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Chemical Compound Review:

KNI-577 (4S)-3-[(2S,3S)-2-hydroxy-3- [(3-hydroxy-2...

Synonyms: CHEMBL54191, JE-533, SureCN6580112, CTK0H7553, AC1L4BN6, ...

Vega, S. et al., Kiso, Y. et al.

Kiso, Matsumoto, Mizumoto, Kimura, Fujiwara, Akaji,

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Disease relevance of JE-533

Among them, a dipeptide-based HIV protease inhibitor, KNI-577, exhibited potent antiviral activities, low cytotoxicity, and good pharmacokinetic properties [1].

High impact information on JE-533

The presence of two asymmetric functional groups, linked by rotatable bonds to the inhibitor scaffold, allows KNI-764 to adapt to the mutated binding site cavity more readily than KNI-577, with a single asymmetric group [2].

References

Small dipeptide-based HIV protease inhibitors containing the hydroxymethylcarbonyl isostere as an ideal transition-state mimic. Kiso, Y., Matsumoto, H., Mizumoto, S., Kimura, T., Fujiwara, Y., Akaji, K. Biopolymers (1999) [Pubmed]
A structural and thermodynamic escape mechanism from a drug resistant mutation of the HIV-1 protease. Vega, S., Kang, L.W., Velazquez-Campoy, A., Kiso, Y., Amzel, L.M., Freire, E. Proteins (2004) [Pubmed]

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