Label-Free Biosensors for Cell Biology

Table 2

Receptors, cell lines, and technologies and key points of the studies related to the use of label-free cellular assays for GPCRs.

Receptors	Cells	Biosensor	Key findings	Ref
Dopamine D3; Muscarinic M1	CHO-D3; CHO-M1	DMR	Ligand pharmacology characterization	[98]
β2-AR	A431	DMR	Systems cell biology of the β2AR	[99]
			Ligand-directed functional selectivity	[100]
			Ligand-directed desensitization	[101]
PACAP1	TM3	RT-CES	PACAP agonists suppress the proliferation of immature mouse Leydig cell line TM3	[102]
CXCR2	NIH-3T3-CXCR2	ECIS	The role of CXCR2 in cell transformation	[103]
Muscarinic M2	CHO-M2	DMR	Novel dualsteric M2 agonists	[104]
				[105]
Muscarinic M1	CHO-M1	DMR	HT screening identified novel M1 ligands	[106]
GPR40/FFA1	1321N1-GPR40; HEK-GPR43; HEK-GPR41; HEK-GPR40	DMR	Discovery of potent and selective agonists for FFA receptors	[107]
GPR41/FFA3				[108]
GPR43/FFA2				[109]
Endogenous muscarinic receptor	HEK-293	DMR	GPCR activation modulates Slack ion channel activity	[110]
Cannabinoid CB2	CHO-CB2	RT- CES	Ligand pharmacology characterization	[111]
mGluR1	CHO-mGluR1
Prostaglandin EP2	C6G-EP2; HCT15-EP2	DMR	Compound nanoparticles act as allosteric potentiators	[112]
mGluR7	HEK-mGluR7	DMR	Negative allosteric modulators	[113]
GPR55	HEK-GPR55	DMR	GPR55 pleiotropic signaling	[114]
Muscarinic M2	CHO-M2	DMR	Pathway deconvolution; GPCR pleiotropic signaling; Novel pathways for M3	[115]
β2-AR	CHO-β2AR
Muscarinic M3	CHO-M3
GPR55	HEK-GPR55
CRTH2	HEK-CRTH2
EP2/3	HEK-EP2/3
GPR40	HEK-GPR40
EP receptors	HaCaT
EP receptors	Keratinocytes
Muscarinic M1	CHO-M1	CDS; BIND; DMR	Label-free reader comparison	[116]
Muscarinic M2	CHO-M2
CRF	CHO-CRF
MC4R	CHO-MC4R
CRTH2	HEK-CRTH2	DMR	Novel function of CRTH2 C-terminal	[117]
Mu opioid	CHO-MOR	DMR	Pathway deconvolution	[118]
Cannabinoid CB1	CHO-CB1
Cannabinoid CB2	CHO-CB2
Delta opioid	CHO-DOR
PAR1	A549	DMR	Ligand-directed functional selectivity on receptor trafficking	[119]
GPR35	HT29	DMR	Discovery of tyrphostins as GPR35 agonists	[120]