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Related Concept Videos

Opioid Receptors: Overview01:22

Opioid Receptors: Overview

Opioid receptors, including the mu (μ, MOR), delta (δ, DOR), and kappa (κ, KOR) types, belong to the rhodopsin family of G protein-coupled receptors. These receptors are located throughout the central and peripheral nervous systems and in non-neuronal tissues such as macrophages and astrocytes. Opioid receptor ligands can be categorized into agonists or antagonists. Highly selective agonists include [d-Ala2, MePhe4, Gly(ol)5]-enkephalin or DAMGO for MOR, [D-Pen2, D-Pen5]-enkephalin or DPDPE for...
Drug-Receptor Interaction: Agonist01:25

Drug-Receptor Interaction: Agonist

Agonists are drugs that interact with specific receptors in the body to produce a biological response. When an agonist binds to a receptor, it activates or enhances the receptor's function, leading to physiological effects. The interaction between agonist drugs and receptors is crucial for their therapeutic action in various medical treatments.
Agonists can bind to receptors in different ways. Some agonists bind directly to the receptor's active site, mimicking the endogenous ligand's action.
Antiasthma Drugs: Muscarinic Receptor Antagonists01:20

Antiasthma Drugs: Muscarinic Receptor Antagonists

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...
Adrenergic Agonists: Indirect-Acting Agents01:25

Adrenergic Agonists: Indirect-Acting Agents

Indirect-acting adrenergic agonists potentiate the effects of endogenous catecholamines through different mechanisms without directly binding to adrenoceptors.
One mechanism involves depleting stored catecholamines by displacing them from synaptic vesicles. These agents, known as "displacers," are transported into vesicles at the expense of noradrenaline. Examples include amphetamine and tyramine, which lack a catechol moiety, resulting in prolonged action, improved oral bioavailability, and...
GPCR Desensitization01:12

GPCR Desensitization

G protein-coupled receptor (GPCR) signaling plays a crucial role in cell functioning. GPCR desensitization is an equally essential process. It allows cells to respond to changing environments and regain sensitivity to new stimuli while preventing unnecessary stimulation when no longer needed. Prolonged exposure to stimuli leads to GPCR desensitization. It involves blocking the receptors from binding and activating additional G proteins. This inhibits activation of downstream effectors, thereby...
Adrenergic Agonists: Direct-Acting Agents01:30

Adrenergic Agonists: Direct-Acting Agents

Drugs that mimic the action of endogenous catecholamines like noradrenaline and adrenaline are called adrenergic agonists or sympathomimetics. Based on their mechanism of action, sympathomimetics can be classified as direct-, indirect-, or mixed-acting sympathomimetics. Direct-acting adrenergic agonists activate adrenoceptors without affecting presynaptic neurons, making them independent of neuronal catecholamine-depleting agents like reserpine and guanethidine.
These agents can be classified...

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Quantifying Agonist Activity at G Protein-coupled Receptors
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Quantifying Agonist Activity at G Protein-coupled Receptors

Published on: December 26, 2011

Kappa agonist CovX-Bodies.

Lee R Roberts1, Kevin Brady, Amy Brown

  • 1Worldwide Medicinal Chemistry, Pfizer Ramsgate Road, Sandwich, Kent CT13 9NJ, UK. lee.roberts@pfizer.com

Bioorganic & Medicinal Chemistry Letters
|May 16, 2012
PubMed
Summary

Small kappa agonists were attached to antibodies, creating new compounds with strong kappa receptor activity and significantly longer effectiveness compared to the original peptides.

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Area of Science:

  • Pharmacology
  • Bioconjugation Chemistry
  • Drug Development

Background:

  • Kappa receptor agonists are peptides with therapeutic potential.
  • Short half-life limits the clinical utility of peptide drugs.
  • Antibody-drug conjugates offer strategies to improve drug pharmacokinetics.

Purpose of the Study:

  • To develop novel kappa receptor agonists with enhanced pharmacokinetic properties.
  • To create bioconjugates by linking small peptidic kappa agonists to an antibody.
  • To evaluate the activity and half-life of the resulting antibody-peptide conjugates.

Main Methods:

  • Covalent linkage of small peptidic kappa agonists to the reactive lysine residues of the CovX antibody.
  • In vitro and in vivo assays to assess kappa receptor binding affinity and functional activity.
  • Pharmacokinetic studies to determine the half-life of the parent peptide versus the antibody-conjugated compound.

Main Results:

  • Successfully synthesized antibody-peptide conjugates with retained kappa receptor activity.
  • Demonstrated potent activity at the kappa receptor for the novel compounds.
  • Observed a greatly extended half-life for the antibody-conjugated kappa agonists compared to the parent peptide.
  • Compound 20 exemplified the successful conjugation and pharmacokinetic improvement.

Conclusions:

  • Covalent conjugation of small peptidic kappa agonists to antibodies is a viable strategy to enhance their pharmacokinetic profiles.
  • The developed antibody-peptide conjugates exhibit potent kappa receptor activity and prolonged in vivo half-life.
  • This approach holds promise for developing more effective therapeutics targeting the kappa receptor system.