Receptors are widely involved in various pathways such as signal transduction, immune response and function regulation in organisms, and are the most important drug targets. CD BioSciences provides comprehensive receptor-targeted peptidomimetic development services to assist global customers in basic research and drug discovery.
Overview of Receptors
Receptors are components of cell membranes or cells that can recognize and bind biologically active molecules. They can correctly amplify the recognized and received signal and transmit it into the cell, resulting in a biological effect. Receptors play important roles in signal transduction, Immunotherapy, and immune responses. Therefore, receptors are often the first choice for drug targets. Currently, more than 50% of drugs on the market target receptors.
Classification of Receptors
Most of the receptors are cell surface receptors and can be divided into three categories according to structure and function:
- G Protein-Coupled Receptors
GPCRs are an important superfamily of transmembrane proteins located on the cell membrane, and ligands that bind and activate these receptors include: light-sensitive compounds, odorants, pheromones, hormones, and neurotransmitters. Due to their involvement in the regulation of most physiological functions, there are currently approximately 370 GPCRs that offer opportunities for drug targeting, and approximately 34% of drugs on the market target G protein-coupled receptors.
Fig. 1 Asymmetry of receptor subunits in dimeric GPCRs. (Zylbergold P & Hébert Terence E, 2009)
- Ion Channel-Linked Receptors
Ion channels connect receptor-bound ligands and open the channel through the membrane, allowing specific ions to pass through. To form channels, this type of cell surface receptor has an extensive transmembrane region. When ligands bind to the extracellular region of the channel, the protein structure undergoes a conformational change that allows ions such as Sodium, Calcium, Magnesium and Hydrogen to pass through.
Fig. 2 Calcium signal transduction. (Clapham D E, et al., 2001)
- Enzyme-Linked Receptors
Enzyme-linked receptors are transmembrane receptors whose ligand-binding domains are located on the outer surface of the plasma membrane. When a ligand binds to the extracellular domain, a signal is transmitted across the membrane, which activates an enzyme, and the activation of the enzyme triggers a series of events within the cell that ultimately lead to various reactions. It is also called catalytic receptor and is often used as a target of many drugs, such as receptor tyrosine kinase (RTK), receptor serine/threonine kinase (RSTK), toll-like receptor (TLR), etc.
Fig. 3 Toll-like receptor signal transduction. (Barton G M & Kagan J C, 2009)
Our Services
CD BioSciences offers a wide range of peptidomimetic development services targeting GPCRs receptors, ion channel receptors, enzyme-linked receptors and other related targeting receptors.
Using our PepDomTM to build a larger-capacity peptidomimetic library and perform high-throughput screening can help customers achieve their goals in a shorter time. In addition, other non-limiting choices based on the specific needs of customers can obtain peptidomimetics with higher stability and longer in vivo half-life as drug lead compounds.
Advantages of Our Peptidomimetics
Features of Our Service
We are committed to providing customers with comprehensive services, and customer first is our philosophy.
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CD BioSciences also focuses on the development of peptidomimetics for other receptor targets other than the above-mentioned receptor targets. As long as you are interested, you can contact us for our professional advice and solutions.
References
- Zylbergold, P., Hébert, Terence E. (2009). A division of labor: asymmetric roles for gpcr subunits in receptor dimers. Nature Chemical Biology, 5(9), 608.
- Clapham, D. E., Runnels, L, W., & Strübing, C. (2001). The TRP ion channel family. Nature Reviews Neuroscience, 2(6):387-96.
- Barton, G. M., & Kagan, J. C. (2009). A cell biological view of toll-like receptor function: regulation through compartmentalization. Nature Reviews Immunology, 9(8), 535-542.
All of our services are intended for preclinical research use only and cannot be used to diagnose, treat or manage patients.
