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Conformationally Restricted Hydantoin‐Based Peptidomimetics as Inhibitors of Caspase‐3 with Basic Groups Allowed at the S 3 Enzyme Subsite
Author(s) -
Vázquez Jesús,
GarcíaJareño Alicia,
Mondragón Laura,
RubioMartinez Jaime,
PérezPayá Enrique,
Albericio Fernando
Publication year - 2008
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.200800020
Subject(s) - hydantoin , peptidomimetic , recombinant dna , chemistry , enzyme , stereochemistry , scaffold , drug discovery , combinatorial chemistry , caspase 3 , molecular model , endogeny , biochemistry , computational biology , biology , apoptosis , peptide , medicine , programmed cell death , biomedical engineering , gene
By using a combination of molecular modeling, combinatorial chemistry, and biological essays, novel scaffold molecules for the inhibition of caspase‐3 have been developed. These compounds have an overall attenuated negative charge and show similar IC 50 values for both recombinant and human endogenous caspase‐3. This might provide the basis for a novel strategy for the discovery of potent and more druglike inhibitors of caspase‐3.