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.
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 |