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Related Concept Videos

Dipeptidyl Peptidase 4 Inhibitors01:23

Dipeptidyl Peptidase 4 Inhibitors

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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...
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Oral Hypoglycemic Agents: α-Glucosidase Inhibitors01:19

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α-glucosidase inhibitors, including acarbose (Precose), miglitol (Glyset), and voglibose (Voglib) (primarily available in Asia), are drugs that control blood sugar levels by delaying the digestion of starch and disaccharides. They achieve this by inhibiting α-glucosidase enzymes in the intestine, which slow the absorption of carbohydrates in the intestine, which in turn leads to a prolonged release of the glucoregulatory hormone GLP-1 from intestinal L-cells.
Acarbose and miglitol are...
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Glucagon-like Receptor Agonists01:24

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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...
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Oral Hypoglycemic Agents: Glinides01:06

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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...
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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...
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Lipid-Lowering Drugs: Statins and Miscellaneous Agents01:20

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Hyperlipidemia, a medical condition often referred to as high cholesterol, is characterized by abnormally elevated levels of lipids in the bloodstream. When present in excess, these lipids, specifically cholesterol and triglycerides, can lead to serious health complications, often involving cardiovascular diseases. Illnesses like atherosclerosis, heart attacks, and pancreatitis have all been linked to untreated hyperlipidemia. This means controlling and regulating cholesterol and triglyceride...
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Sitagliptin Results in a Decrease of Truncated Apolipoprotein C1.

Nicole E B Skinner1, Matthew S Wroblewski2, Julie A Kirihara2

  • 1Department of Laboratory Medicine and Pathology, University of Minnesota, Minneapolis, MN, USA.

Diabetes Therapy : Research, Treatment and Education of Diabetes and Related Disorders
|July 23, 2015
PubMed
Summary
This summary is machine-generated.

Sitagliptin, a diabetes drug, significantly alters Apolipoprotein C1 (ApoC1) forms in the body. This suggests the drug effectively inhibits dipeptidyl peptidase-4 (DPP-4), impacting lipid metabolism.

Keywords:
Apolipoprotein C1Mass spectrometrySitagliptin

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Area of Science:

  • Biochemistry
  • Pharmacology
  • Lipid Metabolism

Background:

  • Apolipoprotein C1 (ApoC1) is crucial for lipid metabolism and transport.
  • ApoC1 exists in full-length and truncated forms.
  • Dipeptidyl peptidase-4 (DPP-4) is implicated in ApoC1 truncation.

Purpose of the Study:

  • To investigate the effect of sitagliptin on ApoC1 isoform proportions in humans.
  • To assess the in vivo inhibition of DPP-4 by sitagliptin through ApoC1 truncation analysis.

Main Methods:

  • Oral administration of sitagliptin to human subjects.
  • Analysis of circulating Apolipoprotein C1 (ApoC1) isoforms.

Main Results:

  • Sitagliptin administration caused a significant shift in ApoC1 isoform proportions.
  • The observed changes in ApoC1 truncation strongly indicate effective DPP-4 inhibition.

Conclusions:

  • Oral sitagliptin effectively inhibits DPP-4 activity in humans.
  • Sitagliptin's impact on ApoC1 isoforms provides a biomarker for DPP-4 inhibition.