Jul2007 Drug Protein Targets
Endogenous retroviral family W, env (C7), member 1 (syncytin)
Endogenous retroviral family W, env (C7), member 1 (syncytin) is expressed in the placental syncytiotrophoblast and is involved in fusion of the cytotrophoblast cells to form the syncytial layer of the placenta. It may play a role in the attack, through oxidation, on the myelin protective covering of the brain and spinal cord and on myelin-making cells themselves.
- GeNeuro are developing a humanized MAb against the immunopathic MSRV/HERV-W envelope proteins of human endogenous retrovirus, for the treatment of multiple sclerosis.
- Scyncytin's Entrez Gene ID is 30816.
G protein-coupled bile acid receptor 1
Bile acid treatment of G protein-coupled bile acid receptor 1 (GPBAR1) induces the production of intracellular cAMP, activation of a MAP kinase signalling pathway, and internalization of GPBAR1. It is implicated in the suppression of macrophage functions and regulation of energy homeostasis by bile acids.
- Intercept Pharmaceuticals is developing agonists to TGR5, a cell-surface receptor that responds to bile acids, for the treatment of diabetes, obesity and immune-related conditions.
- GPBAR1 belongs to the Receptor> GPCR Target Family. Its Entrez Gene ID is 151306.
integrin, alpha 9
Integrin, alpha 9 is a glycoprotein receptor for VCAM1, cytotactin and osteopontin. Integrins mediate cell-cell and cell matrix adhesion. Expression of this gene has been found to be upregulated in small cell lung cancers.
- Gene Techno Science is developing anti-alpha9 integrin MAbs for the treatment of autoimmune diseases, bone diseases and cancer metastasis.
- Integrin alpha 9 belongs to the Receptor Target Family Group. Its Entrez Gene ID is 3680.
SHC (Src homology 2 domain containing) transforming protein 1
SHC (Src homology 2 domain containing) transforming protein 1 (SHC1) is an adaptor in many signal transduction pathways, for example, facilitating the activation of RAS proteins in response to a variety of factors. It is involved in cellular aging, senescence and apoptosis.
- Congenia (Genextra) is developing small-molecule compounds to inhibit 2 mitochondrial targets, SHC1 and permeability transition pore for the treatment of cardiovascular and neurodegenerative disorders.
- The Entrez Gene ID for SHC1 is 6464.
solute carrier family 25 (mitochondrial carrier; dicarboxylate transporter), member 10
- Isis Pharmaceuticals is developing an antisense therapy against the mDIC for the treatment of diabetic obesity.
- mDIC belongs to the Transporter Target Family Group. Its Entrez Gene ID is 1468.
Also known as mitochondrial dicarboxylate carrier (mDIC), this catalyzes the transport of dicarboxylates such as malate and succinate across the mitochondrial membrane in exchange for phosphate, sulphate, and thiosulphate. These are then supplied as substrates for the Krebs cycle, gluconeogenesis, urea synthesis, and sulphur metabolism. Specifically, it has been demonstrated to play an important role in supplying malate for citrate transport required for fatty acid synthesis and that its inhibition might effectively reduce lipid accumulation in adipose tissues.
voltage-dependent anion channels 2 and 3
Voltage-dependent anion channels (VDAC) are found on the outer mitochiondrial membrane. They form voltage-gated pores when incorporated into planar lipid bilayers and are involved in the translocation of adenine nucleotides through the outer membrane. These channels may also function as a mitochondrial binding site for hexokinase and glycerol kinase.
- PRL-93936 is a 2nd-generation chemotherapeutic targeting voltage-dependent anion channels 2 and 3, under development by Prolexys for the treatment of ras-overexpressing cancers.
- Both voltage dependent anion channels belong to the Ion Channel Target Family Group. Their Entrez Gene IDs are 7417 and 7419, repectively.
