Jove
Visualize
Contact Us
JoVE
x logofacebook logolinkedin logoyoutube logo
ABOUT JoVE
OverviewLeadershipBlogJoVE Help Center
AUTHORS
Publishing ProcessEditorial BoardScope & PoliciesPeer ReviewFAQSubmit
LIBRARIANS
TestimonialsSubscriptionsAccessResourcesLibrary Advisory BoardFAQ
RESEARCH
JoVE JournalMethods CollectionsJoVE Encyclopedia of ExperimentsArchive
EDUCATION
JoVE CoreJoVE BusinessJoVE Science EducationJoVE Lab ManualFaculty Resource CenterFaculty Site
Terms & Conditions of Use
Privacy Policy
Policies

Related Concept Videos

Drug-Receptor Bonds01:25

Drug-Receptor Bonds

3.2K
Drug-receptor bonds are formed through various chemical forces when drugs interact with target cells. Covalent bonds, strong and irreversible, are exemplified by DNA-alkylating anticancer agents that inhibit cell division. However, such irreversible drug binding lacks selectivity and can modify the DNA of the surrounding healthy cells. Covalent binding often contributes to tissue toxicity, as seen with chloroform and paracetamol metabolites binding to the liver, causing hepatotoxicity.
In...
3.2K
Ligand Binding Sites02:40

Ligand Binding Sites

13.1K
Proteins are dynamic macromolecules that carry out a wide variety of essential processes; however, the activities of most proteins depend on their interactions with other molecules or ions, known as ligands.
Protein-ligand interactions are quite specific; even though numerous potential ligands surround a cellular protein at any given time, only a particular ligand can bind to that protein. Moreover, a ligand binds only to a dedicated area on the surface of the protein, known as the...
13.1K
The Two-State Receptor Model01:29

The Two-State Receptor Model

2.4K
The two-state receptor model explains a drug's interaction with receptors, such as G protein-coupled receptors and ligand-gated ion channels, to induce or inhibit a biological response. When no natural ligands are present, a receptor exists in an equilibrium of inactive (Ri) and active (Ra) conformations. The inactive form does not produce a response, while the active form generates a basal effect known as constitutive activity.
The binding affinity of a drug determines its interaction with...
2.4K
Drug-Receptor Interactions01:29

Drug-Receptor Interactions

5.9K
Drug-receptor interaction describes the binding of receptors by drugs, but not all drug-receptor interactions result in activation and tissue response. For instance, the binding of agonists activates the receptor to generate a cellular reaction, while antagonists bind to receptors without causing their activation.
Several parameters, such as the drug's affinity for its receptor and its efficacy, which is its ability to activate the receptor, determine the drug's effect on the tissue....
5.9K
Valence Bond Theory02:42

Valence Bond Theory

9.2K
Coordination compounds and complexes exhibit different colors, geometries, and magnetic behavior, depending on the metal atom/ion and ligands from which they are composed. In an attempt to explain the bonding and structure of coordination complexes, Linus Pauling proposed the valence bond theory, or VBT, using the concepts of hybridization and the overlapping of the atomic orbitals. According to VBT, the central metal atom or ion (Lewis acid) hybridizes to provide empty orbitals of suitable...
9.2K
Ligand-Gated Ion Channel Receptor: Gating Mechanism01:30

Ligand-Gated Ion Channel Receptor: Gating Mechanism

2.6K
Ligand-gated ion channels are transmembrane proteins that play a vital role in intercellular communication and functions of the nervous system. They allow the influx of ions across the membrane once the neurotransmitter binds, allowing the subsequent transmission of electrical excitation across the neurons. Other ligand-gated ion channels, like the γ-aminobutyric acid (GABA) receptor, permit anions like chloride into the cells on the binding of the GABA molecule. Their entry into the cell...
2.6K

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by
Same author

Comprehensive Evaluation of Indazole-Based Synthetic Cannabinoid Receptor Agonists with Aliphatic Tail Groups: In Vitro Activities, Metabolic Stability, and In Vivo Pharmacokinetics.

ACS chemical neuroscience·2026
Same author

AB-MDMSBA-Not a Synthetic Cannabinoid Receptor Agonist.

Pharmacology research & perspectives·2026
Same author

The dual role of azoles: lifesaving antifungals and drivers of resistance - a One Health perspective.

Nature communications·2026
Same author

Phylogenetic and Structural Analysis of Miconazole Susceptibility in Malassezia pachydermatis Isolates From Dogs With Otitis Externa.

Veterinary dermatology·2026
Same author

G521 is the gatekeeper and a key transmembrane domain contact residue of <i>Candida albicans</i> Cdr1.

mBio·2026
Same author

The Concise Guide to PHARMACOLOGY 2025/26: G protein-coupled receptors.

British journal of pharmacology·2025

Related Experiment Video

Updated: Sep 8, 2025

Creating Highly Specific Chemically Induced Protein Dimerization Systems by Stepwise Phage Selection of a Combinatorial Single-Domain Antibody Library
10:17

Creating Highly Specific Chemically Induced Protein Dimerization Systems by Stepwise Phage Selection of a Combinatorial Single-Domain Antibody Library

Published on: January 14, 2020

7.9K

Covalent cannabinoid receptor ligands - structural insight and selectivity challenges.

Ian Liddle1, Michelle Glass2, Joel D A Tyndall3

  • 1Department of Chemistry, University of Otago Dunedin New Zealand andrea.vernall@otago.ac.nz +64 3 479 5214.

RSC Medicinal Chemistry
|June 13, 2022
PubMed
Summary

Recent structural insights into G protein-coupled receptors (GPCRs) aid the rational design of cannabinoid receptor type 1 and 2 ligands. This review focuses on heterocyclic covalent ligands for these important targets.

More Related Videos

Covalent Fragment Screening Using the Quantitative Irreversible Tethering Assay
06:17

Covalent Fragment Screening Using the Quantitative Irreversible Tethering Assay

Published on: February 28, 2025

674
Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
07:16

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission

Published on: August 16, 2018

13.7K

Related Experiment Videos

Last Updated: Sep 8, 2025

Creating Highly Specific Chemically Induced Protein Dimerization Systems by Stepwise Phage Selection of a Combinatorial Single-Domain Antibody Library
10:17

Creating Highly Specific Chemically Induced Protein Dimerization Systems by Stepwise Phage Selection of a Combinatorial Single-Domain Antibody Library

Published on: January 14, 2020

7.9K
Covalent Fragment Screening Using the Quantitative Irreversible Tethering Assay
06:17

Covalent Fragment Screening Using the Quantitative Irreversible Tethering Assay

Published on: February 28, 2025

674
Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
07:16

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission

Published on: August 16, 2018

13.7K

Area of Science:

  • Pharmacology
  • Structural Biology
  • Medicinal Chemistry

Background:

  • G protein-coupled receptors (GPCRs) are crucial drug targets.
  • Cannabinoid receptors (CB1 and CB2) are class A GPCRs involved in numerous pathophysiological processes.
  • Advancements in X-ray crystallography and cryo-EM have revealed GPCR structures, enabling rational drug design.

Purpose of the Study:

  • To review heterocyclic covalent ligands for cannabinoid receptors.
  • To discuss ligand selectivity and rational design strategies in light of recent structural data.
  • To highlight the therapeutic potential of targeting CB1 and CB2 receptors.

Main Methods:

  • Literature review of scientific publications.
  • Analysis of recent structural data for cannabinoid receptors.
  • Examination of heterocyclic covalent ligand classes.

Main Results:

  • Recent structural insights enhance understanding of ligand binding pockets and selectivity-determining residues in cannabinoid receptors.
  • Heterocyclic covalent ligands offer a promising avenue for developing selective modulators.
  • Structure-based design principles are crucial for optimizing ligand efficacy and selectivity.

Conclusions:

  • Structural knowledge of cannabinoid receptors is pivotal for the rational design of covalent ligands.
  • Targeting CB1 and CB2 receptors with selective covalent ligands holds significant therapeutic promise.
  • Further research into structure-activity relationships will refine the design of novel cannabinoid receptor modulators.