- 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 ...
A synthetic analog of fumagillin, an antibiotic isolated from the fungus Aspergillus fumigatus fresenius with antineoplastic activity. TNP-470 binds to and irreversibly inactivates methionine animopeptidase-2 (MetAP2), resulting in endothelial cell cycle arrest late in the G1 phase and inhibition of tumor angiogenesis. This agent may also induce the p53 pathway, thereby stimulating the production of cyclin-dependent kinase inhibitor p21 and inhibiting angiogenesis.
Industry:Pharmaceutical
A synthetic analogue of 9-cis retinoic acid with potential antineoplastic and chemopreventive activities. Retinoid 9cUAB30 binds to and activates retinoid X receptor (RXR) homodimers and/or and retinoic acid receptor (RAR)/RXR heterodimers, which may result in the dissociation of corepressor protein and the recruitment of coactivator protein, followed by transcription of downstream target genes into mRNAs and protein translation. Gene transcription regulated by these transcription factors may result in inhibition of cell proliferation, induction of cell differentiation, and apoptosis of both normal cells and tumor cells.
Industry:Pharmaceutical
A synthetic analogue of nucleoside uridine lacking a ring nitrogen in the 3-position. 3-deazauridine inhibits cytidine synthase, thereby reducing intracellular levels of cytidine and deoxycytidine and disrupting DNA and RNA synthesis. This agent may trigger apoptosis and enhance differentiation of neoplastic cells. .
Industry:Pharmaceutical
A synthetic analogue of the naturally occurring prostaglandin F2 alpha. Prostaglandin F2 alpha stimulates myometrial activity, relaxes the cervix, inhibits corpus luteal steroidogenesis, and induces luteolysis by direct action on the corpus luteum.
Industry:Pharmaceutical
A synthetic antifolate agent with antiparasitic, antipsoriatic and antitumor properties. Piritrexim inhibits the enzyme dihydrofolate reductase enzyme, thereby disrupting folate metabolism and DNA synthesis and cell division.
Industry:Pharmaceutical
A synthetic antisense oligodeoxynucleotide (AS ODN) targeting hypoxia-inducible factor-1alpha (HIF-1alpha) with potential antineoplastic activity. Anti-HIF-1alpha LNA antisense oligonucleotide EZN-2968 hybridizes with HIF-1alpha mRNA and blocks t HIF-1 alpha protein expression, which may result in the inhibition of angiogenesis, the inhibition of tumor cell proliferation, and apoptosis. HIF-1alpha, normally activated in response to hypoxia-induced stress, is a key transcription regulator of a large number of genes important in cellular adaptation to low-oxygen conditions, including angiogenesis, cell proliferation, apoptosis, and cell invasion.
Industry:Pharmaceutical
A synthetic antisense oligonucleotide against Bcl-2 messenger RNA with potential antitumor activity. Oligonucleotide SPC2996 binds to and inactivates Bcl-2 mRNA, thereby inhibiting the expression of Bcl-2 protein, promoting tumor cell apoptosis, and potentially enhancing the efficacy of standard cytotoxic chemotherapy. Linked to tumor drug resistance, the antiapoptotic protein Bcl-2 is upregulated in several types of cancers.
Industry:Pharmaceutical
A synthetic antiviral acyclic nucleotide analogue of adenosine 5-monophosphate. Tenofovir is incorporated into human immunodeficiency viral DNA instead of the natural substrate deoxyadenosine 5-triphosphate, thereby inhibiting HIV-1 reverse transcriptase (RT), an RNA-dependent DNA polymerase, and resulting in DNA chain termination and impairment of viral replication and propagation. This agent prevents HIV from reproducing in uninfected cells only. Tenofovir exhibits activity against the hepatitis B virus (HBV).
Industry:Pharmaceutical
A synthetic Arg-Gly-Asp (RGD)-containing cyclic peptide radiolabeled with technetium Tc 99m with integrin-binding and radioisotopic activities. Upon administration, technetium Tc 99m-NC100692 binds to alpha5beta3 integrin and to a lesser extent alpha5beta5; subsequently, alpha5beta3-expressing tumor cells can be visualized using scintigraphy and the degree of tumor angiogenesis can be determined. Integrins, membrane-spanning protein receptors, may be upregulated on proliferating endothelial cells; their overexpression has been associated with neovascularization, differentiation, proliferation of tumor cells and poor prognosis.
Industry:Pharmaceutical
A synthetic benzamide derivative with potential antineoplastic activity. Entinostat binds to and inhibits histone deacetylase, an enzyme that regulates chromatin structure and gene transcription. This agent appears to exert dose-dependent effects in human leukemia cells including cyclin-dependent kinase inhibitor 1A (p21/CIP1/WAF1)-dependent growth arrest and differentiation at low drug concentrations; a marked induction of reactive oxygen species (ROS); mitochondrial damage; caspase activation; and, at higher concentrations, apoptosis. In normal cells, cyclin-dependent kinase inhibitor 1A expression has been associated with cell-cycle exit and differentiation.
Industry:Pharmaceutical
