An ether-based peptide analog as c-AMP-dependent protein kinase inhibitor/substrate

Mengfei Ho; Amy Uhrin; Michelle Huang

doi:10.1016/S0960-894X(01)80153-0

An ether-based peptide analog as c-AMP-dependent protein kinase inhibitor/substrate

Mengfei Ho, Amy Uhrin, Michelle Huang

Research output: Contribution to journal › Article › peer-review

Abstract

Ether-based peptide analog L-EP contains an ether-linkage unit in place of the Ser-Leu-Gly unit of a PKA substrate, Kemptide. L-EP is a competitive inhibitor of Kemptide phosphorylation catalyzed by PKA with a K_i value of 120 μM. It also serves as a weak substrate of PKA with a K_m value 25-fold higher and a V_max value 3.5-fold lower than that of Kemptide.

Original language	English (US)
Pages (from-to)	553-556
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	4
Issue number	4
DOIs	https://doi.org/10.1016/S0960-894X(01)80153-0
State	Published - Feb 24 1994
Externally published	Yes

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/S0960-894X(01)80153-0

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abstract = "Ether-based peptide analog L-EP contains an ether-linkage unit in place of the Ser-Leu-Gly unit of a PKA substrate, Kemptide. L-EP is a competitive inhibitor of Kemptide phosphorylation catalyzed by PKA with a Ki value of 120 μM. It also serves as a weak substrate of PKA with a Km value 25-fold higher and a Vmax value 3.5-fold lower than that of Kemptide.",

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AU - Uhrin, Amy

AU - Huang, Michelle

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AB - Ether-based peptide analog L-EP contains an ether-linkage unit in place of the Ser-Leu-Gly unit of a PKA substrate, Kemptide. L-EP is a competitive inhibitor of Kemptide phosphorylation catalyzed by PKA with a Ki value of 120 μM. It also serves as a weak substrate of PKA with a Km value 25-fold higher and a Vmax value 3.5-fold lower than that of Kemptide.

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An ether-based peptide analog as c-AMP-dependent protein kinase inhibitor/substrate

Abstract

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