G protein-coupled receptors

G protein-coupled receptors (GPCRs) represent the largest family of membrane proteins. Their principal role involves translating a diverse range of external cues—such as biogenic amines, peptides, hormones, neurotransmitters, ions, odorants, and photons—into intracellular signals. These signals govern numerous physiological functions, including cellular metabolism, differentiation, growth, neurotransmission, and sensory perception. GPCRs are also implicated in numerous diseases, including type 2 diabetes mellitus (T2DM), obesity, depression, cancer, Alzheimer’s disease, among others. Consequently, GPCRs have emerged as a highly successful drug target class for addressing various medical conditions.

G-protein-coupled receptors (GPCRs) are known to play central roles in the physiology of many organisms. Members of this seven α-helical transmembrane protein family transduce the extracellular signals and regulate intracellular second messengers through coupling to heterotrimeric G-proteins, adenylate cyclase, cAMPs, and protein kinases. As a result of the critical function of GPCRs in cell physiology and biochemistry, they not only play important roles in cell biology and the medicines used to treat a wide range of human diseases
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The common molecular structure of GPCRs consists of seven transmembrane alpha helices, and these domains divide the receptor into extracellular N-terminus, intracellular C-terminus, three extracellular loops and three intracellular loops. The extracellular ring contains two highly conserved cysteine residues, which can stabilize the spatial structure of the receptor by forming disulfide bonds. There is a G-protein binding site on the intracellular loop.

The common molecular structure of GPCRs consists of seven transmembrane alpha helices, and these domains divide the receptor into extracellular N-terminus, intracellular C-terminus, three extracellular loops and three intracellular loops.
The extracellular ring contains two highly conserved cysteine residues, which can stabilize the spatial structure of the receptor by forming disulfide bonds. There is a G-protein binding site on the intracellular loop. In the case of CCR5.

Targeted GPCRs drug information under research (CLARIVATE Database)

Drug Name	Target	Organization	Highest Phase	Condition
Mogamulizumab	CCR4	Kyowa Hakko Kirin	Launched	Lymphoma Therapy
Eptinezumab	CGRPR	Alder Biopharmaceuticals	Launched	Acute Attacks of Migraine
Leronlimab	CCR5	Beth Israel Deaconess Medical Center	Pre-Registered	Anti-HIV Agents, Cancer
GMA102	GLP1R	Gmax Biopharm	Phase III	Type 2 Diabetes
Ulocuplumab	CXCR4	Bristol-Myers Squibb	Phase II	Small cell lung cancer, Pancreatic cancer, Multiple myeloma, Leukemia
Volagidemab	GCGR	Amgen	Phase II	Type 2 Diabetes,
Talquetamab	CD3, GPRC5D	Janssen	Phase II	Multiple Myeloma Therapy
Avdoralimab	C5AR	Novo Nordisk	Phase II	COVID-19, solid tumors
Nimacimab	CB1	Bird Rock Bio	Phase II	Diabetic Nephropathy
Sonepcizumab	S1PR1	Pfizer & Merck Serono	Phase II	Age-Related Macular Degeneration
BMS-986340	CCR8	Bristol-Myers Squibb	Phase I/II	Solid Tumor Treatments
MCLA-158	EGFR, LGR5	Merus	Phase I	Colorectal Cancer Therapy