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Related Concept Videos

Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship01:29

Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship

Indirect-acting cholinergic agonists are agents that interact with the acetylcholinesterase enzyme in the synaptic cleft, preventing the breakdown of acetylcholine into choline and acetate. Consequently, the concentration of acetylcholine in the synaptic cleft increases. These agonists can be classified into reversible and irreversible inhibitors based on their duration of action.
Reversible inhibitors display short to medium durations of action. Short-acting agents include simple alcohols with...
Indirect-Acting Cholinergic Agonists: Mechanism of Action01:18

Indirect-Acting Cholinergic Agonists: Mechanism of Action

Indirect-acting cholinergic agonists work by interacting with an enzyme called acetylcholinesterase (AChE) in the synaptic cleft. They can be reversible or irreversible inhibitors and have different effects on the enzyme.
Reversible inhibitors like edrophonium bind to a specific part of the enzyme called the anionic catalytic site. They form noncovalent bonds, which means they are not strongly attached to the enzyme. This creates a temporary and less stable enzyme–inhibitor complex, leading to...
Anticholinesterase Agents: Poisoning and Treatment01:26

Anticholinesterase Agents: Poisoning and Treatment

Anticholinesterases, also known as cholinesterase inhibitors, work by blocking the breakdown of acetylcholine, leading to its accumulation in the synaptic cleft. This accumulation indirectly enhances both muscarinic and nicotinic actions. These agents are classified as reversible or irreversible based on their mechanism of action.     
Irreversible agents form a strong bond with the cholinesterase enzyme, making it inactive. The breakdown of the phosphorylated enzyme is slower than the...
Chromatin Immunoprecipitation- ChIP02:36

Chromatin Immunoprecipitation- ChIP

Chromatin immunoprecipitation, or ChIP, is an antibody-based technique used to identify sites on DNA that bind to transcription factors of interest or histone proteins. It also helps determine the type of histone modifications such as acetylation, phosphorylation, or methylation.
Types of ChIP
ChIP can be divided into two types - X-ChIP and N-ChIP. X-ChIP involves in vivo cross-linking of histones and regulatory proteins to DNA, fragmenting the DNA by sonication, and isolating the protein-DNA...
Indirect-Acting Cholinergic Agonists: Pharmacological Actions01:30

Indirect-Acting Cholinergic Agonists: Pharmacological Actions

Indirect-acting cholinergic agonists, also known as anticholinesterases, exert their pharmacological effects by enhancing cholinergic transmission in various body parts, including the neuromuscular junction, autonomic cholinergic synapses, and the brain.
At the neuromuscular junction, these agents work by inhibiting the breakdown of acetylcholine, allowing it to remain bound to the receptor and bind to nearby receptors. This process leads to repetitive firing of the endplate, causing muscle...
Enzyme Inhibition01:30

Enzyme Inhibition

Inhibitors are molecules that reduce enzyme activity by binding to the enzyme. In a normally functioning cell, enzymes are regulated by a variety of inhibitors. Drugs and other toxins can also inhibit enzymes. Some inhibitors bind to the enzyme’s active site, while others inhibit enzymatic activity by binding to other sites on the protein structure.

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Updated: May 16, 2026

Identification of Mediators of T-cell Receptor Signaling via the Screening of Chemical Inhibitor Libraries
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Published on: January 22, 2019

Chymase inhibitors.

Eiji Yahiro1, Shin-ichiro Miura, Satoshi Imaizumi

  • 1Department of Cardiology, Fukuoka University School of Medicine, 7-45-1 Nanakuma, Jonan-ku, Fukuoka, 814-0180, Japan. eyahiro@fukuoka-u.ac.jp

Current Pharmaceutical Design
|November 27, 2012
PubMed
Summary
This summary is machine-generated.

Chymase inhibitors may offer new therapeutic strategies for cardiovascular diseases by targeting the local renin-angiotensin system (RAS). This review explores their potential role in managing conditions where alternative angiotensin II (Ang II) pathways are implicated.

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Area of Science:

  • Biochemistry and Pharmacology
  • Cardiovascular Research
  • Enzyme Inhibition

Background:

  • Chymase, a mast cell protease, generates angiotensin II (Ang II) independently of angiotensin-converting enzyme (ACE).
  • The role of alternative Ang II-forming pathways in cardiovascular disease pathogenesis is not fully understood.
  • Current treatments like ACE inhibitors and ARBs primarily target the systemic RAS.

Purpose of the Study:

  • To review the potential applications of chymase inhibitors as novel therapeutic agents.
  • To discuss the inhibition of the local RAS by chymase inhibitors for cardiovascular disease prevention.
  • To highlight the significance of chymase in local Ang II generation relevant to cardiovascular health.

Main Methods:

  • Literature review focusing on chymase, its role in the RAS, and the effects of chymase inhibitors.
  • Analysis of animal model studies investigating chymase inhibitors in cardiovascular disease contexts.
  • Discussion of the comparative role of chymase inhibition versus systemic RAS inhibition.

Main Results:

  • Chymase is a significant enzyme in local Ang II production, independent of ACE.
  • Animal models suggest potential benefits of chymase inhibitors in preventing cardiovascular diseases.
  • Chymase inhibitors may offer a targeted approach to local RAS modulation.

Conclusions:

  • Chymase inhibitors represent a promising class of drugs for targeting the local RAS.
  • Further research is warranted to explore their therapeutic efficacy in human cardiovascular diseases.
  • Chymase inhibition could complement existing therapies by addressing alternative Ang II pathways.