20 November, 2018
Single-use technology, designed for the manufacturing of biopharmaceutical products, has made major inroads over the last 30 years. First introduced in the late 1970s in the form of disposable capsules and a ...
A natural product member of the enediyne class of antitumor antibiotics that generates double strand DNA breaks.
Ricart AD, Tolcher AW. Technology insight: cytotoxic drug immunoconjugates for cancer therapy. Nat Clin Pract Oncol. 2007;4:245-255.
Also See: Calicheamicin
A novel antibiotic, produced by Streptomyces zelensis, active against several experimental tumors in vivo and a broad spectrum of human tumor cells in vitro.
Li LH, Swenson DH, Schpok SLF, Kuentzel SL, Dayton BD, Krueger WC. CC-1065 (NSC 298223), a novel antitumor agent that interacts strongly with double-stranded DNA. Cancer Res.
Cyclin-dependent kinases (CDK)
Cyclin-dependent kinases (CDK) are key positive regulators of cell cycle progression and attractive targets in oncology.
Dinacyclib (SCH 727965), a pyrazolo[1,5-a]pyrimidine with potential antineoplastic activity selectively inhibits cyclin dependent kinases CDK1, CDK2, CDK5, and CDK9; inhibition of CDK1 and CDK2 and may result in cell cycle g> and tumor cell apoptosis.
Pertaining to a toxin or antibody that has a specific toxic action upon cells of special organs.
Dorland’s Illustrated Medical Dictionary. 30th Edition. Philadelphia, Pennsylvania: Saunders, an imprint of Elsevier; 2003:471.
Denaturants are chemical or physical agents that can induce unfolding of the polypeptide chain. Denaturants include Acids (Acetic acid, Trichloroacetic acid 12% in water and Sulfosalicylic acid), Solvents (Ethanol, Methanol), Cross-linking reagents (Formaldehyde, Glutaraldehyde), Chaotropic agents (Urea 6 – 8 mol/l, Guanidinium chloride 6 mol/l, Lithium perchlorate 4.5 mol/l), Disulfide bond reducers (2-Mercaptoethanol, Dithiothreitol, TCEP (tris[2-carboxyethyl]phosphine]), other causes/agents (Picric acid, Radiation Temperature/Heat)
Denaturants either interact directly with the protein, or they can alter the properties of the surrounding aqueous environment. Unfolded proteins adopt a largely disordered structure.
See: Unfolding (protein)
Denaturation is a process in which external stress or compounds cause proteins or nucleic acids to lose the quaternary structure, tertiary structure and secondary structure which is present in their native state. If proteins in a living cell are denatured, this results in disruption of cell activity and possibly cell death. Denatured proteins can exhibit a wide range of characteristics, from loss of solubility to communal aggregation.
See: Unfolding (protein)
A structural unit composed of a linked pair of sulfur atoms (A compound of a base with 2 atoms of sulfur). Disulfide usually refer to a chemical compound that contains a disulfide bond.
Dolastatin 10 and dolastatin 15 were originally isolated from the Indian Ocean sea hare Dollabella auricularia. It is also isolated from the marine cyanobacterium Symploca sp. VP642 from Palau. These small linear peptide molecules are promising anti-cancer drugs showing potency against breast and liver cancers, solid tumors and some leukemias. Preclinical research indicated potency in experimental antineoplastic and tubulin assembly systems. The dolastatins are mitotic inhibitors. They interfere with tubulin formation and thereby disrupt cell division by mitosis. These molecules bind to tubulin at a location known as the vinca/peptide region.
Auristatins are potent synthetic analogs of dolastatin 10.
Also see: Dolastatins
An anthracycline antibiotic produced by Streptomyces peucetius var. caesius having one of the widest spectrums of antitumor activity of any antineoplastic agent.
Dorland’s Illustrated Medical Dictionary. 30th Edition. Philadelphia, Pennsylvania: Saunders, an imprint of Elsevier; 2003:563.
The uptake by a cell of material from the environment by invagination of its plasma membrane.
Dorland’s Illustrated Medical Dictionary. 30th Edition. Philadelphia, Pennsylvania: Saunders, an imprint of Elsevier; 2003:613.
20 November, 2018
05 October, 2018
When the first antibody-drug conjugate (ADC) was approved by the U.S. Food and Drug Administration (FDA) in 2000, only a handful of patent applications claiming ADCs had been published. As research cont...