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Receptors & Sensors
Signaling pathways link extracellular cues to cellular responses, so that cells are able to adapt to the changes in the environment. The signals are processed as a series of molecular events in cells. Proteins responsible for detecting the signal are termed receptors or sensors, which are the first nodes in signaling transduction pathways.
How the receptors receive the signals and initiate the signaling transduction processes is under intensive research, especially ACE2, the entry point for coronaviruses (e.g., HCoV-NL63, SARS-CoV and SARS-CoV-2). CD BioSciences offers a complete portfolio of solutions for uncovering the mystery of receptors and sensors including identification and characterization of receptors and generation agonists and antagonists for receptors.
Introduction of Receptors/Sensors
A signaling pathway is initiated with the binding of a ligand to a receptor, which gives rise to a biochemical cascade. Generally, there are two major classes of receptors: intracellular and extracellular receptors.
Extracellular Receptors are usually transmembrane proteins, which sense signal cues outside the cells and transduce the signals to intercellular pathways. These cell surface receptors are classified by protein structure and ligand characteristics.
- G-protein-coupled Receptors (GPCRs)
Examples：β2-adrenergic receptor (β2AR), Metabotropic glutamate (mGlu) receptors.
GPCRs are the largest family of membrane receptors with nearly 1,000 presented in the human genome. They are found only in eukaryotes (e.g. yeast, plants and animals), and can be activated by neurotransmitters, hormones, pheromones, odors, etc. Being involved in diseases such as cancers, immunological disorders, metabolic disorders, cardiovascular diseases, and mental illnesses, GPCRs are important drug targets and are estimated to be targets of 50% of drugs currently on the market.
- Receptor tyrosine kinases (RTKs)
Examples： EGF receptors (ErbB), Insulin receptors, FGF receptors.
RTKs are transmembrane receptors, with 58 tyrosine kinase receptor encoding genes identified in the human genome. They have a high affinity for growth factors (e.g., insulin), cytokines and hormones. RTKs are key regulators of normal cellular processes and also play critical roles in the development and progression of cancers. As they are involved in abnormalities like cancer, degenerative diseases and cardiovascular diseases，they are hot targets of drug discovery and development.
- Toll-like receptors (TLRs)
Examples：TRL1-13.
TLRs are a class of pattern recognition receptors (PRRs) that initiate innate immune response by recognizing conserved molecular patterns associated with pathogens. As the first responders to infectious and inflammatory signals, TRLs are under intensive study to discover treatments for various infectious and autoimmune diseases as well as cancers.
- Ligand-gated Ion Channels
Examples：Nicotinic acetylcholine receptors (nAChRs), Zinc-activated ion channel (ZAC).
Ligand-gated Ion Channels, also referred to as ionotropic receptors, are a large group of allosteric transmembrane receptors that mediate rapid electrochemical signal (e.g. Na⁺, K⁺, Ca²⁺, Cl⁻) transduction after being activated by specific chemical ligands (e.g. neurotransmitter). They are different from voltage-gated ion channels, which are sensitive to membrane potentials, and GPCRs, which use second messengers. Ligand-gated ion channels are likely affected by anaesthetic agents and ethanol. Understanding the mechanism of those receptors and exploring the chemical/biological/physical component is of great importance for medical purposes.
Intracellular Receptors are located inside the cells as free soluble components, typically in the cytoplasm or nucleus. They sense intracellular ligands such as steroids hormones (e.g., testosterone and progesterone), metabolites (e.g., amino acids and glucose). Intracellular receptors not only function as sensors of steroids, hormones and nutrients, but also mediate crosstalk between signaling pathways.
- Nuclear Hormone Receptors or Nuclear Receptors (NHRs or NRs)
Examples：PPARs (PPARα, PPARγ, PPARδ), LXRα/β, FXR, HNF4α
NHRs are an important family of ligand-sensing transcription factors which sense steroid hormones, retinoic acid, oxysterols, and thyroid hormones, and regulate expressions of genes involved in physiological functions such as homeostasis, reproduction, development, and metabolism. Since NHRs control metabolic homeostasis, particular attention has been focused on them to find therapeutics for metabolic diseases such as cholestasis, type 2 diabetes and cardiovascular diseases.
- Cytoplasmic Receptors
Examples：NOD-like receptors (NLRs), IP3 receptor, Nutrient Sensors
Cytoplasmic receptors are mainly receptors for immune system (e.g., NLRs) and intracellular nutrient sensors (e.g., amino acid sensor SESN2 in mTORC1 pathway). As they are certainly indispensable for immune response and metabolic homeostasis, many immunological diseases and metabolism diseases are associated with them, and therapeutics have been developed or are under development to target them.
Solutions for Receptors/Sensors
CD BioSciences is dedicated to providing personalized solutions for you to study your receptors or signaling pathways of interest.
Receptor/Sensor Identification
- Identifying potential receptors for your ligands of interest.
- Verifying the direct interaction between them.
- Determining the thermodynamic parameters of the interactions.
Receptor Deorphanization
- Identifying potential ligands bind to your receptors of interest.
- Verifying the direct interaction between them.
- Determining the thermodynamic parameters of the interactions.
Structure Analysis
- Analyzing the structures of your receptors before and/or after ligand binding.
- Determining the ligand binding pocket and related features of your receptors.
Compound Screening
- Discovering agonists and/or antagonists for your receptors.
- Determining the thermodynamic parameters of the interactions.
Features
CD BioSciences offers cost-effect, high quality and hassle-free receptors and sensors related solutions to our clients worldwide. We guarantee to deliver our products and results on time. Please feel free to contact us.
For research use only. Not intended for any clinical use.