Cellular Receptors of Relevance to Therapeutics

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Skye McKennon
PharmD, BCPS, CSM-GEI
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This table provides a summary of the various types of cellular receptors that are drug targets.  

Classes Subclasses or families Physiological ligands Transducers, principal effects, or ions

G protein-coupled receptors (GPCRs)a

  • Adhesion
  • Frizzled
  • Glutamate
  • Rhodopsin
  • Secretin

Very large number of endocrine and paracrine factors, but other types of ligands as well

G proteins

  •  Gs: Adenylyl cyclases (stimulation)
  •  Gi: Adenylyl cyclases (inhibition), delayed rectifier K+ channel (stimulation), N-type voltage-gated Ca2+ channel (inhibition)
  •  Gq: Phospholipase C-β (stimulation)

Ligand-gated ion channelsb

Glutaminergic

Glutamate

Na+ and K+ principally, but Ca2+ as well in certain circumstances

Nicotinic cholinergic

ACh

Na+, K+, Ca2+

P2X

ATP

Na+, K+, Ca2+

5-HT3

5-HT3

Na+, K+, Ca2+

TRP
Many ligands

Na+, Ca2+, Mg2+

GABAA

GABA

Cl

Glycine

Glycine

Cl

Enzyme-linked (catalytic) receptors

Receptor tyrosine kinases

Insulin, PDGF, EGF, VEGF, growth factorsd

Proteins containing SH2 and PTB domains

Receptor serine kinases

TGF-β family

SMADs

Membrane bound GC

Natriuretic peptides

Cyclic GMP

Other cell-surface membrane receptors

Cytokine receptors

Interleukins and other cytokines, growth hormone, prolactin

JAK/STATs, soluble tyrosine kinases

Toll-like receptors

PAMPs

TIRAP, TRAM

TNFα receptors

TNF-α

TRADD, RIP-1, TRAF2

Nuclear receptorsc

Steroid receptors (subfamily 3)

Corticosteroids, sex hormones

Coactivators

Nonsteroid receptors (subfamilies 1, 2, 4–6)

Thyroxine, retinoic acid, hydroxycholesterols, bile acids, Vitamin D

Coactivators, corepressors

SMAD, a concatenation of SMA (small worm phenotype in C. elegans) and MAD (Mothers Against Decapentaplegic in Drosophila); TIRAP, toll-interleukin 1 receptor domain-containing adaptor protein; TRADD, TNF receptor–associated death domain; TRAF2, TNF receptor–associated factor 2; TRAM, TRIF-related adapter molecule, wherein TRIF represents TIR domain-containing adapter-inducing interferon-β and TIR is toll-interleukin 1 receptor.

aThe GPCR families are listed according to the GRAFS system (Fredriksson et al., 2003), which is based on phylogenetic analyses of the human genome; other systems of classification exist. It is important to note that each family of GPCRs contains a large number of receptors that respond to agonists and communicate with transducers distinct from the family’s namesake. See Figure 3–14 and legend.

bGlutaminergic receptors comprise the AMPA, kainate, and NMDA receptors. Many permutations of each of these subtypes and of other subclasses of ligand-gated ion channels exist owing to combinatorial diversity in subunit composition. Ion channels that are gated by internal ligands are not listed for the purposes of brevity but are discussed in the text.

cNuclear receptors are generally grouped into six subfamilies. The table groups the subfamilies into two major classes, steroid receptors and nonsteroid receptors, as does the IUPHAR/BPS Guide to Pharmacology.

dThe list comprises only a selection from among many different agonists.

Source

Adapted from: Manning DR, Blumenthal DK. Pharmacodynamics: Molecular Mechanisms of Drug Action. In: Brunton LL, Knollmann BC. eds. Goodman & Gilman's: The Pharmacological Basis of Therapeutics, 14th Edition. McGraw-Hill Education; 2023. Accessed January 14, 2025.