- Branża: Government; Health care
- Number of terms: 6957
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- 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 ...
The orally bioavailable dihydrochloride salt of the thiazolidinedione inolitazone with potential antineoplastic activity. Inolitazone binds to and activates peroxisome proliferation-activated receptor gamma (PPAR-gamma), which may result in the induction of tumor cell differentiation and apoptosis, and so a reduction in tumor cell proliferation. PPAR-gamma is a nuclear hormone receptor and ligand-activated transcription factor controlling gene expression involved in such cellular processes as differentiation, apoptosis, cell-cycle control, carcinogenesis, and inflammation.
Industry:Pharmaceutical
The orally bioavailable copper salt of D-gluconic acid. In addition to its roles as an enzyme cofactor for cytochrome C oxidase and superoxide dismutase, copper forms complexes with the thiocarbamate disulfiram (DSF) forming DSF-copper complexes, which enhances the DSF-mediated inhibition of the 26S proteasome; proteasome inhibition may result in inhibition of cellular protein degradation, cessation of cell cycle progression, inhibition of cellular proliferation, and the induction of apoptosis in susceptible tumor cell populations.
Industry:Pharmaceutical
The orally bioavailable citrate salt of enclomiphene, the trans-isomer of the nonsteroidal triphenylethylene compound clomiphene, with tissue-selective estrogenic and antiestrogenic activities. As a selective estrogen receptor modulator (SERM), enclomiphene binds to hypothalamic estrogen receptors, blocking the negative feedback of endogenous estrogens and stimulating the release of gonadotropin-releasing hormone (GnRH) from the hypothalamus; released GnRH subsequently stimulates the release of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) from the anterior pituitary, resulting in ovulation. In addition, this agent may bind to estrogen receptors on breast cancer cells, resulting in the inhibition of estrogen-stimulated proliferation in susceptible cell populations.
Industry:Pharmaceutical
The orally bioavailable calcium salt of glucaric acid, a natural substance found in many fruits and vegetables, with potential chemopreventive activity. After absorption, glucaric acid is converted to d-glucaro-1,4-lactone which inhibits beta-glucuronidase, an enzyme found in certain bacteria that reside in the human gut. The detoxification of various toxin and sex hormone metabolites depends upon their conjugation to glucuronic acid in the liver and subsequent excretion of glucuronic acid conjugated metabolites in the bile. Bacterial beta-glucuronidase may catalyze the deconjugation of glucuronic acid conjugated metabolites of toxins and sex hormones, thus prolonging exposure to unconjugated and unexcreted toxin and sex hormone metabolites. Accordingly, calcium glucarate supplementation may indirectly inhibit sex hormone-mediated and toxin-mediated tumorigenesis by inhibiting bacterial beta-glucuronidase activity. Elevated bacterial beta-glucuronidase activity may be associated with an increased risk for sex hormone-mediated and toxin-mediated cancers such as breast, prostate, and colon cancers.
Industry:Pharmaceutical
The orally bioavailable C-4 methyl carbonate analogue of paclitaxel, labeled with radioactive carbon 14, with radioisotope and potential antineoplastic activities. 14C BMS-275183 binds to tubulin and inhibits microtubule disassembly, which may result in cell cycle arrest at the G2/M phase and inhibition of cell division, and subsequently cell death. This agent may be useful for treating multi-drug resistant (MDR) tumors because it does not appear to be a substrate for P-glycoprotein.
Industry:Pharmaceutical
The orally bioavailable bismesylate salt of a potent small-molecule thieno(3,2-d)pyrimidine inhibitor of the class I phosphatidylinositol 3 kinase (PI3K) isoforms p100alpha and p100delta with potential antineoplastic activity. PI3K inhibitor GDC-0941 selectively binds to PI3K isoforms in an ATP-competitive manner, inhibiting the production of the secondary messenger phosphatidylinositol-3,4,5-trisphosphate (PIP3) and activation of the PI3K/Akt signaling pathway; inhibition of tumor cell growth, motility and survival in susceptible tumor cell populations may result. Activation of the PI3K/Akt signaling pathway is frequently associated with tumorigenesis; dysregulated PI3K/Akt signaling may contribute to tumor resistance to a variety of antineoplastic agents.
Industry:Pharmaceutical
The non-glycosylated recombinant interferon alpha, subtype 1b, with immunostimulatory and antineoplastic activities. Alpha interferon-1b binds to specific cell-surface receptors, resulting in the transcription and translation of genes whose protein products mediate antiviral, antiproliferative, anticancer, and immune-modulating effects.
Industry:Pharmaceutical
The neurotransmitter analogue 3-nitrobenzylguanidine conjugated to iodine I 123 and used as a gamma-emitting imaging agent. The adrenergic tissue uptake and storage of I-123 metaiodobenzylguanidine (I-123 MIBG) mimics that of norepinephrine (NE). The distribution of this agent enables the scintigraphic imaging of neural crest tumors, such as neuroblastoma and pheochromocytoma.
Industry:Pharmaceutical
The most potent androgen, required for sex development. Dihydrotestosterone is synthesized from testosterone in the prostate gland, testes, hair follicles and adrenal glands by 5-alpha reductase. Dihydrotestosterone exerts its action similar to testosterone, which binds to and activates specific nuclear androgen receptors. After translocation into the nucleus, the activated hormone-receptor complex binds to the androgen response elements on the DNA and activates gene expressions that are required for sex development. Dihydrotestosterone is responsible for the formation of male primary sex characteristics and most male secondary sex characteristics during puberty, such as muscular growth, facial and body hair growth, and deepening of the voice.
Industry:Pharmaceutical
The monohydrate form of creatine similar or identical to endogenous creatine produced in the liver, kidneys, and pancreas. Creatine, in phosphate form, helps supply energy to muscle cells for contraction. After intense effort, when ATP deposits are depleted, creatine phosphate donates phosphate groups toward the fast synthesis of ATP. Dietary supplementation with creatine may improve muscle wasting associated with cancer and other chronic diseases.
Industry:Pharmaceutical
