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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...
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Drugs for Treatment of Crohn's Disease in IBD Using Glucocorticoids

Glucocorticoids, a class of anti-inflammatory drugs, are pivotal in treating moderate to severe Crohn's disease by inducing remission. They exhibit their anti-inflammatory action by inhibiting the production of inflammatory cytokines such as tumor necrosis factor (TNF)-α, interleukin (IL)-1, and chemokines like IL-8. In addition, they reduce the expression of inflammatory cell adhesion molecules and inhibit gene transcription of nitric oxide synthase, phospholipase A2, cyclooxygenase-2 (COX-2),...
Antiasthma Drugs: Inhaled Corticosteroids and Glucocorticoids01:25

Antiasthma Drugs: Inhaled Corticosteroids and Glucocorticoids

Inhaled corticosteroids (ICS) are anti-inflammatory drugs used primarily in treating persistent asthma and providing long-term maintenance. They target the bronchial mucosa, the lining of the airways, to control inflammation, a critical factor in asthma progression and exacerbation.
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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...
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...
Drug-Receptor Interaction: Antagonist01:28

Drug-Receptor Interaction: Antagonist

An antagonist is a drug that binds strongly to a receptor without activating it. An antagonist prevents other molecules, such as neurotransmitters or hormones, from binding to the receptor and triggering a cellular response. Such interaction effectively hinders the normal physiological processes mediated by the receptor, resulting in various pharmacological effects depending on the specific receptor targeted.
Antagonists can be classified as competitive or noncompetitive based on their...

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Biochemical Reconstitution of Steroid Receptor&#x2022;Hsp90 Protein Complexes and Reactivation of Ligand Binding
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Biochemical Reconstitution of Steroid Receptor•Hsp90 Protein Complexes and Reactivation of Ligand Binding

Published on: September 21, 2011

Glucocorticoid receptor antagonists.

Robin D Clark1

  • 1Corcept Therapeutics, 149 Commonwealth Avenue, Menlo Park, CA 94025, USA. rclark@corcept.com

Current Topics in Medicinal Chemistry
|June 10, 2008
PubMed
Summary
This summary is machine-generated.

Selective glucocorticoid receptor (GR) antagonists show therapeutic promise for various conditions. This review details their discovery, applications, and structure-activity relationships for novel drug development.

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Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists
10:51

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Published on: November 15, 2013

Area of Science:

  • Pharmacology and Drug Discovery
  • Endocrinology
  • Medicinal Chemistry

Background:

  • Glucocorticoid receptor (GR) antagonists are crucial for modulating the stress response.
  • Selective GR antagonists offer improved therapeutic profiles over non-selective agents like mifepristone.
  • Recent advancements have expanded the chemical diversity and therapeutic potential of GR antagonists.

Purpose of the Study:

  • To review recent progress in the discovery of selective glucocorticoid receptor (GR) antagonists.
  • To explore potential therapeutic applications and the underlying pharmacological rationale.
  • To present structure-activity relationships (SAR) of various nonsteroidal GR antagonist classes.

Main Methods:

  • Review of steroidal and nonsteroidal GR antagonist research.
  • Analysis of structure-activity relationships (SAR) for diverse chemical scaffolds.
  • Brief overview of assays for evaluating GR antagonist properties (binding, functional, in vivo).

Main Results:

  • Identification of numerous selective GR antagonists across various chemical classes.
  • Demonstration of therapeutic potential in conditions including Cushing's syndrome, psychotic depression, diabetes, obesity, Alzheimer's disease, neuropathic pain, drug abuse, and glaucoma.
  • Detailed SAR for key nonsteroidal scaffolds like octahydrophenanthrenes, spirocyclic dihydropyridines, and diaryl ethers.

Conclusions:

  • Selective GR antagonists represent a promising therapeutic avenue for a wide range of diseases.
  • Continued exploration of SAR for nonsteroidal compounds will drive the development of novel, effective treatments.
  • Targeted GR antagonism offers a refined approach to managing complex physiological and pathological processes.