June 2009 Drug Protein Targets
cyclin E1
Also known as CCNE1, this member of the cyclin family interacts with CDK2 to form a serine/threonine kinase holoenzyme complex. The activity of this holoenzyme is required for cell cycle G1/S transition and is regulated by the cyclin E1 subunit. Overexpression of cyclin E1 has been observed in numerous tumour types.
- Seliciclib (CYC202) is the lead compound in the CYC200 series of small-molecule CDK inhibitors, under development by Cyclacel as an anticancer. It targets the CDK2/cyclin E complex.
- Its Entrez Gene ID is 898.
cyclin E2
Also referred to as CCNE2, this cyclin also interacts with CDK2 and plays a role in cell cycle G1/S transition, but has a different pattern of tissue expression to cyclin E1. Increased levels have been detected in tumour derived cells.
- Seliciclib (CYC202) is the lead compound in the CYC200 series of small-molecule CDK inhibitors, under development by Cyclacel as an anticancer. It targets the CDK2/cyclin E complex.
- Its Entrez Gene ID is 9134.
VP24, Zaire Ebola virus
The Zaire Ebola virus protein VP24 inhibits IFN-alpha/beta and IFN-gamma signalling pathways and as such prevents the cell establishing an antiviral state. It may play a role in viral nucleocapsid assembly and virion budding.
- AVI-6002 is an antisense compound, under co-development by AVI BioPharma and the US Army Medical Research Institute of Infectious Diseases for the treatment of Ebola virus infection. It targets 2 independent sites in the Ebola Zaire virus genome, the VP35 and VP24 proteins.
- Its Entrez Gene ID is 911828.
VP35, Zaire Ebola virus
The Zaire Ebola virus protein VP35 blocks virus-induced phosphorylation and activation of interferon regulatory factor 3, a transcription factor that activates interferon-alpha and beta transcription. It is also a component of the viral RNA polymerase complex.
- AVI-6002 is an antisense compound, under co-development by AVI BioPharma and the US Army Medical Research Institute of Infectious Diseases for the treatment of Ebola virus infection. It targets 2 independent sites in the Ebola Zaire virus genome, the VP35 and VP24 proteins.
- Its Entrez Gene ID is 911827.
nicotinamide phosphoribosyltransferase
More commonly referred to as NAMPT, visfatin or PBEF1, this adipokine catalyses the condensation of nicotinamide to nicotinamide mononucleotide, the first step in the biosynthesis of NAD from nicotinamide.
- TopoTarget is developing NAMPT inhibitors for the treatment of cancer.
- NAMPT belongs to the Enzyme>Transferase Target Family Groups. Its EC number is 2.4.2.12. Its Entrez Gene ID is 10135.
apolipoprotein C-III
Apolipoprotein C-III (APOC3) is a very low density lipoprotein that inhibits lipoprotein liapse and hepatic lipase. It also decreases the uptake of lymph lipoprotein particles by hepatic cells. It may delay catabolism of triglyceride-rich particles and increased levels are associated with hypertriglyceridaemia.
- Isis Pharmaceuticals is developing an antisense oligonucleotide targeting APOC3 for the treatment of cardiovascular disease.
- Its Entrez Gene ID is 345.
apolipoprotein F
Also known as APOF, this minor apolipoprotein inhibits choleteryl ester transfer protein and may regulate cholesterol transport.
- Isis Pharmaceuticals is developing an antisense oligonucleotide targeting APOF for the treatment of cardiovascular disease.
- Its Entrez Gene ID is 319.
TTK protein kinase
This kinase phosphorylates proteins on serine, threonine and tyrosine. Research suggests involvement in cell proliferation.
- MPI-0479605 is a small molecule TTK kinase inhibitor, under development by Myriad Pharmaceuticals for the treatment of cancer.
- TTK belongs to the Enzyme>Transferase & Kinase Target Family Groups. Its EC number is 2.7.12.1. Its Entrez Gene ID is 7272.
Pharmaprojects - New protein targets for drug development
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