Sept2007 Drug Protein Targets
angiopoietin-like 4
Angiopoietin-like 4 is induced under hypoxic conditions in endothelial cells. It is a fasting-induced controller of LPL in adipose tissue, and acts as an unfolding molecular chaperone extracellularly. Inhibition of angiopoeitin-like 4 has been found to lower cholesterol and triglycerides.
- Lexicon Pharmaceuticals is developing antibodies specific for angiopoietin-like 4 for the treatment of insulin-related metabolic syndrome.
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The Entrez Gene ID for angiopoeitin-like 4 is 51129.
bone morphogenetic protein 4
Also known as BMP4, this is a member of the transforming growth factor beta superfamily. It plays a role in the onset of endochondral bone formation in humans and is required in determining the dorsal/ventral axis in embryos. BMP4 and its receptor are expressed in the islet. BMP4 signalling has been found to preserve insulin expression and glucose sensing.
- Betagenon is investigating BMP-4 for the preservation of β cells.
- BMP4 belongs to the Cytokine/GrowthFactor > Cytokine > Growth Factor Target Family Group. Its Entrez Gene ID is 652.
interleukin 25
Interleukin 25 (IL17E) is a cytokine that induces Nf-kappaB and IL8 activation. It might also be involved in the enhancement, prolongation, or both of TH2 cell-mediated allergic diseases, such as asthma. It may therefore have an anti-inflammatory effect.
- Lorus is developing an anticancer targeting IL-17E.
- Interleukin 25 belongs to the Cytokine/Growth Factor > Cytokine > Interleukin Target Family Group. Its Entrez Gene ID is 64806.
transient receptor potential cation channel, subfamily V, member 3
Also known as TRPV3, this channel is a member of non-selective cation channels receptors. It acts to mediate thermosensitivity, and is co-expressed with TRPV1 in the dosal root ganglion of the sensory neurone. Increased expression of these two TRP’s has been found in injured dorsal root ganglion.
- Hydra Biosciences is developing a series of transient receptor potential channel modulators targeting TRPV3 for the treatment of pain.
- TRPV3 belongs to the Ion Channel > Transient receptor potential Target Family Group. Its Entrez Gene ID is 162514.
potassium voltage-gated channel, shaker-related subfamily, member 2
Potassium channels are involved in many diverse functions, including regulating neurotransmitter release, heart rate, insulin secretion, neuronal excitability, epithelial electrolyte transport, smooth muscle contraction, and cell volume. Potassium channels are abundant in every cell. Also known as Kv1.2, this target is uniformly distributed in the brain and heart and allows repolorization of nerve cells following an action potential.
- Evotec is developing Kv1.2 antagonists for the treatment of inflammation.
- Kv1.2 belongs to the Ion Channel > Potassium Target Family Group. Its Entrez Gene ID is 3737.
