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Literature summary for 3.4.21.97 extracted from

  • Cottier, V.; Barberis, A.; Luethi, U.
    Novel yeast cell-based assay to screen for inhibitors of human cytomegalovirus protease in a high-throughput format (2006), Antimicrob. Agents Chemother., 50, 565-571.
    View publication on PubMedView publication on EuropePMC

Activating Compound

Activating Compound Comment Organism Structure
glycerol promotes HCMV protease dimerization and subsequent proteolytic activity Human betaherpesvirus 5

Application

Application Comment Organism
analysis cell growth selection system in the yeast Saccharomyces cerevisiae that can detect and characterize HCMV protease activity and is applicable to screen for HCMV protease inhibitors in a high-throughput format Human betaherpesvirus 5

Cloned(Commentary)

Cloned (Comment) Organism
coexpression of HCMV protease with N-(5'-phosphoribosyl)anthranilate isomerase substrate in Saccharomyces cerevisiae RLY07 strain. HCMV protease expressed from the full-length GAL1 promoter, subcloned on a GAL1 vector series, with discrete protein production levels of 71%, 46%, and 16% compared to the original 100% promoter Human betaherpesvirus 5

Protein Variants

Protein Variants Comment Organism
S132A is inactive Human betaherpesvirus 5

Inhibitors

Inhibitors Comment Organism Structure
BI31 50% inhibitory at 0.0017 mM. Increasing inhibitor concentrations in cells expressing the active protease correlate with increasing cell proliferation Human betaherpesvirus 5
BI36 50% inhibitory at 0.0005 mM. Increasing inhibitor concentrations in cells expressing the active protease correlate with increasing cell proliferation Human betaherpesvirus 5

Organism

Organism UniProt Comment Textmining
Human betaherpesvirus 5
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Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
N-(5'-phosphoribosyl)anthranilate isomerase + H2O site-specific cleavage and functional inactivation of the N-(5'-phosphoribosyl)anthranilate isomerase, thereby leading to an arrest of cell proliferation. Coexpressing N-(5'-phosphoribosyl)anthranilate isomerase1194-M with the protease exhibits a growth reduction of 35%. N-(5'-phosphoribosyl)anthranilate isomerase1132-M- as well as N-(5'-phosphoribosyl)anthranilate isomerase1165-M-expressing cells do not show growth reduction upon coexpressing HCMV protease, thus no cleavage occurs. Cells expressing the modified N-(5'-phosphoribosyl)anthranilate isomerase1194-Me together with the active protease show 85% reduction of cell proliferation, is cleaved in a sequence-specific manner Human betaherpesvirus 5 ?
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Synonyms

Synonyms Comment Organism
HCMV protease
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Human betaherpesvirus 5
human cytomegalovirus protease
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Human betaherpesvirus 5