Amylin structure-function relationships and receptor pharmacology: implications for amylin mimetic drug development
نویسندگان
چکیده
منابع مشابه
Convergent chemoenzymatic synthesis of a library of glycosylated analogues of pramlintide: structure-activity relationships for amylin receptor agonism.
Pramlintide (Symlin®), a synthetic analogue of the naturally occurring pancreatic hormone amylin, is currently used with insulin in adjunctive therapy for type 1 and type 2 diabetes mellitus. Herein we report a systematic study into the effect that N-glycosylation of pramlintide has on activation of amylin receptors. A highly efficient convergent synthetic route, involving a combination of soli...
متن کاملSecondary Structure of Rat and Human Amylin across Force Fields
The aggregation of human amylin has been strongly implicated in the progression of Type II diabetes. This 37-residue peptide forms a variety of secondary structures, including random coils, α-helices, and β-hairpins. The balance between these structures depends on the chemical environment, making amylin an ideal candidate to examine inherent biases in force fields. Rat amylin differs from human...
متن کاملImplications of amylin receptor agonism: integrated neurohormonal mechanisms and therapeutic applications.
Amylin receptor agonism is emerging as part of an integrated neurohormonal therapeutic approach for managing diabetes mellitus (DM) and body weight. Pramlintide acetate, an analogue of the pancreatic hormone amylin, has been studied in the United States as an antihyperglycemic agent in patients with type 1 or type 2 DM treated with mealtime insulin(1). Further clinical testing of pramlintide in...
متن کاملMolecular pharmacology of receptors for calcitonin-gene-related peptide, amylin and adrenomedullin.
Introduction Calcitonin-gene-related peptide (CGRP) is a 37-amino acid neuropeptide which was first identified in 1982 as a product of the calcitonin gene derived by alternative splicing [ 11. This original peptide is now referred to as a-CGRP; a second gene, unrelated to calcitonin, produces P-CGRP [2]. These two forms are closely related in both rat and man (Figure l ) , and are widely distri...
متن کاملAmylin induces hypoglycemia in mice.
Amylin is a 37-aminoacid pancreatic protein that exerts control over several metabolic events such as glycemia and lacticemia. Amylin has long been shown to induce increases in arterial plasma glucose. We decided to investigate whether amylin plays additional roles in the glucose metabolism. We evaluated glucose homeostasis using whole blood from the tail tip of fasting, conscious, unrestrained...
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ژورنال
عنوان ژورنال: British Journal of Pharmacology
سال: 2016
ISSN: 0007-1188
DOI: 10.1111/bph.13496