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Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).
Type III RTKs include PDGFR, CSF-1R (Ems), Kit and FLT3, which function as homo- or heterodimers. Endogenous ligands of PDGF receptors are homo- or heterodimeric: PDGFA, PDGFB, VEGFE and PDGFD (PDGFD, Q9GZP0) combine as homo- or heterodimers to activate homo- or heterodimeric PDGF receptors. SCF is a dimeric ligand for KIT. Ligands for CSF1R are either monomeric or dimeric glycoproteins, while the endogenous agonist for FLT3 is a homodimer.
1. Choi SJ, Moon MJ, Lee SD, Choi SU, Han SY, Kim YC. (2010) Indirubin derivatives as potent FLT3 inhibitors with anti-proliferative activity of acute myeloid leukemic cells. Bioorg. Med. Chem. Lett., 20 (6): 2033-7. [PMID:20153646]
2. Heinrich MC, Griffith D, McKinley A, Patterson J, Presnell A, Ramachandran A, Debiec-Rychter M. (2012) Crenolanib inhibits the drug-resistant PDGFRA D842V mutation associated with imatinib-resistant gastrointestinal stromal tumors. Clin. Cancer Res., 18 (16): 4375-84. [PMID:22745105]
3. Kitagawa D, Yokota K, Gouda M, Narumi Y, Ohmoto H, Nishiwaki E, Akita K, Kirii Y. (2013) Activity-based kinase profiling of approved tyrosine kinase inhibitors. Genes Cells, 18 (2): 110-22. [PMID:23279183]
4. Pearson MA, Fabbro D. (2004) Targeting protein kinases in cancer therapy: a success?. Expert Rev Anticancer Ther, 4 (6): 1113-24. [PMID:15606337]
Database page citation:
Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family. Accessed on 24/11/2014. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=322.
Concise Guide to PHARMACOLOGY citation:
Alexander SPH, Benson HE, Faccenda E, Pawson AJ, Sharman JL, Spedding M, Peters JA and Harmar AJ, CGTP Collaborators. (2013) The Concise Guide to PHARMACOLOGY 2013/14: Catalytic Receptors. Br J Pharmacol. 170: 1676–1705.