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• W2004392237 endingPage "1779" @default.
• W2004392237 startingPage "1770" @default.
• W2004392237 abstract "Cyclophilin A (hCyp-18), a ubiquitous cytoplasmic peptidyl-prolyl cis/trans isomerase (PPIase), orchestrates HIV-1 core packaging. hCyp-18, incorporated into the virion, enables core uncoating and RNA release and consequently plays a critical role in the viral replication process. hCyp-18 specifically interacts with a single exposed loop of the Gag polyprotein capsid domain via a network of nine hydrogen bonds which mainly implicates a 7-mer fragment of the loop. As previously reported, the corresponding linear heptapeptide Ac-Val-His-Ala-Gly-Pro-Ile-Ala-NH2 (2) binds to hCyp-18 with a low affinity (IC50 = 850 ± 220 μM) but a potentially useful selectivity for hCyp-18 relative to hFKBP-12, another abundant PPIase. On the basis of X-ray structures of Gag fragments:hCyp-18 complexes, we generated a series of modified peptides in order to probe the determinants of the interaction and hence to select a peptidic ligand displaying a higher affinity than the capsid domain of Gag. We synthesized a series of heptapeptides to test the energetic contribution of amino acids besides the Gly-Pro moiety. In particular the importance of the histidine residue for the interaction was underscored. We also investigated the influence of N- and C-terminal modifications. Hexapeptides containing either deaminovaline (Dav) in place of the N-terminal valine or substitution of the C-terminal alanine amide with a benzylamide group displayed increased affinities. Combination of both modifications gave the most potent competitor Dav-His-Ala-Gly-Pro-Ile-NHBn (28) which has a higher affinity for hCyp-18 (Kd = 3 ± 0.5 μM) than the entire capsid protein (Kd = 16 ± 4 μM) and a very low affinity for hFKBP-12. Some of our results strongly suggest that the title compound is not a substrate of hCyp-18 and interacts preferentially in the trans conformation." @default.
• W2004392237 created "2016-06-24" @default.
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• W2004392237 date "2000-04-18" @default.
• W2004392237 modified "2023-10-17" @default.
• W2004392237 title "Design of a Gag Pentapeptide Analogue that Binds Human Cyclophilin A More Efficiently than the Entire Capsid Protein: New Insights for the Development of Novel Anti-HIV-1 Drugs" @default.
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• W2004392237 doi "https://doi.org/10.1021/jm9903139" @default.
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