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A targeted covalent small molecule inhibitor of HIV-1 fusion.
- Source :
-
Chemical communications (Cambridge, England) [Chem Commun (Camb)] 2021 May 06; Vol. 57 (37), pp. 4528-4531. - Publication Year :
- 2021
-
Abstract
- We describe a low molecular weight covalent inhibitor targeting a conserved lysine residue within the hydrophobic pocket of HIV-1 glycoprotein-41. The inhibitor bound selectively to the hydrophobic pocket and exhibited an order of magnitude enhancement of anti-fusion activity against HIV-1 compared to its non-covalent counterpart. The findings represent a significant advance in the quest to obtain non-peptide fusion inhibitors.
- Subjects :
- Anti-HIV Agents chemistry
HIV metabolism
HIV Envelope Protein gp41 metabolism
HIV Fusion Inhibitors chemistry
Hydrophobic and Hydrophilic Interactions
Microbial Sensitivity Tests
Molecular Structure
Molecular Weight
Small Molecule Libraries chemistry
Structure-Activity Relationship
Sulfuric Acid Esters chemistry
Anti-HIV Agents pharmacology
HIV drug effects
HIV Envelope Protein gp41 antagonists & inhibitors
HIV Fusion Inhibitors pharmacology
Small Molecule Libraries pharmacology
Sulfuric Acid Esters pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1364-548X
- Volume :
- 57
- Issue :
- 37
- Database :
- MEDLINE
- Journal :
- Chemical communications (Cambridge, England)
- Publication Type :
- Academic Journal
- Accession number :
- 33956029
- Full Text :
- https://doi.org/10.1039/d1cc01013a