Adenine-arginine mimetics as bisubstrate analog inhibitors of cAMP-dependent protein kinase

Mengfei Ho; Brenda A. Wilson; Ibrahim Katampe

doi:10.1016/0960-894X(96)00140-0

Adenine-arginine mimetics as bisubstrate analog inhibitors of cAMP-dependent protein kinase

Mengfei Ho, Brenda A. Wilson, Ibrahim Katampe

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

Abstract

Simple bisubstrate analogs, Ad-E1-Gn, Ad-E2-Gn, and Ad-E3-Gn, are designed to be proto-type adenine-arginine mimetic structures. Both Ad-E1-Gn and Ad-E2-Gn inhibit PKA with IC₅₀ values similar to that of adenosine at 100 μM ATP and are more potent inhibitors than adenosine at physiologically relevant 2 mM ATP. Ad-E3-Gn is 10-fold less potent than the other two analogs.

Original language	English (US)
Pages (from-to)	899-902
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	6
Issue number	7
DOIs	https://doi.org/10.1016/0960-894X(96)00140-0
State	Published - Apr 9 1996
Externally published	Yes

ASJC Scopus subject areas

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

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10.1016/0960-894X(96)00140-0

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title = "Adenine-arginine mimetics as bisubstrate analog inhibitors of cAMP-dependent protein kinase",

abstract = "Simple bisubstrate analogs, Ad-E1-Gn, Ad-E2-Gn, and Ad-E3-Gn, are designed to be proto-type adenine-arginine mimetic structures. Both Ad-E1-Gn and Ad-E2-Gn inhibit PKA with IC50 values similar to that of adenosine at 100 μM ATP and are more potent inhibitors than adenosine at physiologically relevant 2 mM ATP. Ad-E3-Gn is 10-fold less potent than the other two analogs.",

author = "Mengfei Ho and Wilson, {Brenda A.} and Ibrahim Katampe",

note = "Funding Information: This work is supported by the American Heart Association, National Center.",

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AU - Ho, Mengfei

AU - Wilson, Brenda A.

AU - Katampe, Ibrahim

N1 - Funding Information: This work is supported by the American Heart Association, National Center.

PY - 1996/4/9

Y1 - 1996/4/9

N2 - Simple bisubstrate analogs, Ad-E1-Gn, Ad-E2-Gn, and Ad-E3-Gn, are designed to be proto-type adenine-arginine mimetic structures. Both Ad-E1-Gn and Ad-E2-Gn inhibit PKA with IC50 values similar to that of adenosine at 100 μM ATP and are more potent inhibitors than adenosine at physiologically relevant 2 mM ATP. Ad-E3-Gn is 10-fold less potent than the other two analogs.

AB - Simple bisubstrate analogs, Ad-E1-Gn, Ad-E2-Gn, and Ad-E3-Gn, are designed to be proto-type adenine-arginine mimetic structures. Both Ad-E1-Gn and Ad-E2-Gn inhibit PKA with IC50 values similar to that of adenosine at 100 μM ATP and are more potent inhibitors than adenosine at physiologically relevant 2 mM ATP. Ad-E3-Gn is 10-fold less potent than the other two analogs.

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Adenine-arginine mimetics as bisubstrate analog inhibitors of cAMP-dependent protein kinase

Abstract

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