- Industria: Government; Health care
- Number of terms: 6957
- Number of blossaries: 0
- Company Profile:
The National Cancer Institute (NCI) is part of the National Institutes of Health (NIH), which is one of 11 agencies that compose the Department of Health and Human Services (HHS). The NCI, established under the National Cancer Institute Act of 1937, is the Federal Government's principal agency for ...
An orally bioavailable, small-molecule, tryptophan hydroxylase (TPH) inhibitor prodrug with potential antiserotonergic activity. Upon administration, TPH inhibitor LX1606 is converted to its active metabolite LP-778902, which binds to and blocks the activity of TPH. This may result in a reduction in peripheral serotonin (5-HT) production and improvement of serotonin-mediated gastrointestinal effects such as severe diarrhea. TPH, the rate-limiting enzyme in serotonin biosynthesis, is overexpressed in carcinoid tumor cells.
Industry:Pharmaceutical
An orally bioavailable, synthetic organic molecule targeting mitogen-activated protein kinase kinase (MAPK/ERK kinase or MEK) with potential antineoplastic activity. MEK inhibitor PD325901, a derivative of MEK inhibitor CI-1040, selectively binds to and inhibits MEK, which may result in the inhibition of the phosphorylation and activation of MAPK/ERK and the inhibition of tumor cell proliferation. The dual specific threonine/tyrosine kinase MEK is a key component of the RAS/RAF/MEK/ERK signaling pathway that is frequently activated in human tumors.
Industry:Pharmaceutical
An orally bioavailable, synthetic small-molecule antagonist of a subset of the B-cell leukemia 2 (Bcl-2) family of proteins with potential antineoplastic activity. BcI-2 family protein inhibitor ABT-263 selectively binds to apoptosis suppressor proteins Bcl-2, Bcl-XL, and Bcl-w and prevents their binding to the apoptotic effectors Bax and Bak proteins, which may trigger apoptosis in tumor cells overexpressing Bcl-2, Bcl-XL, and Bcl-w. Bcl-2, Bcl-XL, and Bcl-w are frequently overexpressed in a wide variety of cancers, including those of the lymphatic system, breast, lung, prostate, and colon, and have been linked to tumor drug resistance.
Industry:Pharmaceutical
An orally bioavailable, synthetic, highly selective adenosine A3 receptor (A3AR) agonist with potential antineoplastic activity. Adenosine A3 receptor agonist CF102 selectively binds to and activates the cell surface-expressed A3AR, deregulating Wnt and NF-kB signal transduction pathways downstream, which may result in apoptosis of A3AR-expressing tumor cells. A3AR, a G protein-coupled receptor, is highly expressed on the cell surfaces of various solid tumor cell types, including hepatocellular carcinoma (HCC) cells, and plays an important role in cellular proliferation.
Industry:Pharmaceutical
An orally bioavailable, synthetic, second-generation small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity. Hsp90 inhibitor MPC-3100 selectively binds to Hsp90, thereby inhibiting its chaperone function and promoting the degradation of oncogenic signaling proteins involved in tumor cell proliferation and survival; this agent may inhibit the growth and survival of a wide variety of cancer cell types. Hsp90, a chaperone protein upregulated in a variety of tumor cells, regulates the folding, stability, and degradation of many oncogenic signaling proteins.
Industry:Pharmaceutical
An orally bioavailable, synthetic, small-molecule multi-Aurora kinase inhibitor with potential antineoplastic activity. Aurora kinase inhibitor R763 selectively binds to and inhibits multiple Aurora kinases (AKs), which may result in the inhibition of cell division and proliferation, and the induction of apoptosis in tumor cells that overexpress AKs. Overexpressed in certain tumor cell types, AKs, a family of serine-threonine kinases, are important regulators of cell division and proliferation that are involved in controlling chromatid segregation.
Industry:Pharmaceutical
An orally-active agent with potential antineoplastic activity. Carboxyamidotriazole binds to and inhibits non-voltage-operated Ca2+ channels, blocking both Ca2+ influx into cells and Ca2+ release from intracellular stores and resulting in the disruption of calcium channel-mediated signal transduction and inhibition of vascular endothelial growth factor (VEGF) signaling, endothelial proliferation, and angiogenesis. This agent may also inhibit tumor cell growth, invasion and metastasis.
Industry:Pharmaceutical
An orally-active fluoropyrimidine analogue. Eniluracil inhibits dihydropyrimidine dehydrogenase, the rate-limiting enzyme that catabolizes and inactivates 5-fluorouracil (5-FU) in the liver. Co-administration of ethynyluracil permits the oral administration of 5-FU.
Industry:Pharmaceutical
An orally-active polyphenolic aldehyde with potential antineoplastic activity. Derived primarily from unrefined cottonseed oil, gossypol induces cell cycle arrest at the G0/G1 phase, thereby inhibiting DNA replication and inducing apoptosis. This agent also inhibits cell-signaling enzymes, resulting in inhibition of cell growth, and may act as a male contraceptive.
Industry:Pharmaceutical
An orally-active pyrimidine analogue of an aza-substituted cytidine in which the ribose moiety is replaced by an arabinose sugar. Similar in action to cytarabine, fazarabine is phosphorylated by deoxycytidine kinase to a triphosphate form which competes with thymidine for incorporation into DNA; its incorporation into DNA inhibits DNA synthesis, resulting in tumor cell death and tumor necrosis. The presence of deoxycytidine kinase in a tumor is a determinant of tumor sensitivity to this drug.
Industry:Pharmaceutical
