TABLE 2

GPCR-related proteins/genes that are targets for approved drugs

Examples of Proteins/Genes That Are Drug TargetsExamples of Drugs That Target These Proteins/Genes
Protein/gene category: enzymes involved in agonist synthesis
 Prostaglandin I2 synthaseEpoprostenol
 Angiotensin I converting enzymesLisinopril
 Dopamine beta-hydroxylaseHydralazine
 Coagulation factors (e.g., factor 10)Rivaroxaban
Protein/gene category: enzymes involved in agonist degradation
 Monoamine oxidases A and BPhenelzine
 Catechol O-methyltransferaseEntacapone
 AcetylcholinesteraseNeostigmine
 Adenosine deaminasePentostatin
 Dipeptidyl peptidase-4Sitagliptin
Protein/gene category: transporters of GPCR agonists
 Serotonin transportersCitalopram
 Dopamine transporters (SLC6A3)Modafinil
 ATP transporters (SLC25A4)Clodronic acid
Protein/gene category: GPCR ligands
 C-C motif chemokine ligand 2Mimosine
 Coagulation factor II, thrombinArgatroban
Protein/gene category: regulators of second messenger signaling
 PDEs
 PDE1A-CVinpocetine
 PDE4A-DRoflumilast
 Rho Kinases (ROCK1-2)Fasudil