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Related Concept Videos

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...
Oral Hypoglycemic Agents: Glinides01:06

Oral Hypoglycemic Agents: Glinides

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...
Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
Hypoglycemia and Glucagon01:15

Hypoglycemia and Glucagon

Without prolonged fasting, healthy individuals maintain blood glucose levels above 3.5 mM due to a well-adapted neuroendocrine counterregulatory system that effectively prevents acute hypoglycemia, a potentially life-threatening condition. The primary clinical scenarios for hypoglycemia encompass diabetes treatment, inappropriate production of endogenous insulin or insulin-like substances by tumors, and the use of glucose-lowering agents in non-diabetic individuals. Notably, hypoglycemia in the...
Oral Hypoglycemic Agents: α-Glucosidase Inhibitors01:19

Oral Hypoglycemic Agents: α-Glucosidase Inhibitors

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 typically...
Target Cell Response to Hormones01:22

Target Cell Response to Hormones

Hormones intricately bind to receptors on the surface or within target cells, initiating a cascade of cellular responses.
Notably, the cellular response can be regulated by altering the number of receptors expressed in the cell. For example, prolonged exposure to elevated hormone levels results in a gradual decline or down-regulation in the number of receptors for that specific hormone on the cell surface. Conversely, in response to low hormone levels, cells may use up-regulation, producing an...

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Related Experiment Video

Updated: Jul 19, 2026

Comparative Analysis of Human Growth Hormone in Serum Using SPRi, Nano-SPRi and ELISA Assays
11:17

Comparative Analysis of Human Growth Hormone in Serum Using SPRi, Nano-SPRi and ELISA Assays

Published on: January 7, 2016

Growth hormone receptor antagonists.

A J van der Lely1, John J Kopchick

  • 1Department of Internal Medicine, Erasmus MC, Rotterdam, The Netherlands. a.vanderlelij@erasmusmc.nl

Neuroendocrinology
|October 19, 2006
PubMed
Summary

New treatments for acromegaly show promise. Pegvisomant normalizes insulin-like growth factor-I levels in most patients, and combined therapy with somatostatin analogs may be effective.

Area of Science:

  • Endocrinology
  • Pharmacology

Background:

  • Acromegaly treatment often involves somatostatin analogs.
  • These analogs normalize growth hormone (GH) and insulin-like growth factor-I (IGF-I) in about 60% of patients.
  • A significant portion of patients remain inadequately treated.

Purpose of the Study:

  • To evaluate the efficacy of pegvisomant, a GH receptor antagonist, in acromegaly.
  • To explore the potential of combined therapy with somatostatin analogs and pegvisomant.

Main Methods:

  • Review of current treatment options for acromegaly.
  • Analysis of data on pegvisomant's efficacy in normalizing IGF-I levels.
  • Consideration of combined treatment strategies.

Main Results:

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In Vitro Imaging and Quantification of the Drug Targeting Efficiency of Fluorescently Labeled GnRH Analogues
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In Vitro Imaging and Quantification of the Drug Targeting Efficiency of Fluorescently Labeled GnRH Analogues

Published on: March 21, 2017

Related Experiment Videos

Last Updated: Jul 19, 2026

Comparative Analysis of Human Growth Hormone in Serum Using SPRi, Nano-SPRi and ELISA Assays
11:17

Comparative Analysis of Human Growth Hormone in Serum Using SPRi, Nano-SPRi and ELISA Assays

Published on: January 7, 2016

In Vitro Imaging and Quantification of the Drug Targeting Efficiency of Fluorescently Labeled GnRH Analogues
10:36

In Vitro Imaging and Quantification of the Drug Targeting Efficiency of Fluorescently Labeled GnRH Analogues

Published on: March 21, 2017

  • Pegvisomant normalizes IGF-I levels in nearly all acromegalic subjects.
  • No correlation found between elevated GH and tumor size.
  • Pegvisomant monotherapy is daily, costly, and requires ongoing safety studies.

Conclusions:

  • Pegvisomant offers a highly effective option for normalizing IGF-I in acromegaly.
  • Combined therapy with somatostatin analogs and pegvisomant presents a rational and potentially more effective treatment approach.