Biological activity of EXf, a peptide analogue of exendin-4

European Journal of Pharmacology
Guang-ming SongZhu-fang Shen

Abstract

Exendin-4 is an incretin mimetic that has been developed for the treatment of patients with type 2 diabetes. EXf is an available carboxy-terminal truncated fragment of exendin-4 with two amino acid substitutions. The purpose of these studies was to evaluate the biological activity of EXf. After a single subcutaneous injection, EXf significantly decreased plasma glucose concentration and glucose excursion following the administration of an oral glucose challenge both in non-diabetic (ICR), monosodium l-glutamate induced insulin resistance (MSG-IR) and diabetic KK-ay mice. Meanwhile, EXf resulted in an increase of first-phase insulin secretion in normal mice and KK-ay mice following the glucose challenge. EXf was also shown to inhibit small intestinal transit in rodent models. EXf activated the cAMP response element (CRE) of the rat insulin I gene promoter (RIP1) GFP-construct in a dose-dependent manner in the cultured mouse insulinoma cell line, termed NIT-1, and this agonist activity was blocked by the glucagon-like peptide 1 (GLP-1) receptor antagonist exendin(9-39). In summary, EXf, an analogue of exendin-4, has agonist activity to GLP-1 receptor in vitro and glucoregulatory activities in vivo, thus it can be considered as a ...Continue Reading

References

Feb 11, 1976·The Journal of Clinical Endocrinology and Metabolism·J D BrunzellD Porte
Jun 26, 2001·Diabetes/metabolism Research and Reviews·S Del Prato, A Tiengo
Mar 13, 2002·The Journal of Clinical Endocrinology and Metabolism·Josephine M EganDariush Elahi
Dec 7, 2002·Diabetes/metabolism Research and Reviews·Jens Juul Holst
Oct 27, 2004·Diabetes Care·John B BuseUNKNOWN Exenatide-113 Clinical Study Group
Jan 19, 2005·Hormone and Metabolic Research = Hormon- Und Stoffwechselforschung = Hormones Et Métabolisme·M A Nauck
May 18, 2005·Drug Discovery Today·Loretta L Nielsen

❮ Previous
Next ❯

Related Concepts

Related Feeds

Cardiovascular Biology of GLP-1

Glucagon-like peptide 1 (GLP-1) plays a role in glucose metabolism, energy homeostasis, and inflammation suppression. GLP-1 receptor signaling has been shown to impact cardiovascular function. This feed focuses on the role of GLP-1 and GLP-1 receptor agonists on cardiovascular biology.

Biomarkers for Type 2 Diabetes

Biomarkers can help understand chronic diseases and assist in risk prediction for prevention and early detection of diseases. Here is the latest research on biomarkers in type 2 diabetes, a disease in which the body is unable to produce or properly use insulin.