August 2008 Drug Protein Targets
TIMP metallopeptidase inhibitor 3
This member of the tissue inhibitor of metalloproteinase (TIMP) family is more commonly referred to as TIMP3. It complexes with and permanently inactivates matrix metalloproteinases, a group of endopeptidases involved in the degradation of the extracellualr matrix. Mutations in TIMP3 cause Sorsby's fundus dystrophy (SFD), a macular degenerative disease. Research also suggests that VEGF inhibitor activity.
- Oscotec is developing orally-administered TIMP-3 secretion inducers for the treatment of osteoarthritis.
- TIMP3 belongs to the Enzyme>Protease/peptidase Target Family Group and its EC number is 3.4.24.17 Its Entrez Gene ID is 7078.
integral membrane protein 2B
Integral membrane protein 2B (ITM2B or BRI2) is a putative type II transmembrane protein believed to interact with amyloid precursor protein and regulate amyloid-ß production. Defects in ITM2B have been linked with Familial British and Danish Dementias.
- RemeGenix is developing peptides derived from the BRI2, to reduce the toxic impact of Amyloid beta, for the treatment of Alzheimer's disease.
- Its Entrez Gene ID is 9445.
nucleoporin 85kDa
Nuclear Pore Complexes (NPCs) are large protein complexes that cross the nuclear membrane and are responsible for the transport of macromolecules between the cytoplasm and nucleus. NPCs are composed of subcomplexes and nucleoporin 85kDa (NUP85) is part of one of these sub complexes. Research suggests NUP85 may bind to the pro-C-terminal domain of CCR2 and play a role in polarization and chemotaxis.
- Effector Cell Institute is developing a NUP85 inhibitor for the treatment of inflammatory diseases.
- NUP85 belongs to the Transporter Target Family Group. Its Entrez Gene ID is 79902.
aquaporin 2 (collecting duct)
This protein, also known as AQP2, belongs to the MIP/aquaporin family and is located in the renal collecting tubes. Research has shown that mutations in this gene are linked to autosomal dominant, and recessive forms of nephrogenic diabetes insipidus.
- DNAVEC is developing a Sendai virus/DeltaF vector expressing AQP2, for the treatment of congenital diabetes insipidus.
- AQP2 belongs to the Transporter Target Family Group. Its Entrez Gene ID is 359.
serine peptidase inhibitor, Kunitz type 1
Also known as HAI-1, this protein is a potent inhibitor of HGF activator. It has been found to be involved in the regulation of the proteolytic activation of HGF in injured tissues It is expressed in a variety of tissues including adult placenta, kidney, pancreas, prostate, small intestine, and in foetal kidney and lung.
- Morvus Technology is developing a combination of hepatocyte growth factor activator inhibitors 1 and 2 (HAI-1 and -2), for the treatment of prostate cancer.
- Its Entrez Gene ID is 6692.
microRNA 21
Also known as MIRN21 this microRNA is overexpressed in a number of tumour types and has been linked to cellular proliferation, apoptosis and migration. Some reaserch suggests programmed cell death 4 is regulated by MIRN21.
- Regulus Therapeutics is developing MIRN21-targeted antisense therapeutics for treatment of glioblastoma multiforme.
- Its Entrez Gene ID is 406991.
toll-like receptor 2
This member of the Toll-like receptor family, commonly referred to as TLR2, is believed to play a role in the immune response to bacterial lipoproteins and other microbial cell wall components. It leads to activation of NF-kappa-B and the inflammatory response through interactions with MYD88 and TRAF6.
- Dainippon Sumitomo Pharma is developing SMP-105 a cell-wall skeleton purified from Mycobacterium bovis BCG Tokyo 172 strain, which activates TLR2 as an immunotherapeutic anticancer agent.
- TLR2 belongs to the Receptor Target Family Group. Its Entrez Gene ID is 7097.
adenylate cyclase activating polypeptide 1 (pituitary) receptor type I
Also known as ADCYAP1R1 or PACAPRI, this protein is a type I adenylate cyclase activating polypeptide receptor for PACAP-27 and PACAP-38. It is believed to modulate neurotransmission and neurotrophic actions and is implicated in both pronociception and antinociception.
- Abbott is developing a series of novel, small-molecule ADCYAP1R1 antagonists, as broad-spectrum analgesics for the treatment of inflammatory and neuropathic pain.
- ADYAP1R1 belongs to the Receptor > GPCR Target Family Group. Its Entrez Gene ID is 117.
Pharmaprojects - New protein targets for drug development
© Informa UK Ltd 2008
Registered Office: Mortimer House, 37-41 Mortimer Street, London W1T 3JH, UK.
Registered in England and Wales No: 1072954
