September 2008 Drug Protein Targets
deoxycytidine kinase
Deoxycytidine kinase (DCK) is required for the phosphorylation of the deoxyribonucleosides deoxycytidine deoxyguanosine and deoxyadenosine. It is also involved in the activation of many nucleoside analogues commonly used as antivirals and chemotherapeutics.
- Lexicon Pharmaceuticals is developing a deoxycytidine kinase inhibitor, LP-661438, and believes it has potential for the treatment of cancer, immunological disorders and viral infections.
- DCK belongs to the Enzyme>Kinase Target Family Group and its EC number is 2.7.1.74. Its Entrez Gene ID is 1633.
C-type lectin domain family 9, member A
Also referred to as CLEC9A or DNGR-1, this protein is a group V C-type lectin-like receptor that acts as an activation receptor. Evidence suggests it is expressed on dendritic cells known to be involved in cross presentation of foreign and self-antigens.
- Cancer Research Technology is developing an anti-CLEC9A antibody conjugated to tumour antigens for the treatment of cancer and infectious diseases.
- CLEC9A belongs to the Receptor Target Family Group. Its Entrez Gene ID is 283420.
Bernardinelli-Seip congenital lipodystrophy 2 (seipin)
This protein, more commonly referred to as BSCL2 or seipin, is an integral membrane protein of the endoplasmic reticulum. Research supports a role in the regulation of a gene involved in lipid metabolism. Mutations in seipin are associated with Berardinelli-Seip syndrome, a disease characterized by a near absence of adipose tissue and severe insulin resistance.
- NewSouth Innovations (NSI) is developing inhibitors of seipin for the treatment of lipodystrophy and and metabolic diseases such as Syndrome X. NSI believes they also have potentioal in HIV-related lipodystrophy and obesity.
- Its Entrez Gene ID is 26580.
bone gamma-carboxyglutamate (gla) protein
Bone gamma-carboxyglutamate (gla) protein (BGLAP or osteocalcin) is associated with the bone matrix and is known to play an important role in bone formation. Research indicates roles in the regulation of blood glucose and fat deposits. It may also raise insulin sensitivity and cause insulin release from the pancreas.
- Escoublac is developing human osteocalcin, or a derivative thereof, for the treatment of metabolic disorders and related conditions, such as obesity and Type II diabetes.
- Its Entrez Gene ID is 632.
neuroblastoma RAS viral (v-ras) oncogene homologue
This membrane protein, also known as NRAS, is commonly found in the Golgi apparatus and the plasma membrane, transfer between these two locations is believed to be controlled by palmitoylation and depalmitoylation. It has GTP/GDP binding and GTPase activity and may play a role in the regulation of normal cell growth. Mutations in NRAS are a known cause of a variety of cancers.
- MT-477 is an NRAS inhibitor, under development by Medisyn Technologies for the treatment of non-small cell lung cancer.
- Its Entrez Gene ID is 4893.
phosphoinositide-3-kinase, catalytic, beta polypeptide
Also referred to as PIK3CB, this protein is a 110-kD catalytic subunit of PI3k. PI3 kinases are commonly deregulated in cancer. They have been implicated as participants in signalling pathways regulating cell growth by virtue of their activation in response to various mitogenic stimuli.
- Roche and Genentech are developing a PI3k inhibitor for the treatment of cancer.
- PIK3CB belongs to the Enzyme>kinase Target Family Group. Its Entrez Gene ID is 5291.
- Alnylam is investigating siRNA agents for the treatment of malaria, targeting scavenger receptor BI.
- SCARB1 belongs to the Receptor and the Transporter Target Family Group. Its Entrez Gene ID is 949.
- Rosetta Genomics is developing mimetics of miR-451, for the treatment of glioblastoma multiforme.
- Its Entrez Gene ID is 574411.
- Boehringer Ingelheim is developing inhibitors of Pim-2, for the treatment of inflammation.
- PIM2 belongs to the Enzyme>Kinase and Transferase Target Family Group and its EC number is 2.7.11.1 Its Entrez Gene ID is 11040.
scavenger receptor class B, member 1
The scavenger receptor B1 is a major regulator of cholesterol uptake by the liver. It has been identified as a critical host factor for the liver infection stage of malaria.
microRNA 451
microRNA 451 is involved in activating the expression of P-glycoprotein, the MDR1 gene product that confers cancer cell resistance to a broad range of chemotherapeutics.
pim-2 oncogene
Also known as PIM2, this member of the Pim family of serine/threonine protein kinases promotes cell cycle progression and inhibits apoptosis. Some research suggests PIM2 down-regulates p27. Deregulation of PIM2 has been observed in several malignancies.
