May2007 Drug Protein Targets
3-phosphoinositide dependent protein kinase-1
3-Phosphoinositide dependent protein kinase-1 (PDPK1) is central to growth factor-stimulated signal transduction, and plays a key role in cancer cell growth, survival and tumour angiogenesis. PDPK1 phosphorylates protein kinase B, causing its activation.
- Wyeth is investigating a series of PDPK1 inhibitors for the treatment of cancer.
- PDPK1 belongs to the Enzyme>Kinase Target Family Group.
- Its Entrez Gene ID is 5170.
CUB domain-containing protein 1
CUB domain-containing protein 1 (CDCP1) is a transmembrane protein containing three extracellular CUB domains. It has been found to be overexpressed in colon and lung cancers. Its expression level is correlated with the metastatic ability of carcinoma cells. This protein is located on the cell surface. It has been shown to be tyrosine phosphorylated in a cancer cell line.
- Chugai (Roche) is investigating antibodies targeting CDCP1 (CUB domain-containing protein 1), for the treatment of cancer.
- Its Entrez Gene ID is 64866.
endothelial differentiation, lysophosphatidic acid G-protein-coupled receptor, 4
The EDG4 receptor is activated by lysophosphatidic acid (LPA). LPA elicits diverse biologic functions, including proliferation, platelet aggregation, smooth muscle contraction, inhibition of neuroblastoma cell differentiation, chemotaxis, and tumor cell invasion. The receptor is overexpressed in many types of tumour cells, including colorectal and kidney.
- Amgen is investigating a series of EDG4 antagonists as anticancer agents.
- EDG4 belongs to the Receptor>GPCR Target Family Group.
- Its Entrez Gene ID is 9170.
integrin, alpha E (antigen CD103, human mucosal lymphocyte antigen 1; alpha polypeptide)
Integrins are a family of cell surface adhesion molecules that play a major role in morphogenesis, haemostasis, leucocyte activation and cellular adhesion. Immune responses at mucosal sites are mediated by lymphocytes associated with mammary glands and the gastrointestinal, genitourinary, and respiratory tracts. Integrin, alpha E is preferentially expressed on human intestinal intraepithelial lymphocytes (IEL), and in addition to adhesion, it may serve as an accessory molecule for IEL activation.
- LigoCyte is developing a compound targeting CD103 for the treatment of asthma, COPD and rheumatoid arthritis.
- Integrin, alpha E belongs to the Receptor Target Family Group.
- Its Entrez Gene ID is 3682.
Plexin domain-containing 1
Plexin domain-containing 1 (TEM7) is a type 1 membrane receptor selectively expressed by tumour endothelial cells. It has been suggested to have a link with tumour vasculature.
- Kirin Brewery and Genzyme are developing fully-human MAbs specific for tumour endothelial markers (TEMs), including TEM7, as antiangiogenics in the treatment of solid tumours.
- TEM7 belongs to the Receptor Target Family.
- Its Entrez Gene ID is 57125.
solute carrier family 2, (facilitated glucose transporter) member 8
The Glut8 transporter is a putative facilitative transporter for the cellular import and export of glucose. It recycles between an intracellular site and the plasma mambrane.
- Viventia Biotech is developing VB1-050, a human anti-Glut8 Mab for the treatment of cancer.
- Glut8 belongs to the Transporters>Porters (uni, sym and anti) Target Family Group.
- Its Entrez Gene ID is 29988.
ubiquitin-activating enzyme E1C (UBA3 homologue, yeast)
Ubiquitin-activating enzyme E1C (Nedd8 activating enzyme; NAE) acts upstream of the proteasome and associates with AppB1, an amyloid beta precursor binding protein, to activate Nedd8, a ubiquitin-like protein which regulates cell division, signalling and embryogenesis.
- Millennium is developing an inhibitor of NAE for the treatment of cancer.
- NAE belongs to the Enzyme Target Family Group and its EC number is 6.3.2.
- Its Entrez Gene ID is 9039.
