Virology (New York, N.Y.), 2006-12, Vol.356 (1), p.217-224
2006
Details
- Autor(en) / Beteiligte
- Titel
- Determinants of activity of the HIV-1 maturation inhibitor PA-457
- Ist Teil von
- Virology (New York, N.Y.), 2006-12, Vol.356 (1), p.217-224
- Ort / Verlag
- United States: Elsevier Inc
- Erscheinungsjahr
- 2006
- Link zum Volltext
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- 3- O-(3′,3′-dimethylsuccinyl) betulinic acid, also termed PA-457 or DSB, is a novel HIV-1 inhibitor that blocks virus maturation by disrupting cleavage of the capsid precursor, CA-SP1. To better define the molecular target for PA-457, we prepared a panel of mutant viruses with point deletions spanning the CA-SP1 cleavage domain and characterized each of these viruses for PA-457 sensitivity. Our results indicate that amino acid residues in the N-terminal half of SP1 serve as determinants of PA-457 activity, while residues in the C-terminal half of SP1 were not involved in compound activity. These findings support and extend previous observations that PA-457 is a specific inhibitor of CA-SP1 cleavage and identify the CA-SP1 domain as the primary viral determinant for this novel inhibitor of HIV-1 replication.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0042-6822eISSN: 1096-0341DOI: 10.1016/j.virol.2006.07.023Titel-ID: cdi_proquest_miscellaneous_68163593
- Format
- –
- Schlagworte
- Amino Acid Sequence, Anti-HIV Agents - pharmacology, CA-SP1 cleavage, Capsid Proteins - chemistry, Capsid Proteins - genetics, Capsid Proteins - metabolism, Gene Products, gag - chemistry, Gene Products, gag - genetics, Gene Products, gag - metabolism, HIV, HIV-1 - drug effects, HIV-1 - genetics, HIV-1 - physiology, Human immunodeficiency virus 1, Humans, Jurkat Cells, Maturation inhibitor, Microbial Sensitivity Tests - methods, PA-457, Point Mutation, Protein Precursors - chemistry, Protein Precursors - genetics, Protein Precursors - metabolism, Succinates - pharmacology, Triterpenes - pharmacology, Viral determinants, Virus Replication - drug effects