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

Mengfei Ho, Brenda A. Wilson, Ibrahim Katampe

Research output: Contribution to journalArticle

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 languageEnglish (US)
Pages (from-to)899-902
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume6
Issue number7
DOIs
StatePublished - Apr 9 1996

Fingerprint

Adenine
Cyclic AMP-Dependent Protein Kinases
Adenosine
Arginine
Adenosine Triphosphate
Inhibitory Concentration 50

ASJC Scopus subject areas

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

Cite this

Adenine-arginine mimetics as bisubstrate analog inhibitors of cAMP-dependent protein kinase. / Ho, Mengfei; Wilson, Brenda A.; Katampe, Ibrahim.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 6, No. 7, 09.04.1996, p. 899-902.

Research output: Contribution to journalArticle

@article{c7bf222633e04019a1c0e4e0baabf9f5,
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",
year = "1996",
month = "4",
day = "9",
doi = "10.1016/0960-894X(96)00140-0",
language = "English (US)",
volume = "6",
pages = "899--902",
journal = "Bioorganic and Medicinal Chemistry Letters",
issn = "0960-894X",
publisher = "Elsevier Limited",
number = "7",

}

TY - JOUR

T1 - Adenine-arginine mimetics as bisubstrate analog inhibitors of cAMP-dependent protein kinase

AU - Ho, Mengfei

AU - Wilson, Brenda A.

AU - Katampe, Ibrahim

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.

UR - http://www.scopus.com/inward/record.url?scp=0029915811&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0029915811&partnerID=8YFLogxK

U2 - 10.1016/0960-894X(96)00140-0

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

M3 - Article

AN - SCOPUS:0029915811

VL - 6

SP - 899

EP - 902

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

SN - 0960-894X

IS - 7

ER -