GPCR Drug Discovery Services
As a pioneer and the undisputed global leader in membrane protein drug discovery, Creative Biolabs is proud to offer our clients a series of GPCR drug discovery services with the best quality and most competitive price. Here, we are happy to introduce our professional service of GPCR drug discovery with our diverse technologies.
G protein-coupled receptors (GPCRs) represent the largest and most important membrane protein family encoded by the human genome. Their endogenous ligands vary from photons, amines, carbohydrates, lipids, peptides to proteins. These receptors have been implicated in a large number of diseases, such as inflammatory disorders, cardiac disorders, and cancer, and serve as increasingly attractive drug targets. The GPCR family is divided into classes A (rhodopsin), classes B (secretin and adhesion), classes C (glutamate), and classes F (Frizzled) subfamilies.
Fig.1 Phylogenetic tree of GPCRs as drug targets. (Yang, et
al., 2021)
GPCR Cell-based Drug Screening In Vitro Assay Development Services
Creative Biolabs offers one-stop services from GPCR cell lines development to drug discovery in vitro assay.
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GPCR Antibody Discovery and Development Services
Creative Biolabs is specialized in GPCR antibody discovery with our reliable, fast methodologies and diverse technologies.
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GPCR Profiling Services with Various Panels
Creative Biolabs offers various panels include different GPCR targets to decrease wasted time on investigating suboptimal leads.
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GPCR Biosensors Screening Services
Creative Biolabs offers GPCR biosensors screening services to learn the signal pathway of different GPCRs.
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GPCR Ligands Screening Services
Creative Biolabs offers GPCR ligands screening services to satisfy various client needs.
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GPCR Small-molecule Drug Discovery Services
Creative Biolabs offers GPCR small-molecule drug discovery services to uncover and utilize more effective pharmacological mechanisms.
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GPCR Biologics Drug Discovery Services
Creative Biolabs offers GPCR biologics drug discovery services to help the development of GPCR biologics for therapeutic use.
Learn MoreGPCR Cell-based Drug Screening In Vitro Assay Development Services
GPCR cell-based drug screening in vitro assay development services rely on changes in the intracellular concentration of secondary messengers upon ligand binding, such as cAMP, IP3, Ca2+, β-arrestin, etc. These changes result from the activation of one or more G proteins. From GPCR cell line development to drug discovery in vitro assay, Creative Biolabs is a one-stop shop for GPCR drug screening.
Fig.2 Diagrammatic representation of how G protein inhibition can bias GPCR signaling.
(Campbell & Smrcka, 2018)
GPCR Antibody Discovery and Development Services
As a pioneer and the undisputed global leader in antibody discovery, Creative Biolabs is specialized in membrane protein antibody discovery with our reliable, fast methodologies and diverse technologies. Our membrane protein antibody discovery process includes target selection and antigen preparation, assay development, hit generation, lead selection, lead optimization and characterization, candidate selection, and antibodies application.
Fig.3 Schematic representation of different antibody discovery strategies. (Laustsen, et
al., 2021)
GPCR Profiling Services with Various Panels
Creative Biolabs offers various panels including different GPCR targets to decrease wasted time on investigating suboptimal leads. Functional assays are used in Creative Biolabs' panels to circumvent the limits of binding assays for allosteric or non-functional binders, as well as to eliminate binding false positives.
GPCR Biosensors Screening Services
Creative Biolabs offers GPCR biosensors screening services to obtain a high spatiotemporal resolution in elucidating the molecular mechanisms of GPCR activation. Our objective is to enhance GPCR drug development by exploring the pluridimensionality of GPCR signal transduction.
GPCR Ligand Screening Services
Creative Biolabs offers GPCR ligand screening services using a variety of experimental methodologies, including binding-based ligand screening and stability-based ligand screening. The overall rates of false-positive and false-negative outcomes would decrease with the combined application of complimentary approaches.
GPCR Small-molecule Drug Discovery Services
Small-molecule ligands stabilize distinct receptor conformations with differing degrees of efficacy, which contributes to ligands' functional selectivity. GPCR small-molecule drug development services are provided by Creative Biolabs, which can model both the structural model of the receptor and the small-molecule-binding site inside it.
GPCR Biologics Drug Discovery Services
With small-molecule drugs, it is impossible to achieve some unique properties of biologics. Creative Biolabs offers a service called GPCR biologics, which has the ability to produce peptides, antibodies, and antibody fragments with desired drug-like properties.
Please contact us for more details about our GPCR drug discovery services. Our experts will help design an optimal solution for your project and trouble-shoot for you throughout the whole process.
Please contact us for more details about our GPCR drug discovery services. Our experts will help design an optimal solution for your project and troubleshoot for you throughout the whole process.
References
- Yang, D.; et al. G protein-coupled receptors: structure- and function-based drug discovery. Sig Transduct Target Ther. 2021; 6 (7).
- Campbell, AP.; Smrcka, AV. Targeting G protein-coupled receptor signaling by blocking G proteins. Nature Reviews Drug Discovery. 2018;17(11): 789.
- Laustsen, A.H.; et al. Animal immunization, in vitro display technologies, and machine learning for antibody discovery. Trends in Biotechnology. 2021; 39(12): 1263-1273.
- Yang, D., et al. G protein-coupled receptors: structure- and function-based drug discovery. Sig Transduct Target Ther. 2021; 6 (7).
