Enzyme-linked receptors are a group of multi-subunit transmembrane proteins that contain either intrinsic enzyme activity on their intracellular domain or associate directly with an intracellular enzyme. Upon ligand binding a conformational change is transmitted via a transmembrane helix which activates the enzyme, initiating signaling cascades.
Products for Enzyme-Linked Receptors
There are five main types of enzyme-linked receptors:
- Receptor Tyrosine Kinase (RTK): Contains intrinsic tyrosine kinase activity (EGFR, VEGFR)
- Receptor Serine/Threonine Kinase: Contains intrinsic serine/threonine kinase activity (TGF-βR)
- Receptor Guanylyl Cyclases: Contain intrinsic cyclase activity (ANP)
- Tyrosine-Kinase Associated Receptors: Receptors that associate with proteins that have tyrosine kinase activity (Cytokine Receptors)
- Receptor Tyrosine Phosphatases
Physiology and Disease
Enzyme-linked receptors are the receptors for many growth factors, cytokines and hormones and have a major role in regulation of cell growth, proliferation and differentiation. Mutations in receptor tyrosine kinases are responsible for a wide array of diseases, including cancers, neurodegeneration, achondroplasia and atherosclerosis.
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Potent, selective LRRK2 inhibitor
Tocris is the first to launch GSK2578215A, licensed from GlaxoSmithKline, for the study of Parkinson's Disease.