Figure Legends:
Figure 1: FDA approved compounds and compounds in clinical trial
targeting GPCRs. (A) 106 (31.64%) de-orphaned GPCRs currently have an
FDA approved compound to target them, compared to only 1 (1.14%) oGPCR
(left). Further, there are currently 57 (17.01%) de-orphaned GPCRs that
have a drug in ongoing clinical trials, compared to only 2 (2.27%)
drugs targeting oGPCR (right). (B) Of the total number of FDA
approved drugs targeting de-orphaned GPCRs, 130 (27.08%) are for CNS
indications, whilst there are no approved drugs targeting oGPCRs for CNS
indications. Further, 27 (35.53%) of the de-orphaned GPCRs currently
being targeted in ongoing clinical trials are for CNS indications,
whilst no oGPCRs are currently being targeted in ongoing clinical trials
for CNS indications.
Figure 2: Orphan neuropeptide and receptor expression in key
brain regions implicated in alcohol use disorder, colour-coded
according to the three key phases of the addiction cycle
(binge/intoxication, withdrawal/negative affect,
preoccupation/anticipation). Amyg., amygdala; CART, cocaine- and
amphetamine-regulated transcript; Hab., habenula; Hipp., hippocampus;
Hypo., hypothalamus; PFC, prefrontal cortex; VTA, ventral tegmental
area.