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Glucagon-like Receptor Agonists01:24

Glucagon-like Receptor Agonists

Incretins include glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), which stimulate insulin secretion post-meals. In type 2 diabetes, GIP's efficacy is reduced, making GLP-1 a viable drug target. GIP originates from preproGIP.
GLP-1, when administered in high doses intravenously, triggers insulin secretion, inhibits glucagon release, slows gastric emptying, reduces food intake, and restores normal insulin secretion. However, its rapid inactivation by the...
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Dipeptidyl peptidase 4 (DPP-4) is a serine protease widely distributed in the body. It's involved in the inactivation of GLP-1 and GIP hormones, which are crucial for insulin regulation. DPP-4 inhibitors, such as sitagliptin (Januvia), saxagliptin (Onglyza), linagliptin (Tradjenta), alogliptin (Nesina), and vildagliptin (Galvus), help increase the proportion of active GLP-1, enhancing insulin secretion. These inhibitors work by competitively binding to DPP-4. This binding causes a significant...
Insulin: Biosynthesis, Chemistry, and Preparation01:25

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The endoplasmic reticulum (ER) of pancreatic β-cells synthesizes preproinsulin, which consists of a signal peptide, A and B chains, and a C-peptide. Preproinsulin is then cleaved and folded into proinsulin, which translocates to the Golgi apparatus for sorting and packaging into secretory granules. In these granules, enzymatic clipping generates insulin and C-peptide.
Damage or functional impairment of β-cells inhibits insulin production, leading to diabetes. Diabetes treatment primarily uses...
Oral Hypoglycemic Agents: Biguanides and Glitazones01:26

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Biguanides, particularly metformin (Glucophage), are insulin sensitizers that enhance glucose uptake, thereby reducing insulin resistance. Unlike sulfonylureas, metformin doesn't prompt insulin secretion, which helps to curb hypoglycemia risk. Metformin is beneficial in treating conditions like polycystic ovary syndrome due to its insulin-resistance reduction capability. The drug's primary action involves curtailing hepatic gluconeogenesis, a significant contributor to high blood glucose levels...
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Repaglinide (Prandin) and Nateglinide (Starlix), known as glinides, are oral insulin secretagogues that stimulate insulin release from pancreatic β cells by closing the ATP-sensitive potassium channels (KATP channel). Repaglinide controls insulin release from pancreatic β cells by managing potassium efflux. It shares two binding sites with sulfonylureas and also has a unique site, indicating overlapping mechanisms of action. With a rapid onset and a 4-7 hour duration, it effectively manages...
Glucose Homeostasis: Pancreatic Islets and Insulin Secretion01:27

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An In Ovo Model for Testing Insulin-mimetic Compounds
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Published on: April 23, 2018

Potential therapies based on antidiabetic peptides.

Tom Billyard1, Philip McTernan, Sudhesh Kumar

  • 1Warwick Medical School, University of Warwick, Clifford Bridge Road, University Hospital, Coventry CV2 2DX, UK.

Best Practice & Research. Clinical Endocrinology & Metabolism
|December 7, 2007
PubMed
Summary

Adipose tissue and gut hormones like leptin and peptide YY influence appetite and glucose metabolism. These peptides show potential as novel therapies for obesity and diabetes.

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Published on: January 26, 2016

Area of Science:

  • Endocrinology
  • Metabolic research
  • Pharmacology

Background:

  • Adipose tissue is recognized for its endocrine functions, producing cytokines involved in energy balance and insulin resistance.
  • Gut hormones, including peptide YY, ghrelin, and oxyntomodulin, have diverse physiological effects.
  • Several peptide hormones are being explored for their therapeutic potential in metabolic disorders.

Purpose of the Study:

  • To review the actions of four key peptides: leptin, adiponectin, obestatin, and peptide YY.
  • To synthesize current data on their effects on appetite and glucose metabolism.
  • To evaluate the therapeutic potential of these peptides for diabetes and obesity.

Main Methods:

  • Literature synthesis of existing data on peptide actions.
  • Analysis of roles in energy homeostasis, appetite regulation, and glucose metabolism.
  • Assessment of therapeutic applicability for metabolic diseases.

Main Results:

  • Leptin, adiponectin, obestatin, and peptide YY modulate appetite.
  • These peptides exert direct or indirect effects on glucose metabolism.
  • Each peptide presents unique mechanisms relevant to metabolic regulation.

Conclusions:

  • Leptin, adiponectin, obestatin, and peptide YY are promising candidates for novel anti-obesity and anti-diabetic therapies.
  • Further research into these peptides could lead to significant advancements in metabolic disease treatment.
  • Understanding their complex roles is crucial for developing effective therapeutic strategies.