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Receptors refer to any biological macromolecule located on the cell surface or within the cells that can act as recognition sites for endogenous hormones, neurotransmitters, neuromodulators or intracellular signaling molecules and cause changes in cell function. Receptors are defined in pharmacological terms as having specific interactions with ligands belonging to a given pharmacological class. Receptors can be defined by the selectivity, the saturability and reversibility of ligand binding, and functionality. The binding of receptors to ligands can induce cell growth, division and death; control membrane channels or regulate cell binding to modify cellular activity and regulate responses. Receptors play an important role in regulating responses to the cellular/tissue microenvironment at the biophysical, biochemical, and/or genomic level. They are useful drug targets in various disease states such as genetic diseases.
Figure 1. Disease associations for all 398 non-olfactory GPCRs. (Hauser, A. S., et al., 2017)
Creative Biolabs provides a comprehensive target validation services to help confirm various types of receptors as therapeutic targets of drug discovery process thus to deal with data reproducibility crisis which is a big obstacle for drug research and development and may lead to failure and high risk of investment.
Creative Biolabs provides a comprehensive list of assays on multiple high-quality platforms to characterize the features of different receptors as your drug targets to advance your drug discovery. With experienced experts and cutting-edge technologies, we can provide high-quality and reliable target validation services in a time-saving and cost-efficient manner. We offer professional target validation services for the following types of receptors.
G Protein-Coupled Receptors (GPCRs)
G protein-coupled receptors (GPCRs), also known as seven-(pass)-transmembrane domain receptors, are the largest class of membrane proteins in the human genome and have now been the largest category of drug targets due to their central role in physiology and disease. GPCRs can detect molecules outside the cells, activate internal signal transduction pathways and cellular responses. They involve a wide range of physiological processes, such as visual sense, gustatory sense, sense of smell, regulation of immune system activity and inflammation, as well as autonomic nervous system transmission. Because of their important functions, GPCRs have important role in multiple diseases, including cardiovascular diseases, autoimmune diseases, inflammation, cancer, and neurological disorders.
Nuclear Receptors (NRs)
Nuclear receptors (NRs), a large superfamily within cells, are ligand-activated transcription factors that regulate the activation of a wide range of important target genes. They are responsible for sensing thyroid hormones, steroid hormone, vitamin D, fatty acid, sterol oxide and certain other molecules. Nuclear receptors have two subtypes, steroid and non-steroid. When a ligand is present, activated nuclear receptors can directly bind to DNA and regulate the expression of specific genes to control the metabolism and development of organisms. The unique characteristic of nuclear receptors is to serve as on-off switches for genes that regulate cell proliferation, differentiation, and metabolism. Therefore, they can be therapeutic targets of various diseases such as cancer, inflammation, cardiovascular diseases, diabetes, rheumatoid arthritis and asthma.
Enzyme-Linked Receptors
Enzyme-linked receptors, also known as catalytic receptors, are transmembrane receptors possessing both enzymatic catalytic and receptor functions. They have an extra-cellular ligand binding domain which is on the outer surface of the plasma membrane and an intracellular domain which has a catalytic function. The binding of an extracellular ligand can cause enzymatic activity on the intracellular side. Enzyme-linked receptors include a great many drug targets such as receptor tyrosine kinases (RTKs), receptors serine/threonine kinases (RSTKs) and receptor protein tyrosine phosphatases (RPTPs).
Creative Biolabs has a dedicated assay development team that will work closely with you to design customized assays for your specific drug target. Our service will meet your specific needs fast at extremely competitive prices. If you need more information, please feel free to contact us at anytime. We look forward to working with you and helping your drug research and development project succeed.