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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...
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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.
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Enzyme Inhibition01:30

Enzyme Inhibition

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Lipid-Lowering Drugs: Statins and Miscellaneous Agents

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...
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.
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Updated: Jun 1, 2026

Functional Characterization of Carboxylesterases in Insecticide Resistant House Flies, Musca Domestica
08:17

Functional Characterization of Carboxylesterases in Insecticide Resistant House Flies, Musca Domestica

Published on: August 23, 2018

Carboxylesterase inhibitors.

M Jason Hatfield1, Philip M Potter

  • 1Department of Chemical Biology and Therapeutics, St. Jude Children’s Research Hospital, Memphis, TN 38105, USA.

Expert Opinion on Therapeutic Patents
|May 26, 2011
PubMed
Summary
This summary is machine-generated.

Selective carboxylesterase inhibitors offer a novel approach to drug discovery. These compounds can enhance drug efficacy and reduce toxicity by modulating esterase activity, with broad applicability across various esterified drugs.

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Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
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Functional Characterization of Carboxylesterases in Insecticide Resistant House Flies, Musca Domestica
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Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
10:33

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors

Published on: October 26, 2015

Area of Science:

  • Biochemistry
  • Pharmacology
  • Drug Discovery

Background:

  • Carboxylesterases are crucial enzymes in the hydrolysis of many therapeutic compounds.
  • The role of carboxylesterases in drug stability and pharmacokinetics is often overlooked during development.
  • Selective inhibitors could modulate drug metabolism, distribution, and toxicity.

Purpose of the Study:

  • To review the development of carboxylesterase inhibitors since 1986.
  • To highlight recent advancements in selective human carboxylesterase inhibitors.

Main Methods:

  • Literature review of carboxylesterase inhibitor development.
  • Focus on recent identification of selective human carboxylesterase inhibitors.

Main Results:

  • Carboxylesterase inhibitors have the potential to revolutionize drug discovery.
  • These inhibitors can improve efficacy and reduce toxicity of esterified drugs.
  • Lack of carboxylesterase activity has no apparent biological consequence, suggesting wide applicability.

Conclusions:

  • Carboxylesterase inhibitors can significantly alter drug hydrolysis and distribution in vivo.
  • Their implementation may lead to improved drug efficacy and safety profiles.
  • The review discusses properties and potential uses of these agents.