February 2009 Drug Protein Targets
apolipoprotein B mRNA editing enzyme, catalytic polypeptide-like 4 (putative)
Also known as APOBEC4, this protein is a member of the APOBEC family of cytidine deaminases. Primarily expressed in testis, research suggests a role as an editing enzyme for mRNAs involved in spermatogenesis. Involvement in somatic hypermutation and recombination of immunoglobulin genes, and innate immunity to retroviral infection have also been suggested.
- ipal is developing an APOBEC4 gene therapy for the treatment of retroviral infections, including HIV-1 and HIV-2 infection.
- APOBEC4 belongs to the Enzyme Target Family Group. Its Entrez Gene ID is 403314.
guanine nucleotide binding protein (G protein), q polypeptide
Heterotrimeric G proteins consist of alpha, beta and gamma subunits and are activated in response to conformational changes in G-protein coupled receptors. More commonly referred to as GNAQ or G-alpha-q, guanine nucleotide binding protein (G protein), q polypeptide is the alpha subunit of a heterotrimeric G protein that stimulates phospholipase C-beta. Mutations in GNAQ are associated with uveal melanoma.
- Alnylam is developing a small interfering RNA targeting GNAQ, for the treatment of metastatic uveal melanoma.
- Its Entrez Gene ID is 2776.
pim-3 oncogene
Also known as PIM3, this serine/threonine protein kinase belongs to the PIM family of protooncogenes that are believed to bind to and downregulate CDK inhibitor p27(Kip1), promoting cell cycle progression and tumourigenesis.
- SuperGen is developing SGI-1776, an orally-available inhibitor of PIM1, PIM2 and PIM3, for the treatment of acute myelogenous leukaemia, acute lymphocytic leukaemia and other malignancies.
- PIM3 belongs to the Enzyme>Kinase and Transferase Target Family Groups and its EC number is 2.7.11.1. Its Entrez Gene ID is 415116.
toll-like receptor 5
Members of the toll-like receptor family are responsible for recognition of structurally similar molecules present on pathogens and subsequent activation of innate immunity. Toll-like receptor 5 (TLR5) mediates detection of bacterial flagellin, a component of flagella. Activation leads to NF-KappaB mobilisation via MYD88 and TRAF6.
- Microbiotix is developing TLR5 antagonists for the treatment of Pseudomonas and Burkholderia infections.
- TLR5 belongs to the Receptor Target Family Group. Its Entrez Gene ID is 7100.
eukaryotic elongation factor-2 kinase
Eukaryotic elongation factor-2 kinase (EEF2K) is a serine/threonine protein kinase in the calmodulin-mediated signalling pathway. Phosphorylation of elongation factor 2 (EEF2), a key component for protein synthesis, by EEF2K results in EEF2 inactivation. Increased EEF2K activity is associated with many cancers.
- Longevica Pharmaceuticals is developing EEF2K inhibitors as chemoprotectives. They also have potential in the treatment of stroke and Alzheimer's and Parkinson's diseases.
- EEF2K belongs to the Enzyme>Kinase and Transferase Target Family Groups and its EC number is 2.7.11.20. Its Entrez Gene ID is 29904.
poliovirus receptor-related 1 (herpesvirus entry mediator C)
Also known as PVRL1 or nectin-1, this protein plays a key role in cell-cell adhesion through interactions with itself, nectin-3 and nectin-4. Binding to afadin has also been demonstrated. It also acts as an endogenous host receptor for HSV-1 and -2 and pseudorabies virus. Mutations in nectin-1 are the cause of ectodermal dysplasia Margarita Island type.
- Alnylam is developing small interfering RNA oligonucleotides as topical vaginal microbicides for the prevention of herpes simplex virus-2 transmission. The oligonucleotides target UL29 and nectin-1, and are conjugated with cholesterol.
- Nectin-1 belongs to the Receptor Target Family Group. Its Entrez Gene ID is 5818.
single-stranded DNA-binding protein, herpes simplex virus-2
Commonly referred to as UL29, this member of the herpesviridae DNA-binding protein family is a single-stranded DNA-binding protein essential for DNA replication.
- Alnylam is developing small interfering RNA oligonucleotides as topical vaginal microbicides for the prevention of herpes simplex virus-2 transmission. The oligonucleotides target UL29 and nectin-1, and are conjugated with cholesterol.
- Its Entrez Gene ID is 1487314.
Pharmaprojects - New protein targets for drug development
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