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.
|Nicotinic cholinergic receptors|
|Anthrax toxin receptor|
|Nuclear receptor coactivator|
|Hepatitis A virus cellular receptor|
|Aryl hydrocarbon receptor|
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.