Jan2008 Drug Protein Targets
indoleamine-pyrrole 2,3 dioxygenase
Indoleamine-pyrrole 2,3 dioxygenase (IDO) catalyzes the conversion of tryptophan to N-formylkynurenine, the first and rate-limiting step of tryptophan catabolism through the kynurenine pathway. Over expressed in tumour cells, IDO enables cancer cells to escape immune response, as depleted tryptophan levels sensitize activated T cells to apoptosis. Reduced tryptophan levels also halt microbe growth.
- NewLink Genetics is developing NLG-001, a small molecule IDO inhibitor for the treatment of cancer.
- IDO belongs to the Enzyme > Oxygenase Target Family Group and its EC number is 1.13.11.52. Its Entrez Gene ID is 3620.
peptidylprolyl isomerase B (cyclophilin B)
Sometimes referred to as CYPB or PPIB, this enzyme is predominantly located in the endoplasmic reticulum. Interactions with HIV-1 gp120 and Pr55gag as well as stimulation of the RNA binding activity of the Hepatitis C RNA polymerase NS5B have been reported.
- Scynexis is developing SCY-635, a CYPB inhibitor for the treatment of HCV and HIV infection.
- CYPB belongs to the Enzyme > Isomerase Target Family Group and its EC number is 5.2.1.8. Its Entrez Gene ID is 5479.
pyruvate dehydrogenase kinase, isozyme 1
Pyruvate dehydrogenase kinase, isozyme 1 (PDK1) is a key regulator of the mitochondrial pyruvate dehydrogenase complex (PDC). PDC is responsible for the conversion of pyruvate into Acetyl-CoA and thus plays an important role in the regulation of glucose metabolism. PDC is comprised of multiple copies of three enzymes: E1, E2 and E3. Phosphorylation of the E1 alpha subunit by PDK1 inactivates E1 and consequently the entire PDC.
- SBIO is developing a PDK1 inhibitor, for the treatment of cancer.
- PDK1 belongs to the Enzyme > Dehydrogenase and Kinase Target Family Groups and its EC number is 2.7.11.2. Its Entrez Gene ID is 5163.
sphingosine-1-phosphate lyase 1
Also known as SGPL1, this enzyme catalyses the cleavage of the signalling molecule sphingosine 1-phosphate. Research shows potential roles in stress-induced ceramide generation and apoptosis as well as the control of lymphocyte trafficking during inflammatory responses.
- Lexicon Pharmaceuticals is developing LX-2931 a sphingosine-1-phosphate lyase inhibitor for the treatment of rheumatoid arthritis and multiple sclerosis.
- SGPL1 belongs to the Enzyme Target Family Group and its EC number is 4.1.2.27. Its Entrez Gene ID is 8879.
CD274 molecule
More commonly known as PDL1 or B7-H1, this molecule is a ligand for programmed cell death 1 (PDCD1). Interaction with PDCD1 results in inhibition of T-cell proliferation and cytokine production.
- Medarex is developing MDX-1105, an anti-CD274 monoclonal antibody as an anticancer and believes it has potential in melanoma, prostate, lung, oesophageal and colorectal cancers.
- CD274 belongs to the Receptor Target Family Group. Its Entrez Gene ID is 29126.
V-set and immunoglobulin domain containing 1
V-set and immunoglobulin domain containing 1 (VSIG1) is a glycoprotein member of the junctional adhesion molecule family. It is primarily located in the stomach mucosa and in testicular germ cells. It is expressed at high levels in gastric, oesophageal and ovarian cancer tumour cells.
- Recepta biopharma is developing A34 (209-342), a MAb targeting VSIG1 for the treatment of cancer.
- The Entrez Gene ID for VSIG1 is 340547.
kinase suppressor of ras 1
Kinase suppresor of ras 1 (KSR1) acts as a positive regulator of Ras-dependant signalling. It interacts with several members of the MAPK pathway, including Raf, MEK and ERK. KSR1 may act as a scaffold, facilitating the assembly of the Raf/MEK complex.
- Ras Therapeutics is developing RAS-001, an antisense oligonucleotide that targets KSR1 for the treatment of cancer.
- KSR1 belongs to the Enzyme > Kinase Target Family Group and its EC number is 2.7.1. Its Entrez Gene ID is 8844.
- Omeros is developing antibodies against MASP2 and believes they may have potential in age-related macular degeneration, rheumatoid arthritis, ischaemia-reperfusion injury associated with myocardial infarction and renal disease.
- MASP2 belongs to the Enzyme > Peptidase/protease Target Family Group and its EC number is 3.4.21.104. Its Entrez Gene ID is 10747.
mannan-binding lectin serine peptidase 2
Also known as MASP2, this is a member of the serine protease family involved in the activation of the complement system via the mannan-binding lectin pathway. It cleaves complement components C4 and C2, leading to the generation of the C3 convertase C4bC2b.
Pharmaprojects - New protein targets for drug development
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