G Protein-Coupled Receptors as Targets for Approved Drugs: How Many Targets and How Many Drugs?
Level 5 - mechanism / opinion, no new human data
Database curation and narrative review (non-clinical bibliometric/pharmacological analysis)
PubMed 29298813 · doi:10.1124/mol.117.111062
What was done
Authors integrated and cross-curated data from public pharmacology databases (ChEMBL, Guide to PHARMACOLOGY, DrugBank) and the Broad Institute Drug Repurposing Hub to establish an accurate count of G protein-coupled receptors (GPCRs) targeted by approved therapeutics as of November 2017.
What was found
As of November 2017, 134 GPCRs were targeted by drugs approved in the US or EU, and 128 were targeted by drugs listed in the FDA Orange Book. An estimated ~700 approved drugs target GPCRs, accounting for approximately 35% of all approved drugs. GPCRs represent ~12% of all protein targets for approved therapeutics (rising to ~17% when including upstream or downstream GPCR-related proteins). These therapeutics are primarily small molecules and peptides. Additionally, ~100 of the ~360 non-sensory human endo-GPCRs remain orphan receptors without known physiologic agonists.
Why it matters
This review resolves discrepancies across pharmacology databases to establish a definitive baseline showing that GPCRs constitute the largest single family of therapeutic drug targets.
Limits
The analysis relies on the accuracy, curation definitions, and cross-referencing of existing databases up to November 2017. Clinical efficacy, target selectivity profiles, and adverse drug mechanisms were not evaluated within this aggregate target mapping.
Cited by
- supports Approximately 35% of all FDA-approved drugs (around 700 drugs) interact with G-protein coupled receptors (GPCRs).