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Related Concept Videos

Dipeptidyl Peptidase 4 Inhibitors01:23

Dipeptidyl Peptidase 4 Inhibitors

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...
Antihypertensive Drugs: Direct Renin Inhibitors01:25

Antihypertensive Drugs: Direct Renin Inhibitors

The renin-angiotensin-aldosterone system (RAAS) is an intricate physiological pathway involving numerous enzymes and hormones, including renin, angiotensin-converting enzyme (ACE), angiotensin I and II, and aldosterone. Imbalances within this system increase the production of angiotensin II and aldosterone. Increased angiotensin II levels promote vasoconstriction and blood pressure elevation. Concurrently, higher aldosterone levels stimulate sodium and water reabsorption in the kidneys,...
Heart Failure Drugs: Inhibitors of Renin-Angiotensin System01:26

Heart Failure Drugs: Inhibitors of Renin-Angiotensin System

The activation of the sympathetic nervous system and the renin-angiotensin-aldosterone system (RAAS) contributes to cardiac remodeling, and inhibiting the RAAS is a pharmacological target in heart failure management. As a result, neurohumoral modulation is a crucial treatment principle for managing heart failure. This approach involves using medications like ACE inhibitors (ACEIs), angiotensin receptor blockers (ARBs), β-blockers, mineralocorticoid receptor antagonists (MRAs), and neutral...
Antihypertensive Drugs: Angiotensin-Converting Enzyme Inhibitors01:30

Antihypertensive Drugs: Angiotensin-Converting Enzyme Inhibitors

Angiotensin-converting enzyme (ACE), a vital component of the renin-angiotensin-aldosterone system, is abundant in lung endothelial cells. ACE converts the inactive decapeptide, angiotensin I, into the active octapeptide, angiotensin II. This potent vasoconstrictor narrows blood vessels, increasing resistance to blood flow and elevating blood pressure. Angiotensin II also stimulates aldosterone production, encouraging kidney cells to reabsorb more sodium and water from urine, thereby increasing...
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Histamine H2 receptors, which are intricately located on the basolateral membrane of parietal cells, play a crucial role in modulating gastric acid secretion. When released from enterochromaffin-like cells, histamine engages H2 receptors, initiating the cyclic AMP (cAMP) pathway. In this pathway, adenylyl cyclase converts ATP into cAMP, elevating intracellular cAMP levels. The activation of protein kinase A follows, stimulating the proton pump. This stimulation prompts the secretion of hydrogen...
Inhibition of CDK Activity02:34

Inhibition of CDK Activity

The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...

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Related Experiment Video

Updated: Jun 15, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
09:11

Assays for Validating Histone Acetyltransferase Inhibitors

Published on: August 6, 2020

Inside HDAC with HDAC inhibitors.

Philippe Bertrand1

  • 1Laboratoire Synthèse et Réactivité des Substances Naturelles, Université de Poitiers, CNRS-UMR 6514, 40 Avenue du Recteur Pineau, Poitiers, F-86022, France. Philippe.bertrand@univ-poitiers.fr

European Journal of Medicinal Chemistry
|March 13, 2010
PubMed
Summary
This summary is machine-generated.

Histone deacetylase inhibitors (HDAC inhibitors) show promise in cancer therapy by inhibiting cell proliferation and inducing apoptosis. Research focuses on developing isoform-selective HDAC inhibitors for targeted cancer treatment.

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09:14

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Published on: January 14, 2016

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • Histone deacetylase inhibitors (HDAC inhibitors) are a diverse class of molecules that inhibit cancer cell proliferation.
  • Their anti-cancer effects are linked to histone acetylation, chromatin remodeling, and tumor suppressor gene expression.
  • The full biological impact of HDAC inhibitors is not yet understood, necessitating further research.

Purpose of the Study:

  • To review current approaches in synthesizing HDAC inhibitors.
  • To explore the use of modeling studies in designing new HDAC inhibitors.
  • To discuss strategies for achieving HDAC isoform selectivity.

Main Methods:

  • Review of literature on HDAC inhibitor synthesis.
  • Analysis of computational modeling studies applied to HDAC inhibitor design.
  • Examination of strategies for developing isoform-selective HDAC inhibitors.

Main Results:

  • Diverse synthetic strategies for HDAC inhibitors have been developed.
  • Modeling studies guide the design of novel HDAC inhibitors.
  • Progress has been made in creating HDAC inhibitors with potential isoform selectivity.

Conclusions:

  • HDAC inhibitors represent a significant therapeutic strategy for cancer.
  • Developing isoform-selective HDAC inhibitors is crucial for understanding their mechanisms and improving efficacy.
  • Continued research integrating modeling and synthesis is key to advancing HDAC inhibitor development.