Insulin Receptor

Protein tyrosine kinases (PTKs) are key signaling molecules and important drug targets. Two classes of PTKs are present in cells: the transmembrane receptor PTKs (RTKs) and the nonreceptor PTKs. The RTK family includes the receptors for insulin and for many growth factors, such as EGFR, FGFR, PDGFR, VEGFR, and NGFR. RTKs are transmembrane glycoproteins that are activated by the binding of their ligands, and they transduce the extracellular signal to the cytoplasm by phosphorylating tyrosine residues on the receptors themselves (autophosphorylation) and on downstream signaling proteins. Their principal functions of PTKs involve the regulation of multicellular aspects of the organism. Cell to cell signals concerning growth, differentiation, adhesion, motility, and death are frequently transmitted through tyrosine kinases. In humans, tyrosine kinases have been demonstrated to play significant roles in the development of many disease states, including diabetes and cancers.

MCE designs a unique collection of 1055 compounds that act as a useful tool for PTKs-related drug screening and disease research.

Diabetes mellitus, usually called diabetes, is a group of metabolic disorders characterized by a high blood sugar level over a prolonged period of time. The most common types are Type I and Type II. Type I diabetes (T1D), also called juvenile onset diabetes mellitus or insulin-dependent diabetes mellitus, is characterized by destruction of the β-cells of the pancreas and insulin is not produced, whereas type II diabetes (T2D), also called non-insulin-dependent diabetes mellitus, is characterized by a progressive impairment of insulin secretion and relative decreased sensitivity of target tissues to the action of this hormone. Type 2 diabetes accounts for the vast majority of all diabetes mellitus. Diabetes of all types can lead to complications in many parts of the body and can increase the overall risk of dying prematurely. Possible complications include kidney failure, leg amputation, vision loss and nerve damage.

The pathogenesis of diabetes is complicated, and development of the safe and effective drugs against diabetes is full of challenge. Increasing studies have confirmed that the pathogenesis of diabetes is related to various signaling pathways, such as insulin signaling pathway, AMPK pathway, PPAR regulation and chromatin modification pathways. These signaling pathways have thus become the major source of the promising novel drug targets to treat metabolic diseases and diabetes.

MCE Anti-diabetic Compound Library owns a unique collection of 740 compounds, which mainly target SGLT, PPAR, DPP-4, AMPK, Dipeptidyl Peptidase, Glucagon Receptor, etc. This library is a useful tool for discovery anti-diabetes drugs.