Enzyme Linked Receptors

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
2467 (+)-ITD-1 Selective inhibitor of TGFβ/Smad signaling that promotes cardiogenesis €165.00
1892 1-NM-PP1 Potent tyrosine kinase inhibitor (TKI) of multiple targets (Src, Fyn, Abl, CDK, Trk) €95.00
2089 7,8-Dihydroxyflavone Tyrosine kinase receptor B (TrkB) agonist €55.00
1744 A 77-01 TGF-βR 1 inhibitor; ALK 5 inhibitor €80.00
1421 A 83-01 TGF-βR 1 inhibitor; ALK 5 inhibitor €70.00
1419 AB 1010 PDGFR, c-KIT and FGFR3 tyrosine kinase inhibitor €70.00
3040 Abivertinib Potent oral, irreversible, third-generation EGFR TKI with selectivity for mutant EGFRs €95.00
1638 ABT 869 PDGFR, c-KIT and VEGFR tyrosine kinase inhibitor €85.00
1653 AEE 788 EGFR, ErbB2 and VEGFR tyrosine kinase inhibitor €80.00
1414 AG 013736 PDGFR,c-KIT and VEGFR tyrosine kinase inhibitor €50.00
1884 Alectinib Orally available and selective ALK inhibitor €70.00
2930 Alofanib Allosteric inhibitor of FGFR2 €90.00
3946 Altiratinib Balanced inhibitor for MET, TIE2 (TEK), and VEGFR2 (KDR) kinases Inquire
1916 AMG 208 Inhibitor of c-MET receptor tyrosine kinase (RTK) €95.00
1768 AMG 706 Multiple receptor tyrosine kinase inhibitor €105.00
3945 AMG-337 Potent and exquisitely selective inhibitor of wild-type and some mutant forms of c-Met Inquire
4071 AMG-925 Potent, selective, and orally available FLT3/CDK4 dual inhibitor Inquire
2368 Amuvatinib RTK inhibitor which effectively inhibits PDGFR, c-Kit and c-Met €105.00
2468 ANA 12 Selective TrkB antagonist with anxiolytic and antidepressant activity in mice €90.00
2849 Apatinib Inhibitor of VEGFR2 €120.00
1838 ARQ 197 c-MET tyrosine kinase Inhibitor €90.00
1986 AST 1306 tosylate ErbB2 and EGFR inhibitor €90.00
1610 AZ 23 TrkA and TrkB inhibitor €80.00
4074 AZ5104 EGFR inhibitor Inquire
2153 AZD3463 Potent inhibitor of ALK and IGF1R €105.00
2563 AZD3759 Potent, orally active, brain-penetrant, EGFR tyrosine kinase inhibitor €85.00
1917 AZD4547 Potent and selective FGFR inhibitor €85.00
2342 AZD9291 Potent oral, irreversible, third-generation EGFR TKI with selectivity for mutant EGFRs €95.00
3862 BGB-283 Orally available dual RAF kinase/EGFR inhibitor Inquire
1544 BIBW 2992 EGFR and ErbB-2/HER2 tyrosine kinase inhibitor €50.00

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