July 2009 Drug Protein Targets
eukaryotic translation initiation factor 2, subunit 1 alpha, 35kDa
Required for initiation of translation, the eukaryotic initiation factor 2 (eIF2) consists of an alpha, beta and gamma subunit. Phosphorylation of the alpha subunit (EIF2S1) regulates the rate of formation of eIF2.
- Egenix is developing small-molecule inhibitors of EIF2S1 and for the treatment of cancer.
- Its Entrez Gene ID is 1965.
tumor necrosis factor (ligand) superfamily, member 14
Also known as TNFSF14, this protein activates NFKB and stimulates the proliferation of T-cells. It acts as a receptor for herpes simplex virus.
- Kyowa Hakko Kirin is developing a fully human monoclonal anti- TNFSF14 antibody for the treatment of inflammatory diseases including ulcerative colitis and Crohn's disease.
- TNFSF14 belongs to the Cytokine/Growth factor>Cytokine Target Family Groups. Its Entrez Gene ID is 8740.
midkine (neurite growth-promoting factor 2)
Midkine (neurite growth-promoting factor 2) (MK, MDK or NEGF) is a heparin-binding growth factor that has angiogenic, mitogenic and chemotactic activities. Increased expression of midkine has been observed in numerous cancer types.
- Medical Therapies is developing midkine antagonist RNAi technology and antisense oligonucleotides, for the treatment of solid tumours and carcinomas.
- Midkine belongs to the Cytokine/growth factor>Growth factor, non-cytokine Target Family Groups. Its Entrez Gene ID is 4192.
CD300 molecule-like family member f
CD300 molecule-like family member f (CD300LF) is a member of the Ig family of receptors. It acts as an inhibitory receptor for myeloid and mast cells and possibly inhibits osteoclast formation.
- Arca biopharma is developing MAbs against the extracellular domain of CD300LF, for the treatment of acute myeloid leukaemia.
- CD300LF belongs to the Receptor>Cytokine receptor>Immunoglobulin family Target Family Groups. Its Entrez Gene ID is 146722.
LMP-1, Epstein-Barr virus
Epstein-Barr virus (EBV) latent membrane protein 1 (LMP-1) is a transmembrane protein involved in the conversion of B-lymphocytes into indefinitely proliferating lymphoblastoid cell lines. It acts as a CD40 functional homologue that leads to the up-regulation of anti-apoptotic proteins.
- Cancer Research Technology is developing an immunotherapeutic for the treatment of Epstein-Barr virus-induced cancers. It consists of the B-subunit of Escherichia coli enterotoxin protein (EtxB) and the Epstein-Barr virus tumour antigens LMP1 and LMP2.
- Its Entrez Gene ID is 3783750.
LMP-2A, Epstein-Barr virus
Epstein-Barr virus (EBV) latent membrane protein 2A (LMP-1) is a transmembrane protein that maintains EBV infection of B-lymphocytes. It acts as a molecular scaffold to recruit LYN and SYK tyrosine kinase and E3 protein-ubiquitin ligases which leads to the ubiquitination and possibly degradation of both tyrosine kinases.
- Cancer Research Technology is developing an immunotherapeutic for the treatment of Epstein-Barr virus-induced cancers. It consists of the B-subunit of Escherichia coli enterotoxin protein (EtxB) and the Epstein-Barr virus tumour antigens LMP1 and LMP2.
- Its Entrez Gene ID is 3783751.
CD79b molecule, immunoglobulin-associated beta
CD79 is composed of 2 separate proteins CD79a and CD79b. CD79 forms a complex with the B-cell receptor and leads to a signalling cascade following recognition of antigen by the B-cell receptor.
- Cancer Research Technology is developing an anti-CD79b Ab for the treatment of B-cell derived cancers, autoimmune diseases, such as systemic lupus erythematosis and multiple sclerosis and inflammatory diseases, such as rheumatoid arthritis.
- CD79B belongs to the Receptor Target Family Groups. Its Entrez Gene ID is 974.
interleukin 17F
Commonly known as IL17F, this protein is predominantly expressed on activated T-cells. Research has shown it can stimulate the production of other cytokines such as IL-6, IL-8 and colony-stimulating factor and inhibit angiogenesis.
- NI-1401 is a fully-human MAb against IL-17A/F, under development by NovImmune for the treatment of autoimmune and inflammatory diseases.
- IL17F belongs to the Cytokine/Growth factor>Cytokine>Interleukin Target Family Groups. Its Entrez Gene ID is 112744.
fibroblast growth factor 23
Also known as FGF23, this protein plays a role in phosphate metabolism. Defects in FGF23 are known to cause autosomal dominant hypophosphataemic rickets and hyperphosphataemic familial tumoural calcinosis, while mutations cause familial tumoural calcinosis with hyperphosphataemia. Increased expression has been observed in hypophosphataemic osteomalacia.
- Kyowa Hakko Kirin is developing KRN-23, an injectable fully-human MAb which binds to and neutralizes FGF23, for the treatment of hypophosphataemia.
- FGF23 belongs to the Cytokine/Growth factor>Growth factor, non-cytokine Target Family Groups. Its Entrez Gene ID is 8074.
retinol binding protein 4, plasma
More commonly referred to as RBP4, this lipoprotein is a carrier for retinol in the blood. It delivers retinol from liver stores to peripheral tissues. Defects in RBP4 are associated with retinol-binding protein deficiency.
- Isis Pharmaceuticals is investigating an antisense oligonucleotide against RBP4 for the treatment of Type II diabetes and cardiomyopathy associated with diabetes.
- Its Entrez Gene ID is 5950.
nuclear receptor co-repressor 2
Nuclear receptor co-repressor 2 (NCOR2 or SMRT) is a transcriptional regulatory protein. A role in the recruitment of histone deacetylases to DNA promoter regions has been proposed.
- Isis Pharmaceuticals is investigating an antisense oligonucleotide inhibiting silencing mediator for NCOR2 for the treatment of Type II diabetes.
- Its Entrez Gene ID is 9612.
activated leukocyte cell adhesion molecule
ALCAM or CD166 is a cell adhesion molecule which binds CD6. It may be involved in the binding of T- and B-cells to activated leukocytes and in interactions between cells of the nervous system.
- AT-002 (CBAS-173) is an antibody targeting CD166 cell surface protein, under development by Affitech for the treatment of neuroinflammatory diseases.
- Its Entrez Gene ID is 214.
