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GPCR Profiling Services with 48-targets Safety Panel

GPCRs are the most abundant superfamily of cell surface transmembrane receptors and are widely used as targets in drug discovery. GPCR drugs are used extensively in medicine, especially in the domains of neurology, cardiology, and inflammation. There are now fewer GPCR medicines used in oncology, but this will change as additional immune cell-targeting medications, recently identified ADCs, and new disease correlations are found.

Success in the screening cascade depends on selecting the best cell system for the type of assay and tier. A suitable recombinant or endogenous GPCR cell model is necessary to advance into in vivo translational investigations and mechanistic receptor-ligand interactions. The incidence of undesired false positives will be lower with proximal readouts since there will be fewer potential off-targets in between. Post-receptor signal amplification boosts the signal-to-noise ratio of distal signals but also raises the risk of false positives. Overall, the likelihood of compound development is increased by using a properly chosen suite of tests to discover hits, followed by confirmation in orthogonal assays. Creative Biolabs can provide GPCR profiling services with 48-targets safety panel for different therapeutic areas. Our 48 safety panels are all high disease-gene.

Therapeutic Areas in Creative Biolabs' 48-targets Safety Panel

  • Metabolism Panel

GPCRs govern almost all metabolic processes, such as the synthesis and absorption of glucose, the action and release of insulin, and the differentiation and proliferation of many cell types. The relationship between several endogenous ligands, such as free fatty acids and their receptors, and the control of insulin secretion, insulin sensitization, β-cell enlargement, and glucose homeostasis has been well investigated. Type 2 diabetes (T2D) can be treated by pharmacologically targeting GPCRs and their signaling pathways in order to increase insulin sensitivity. Consequently, GPCRs have gained popularity as drug targets for metabolic diseases like type 2 diabetes and obesity. Creative Biolabs provides metabolism panels with 48 GPCR targets.

ADRA1A BRS3 CHRM2 EDNRB GLP1R LHCGR NPY2R S1PR2
ADRB1 CALCR CHRM3 FFAR1 GIPR MC1R NPY5R SSTR1
ADRB2 CASR CNR1 FSHR GNRHR MC2R OPRM1 SSTR2
ADRB3 CCR5 CXCR4 GCGR HTR2A MC4R PTH1R TACR3
AGTR1 CCKAR DRD2 GHRHR HTR2C MTNR1B PTGER4 TRHR
AVPR2 CCKBR EDNRA GHSR KISS1R NPY1R PROKR2 TSHR
  • Psychiatry Panel

Different synaptic transmission modalities are used by the two groups of receptors. Ionotropic receptors consist of the ligand-gated ion channels that result in fast synaptic transmission. The metabotropic receptors are composed of GPCRs. GPCRs bind to neurotransmitters and activate the genes necessary for antipsychotic action, which causes intracellular signaling pathways to delay synaptic transmission. It has been demonstrated that GPCRs significantly contribute to the reduction of schizophrenia symptoms. Many GPCRs, including the dopamine D2 receptor, are antagonistically affected by both traditional and non-conventional antipsychotics. So, we also provide psychiatry panels with 48 GPCR targets.

ADORA2A AVPR1A CHRM4 DRD2 GABBR2 HRH2 HTR5A OPRD1
ADRA2A CCKAR CHRM5 DRD3 GRM2 HRH3 HTR6 OPRK1
ADRA2B CCKBR CNR1 DRD4 GRM8 HTR1A HTR7 OPRM1
ADRB1 CHRM1 CRHR1 DRD5 GRPR HTR1B NPY1R OPRL1
ADRB2 CHRM2 CRHR2 EDNRA HCRTR1 HTR2A NPY2R OXTR
ADCYAP1R1 CHRM3 DRD1 GABBR1 HRH1 HTR2C NTSR1 TACR1

We also provide other therapeutic area panels, including Immunology Panel, Oncology Panel, Hematology Panel, Neurology Panel, Ophthalmology Panel, Cardiology Panel, Respiratory Panel, Gastrointestinal Panel, Dermatology Panel, Musculoskeletal Panel, Reproduction Panel and so on. Please contact us for more information.

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.
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