RTK

Many of the Axon Ligands™ in this class of compounds target receptors of various growth factors, such as EGF, VEGF, and PDGF. These receptors are members of the class of enzyme linked receptors, which, as integral membrane proteins, possess both receptor functionality (extra-cellular) as well as enzymatic catalytic functionality (intracellular)[1],[2]. The majority of the enzymatic activity of this class of receptors is characterized by kinase-like activity. Based on this feature, five main classes can be distinguished[3]: Receptor Tyrosine Kinases (RTKs), and Receptor Serine/Threonine Kinases (RSTKs, participating in MAPK and TGF-beta signaling pathways, among others) are well known. Additionally, there are classes of Receptor Guanylyl Cyclases, Histidine Kinase associated Receptors (receptors that associate with proteins that have histidine kinase activity), and finally a class of Tyrosine Kinase associated Receptors (e.g. Cytokine Receptors). In addition, some transmembrane tyrosine phosphatases (Receptor-like) Protein Tyrosine Phosphatases (PTPs)), which remove phosphate from phosphotyrosine side chains of specific proteins, are thought to function as receptors, although for the most part their ligands are unknown. Within each of these main classes, sub-classes exist, based on the specific endogenous ligands. Many of the enzyme linked receptors play a role in the regulation of cell proliferation, programmed cell death (apoptosis), cell differentiation, and embryonic development, and therefore are of great interest as targets for the treatment of cancer[4]. Furthermore, malfunctioning of receptors of this kind is associated with the development of neurodegenerative diseases, such as multiple sclerosis and Alzheimer's disease[5].


[1] Catalytic Receptors. S.P.H. Alexander, A. Mathie, and J.A. Peters. Br. J. Pharmacol. 2007, 150(S1): S122–S127. 
[2] Cell Signaling by Receptor Tyrosine Kinases. M.A. Lemmon, J. Schlessinger. Cell 2010, 141, 1117-1134.
[3] Molecular Biology of the Cell. 4th edition. Alberts B, Johnson A, Lewis J, et al.New York:Garland Science; 2002.
[4] Tyrosine kinase receptors as attractive targets of cancer therapy. Bennasroune A, Gardin A., Aunis D., Crémel G., Hubert P. Crit. Rev. Oncol. Hematol. 2004, 50, 23-38.
[5] The EGF receptor family: spearheading a merger of signaling and therapeutics. Bublil E.M., Yarden Y. Curr. Opin. Cell Biol. 2007, 19,124-134.

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Axon ID Name Description From price
1537 CP 724714 ErbB-2/HER2 kinase inhibitor €80.00
1415 CT 53518 PDGFR, c-KIT and FLT3 tyrosine kinase inhibitor €75.00
2265 DDR1-IN-1 Selective DDR1 receptor tyrosine kinase (RTK) inhibitor €95.00
2089 Dihydroxyflavone, 7,8- Tyrosine kinase receptor B (TrkB) agonist €55.00
1942 E 3810 dihydrochloride Dual VEGFR/FGFR tyrosine kinase inhibitor €95.00
2680 EAI045 Allosteric EGFR inhibitor (L858R/T790M-specific) €105.00
1760 EGFR Inhibitor [879127-07-8] Highly selective EGFR tyrosine kinase inhibitor €125.00
1128 Erlotinib hydrochloride EGFR tyrosine kinase inhibitor €70.00
1582 Foretinib c-MET and VEGFR2 tyrosine kinase inhibitor €90.00
1393 Gefitinib EGFR tyrosine kinase inhibitor €70.00
2248 GNF 5837 Potent, selective, and orally bioavailable tropomyosin receptor kinase (Trk) inhibitor €90.00
1959 Golvatinib Potent and orally available inhibitor of c-MET (HGFR) and VEGFR2 €95.00
2267 GSK 1838705A Potent IGF-IR and insulin receptor (IR) kinase inhibitor with additional affinity for ALK €110.00
2571 GW 2580 Orally bioavailable inhibitor of cFMS kinase and CSF1R €75.00
1251 GW 441756 TrkA inhibitor €75.00

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