-resistant isolates. These findings may have important implications for the rational design of effective rectal microbicides.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.