Other Receptors as Drug Targets

Other Receptors as Drug Target Background

Receptors are proteins that binding of a ligand to a receptor changes its shape or activity, allowing it to transmit a signal or directly produce a change inside of the cell. Receptors consist of 45% in drug targets.

Adenosine signalling has long been a therapeutic target for drug development, with adenosine itself or its derivatives being used clinically since the 1940s.

In addition, methylxanthines such as caffeine have profound biological effects as antagonists at adenosine receptors. Moreover, drugs such as dipyridamole and methotrexate act by enhancing the activation of adenosine receptors.

Evidence has shown that adenosine has a functional role in many diseases, and several pharmacological compounds specifically targeting individual adenosine receptors — either directly or indirectly — are now under the clinic.

Other Receptors as Drug Target List

Category Drug target
Nicotinic cholinergic receptors
CHRNA3 CHRNA5 CHRNA7 CHRNB3
CHRNG      
GABA receptors
GABRA1 GABRA3 GABRA4 GABRB1
GABRB2 GABRB3 GABRD GABRE
GABRG1 GABRP GABRR1 GABRR2
GABRQ      
Glutamate receptors
GRIA1 GRIA2 GRIA3 GRID2
GRIK2      
Glycine receptor
GLRA2 GLRA3 GLRB  
Purinergic receptor
P2RX1 P2RX2    
Scavenger receptor
SCARA5 SCARB1 SCARB2 MSR1
LDL receptor
LDLR LRP1 LRP5 LRP6
LRP8 VLDLR LRPAP1 LDLRAD4
Anthrax toxin receptor
ANTXR1 ANTXR2    
TNF receptor-associated
TRAF6 TRAF7 TRAP1 TRAF3
Nuclear receptor coactivator
NCOA1 NCOA3    
Hepatitis A virus cellular receptor
HAVCR1 HAVCR2    
Aryl hydrocarbon receptor
AHR AIPL1 ARNTL  

References

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

2. Rudolph U, et al. GABA A receptor subtypes: dissecting their pharmacological functions[J]. Trends in pharmacological sciences, 2001, 22(4): 188-194.