ArticleAntimicrobial agents and chemotherapy2018
HIV-1 Integrase Inhibitors That Are Broadly Effective against Drug-Resistant Mutants.
Article in Antimicrobial agents and chemotherapy, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 25 citations in OpenAlex.
- Review
- Pi-pi stacking interactions with viral DNA contribute to the potency of naphthyridine-based HIV-1 integrase inhibitors.NAR molecular medicine · 2025Article
- Article
- Mechanisms of HIV-1 integrase resistance to dolutegravir and potent inhibition of drug-resistant variants.Science advances · 2023Article
- INSTIs and NNRTIs Potently Inhibit HIV-1 Polypurine Tract Mutants in a Single Round Infection Assay.Viruses · 2021Article
- HIV-1 Integrase Inhibitors with Modifications That Affect Their Potencies against Drug Resistant Integrase Mutants.ACS infectious diseases · 2021Article
- The Extremophilic Actinobacteria: From Microbes to Medicine.Antibiotics (Basel, Switzerland) · 2021Review
- Structure-based non-nucleoside inhibitor design: Developing inhibitors that are effective against resistant mutants.Chemical biology & drug design · 2021Article
- Close-up: HIV/SIV intasome structures shed new light on integrase inhibitor binding and viral escape mechanisms.The FEBS journal · 2021Review
- Retroviral integrase: Structure, mechanism, and inhibition.The Enzymes · 2021Article
- Structural Biology of HIV Integrase Strand Transfer Inhibitors.Trends in pharmacological sciences · 2020Review
- HIV-1 Integrase Inhibitors That Are Active against Drug-Resistant Integrase Mutants.Antimicrobial agents and chemotherapy · 2020Article
- Effective estimation of the inhibitor affinity of HIV-1 proteaseRSC advances · 2020Article
- Structural basis for strand-transfer inhibitor binding to HIV intasomes.Science (New York, N.Y.) · 2020Article
- Recent Advances in the Development of Integrase Inhibitors for HIV Treatment.Current HIV/AIDS reports · 2020Review
- Multifaceted HIV integrase functionalities and therapeutic strategies for their inhibition.The Journal of biological chemistry · 2019Review
- Rapid Development of High-Level Resistance to Dolutegravir With Emergence of T97A Mutation in 2 Treatment-Experienced Individuals With Baseline Partial Sensitivity to Dolutegravir.Open forum infectious diseases · 2018Article
Corrections and comments
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Authors and funding
4 authors at 2 institutions in 1 country.
Funding
Abstract
Integrase strand transfer inhibitors (INSTIs) have emerged as clinically effective therapeutics that inhibit HIV-1 replication by blocking the strand transfer reaction catalyzed by HIV-1 integrase (IN). Of the three FDA-approved INSTIs, dolutegravir (DTG) is the least apt to select for resistance. However, recent salvage therapy regimens had low response rates with therapies that included DTG, suggesting that DTG resistance can be selected in patients. Using a single-round infection assay, we evaluated a collection of our best inhibitors and DTG against a broad panel of INSTI-resistant mutants. Two of the new compounds, 4c and 4d, had antiviral profiles against the mutants we tested superior to that of DTG. The susceptibility profiles of 4c and 4d suggest that the compounds are candidates for development as INSTIs. Modeling the binding of 4d to HIV-1 IN reinforced the significance of mimicking the DNA substrate in developing compounds that are broadly effective in their abilities to inhibit HIV-1 INs with mutations in the active site.
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Registered trials
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.