Feb2007 Drug Protein Targets
cadherin 3, type 1, P-cadherin (placental)
Cadherin 3, type 1, P-cadherin (placental), more commonly known as P-cadherin, is a calcium-dependent cell-cell adhesion integral membrane glycoprotein that plays a role in the maintenance of the epithelial structure. It is predominantly expressed in the proliferative compartment of stratified squamous epithelia, the basal layer, and its expression decreases as cells differentiate. It is located on the long arm of chromosome 16, which is involved in loss of heterozygosity in prostate and breast cancers. Aberrant P-cadherin expression is often observed in squamous cell carcinomas, indicating that regulated expression is required for maintaining a 'normal' epidermal structure.
- PF-3732010 is a P-cadherin MAb, under development by Pfizer for the treatment of cancer.
- The Entrez Gene ID for P-cadherin is 1001.
Delta-like 4 (Drosophila)
Delta-like 4 (Drosophila) (DLL4) is a member of the delta family of notch ligands characterized by EGF repeats, a DSL and a transmembrane domain. Its expression has been found to be initially restricted to large arteries in the embryo and then to smaller arteries and microvessels in adults and tumour models. DLL4 has been shown to increase the formation of blood vessels, which are not fully-functional that then 'choke' the tumour.
- Regeneron Pharmaceuticals is developing a novel drug that inhibits angiogenisis by targeting DLL4.
- Its Entrez Gene ID is 54567.
guanylate binding protein 1, interferon-inducible, 67kDa
Human guanylate-binding protein-1 (GBP1) is a large farnesylated GTPase, similar in structure to the dynamins, and whose expression is induced by interferon. Guanylate binding proteins specifically bind guanine nucleotides (GMP, GDP, and GTP). GBP1 is distinguished from the GTP-binding proteins by the presence of 2 binding motifs rather than 3. GBP1 has been shown to prevent angiogenesis when expressed in or near tumours which consequently can lead to a reduction in their growth or even elimination.
- Austrianova is developing a GBP1 gene therapy for the treatment of cancer.
- The Entrez Gene ID for GBP1 is 2633.
