(Des-Histidine1) (Nϵ-phenylthiocarbamoyllysine12)-glucagon: Effects on glycogenolysis in perfused rat liver

B. A. Khan; Marvin D. Bregman; C. A. Nugent; Victor J. Hruby; K. Brendel

doi:10.1016/0006-291X(80)91138-9

(Des-Histidine1) (Nϵ-phenylthiocarbamoyllysine12)-glucagon: Effects on glycogenolysis in perfused rat liver

B. A. Khan
, Marvin D. Bregman
, C. A. Nugent
, Victor J. Hruby
, K. Brendel

Chemistry & Biochemistry - Sci

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

15 Scopus citations

Abstract

(Des-Histidine¹) (N^ε{lunate}-phenylthiocarbamoyllysine¹²)-glucagon, synthesized by the one-step Edman degradation procedure is a competitive inhibitor of glucagon action in the rat liver plasma membrane adenylate cyclase system. However, in the perfused rat liver, the compound did not inhibit glucagon stimulated glycogenolysis even when used at a concentration 100-fold in excess of native glucagon. Instead, it showed a weak potency, but full agonist activity, stimulating liver glycogenolysis to 100% of the level obtained by glucagon. These results are discussed in terms of the possible mechanism(s) of glucagon action.

Original language	English (US)
Pages (from-to)	729-736
Number of pages	8
Journal	Biochemical and Biophysical Research Communications
Volume	93
Issue number	3
DOIs	https://doi.org/10.1016/0006-291X(80)91138-9
State	Published - Apr 14 1980

ASJC Scopus subject areas

Biophysics
Biochemistry
Molecular Biology
Cell Biology

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title = "(Des-Histidine1) (Nϵ-phenylthiocarbamoyllysine12)-glucagon: Effects on glycogenolysis in perfused rat liver",

abstract = "(Des-Histidine1) (Nε\{lunate\}-phenylthiocarbamoyllysine12)-glucagon, synthesized by the one-step Edman degradation procedure is a competitive inhibitor of glucagon action in the rat liver plasma membrane adenylate cyclase system. However, in the perfused rat liver, the compound did not inhibit glucagon stimulated glycogenolysis even when used at a concentration 100-fold in excess of native glucagon. Instead, it showed a weak potency, but full agonist activity, stimulating liver glycogenolysis to 100\% of the level obtained by glucagon. These results are discussed in terms of the possible mechanism(s) of glucagon action.",

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TY - JOUR

T1 - (Des-Histidine1) (Nϵ-phenylthiocarbamoyllysine12)-glucagon

T2 - Effects on glycogenolysis in perfused rat liver

AU - Khan, B. A.

AU - Bregman, Marvin D.

AU - Nugent, C. A.

AU - Hruby, Victor J.

AU - Brendel, K.

PY - 1980/4/14

Y1 - 1980/4/14

N2 - (Des-Histidine1) (Nε{lunate}-phenylthiocarbamoyllysine12)-glucagon, synthesized by the one-step Edman degradation procedure is a competitive inhibitor of glucagon action in the rat liver plasma membrane adenylate cyclase system. However, in the perfused rat liver, the compound did not inhibit glucagon stimulated glycogenolysis even when used at a concentration 100-fold in excess of native glucagon. Instead, it showed a weak potency, but full agonist activity, stimulating liver glycogenolysis to 100% of the level obtained by glucagon. These results are discussed in terms of the possible mechanism(s) of glucagon action.

AB - (Des-Histidine1) (Nε{lunate}-phenylthiocarbamoyllysine12)-glucagon, synthesized by the one-step Edman degradation procedure is a competitive inhibitor of glucagon action in the rat liver plasma membrane adenylate cyclase system. However, in the perfused rat liver, the compound did not inhibit glucagon stimulated glycogenolysis even when used at a concentration 100-fold in excess of native glucagon. Instead, it showed a weak potency, but full agonist activity, stimulating liver glycogenolysis to 100% of the level obtained by glucagon. These results are discussed in terms of the possible mechanism(s) of glucagon action.

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ER -

(Des-Histidine1) (Nϵ-phenylthiocarbamoyllysine12)-glucagon: Effects on glycogenolysis in perfused rat liver

Abstract

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