Receptors by Drug Target

Receptors by Drug Target Background

Receptors, which locate on both the cell surface and within the cell, are drug targets where medicine produce their beneficial effects in various disease states.

Receptors are typically envisaged as cell surface recognition sites for endogenous hormones, neurotransmitters, and neuromodulators. They are coupled to various signal transduction systems located both within the membrane and intracellularly, and can therefore regulate responses to the cellular/tissue microenvironment.

Receptors can be defined in terms of their selectivity, the saturability and reversibility of ligand binding, and functionality. The definition of a receptor in both pharmacological and physiological terms requires that it has specific interactions with ligands that belong to a given pharmacological class.

Receptors are complex proteins with multiple potential ligand recognition sites, including sites that may be distinct from the endogenous agonist recognition site and may actually reside on distinct proteins that are part of the receptor complex.

Such receptor modulatory sites may represent novel drug targets, e.g., allosteric or modulatory sites. The effect of benzodiazepines (BZs) on GABAA receptor function illustrates the conceptualization of ancillary drug targets and the elusive nature of the proposed endogenous modulator, presumed to be a "BZ-like" substance.

In septic shock, the induction of a toxic cytokine receptor-mediated cascade has significantly complicated the search for new drugs to treat this condition. This emphasizes the need to define key targets in critical pathways rather than attempt to treat their sequelae.

It is possible that many diseases are the result of multifactorial events that vary during the pathophysiological course of the illness. For instance, >32 discrete gene loci have been associated with schizophrenia. Therefore, drug targets that are downstream from key points in the disease transduction pathway may not be the optimal targets for treating the disorder.

Hot Receptors by Drug Target

Host Defense Receptors as Drug Target Cell Adhesion Receptors as Drug Target
Nuclear Hormone Receptors/NHRs as Drug Target Receptor Tyrosine Phosphatases as Drug Target
G‐Protein‐Coupled Receptors/GPCRs as Drug Target Receptor Tyrosine Kinases/RTKs as Drug Target
Receptor Serine/Threonine Kinases (RSTKs) as Drug Target G‐Protein‐Coupled Receptor/GPCR Ligands as Drug Target


1. Williams M. Receptors as drug targets[J]. Current Protocols in Pharmacology, 2006.

2. Chen J F, et al. Adenosine receptors as drug targets—what are the challenges?[J]. Nature reviews Drug discovery, 2013, 12(4): 265-286.

Receptors Classification
What are Receptors
Cytokine Receptors
Growth Factor Receptors
Fc Receptor / FcR
Receptors by Differentiation Cells
B Cell Receptor
Dendritic Cell Receptor
Granulocyte Receptor
Monocyte Receptor
NK Cell Receptor
Stem Cell Receptor
T Cell Receptor
Receptors by Drug Target
GPCRs as Drug Target
GPCR Ligands as Drug Target
Nuclear Hormone Receptors as Drug Target
Cell Adhesion Receptors as Drug Target
Host Defense Receptors as Drug Target
Enzyme-Linked Receptors as Drug Target
Other Receptors as Drug Target
Receptors by Functions
Receptors Related to Innate Immunity
Receptors Related to Cell Activation
Receptors Related to CD Antigens
Receptors Related to Cell Adhesion
Receptors Related to Signaling Pathways
Receptors Reagent Products
Receptors Recombinant Protein
Receptors cDNA Clones
Anti-Receptors Antibody
Receptors ELISA Kits
Receptors by Species
Human Receptor
Mouse Receptor