TY - JOUR
T1 - [des His1, des Phe6, Glu9]glucagon amide
T2 - A newly designed "pure" glucagon antagonist
AU - Azizeh, Bassem Y.
AU - Van Tine, Brian A.
AU - Sturm, Noel S.
AU - Hutzler, Ann Marie
AU - David, Clinton
AU - Trivedi, Dev
AU - Hruby, Victor J.
PY - 1995/8/17
Y1 - 1995/8/17
N2 - We report the synthesis and biological activity of a new glucagon analog that was designed as a glucagon receptor antagonist by appropriate modifications in the N-terminal region of glucagon. The structure of the new analog is [des His1, des Phe6, Glu9]glucagon amide, and its binding potency IC50 value of 48 nM. The compound was found to be a pure antagonist in a new much more sensitive assay for glucagon stimulated cAMP accumulation activity and showed a pA2 value of 8.20 in this assay. We report the sythesis and biological activity of a new glucagon analog that was designed as a glucagon receptor antagonist. The new analog, [des His1, des Phe6, Glu9]glucagon, amide, was found to be a pure antagonist in a new more sensitive assay for partial agonist activity, with a binding potency IC50 of 48 nM and a pA2 valueof 8.20.
AB - We report the synthesis and biological activity of a new glucagon analog that was designed as a glucagon receptor antagonist by appropriate modifications in the N-terminal region of glucagon. The structure of the new analog is [des His1, des Phe6, Glu9]glucagon amide, and its binding potency IC50 value of 48 nM. The compound was found to be a pure antagonist in a new much more sensitive assay for glucagon stimulated cAMP accumulation activity and showed a pA2 value of 8.20 in this assay. We report the sythesis and biological activity of a new glucagon analog that was designed as a glucagon receptor antagonist. The new analog, [des His1, des Phe6, Glu9]glucagon, amide, was found to be a pure antagonist in a new more sensitive assay for partial agonist activity, with a binding potency IC50 of 48 nM and a pA2 valueof 8.20.
UR - http://www.scopus.com/inward/record.url?scp=0029133968&partnerID=8YFLogxK
U2 - 10.1016/0960-894X(95)00307-F
DO - 10.1016/0960-894X(95)00307-F
M3 - Article
AN - SCOPUS:0029133968
SN - 0960-894X
VL - 5
SP - 1849
EP - 1852
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 16
ER -