Label-Free Biosensors for Cell Biology

Table 1

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

Receptors	Cells	Biosensors	Key findings	Ref
PAR2; Bradykinin B2	A431	DMR	Biosensor signal is originated from DMR	[8]
Adenosine A2B	A431	DMR	Similarity analysis segregates ligands into clusters	[38]
Bradykinin B2
β2-adrenergic
EP4			DMR signatures of distinct classes of GPCRs	[92]
H1
LPA receptors
P2Y1			Integrative roles of adenylyl cyclases in GPCRs	[93]
PAR1
PAR2
S1P receptors
VPAC1
P2Y1/2/11	HEK293	DMR	ECM coatings impact receptor signaling	[59]
LPA receptors	Porcine brain endothelial cells	ECIS	LPA increases tight junction permeability	[62]
PAR1	Primary endothelial cells	ECIS	Thrombin promotes the formation of intercellular gaps	[64]
PAR1	HMEC-1	ECIS	Functional selectivity of PAR1 agonists	[65]
Bradykinin B2	A431	DMR	Systems cell biology of B2 receptor	[86]
PAR1	A431	DMR	HTS compatibility test	[87]
Endogenous receptors	HeLa; U-937; U2OS; TE671	CDS	Receptor panning	[88]; [89]
LPA receptors; S1P receptors	Rabit corneal epithelial cell; Rabit corneal endothelial cells	ECIS	The role of Gi signaling in cell monolayer permeability	[90]
Histamine H1	CHO-H1	RT-CES	Impedance signals were correlated with morphological changes	[91]
Vasopressin V1a	1321-N1-V1a
5-HT1A	CHO-5HT1A
D1	CHO-D1
PAR1; PAR2	A431	DMR	Receptor cross-desensitization	[94]
Dopamine D2S	CHO-D2S	CDS	Ligand pharmacology characterization	[95]
Muscarinic M4	CHO-M4
Dopamine D5	CHO-D5	CDS	Ligand-directed functional selectivity; GPCR pleiotropic signaling	[96]
Muscarinic M1	CHO-M1
Melanocortin MC4	CHO-MC4
	HEK-MC4
Cannabinoid CB1	CHO-CB1
Cannabinoid CB2	CHO-CB2
Histamine H1; β2-AR	A431	DMR	Duplexed receptor assays for HT screening	[97]