ArticleNature communications2019
Lattice engineering enables definition of molecular features allowing for potent small-molecule inhibition of HIV-1 entry.
Article in Nature communications, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers.
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Who cites it
29 citing papers in PubMed.
- Fostemsavir analog BMS-818251 has enhanced viral neutralization potency and similar escape mutation profile.Antimicrobial agents and chemotherapy · 2025Article
- Article
- Structure-function analyses reveal key molecular determinants of HIV-1 CRF01_AE resistance to the entry inhibitor temsavir.Nature communications · 2023Article
- A classification algorithm based on dynamic ensemble selection to predict mutational patterns of the envelope protein in HIV-infected patients.Algorithms for molecular biology : AMB · 2023Article
- Temsavir blocks the immunomodulatory activities of HIV-1 soluble gp120.Cell chemical biology · 2023Article
- Vaccination with immune complexes modulates the elicitation of functional antibodies against HIV-1.Frontiers in immunology · 2023Article
- Article
- Bio-Inorganic Layered Double Hydroxide Nanohybrids in Photochemotherapy: A Mini Review.International journal of molecular sciences · 2022Review
- Characterization of Human Immunodeficiency Virus (HIV-1) Envelope Glycoprotein Variants Selected for Resistance to a CD4-Mimetic Compound.Journal of virology · 2022Article
- Structural dynamics reveal isolate-specific differences at neutralization epitopes on HIV Env.iScience · 2022Article
- Antigenic analysis of the HIV-1 envelope trimer implies small differences between structural states 1 and 2.The Journal of biological chemistry · 2022Article
- The Genesis and Future Prospects of Small Molecule HIV-1 Attachment Inhibitors.Advances in experimental medicine and biology · 2022Review
- Asymmetric Structures and Conformational Plasticity of the Uncleaved Full-Length Human Immunodeficiency Virus Envelope Glycoprotein Trimer.Journal of virology · 2021Article
- Structurally related but genetically unrelated antibody lineages converge on an immunodominant HIV-1 Env neutralizing determinant following trimer immunization.PLoS pathogens · 2021Article
- HIV-1 Envelope Conformation, Allostery, and Dynamics.Viruses · 2021Review
- Small Molecule HIV-1 Attachment Inhibitors: Discovery, Mode of Action and Structural Basis of Inhibition.Viruses · 2021Review
- Article
- Cryo-EM structures of HIV-1 trimer bound to CD4-mimetics BNM-III-170 and M48U1 adopt a CD4-bound open conformation.Nature communications · 2021Article
- HIV-1 Entry and Prospects for Protecting against Infection.Microorganisms · 2021Review
- Innovation in the discovery of the HIV-1 attachment inhibitor temsavir and its phosphonooxymethyl prodrug fostemsavir.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2021Review
Corrections and comments
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20 authors.
Funding
Abstract
Diverse entry inhibitors targeting the gp120 subunit of the HIV-1 envelope (Env) trimer have been developed including BMS-626529, also called temsavir, a prodrug version of which is currently in phase III clinical trials. Here we report the characterization of a panel of small-molecule inhibitors including BMS-818251, which we show to be >10-fold more potent than temsavir on a cross-clade panel of 208-HIV-1 strains, as well as the engineering of a crystal lattice to enable structure determination of the interaction between these inhibitors and the HIV-1 Env trimer at higher resolution. By altering crystallization lattice chaperones, we identify a lattice with both improved diffraction and robust co-crystallization of HIV-1 Env trimers from different clades complexed to entry inhibitors with a range of binding affinities. The improved diffraction reveals BMS-818251 to utilize functional groups that interact with gp120 residues from the conserved β20-β21 hairpin to improve potency.
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