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Chemical Compound Review

CHEMBL432614     methyl(2S)-2-[[(2S,3S)-2- [[(2S)-1-[(3S)-3...

Synonyms: CHEBI:284653, AC1L9PUN, JG 365, (R/S)-JG365, Ac-Ser-Leu-Asn-[Phe-HEA-Pro]-Ile-Val-OMe
 
 
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Disease relevance of JG 365

  • These results establish that good inhibitors of HIV protease that inhibit viral replication in infected lymphocytes in in vitro cell assays can be obtained from JG-365 when the AcSerLeu unit is replaced by aromatic acyl derivatives [1].
 

High impact information on JG 365

  • The sequence of the inhibitor JG-365 is Ac-Ser-Leu-Asn-Phe-psi[CH(OH)CH2N]-Pro-Ile-Val-OMe; the Ki is 0.24 nM [2].

References

  1. New hydroxyethylamine HIV protease inhibitors that suppress viral replication. Rich, D.H., Prasad, J.V., Sun, C.Q., Green, J., Mueller, R., Houseman, K., MacKenzie, D., Malkovsky, M. J. Med. Chem. (1992) [Pubmed]
  2. X-ray crystallographic structure of a complex between a synthetic protease of human immunodeficiency virus 1 and a substrate-based hydroxyethylamine inhibitor. Swain, A.L., Miller, M.M., Green, J., Rich, D.H., Schneider, J., Kent, S.B., Wlodawer, A. Proc. Natl. Acad. Sci. U.S.A. (1990) [Pubmed]
 
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