The Concise Guide to PHARMACOLOGY 2023/24: Catalytic receptors
Stephen P H Alexander1, Doriano Fabbro2, Eamonn Kelly3
1School of Life Sciences, University of Nottingham Medical School, Nottingham, NG7 2UH, UK.
British Journal of Pharmacology
|December 20, 2023
Summary
The Concise Guide to Pharmacology 2023/24 offers a comprehensive overview of drug targets and their interactions. This biennial publication provides essential pharmacology data for researchers and clinicians.
Area of Science:
- Pharmacology
- Drug Discovery
- Biomedical Research
Background:
- The Concise Guide to Pharmacology is a biennial publication series.
- It summarizes key properties of drug targets and their interactions.
- The guide links to an open-access knowledgebase for detailed information.
Purpose of the Study:
- To provide a concise, citable, point-in-time record of pharmacological data.
- To offer an overview of approximately 1800 drug targets and 6000 ligand interactions.
- To present official IUPHAR classification and nomenclature for human drug targets.
Main Methods:
- Data compilation in a tabular format.
- Inclusion of selective pharmacology where available.
- Cross-referencing with the online guide (https://www.guidetopharmacology.org/).
Main Results:
- Overview of ~1800 drug targets and ~6000 ligand interactions.
- Categorization of targets into six major groups: catalytic receptors, G protein-coupled receptors, ion channels, nuclear hormone receptors, enzymes, and transporters.
- Inclusion of nomenclature guidance and information on pharmacological tools.
Conclusions:
- The Concise Guide serves as a permanent, citable record of pharmacology data.
- It facilitates comparison of related targets.
- The publication provides essential resources for researchers in pharmacology and drug discovery.
More Related Videos
Related Concept Videos
G Protein-coupled Receptors
12.1K
G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
12.1K
GPCRs Regulate Adenylyl Cylase Activity
5.6K
Some GPCRs transmit signals through adenylyl cyclase (AC), a transmembrane enzyme. AC helps synthesize second messenger cyclic adenosine monophosphate (cAMP). AC catalyzes cyclization reaction and converts ATP to cAMP by releasing a pyrophosphate. The pyrophosphate is further hydrolyzed to phosphate by the enzyme pyrophosphatase, which drives cAMP synthesis to completion. However, cAMP is rapidly degraded to 5′ AMP by the enzymes phosphodiesterase (PDE), preventing overstimulation of...
5.6K
Pharmacodynamics: Overview and Principles
1.2K
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...
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...
1.2K
The Two-State Receptor Model
1.9K
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...
The binding affinity of a drug determines its interaction with...
1.9K
Drug Discovery: Overview
7.9K
Drug discovery is a multifaceted process involving extensive screening, testing, and optimization of lead compounds to identify potential new drugs for therapeutic use. It combines several approaches, including screening large numbers of natural products, chemical modification of known active molecules, identification of new drug targets, and rational design based on biological mechanisms and drug-receptor structure. These approaches are carried out in both academic research laboratories and...
7.9K
Drug-Receptor Interactions
5.2K
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....
5.2K


