Mammalian Esterase Activity: Implications for Peptide Prodrugs DOI
Yana Petri, Ruben Verresen, Clair S. Gutierrez

et al.

Biochemistry, Journal Year: 2024, Volume and Issue: unknown

Published: Oct. 3, 2024

As a traceless, bioreversible modification, the esterification of carboxyl groups in peptides and proteins has potential to increase their clinical utility. An impediment is lack strategies quantify esterase-catalyzed hydrolysis rates for esters esterified biologics. We have developed continuous Förster resonance energy transfer (FRET) assay esterase activity based on peptidic substrate protease, Glu-C, that cleaves glutamyl peptide bond only if side chain free acid. Using pig liver (PLE) human carboxylesterases, we validated with substrates containing simple (

Language: Английский

Mammalian Esterase Activity: Implications for Peptide Prodrugs DOI
Yana Petri, Ruben Verresen, Clair S. Gutierrez

et al.

Biochemistry, Journal Year: 2024, Volume and Issue: unknown

Published: Oct. 3, 2024

As a traceless, bioreversible modification, the esterification of carboxyl groups in peptides and proteins has potential to increase their clinical utility. An impediment is lack strategies quantify esterase-catalyzed hydrolysis rates for esters esterified biologics. We have developed continuous Förster resonance energy transfer (FRET) assay esterase activity based on peptidic substrate protease, Glu-C, that cleaves glutamyl peptide bond only if side chain free acid. Using pig liver (PLE) human carboxylesterases, we validated with substrates containing simple (

Language: Английский

Citations

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