Related Experiment Video
Updated: Jul 15, 2026
10:49
Identification of Small Molecule-binding Proteins in a Native Cellular Environment by Live-cell Photoaffinity Labeling
Published on: September 20, 2016
Targets of drug action
1Department of Pharmacology, University of Cambridge, United Kingdom. asvb@cam.ac.uk
Annual Review of Pharmacology and Toxicology
|June 3, 2000
Summary
This study explores muscarinic receptor characteristics and conformational variability. Advances in nuclear magnetic resonance and 3D receptor structures are advancing drug development and understanding receptor function.
Area of Science:
- Pharmacology
- Biochemistry
- Structural Biology
Background:
- Muscarinic receptors play crucial roles in various physiological processes.
- Understanding receptor subtypes and conformational variability is key to targeted drug design.
- Early research focused on receptor specificity and early applications of nuclear magnetic resonance (NMR).
Purpose of the Study:
- To review early laboratory work on muscarinic receptor specificity, subtypes, and conformational variability.
- To discuss the application of NMR in pharmacology.
- To explore current drug development strategies influenced by receptor structural knowledge.
Main Methods:
- Review of early laboratory findings on muscarinic receptors.
- Application of nuclear magnetic resonance (NMR) spectroscopy.
- Analysis of dihydrofolate reductase conformational variants.
- Examination of three-dimensional receptor structures.
Main Results:
- Characterization of muscarinic receptor specificity, subtypes, and conformational states.
- Demonstration of NMR's utility in pharmacological studies.
- Insights into receptor function based on structural data.
Conclusions:
- Early work laid the foundation for understanding receptor complexity.
- Advancements in structural biology, particularly 3D receptor structures, are revolutionizing drug development.
- Knowledge of receptor conformation is critical for designing effective therapeutics.
Related Concept Videos
01:29Drug-Receptor Interactions
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.
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.
01:24Principles of Drug Action
Drugs are chemical substances that modify biological responses by interacting with macromolecular targets such as receptors, ion channels, transporters, and enzymes. Pharmacodynamics describes the course of action of drugs leading to the physiological effect at a specific site in the body.
Drugs can be agonists or antagonists. Like the endogenous ligands, agonists always bind and activate the target to produce a cellular response. Agonist binding induces a conformational change which in turn...
Drugs can be agonists or antagonists. Like the endogenous ligands, agonists always bind and activate the target to produce a cellular response. Agonist binding induces a conformational change which in turn...
01:26Targets for Drug Action: Overview
Drugs target macromolecules to modify ongoing cellular processes. Primary drug targets include receptors, ion channels, transporters, and enzymes.
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...
01:25Dose-Response Relationship: Selectivity and Specificity
Drugs exert their therapeutic effects by interacting with receptors, enzymes, or ion channels that are present throughout the human body. The strength and duration of the interaction between a drug and its target receptor are characterized by the selectivity and specificity of the drug. Selectivity refers to a drug's strong preference for its intended target over other targets. For instance, isoprenaline, a non-selective β-adrenergic agonist, interacts with both β1- and β2-adrenergic receptors...
01:28Drug-Receptor Interaction: Antagonist
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...
Antagonists can be classified as competitive or noncompetitive based on their...
01:21Pharmacodynamics: Overview and Principles
Pharmacodynamics is a scientific field that delves into drugs' intricate biochemical, cellular, and physiological effects on the human body. The study of pharmacodynamics helps us understand how drugs interact with the body and elicit various responses.
Most drugs' effects result from their interactions with drug receptors or targets within the body. These interactions trigger specific responses at the cellular or systemic level. Drug receptors can be found on the surfaces of cells or within...
Most drugs' effects result from their interactions with drug receptors or targets within the body. These interactions trigger specific responses at the cellular or systemic level. Drug receptors can be found on the surfaces of cells or within...