May 2009 Drug Protein Targets
peroxisome proliferator-activated receptor gamma, coactivator 1 beta
Also known as PPARGC1B, this protein is involved in the stimulation of transcription factor and nuclear receptor activity. Activation of estrogen receptor alpha, nuclear respiratory factor 1 and glucocorticoid receptor have been demonstrated. Variations in PPARGC1B may be associated with obesity.
- Isis Pharmaceuticals is developing an antisense oligonucleotide targeting PPARGC1B for the treatment of fructose-induced insulin resistance.
- Its Entrez Gene ID is 133522.
mitogen-activated protein kinase-activated protein kinase 5
This serine/threonine kinase, more commonly referred to as MAPKAPK5, is activated in response to cellular stress and proinflammatory cytokines. It phosphorylates heat shock protein 27.
- GLPG-0259 is a small molecule MAPKAPK5 inhibitor, under development by Galapagos for the treatment of rheumatoid arthritis.
- MAPKAPK5 belongs to the Enzyme>Kinase Target Family Groups. Its EC number is 2.7.11.1. Its Entrez Gene ID is 8550.
tyrosyl-DNA phosphodiesterase 1
Tyrosyl-DNA phosphodiesterase 1 (TDP1) is a DNA repair enzyme responsible for the removal of a number of covalent adducts from DNA through the hydrolysis of a 3'-phosphodiester bond. Mutations in TDP1 are associated with spinocerebeller ataxia amd axonal neuropathy.
- Aphios is developing a phospholipid nanosome formulation of camptothecin and a TDP1 inhibitor for the treatment of cancer.
- TDP1 belongs to the Enzyme>Esterase & Nuclease Target Family Groups. Its EC number is 3.1.4.1. Its Entrez Gene ID is 55775.
lysophosphatidic acid receptor 1
Also known as LPAR1, this protein is a member of the EDG sub-family of GPCRs. Coupling to the G(i)/G(o), G(12)/G(13) and G(q) families of G proteins has been demonstrated. EDG receptors are known to mediate a number of functions including proliferation, platelet aggregation, smooth muscle contraction, inhibition of neuroblastoma cell differentiation, chemotaxis and tumour cell invasion.
- Debio-0719 is a LPAR1 and LPAR3 inhibitor, under development by Kyowa Hakko Kirin for the treatment of cancer.
- LPAR1 belongs to the Receptor>GPCR Target Family Groups. Its Entrez Gene ID is 1902.
lysophosphatidic acid receptor 3
Lysophosphatidic acid receptor 3 (LPAR3) appears to couple to the G(i)/G(o) and G(q) families of G proteins. Involvement in lysophosphatidic acid-evoked calcium mobilization has been suggested.
- Debio-0719 is a LPAR1 and LPAR3 inhibitor, under development by Kyowa Hakko Kirin for the treatment of cancer.
- LPAR3 belongs to the Receptor>GPCR Target Family Groups. Its Entrez Gene ID is 23566.
Pharmaprojects - New protein targets for drug development
© Informa UK Ltd 2008
Registered Office: Mortimer House, 37-41 Mortimer Street, London W1T 3JH, UK.
Registered in England and Wales No: 1072954
