Exploratory studies on CA-15L, an anti-HIV active HIV-1 capsid fragment.

Exploratory studies on CA-15L, an anti-HIV active HIV-1 capsid fragment. Bioorg Med Chem. 2020 Apr 08;:115488 Authors: Tsuji K, Owusu KB, Kobayakawa T, Wang R, Fujino M, Kaneko M, Yamamoto N, Murakami T, Tamamura H Abstract Utilizing overlapping fragment peptide libraries covering the whole sequence of an HIV-1 capsid (CA) protein with the addition of an octa-arginyl moiety, we had previously found several peptides with anti-HIV-1 activity. Herein, among these potent CA fragment peptides, CA-15L was examined because this peptide sequence overlaps with Helix 7, a helix region of the CA protein, which may be important for oligomerization of the CA proteins. A CA-15L surrogate with hydrophilic residues, and its derivatives, in which amino acid sequences are shifted toward the C-terminus by one or more residues, were synthesized and their anti-HIV activity was evaluated. In addition, its derivatives with substitution for the Ser149 residue were synthesized and their anti-HIV activity was evaluated because Ser149 might be phosphorylated in the step of degradation of CA protein oligomers. Several active compounds were found and might become new anti-HIV agents and new tools for elucidation of CA functions. PMID: 32305183 [PubMed - as supplied by publisher]
Source: Bioorganic and Medicinal Chemistry - Category: Chemistry Authors: Tags: Bioorg Med Chem Source Type: research