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Related Concept Videos

Cholinergic Antagonists: Pharmacokinetics01:24

Cholinergic Antagonists: Pharmacokinetics

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Cholinergic antagonists—such as antimuscarinics—are available in oral, topical, ocular, parenteral, and inhalational formulations. Most antimuscarinics are oral formulations,  while scopolamine is available as a topical patch, and ipratropium and tiotropium are available as inhalation aerosols or powders. Atropine, tropicamide, and cyclopentolate are topically instilled in the eye. Most antimuscarinics are lipid-soluble and readily absorbed from the gastrointestinal tract and...
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Cholinergic Antagonists: Therapeutic Uses01:26

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Antimuscarinic drugs have various therapeutic applications by inhibiting parasympathetic stimulation in different systems. Here are the key therapeutic uses of antimuscarinics:    
Respiratory Tract: Ipratropium, aclidinium, and tiotropium treat asthma, chronic bronchitis, and chronic obstructive pulmonary disease (COPD). They protect against bronchoconstriction caused by irritants like cigarette smoke, sulfur dioxide, and ozone. They also help reduce nasopharyngeal...
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Cholinergic Antagonists: Pharmacological Actions01:28

Cholinergic Antagonists: Pharmacological Actions

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Antimuscarinic drugs block muscarinic receptors in multiple systems, including the gut, eye, smooth muscles, respiratory tract, cardiovascular, and central nervous systems. They produce similar effects with varying selectivity depending on the specific agent and tissue. Here are the key pharmacological actions of antimuscarinics:
Gastrointestinal Effects: Antimuscarinics reduce gut contractions, increase gastric emptying, and slow intestinal transit. They partly inhibit gastric acid secretion...
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Drug-Receptor Interaction: Antagonist01:28

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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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Antiepileptic Drugs: Glutamate Antagonists01:14

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Glutamate is a fundamental neurotransmitter in the central nervous system, playing a vital role in neuronal communication and various cognitive processes. Glutamate stands as the principal excitatory neurotransmitter in the brain. Its presence is crucial for the communication between neurons, underpinning essential processes such as synaptic transmission, neuronal excitability, and plasticity. These functions are vital for higher-order cognitive processes, including learning and memory. The...
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Antiasthma Drugs: Muscarinic Receptor Antagonists01:20

Antiasthma Drugs: Muscarinic Receptor Antagonists

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Muscarinic receptor antagonists, also known as antimuscarinic agents, are a class of bronchodilators used to treat asthma, although they are more commonly used to treat COPD. They work by inhibiting the action of acetylcholine (ACh), a neurotransmitter, on muscarinic receptors found in the airways.
Antimuscarinic agents compete with ACh for the same binding site on the muscarinic receptors. By binding to these receptors, they inhibit the downstream effects of ACh and block the parasympathetic...
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Honokiol is a FOXM1 antagonist.

Marianna Halasi1, Ben Hitchinson2, Binal N Shah1

  • 1Department of Medicine, University of Illinois, Chicago, IL, USA.

Cell Death & Disease
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PubMed
Summary

Honokiol, a natural compound, inhibits cancer cell growth by targeting the oncogenic transcription factor FOXM1. This inhibition occurs through specific binding, revealing a novel anticancer mechanism for honokiol.

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Area of Science:

  • Natural Products Chemistry
  • Molecular Oncology
  • Drug Discovery

Background:

  • Honokiol exhibits broad-spectrum anticancer activity against diverse malignancies.
  • Overexpression of the oncogenic transcription factor FOXM1 is common in human cancers.
  • The precise mechanism underlying honokiol's anticancer effects requires elucidation.

Purpose of the Study:

  • To investigate the molecular mechanism by which honokiol exerts its anticancer effects.
  • To determine if honokiol targets the transcription factor FOXM1.
  • To elucidate the specific interactions between honokiol and FOXM1.

Main Methods:

  • In vitro assays to assess honokiol's effect on FOXM1-mediated transcription.
  • Western blotting to evaluate FOXM1 protein expression levels.
  • Biochemical binding studies to confirm direct interaction between honokiol and FOXM1.

Main Results:

  • Honokiol significantly inhibits FOXM1-mediated transcription and reduces FOXM1 protein expression.
  • Direct binding of honokiol to FOXM1 was demonstrated.
  • Specific structural features of honokiol, including dimerization and allylphenol substitution, are crucial for FOXM1 binding.

Conclusions:

  • Honokiol inhibits cancer progression through a novel mechanism involving direct binding and inhibition of the oncogenic transcription factor FOXM1.
  • The specific interaction highlights honokiol as a potential therapeutic agent for cancers driven by FOXM1.
  • Understanding this mechanism provides a basis for developing targeted therapies against FOXM1.