- Industry: 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 small-molecule pyridylsulfonamide inhibitor of phosphatidylinositol 3-kinase (PI3K) with potential antineoplastic activity. PI3K inhibitor GSK2126458 binds to and inhibits PI3K in the PI3K/mTOR signaling pathway, which may trigger the translocation of cytosolic Bax to the mitochondrial outer membrane, increasing mitochondrial membrane permeability and inducing apoptotic cell death. Bax is a member of the proapoptotic Bcl2 family of proteins. PI3K, often overexpressed in cancer cells, plays a crucial role in tumor cell regulation and survival.
Industry:Pharmaceutical
A small-molecule radiopharmaceutical consisting of the beta-emitting radioisotope iodine I 131 attached to a phospholipid ether (PLE) analogue, comprised of a linear 18 carbon backbone, with potential antineoplastic activity. Iodine I 131 phospholipid ether analogue CLR1404 selectively accumulates in tumor cells, thereby delivering a cytotoxic dose of radiation to cancer cells. Compared to normal cells, tumor cells are unable to metabolize and eliminate PLEs possibly due to deficiency of the enzyme phospholipase-D. In addition, the radioiodine moiety of this agent is resistant to de-iodination.
Industry:Pharmaceutical
A small-molecule Toll-like receptor 8 (TLR8) agonist with potential immunostimulating and antineoplastic activities. TLR8 agonist VTX-2337 binds to TLR8, present in cutaneous dendritic cells, monocytes/macrophages, and mast cells, which may result in the activation of the central transcription factor nuclear factor-B, the secretion of proinflammatory cytokines and other mediators, and a Th1-weighted antitumoral cellular immune response. Primarily localized to endosomal membranes intracellularly, TLR8, like other TLRs, recognizes pathogen-associated molecular patterns (PAMPs) and plays a key role in the innate immune system.
Industry:Pharmaceutical
A small-molecule wortmannin analogue inhibitor of the alpha, gamma, and delta isoforms of phosphoinositide 3-kinase (PI3K) with potential antineoplastic activity. PI3K inhibitor PX-866 inhibits the production of the secondary messenger phosphatidylinositol-3,4,5-trisphosphate (PIP3) and activation of the PI3K/Akt signaling pathway, which may result in inhibition of tumor cell growth and survival in susceptible tumor cell populations. Activation of the PI3K/Akt signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K/Akt signaling may contribute to tumor resistance to a variety of antineoplastic agents.
Industry:Pharmaceutical
A soluble fusion protein composed of the extracellular domain of the activin receptor type IIA (ActRIIA) linked to the Fc portion of human IgG1 with anabolic bone activity. Decoy activin receptor ACE-011 selectively binds to activin, inhibiting its binding to ActRIIA and ActRIIA signaling, resulting in the stimulation of osteoblast activity and the inhibition of osteoclast activity and so normal bone formation and increased bone mineral density and strength. The Fc moiety of this fusion protein binds to the salvage receptor FcRN, preventing its lysosomal degradation and so extending its half-life in the circulatory system.
Industry:Pharmaceutical
A soluble fusion protein consisting of the extracellular domain of human fibroblast growth factor receptor 1 (FGFR1) fused to the Fc portion of human immunoglobulin G1 (IgG1) with potential antineoplastic and anti-angiogenic activities. FGFR1 receptor antagonist FP-1039 prevents FGFR ligands, such as FGF1, FGF2, FGF4, from binding to their cognate receptors, thereby inhibiting the activation of the related FGFR tyrosine kinases. Inhibition of FGFR1 by this agent may retard tumor cell proliferation and induce tumor cell death. FP-1039 may also inhibit vascular endothelial growth factor (VEGF)-induced angiogenesis. FGFR1 is a receptor tyrosine kinase upregulated in certain tumor cells and involved in tumor cellular proliferation, differentiation, angiogenesis, and survival; most ligands that bind to FGFR1 also bind to the related receptors FGFR3 and FGFR4.
Industry:Pharmaceutical
A soluble fusion protein containing the extracellular domain of activin receptor-like kinase-1 (ALK1) fused to a human Fc domain (ALK1-Fc fusion protein), with potential antiangiogenic and antineoplastic activities. Upon administration, ALK1 inhibitor ACE-041 binds to various ALK1 ligands, preventing activation of tumor cell ALK1 receptors and so inhibiting the ALK1 signaling pathway; growth factor-induced angiogenesis is thus inhibited, which may result in the inhibition of tumor cell proliferation and tumor cell death. ALK1 is a type I cell surface receptor with serine/threonine kinase activity that mediates signaling by members of the transforming growth factor-beta (TGFbeta) superfamily and plays a key role in angiogenesis; ligands for this receptor include TGFbeta1 and TGFbeta2. The Fc moiety of this fusion protein mediates clearance of ligand-fusion protein complexes by the reticuloendothelial system (RES).
Industry:Pharmaceutical
A soluble, thapsigargin prodrug containing the cytotoxic analog of thapsigargin, 8-O-(12Aminododecanoyl)-8-O debutanoylthapsigargin (12-ADT) linked, via a carboxyl group, to the targeting peptide containing aspartic acid with potential antineoplastic activity. Upon intravenous administration, the non-toxic prodrug targets prostate specific membrane antigen (PSMA), a type II membrane carboxypeptidase, which is overexpressed in prostate cancer cells and in the neovasculature of most solid tumors but not in normal blood vessels. G-202 is subsequently converted, through hydrolysis, into the active cytotoxic analog of thapsigargin 12-ADT-Asp. 12-ADT binds to and blocks the Sarcoplasmic/Endoplasmic Reticulum Calcium ATPase (SERCA) pump, thereby increasing the concentration of cytosolic calcium which leads to an induction of apoptosis. By preventing nutrient supply to tumor cells, G-202 may be able to inhibit tumor growth. Compared to thapsigargin alone, thapsigargin prodrug G-202 is able to achieve higher concentrations of the active agents at the tumor site while avoiding systemic toxicity.
Industry:Pharmaceutical
A solution of formaldehyde-deactivated toxin isolated from the bacterium Clostridium tetani. Tetanus toxoid stimulates the production of antitoxin antibodies. This agent may be used as an adjuvant in cancer vaccines.
Industry:Pharmaceutical
A soy-based powdered nutritional supplement drink containing carrot, Jilin ginseng, licorice root and tangerine peel with potential antioxidant, immunomodulating and protective activities. Besides vitamin C, E and other phytochemicals, carrot/Jilin ginseng/licorice root/tangerine peel/soy beverage contains a high amount of soy protein. This beverage may have a beneficial effect on overall nutrition and the immune system.
Industry:Pharmaceutical
