October 2008 Drug Protein Targets
fibroblast growth factor receptor 4
This member of the fibroblast growth factor receptor family, more commonly referred to as FGFR4, binds fibroblast growth factor 19 and may play a role in systemic lipid and glucose homeostasis.
- Verva Pharmaceuticals and Isis Pharmaceuticals are developing FGFR4 antisense oligonucleotides for the treatment of obesity.
- FGFR4 belongs to the Receptor and Enzyme>Kinase Target Family Group and its EC number is 2.7.10.1 Its Entrez Gene ID is 2264.
Gardner-Rasheed feline sarcoma viral (v-fgr) oncogene homologue
Also known as SRC2 or FGR, this tyrosine kinase is present at the plasma membrane and regulates cell migration and adhesion. Research has shown it to be activated in B-lymphocytes following infection with Epstein-Barr virus.
- DCC-2036 is an orally-administered Bcr-abl, LYN, HCK and FGR inhibitor, under development by Deciphera Pharmaceuticals for the treatment of chronic myelogenous leukaemia.
- SRC2 belongs to the Enzyme>Kinase Target Family Group and its EC number is 2.7.10.2 Its Entrez Gene ID is 2268.
haemopoietic cell kinase
Haemopoietic cell kinase (HCK) is a member of the Src family of tyrosine kinases expressed in myeloid and B-lymphoid cells. It is located on chromosome 20 at a region known to be affected by deletions in certain acute myeloid leukaemias and myeloproliferative disorders. It may play a role in mast cell activation, cytokine production and neutrophil migration and degranulation.
- DCC-2036 is an orally-administered Bcr-abl, LYN, HCK and FGR inhibitor, under development by Deciphera Pharmaceuticals for the treatment of chronic myelogenous leukaemia.
- HCK belongs to the Enzyme>Kinase Target Family Group and its EC number is 2.7.10.1 Its Entrez Gene ID is 3055.
smoothened homologue (Drosophila)
This G-protein coupled receptor, often referred to as SMO, is a member of the hedgehog pathway. It plays a role in gene expression through regulation of transcription factors belonging to the Gli family. Research has shown that SMO is in turn regulated by members of the patched family of proteins. Defects in SMO have been observed in basal cell carcinoma.
- Curis and Genentech are developing small-molecules, including GDC-0449, that target SMO for the treatment of cancer.
- SMO belongs to the Receptor>GPCR Target Family Group. Its Entrez Gene ID is 6608.
NEL-like 1 (chicken)
NEL-like 1 (chicken) (NELL1) contains chordin-like, cysteine rich domans, a NH2-terminal thrombospondin-like module, and EGF-like repeats. It has been implicated in cell growth regulation and differentiation.
- NellOne Therapeutics is developing a protein therapeutic based on Nell1, for the restoration of extracellular matrix constitution and orientation of damaged cardiac muscle in heart attack patients.
- NELL1 belongs to the Enzyme>Kinase Target Family Group. Its Entrez Gene ID is 4745.
cyclin-dependent kinase inhibitor 2C (p18, inhibits CDK4)
More commonly known as CDKN2C or p18, this protein is a member of the INK4 family of cyclin-dependent kinase inhibitors. It is known to interact strongly with CDK6 and weakly with CDK4, and as such plays a role in regulation of cell cycle G1 progression.
- CP-p18 (cell permeable-p18) is an anti-p18 monoclonal antibody, under development by ProCell Therapeutics for the treatment of cancer.
- Its Entrez Gene ID is 1031.
catenin (cadherin-associated protein), beta 1, 88kDa
Catenin (cadherin-associated protein), beta 1, 88kDa (CTNNB1) is an adherens junction protein. It may regulate cell adhesion and signal transduction through the Wnt pathway. Mutations in CTNNB1 have been described in colon cancer cell lines.
- CEQ-501 is an RNAi therapeutic that targets CTNNB1, under development by Cequent Pharmaceuticals for the treatment of familial adenatomous polyposis.
- Its Entrez Gene ID is 1499.
F11 receptor
This member of the immunoglobulin superfamily is believed to play a role in epithelial tight junction formation and platelet activation. It also acts as a receptor for orthoreovirus.
- 6F4 is a monoclonal antibody against the F11 receptor, under development by Pierre Fabre for the treatment of cancer.
- Its Entrez Gene ID is 50848.
glypican 3
Glypicans consist of a protein core attached to heparin sulphate chains anchored to cell membranes. This glypican, also known as GPC3, may play a role in the regulation of cell division and growth. Some research suggests GPC3 is a novel tumour marker for hepatocellular carcinoma.
- Chugai is developing GC-33, an anti-GPC3 antibody as an anticancer.
- Its Entrez Gene ID is 2719.
Pharmaprojects - New protein targets for drug development
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