Dec2006 Drug Protein Targets
Myo-inositol oxygenase
Myo-inositol (MI) oxygenase is a renal-specific aldo-keto reductase. It catalyses the first committed step in MI catabolism. It has been implicated in complications of diabetes including diabetic nephropathy.
- Researchers at the Maurice Wilkins Centre for Molecular Biodiscovery, Auckland, NZ, in collaboration with Industrial Research Limited, Auckland, NZ, are developing MIOX inhibitors to treat diabetes.
- The Entrez Gene ID for Myo-inositol oxygenase is 55586.
- MI belongs to the Enzyme > oxygenase Target Family Group on Pharmaprojects and its EC number is 2.7.1.
Protein kinase N3
Protein kinase N3 is a protein kinase C-related molecule regulated by P13K at both the expression and catalytic activity level.
- Atugen (SR Pharma) is developing Atu027, small interfering RNA (siRNA) inhibitors of PKN3 for the treatment of epithelial cancers.
- The Entrez Gene ID for protein kinase N3 is 29941.
- Protein kinase N3 belongs to the Enzyme > Kinase Target Family Group on Pharmaprojects and its EC number is 1.13.99.1.
Prostaglandin D2 synthase 21kDa (brain)
Prostaglandin D2 synthase catalyzes the conversion of prostaglandin H2 (PGH2) into prostaglandin D2 (PGD2) in the brain. PGD2 is a potent inhibitor of platelet aggregation and is involved in smooth muscle contraction. It also functions as a neuromodulator and tropoic factor in the CNS.
- AstraZeneca is developing prostaglandin D2 synthase (PGD2S) inhibitors for the treatment of inflammatory disorders, including asthma and rhinitis.
- The Entrez Gene ID for prostaglandin D2 synthase is 5730.
- PGD2S belongs to the Enzyme > Synthase Target Family Group on Pharmaprojects and its EC number is 5.3.99.2.
Angiopoietin-2
Angiopoietin-2 destabilizes vessels by competing with, and thereby blocking Tie2 signalling. It is a natural antagonist of angiopoietin-1. It acts with vascular endothelial growth factor to initiate angiogenisis.
- CovX is developing an angiopoietin-2 inhibitor for the treatment of cancer.
- The Entrez Gene ID for Angiopoietin 2 is 285
YME1L1 YME1-like 1 (S. cerevisiae)
The protein encoded by this gene is the human ortholog of yeast mitochondrial AAA metalloprotease, YME1P. In yeast, YME1P, also known as PAMP, performs roles in the assembly and turnover of respiratory chain complexes. It is localized in the mitochondria.
- EvoGenix is developing antibodies against PAMP, for the treatment of cancer.
- The Entrez Gene ID for YME1-like 1 (S. cerevisiae) is 10730.
- YME1-like 1 (S cerevisiae) belongs to the Enzyme > Protease/peptidase Target Family Group on Pharmaprojects.
Low density lipoprotein receptor-related protein
The low density lipoprotein receptor (LDLR) gene family consists of cell surface proteins involved in receptormediated endocytosis of specific ligands. LDLR6 plays a role in bone mineral density in old age and fractures, the main clinical endpoint of osteoporosis. MESD is a chaperone protein required for the correct folding of LDLR6.
- Raptor is developing MESD-based peptides for the treatment of cancer and osteoporosis.
- The Entrez Gene ID for LDLR-related protein 6 is 4040.
- LDLR-related protein 6 belongs to the Receptor Target Family Group on Pharmaprojects.
