GPCR Biosensors Screening Services

Creative Biolabs has developed a series of GPCR biosensor approaches that allow real-time monitoring of GPCR activation in living cells, which is necessary to gain a high spatiotemporal resolution in understanding the molecular underpinnings of GPCR activation. We offer screening services for GPCR biosensors to satisfy all of your needs. To enhance GPCR drug discovery, we aim to explore the pluridimensionality of GPCR signal transduction.

The Types of GPCR Biosensors in Creative Biolabs

G protein activation biosensors and β-arrestins

Heterotrimeric G proteins bind to the GPCR to initiate the GPCR signaling cascade. When a receptor is activated, a Gα-bound GDP is exchanged for GTP, which causes the heterotrimeric G protein to reorganize conformationally and encourage the separation of the Gα and Gβ/γ subunits. G proteins are categorized into families according to the signaling consequences that arise from the Gα subunit's activation. Fourteen unique heterotrimeric G proteins biosensors and two β-arrestins biosensors are available, namely the Gs family (Gαs, Gαolf), the Gi family (Gαi1, Gαi2, Gαi3, GαoA, GαoB and Gαz), Gq family (Gαq, Gα11, Gα14 and Gα15), G12/13 family (Gα12 and Gα13) and β-arrestins 1 and 2.

G proteins and β-arrestins can bind to the GPCRs. (Kim, et al, 2022) Fig.1 The GPCRs induce the recruitment of G proteins and β-arrestins.¹

Second messenger biosensors

Cyclic adenosine monophosphate (cAMP), and Ca²⁺ are important second messengers that modulate several downstream destinations and increase the signal. The primary way that G protein coupled receptors (GPCRs) associated with Gαs or Gαi/o family members carry out their biological activities is by regulating the generation of cAMP, or second messenger. Ca²⁺ and phospholipase C-β (PLCβ) form the Gαq/11 pathway. For GPCR biosensor screening services, we can provide second messenger biosensors such as cAMP, DAG, and PIP3 biosensors.

Downstream effector proteins biosensors

RhoA cycle between an inactive GDP-bound state and an active GTP-bound state, just as heterotrimeric G proteins. It has been demonstrated that RhoA is a significant proximal downstream effector of several GPCRs connected to Gα12/13. Our RhoA biosensor can detect ligand-induced activation of RhoA at the plasma membrane.

Our GPCR biosensor screening services can be applied to the screening of drug candidates that target GPCRs as well as the precise molecular mechanisms of GPCR activation and function. The fluorescence signals of GPCR biosensors in living cells can be quantified in order to screen and choose the most effective agonists. The GPCR biosensors can access the functional kinetics of the agonist-induced GPCR activation for the chosen candidates. As a result, GPCR biosensors are effective instruments for screening and assessing potential medications that target GPCRs. Please contact us for more information.

Reference

Kim, et al.; "Genetically encoded fluorescent biosensors for GPCR research." Frontiers in Cell and Developmental Biology 10 (2022): 1007893.

Note: All of our products are for Research Use Only (RUO). NOT intended for diagnostic, therapeutic or clinical use. We DO NOT offer patients any direct products or services. No products from Creative Biolabs may be resold, modified for resale or used to manufacture commercial products without prior written approval from Creative Biolabs.