July 2008 Drug Protein Targets
microRNA 208a
Also known as MIRN208A this microRNA is encoded by an intron of the MYH6 gene and is expressed in cardiac tissue. Overexpression induces cardiomyocyte hypertrophy, fibrosis and ß-MHC expression. Knockout mice lacking this miRNA did not develop heart failure folllowing thoracic aortic banding.
- Miragen is developing inhibitors of endogenous microRNAs for the treatment of heart failure. One of the targets under investigation is MIRN208A
- Its Entrez Gene ID is 406990.
ras homologue gene family, member C
This member of the Rho family of small GTPases is more commonly referred to as RHOC and is believed to play a role in cell locomotion. Interactions with DIAPH1, ROCK1, ROCK2, RTKN and AKAP13 have been demonstrated and research suggests involvement in tumour cell invasion. Over-expression of RHOC enhances metastasis.
- CompleGen is developing RHOC inhibitors as anticancers.
- Its Entrez Gene ID is 389.
glutaminyl-peptide cyclotransferase (glutaminyl cyclase)
More commonly known as glutaminyl cyclase, this transferase converts glutaminyl peptides to cyclic pyroglutamyl peptides and is responsible for the presence of pyroglutamyl residues in many neuroendocrine peptides.
- Probiodrug is developing glutaminyl cyclase inhibitors for the treatment of Alzheimer's disease.
- Glutaminyl cyclase belongs to the Enzyme>Transferase Target Family Group and its EC number is 2.3.2.5 Its Entrez Gene ID is 25797.
Prominin 1
Also known as CD133, prominin 1 is a pentaspan transmembrane glycoprotein. It was initially found to be expressed on primitive hematopoietic stem and progenitor cells and retinoblastoma. No naturally-occuring ligand has been found for CD133.
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ImmunoCellular Therapeutics is developing peptide vaccines that elicit a T-cell response targeting CD133-positive cancer stem cells, for the treatment of gliomas.
- Its Entrez Gene ID is 8842.
Nonstructural polyprotein, Norwalk virus
This protein is a viral protease similar to the picornovirus 3C protease and cleaves the first ORF polyprotein into non structural proteins.
- Microbial Novoteqs is developing inhibitors of Norwalk virus 3CL protease.
- Its Entrez Gene ID is 1491970.
triggering receptor expressed on myeloid cells 2
More commonly referred to as TREM2, this membrane protein forms a receptor signalling complex with TYRO protein tyrosine kinase binding protein (TYROBP or DAP12) and triggers an immune response in macrophages and dendritic cells. Loss of function mutations in either TREM2 or TYROBP are a known cause of polycystic lipomembranous osteodysplasia with sclerosing leukoencephalopathy (PLOSL).
- BioXell is developing therapeutics that target TREM2 for the treatment of inflammatory, neurodegenerative and metabolic disorders.
- TREM2 belongs to the Receptor Target Family Group. Its Entrez Gene ID is 54209.
CD300 molecule-like family member g
Like other members of the CD300L family, CD300 molecule-like family member g (CD300LG or TREM4) is a type I cell surface glycoprotein widely expressed on haematopoietic cells. Research suggests IgA and IgM as possible ligands.
- BioXell is developing therapeutics that target CD300LG for the treatment of inflammatory, neurodegenerative and metabolic disorders.
- CD300LG belongs to the Receptor Target Family Group. Its Entrez Gene ID is 146894.
CD300 molecule-like family member b
Like other members of the CD300L family, CD300 molecule-like family member b (CD300LB or TREM5) is a type I cell surface glycoprotein widely expressed on haematopoietic cells. Research has shown interactions with TYRO protein tyrosine kinase binding protein (TYROBP or DAP12).
- BioXell is developing therapeutics that target CD300LB for the treatment of inflammatory, neurodegenerative and metabolic disorders.
- CD300LB belongs to the Receptor Target Family Group. Its Entrez Gene ID is 124599.
