Modern interest in muscarinic acetylcholine receptor (mAChR) activators for schizophrenia
began in the 1990s when xanomeline, an M 1/M 4-preferring mAChR agonist developed for …

This Perspective is the seventh in an annual series that summarizes successful Fragment-to-
Lead (F2L) case studies published in a given year. A tabulated summary of relevant articles …

The M4 muscarinic acetylcholine receptor (M4 mAChR) has emerged as a drug target of
high therapeutic interest due to its expression in regions of the brain involved in the …

Despite 50+ years of drug discovery, current antipsychotics have limited efficacy against
negative and cognitive symptoms of schizophrenia, and are ineffective—with the exception …

The lipid prostaglandin E2 (PGE2) mediates inflammatory pain by activating G protein-
coupled receptors, including the prostaglandin E2 receptor 4 (EP4R). Nonsteroidal anti …

Histamine receptors are a group of G protein-coupled receptors (GPCRs) that play important
roles in various physiological and pathophysiological conditions. Antihistamines that target …

G protein-coupled receptors (GPCRs) play critical roles in human physiology and are one of
the prime targets for marketed drugs. While traditional drug discovery programs have …

Type 2 bradykinin receptor (B2R) is an essential G protein-coupled receptor (GPCR) that
regulates the cardiovascular system as a vasodepressor. Dysfunction of B2R is also closely …

Alzheimer's disease (AD) remains a major cause of morbidity and mortality worldwide, and
despite extensive research, only a few drugs are available for management of the disease …

Biased G protein–coupled receptor (GPCR) ligands, which preferentially activate G protein
or β-arrestin signaling pathways, are leading to the development of drugs with superior …