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  • Interactions
  • Reduced drug-HSA interactions could result in improved activity. (wikipedia.org)
  • Silatecans or 7-silylcampthothecins have shown reduced drug-HSA interactions which contributes to its blood stability and they can also cross the blood brain barrier. (wikipedia.org)
  • The idea that the effect of a drug in the human body is mediated by specific interactions of the drug molecule with biological macromolecules, (proteins or nucleic acids in most cases) led scientists to the conclusion that individual chemicals are required for the biological activity of the drug. (wikipedia.org)
  • Ligand binding assays provide a measure of the interactions that occur between two molecules, such as protein-bindings, as well as the degree of affinity (weak, strong, or no connection) for which the reactants bind together. (wikipedia.org)
  • compounds
  • Inhibition of Abl kinase in biochemical assays was maintained for most compounds, but in general the kinase selectivity profile differed from that of 1 with nearly equipotent inhibition of the wild-type and the Imatinib resistant Abl T(315)I mutant. (uni-regensburg.de)
  • Many natural compounds have led to the discovery of drugs used to treat human disease. (wikipedia.org)
  • In 1969, Stähelin made the key decision to include a test system for immunosuppression into the general screening program at Sandoz for compounds and extracts. (wikipedia.org)
  • One of the most potent compounds is the oxyiminomethyl derivative ST1481 that has the advantage to overcome drug resistance caused by transport systems. (wikipedia.org)
  • Examples of drug compounds isolated from crude preparations are morphine, the active agent in opium, and digoxin, a heart stimulant originating from Digitalis lanata. (wikipedia.org)
  • Later, small molecules were synthesized to specifically target a known physiological/pathological pathway, avoiding the mass screening of banks of stored compounds. (wikipedia.org)
  • ligands
  • From a mechanistic perspective, the FR functions to concentrate exogenous ligands (e.g. folates and folate-drug conjugates) into the cell cytosol by endocytosis. (wikipedia.org)
  • Some newer types are called "mix-and-measure" assays because they do not require separation of bound ligands. (wikipedia.org)
  • Combinations
  • Chemotherapy may be given with a curative intent (which almost always involves combinations of drugs), or it may aim to prolong life or to reduce symptoms (palliative chemotherapy). (wikipedia.org)
  • reactions
  • Essential aspects of binding assays include, but are not limited to, the concentration level of reactants or products (see radioactive section), maintaining the equilibrium constant of reactants throughout the assay, and the reliability and validity of linked reactions. (wikipedia.org)
  • paclitaxel
  • Assess response to paclitaxel therapy in patients who have undergone a pretreatment EDR assay. (clinicaltrials.gov)
  • Paclitaxel drug eluting coated stents for coronary artery placement are sold under the trade name Taxus by Boston Scientific in the United States. (wikipedia.org)
  • Paclitaxel is one of several cytoskeletal drugs that target tubulin. (wikipedia.org)
  • competitive
  • BMS-354825 (dasatinib) is an ATP-competitive small-molecule inhibitor effective in treating drug-resistant tumors with mutant BCR-ABL, KIT, and epidermal growth factor receptor by blocking tyrosine phosphorylation sites that are critical in tumorigenesis. (biomedsearch.com)
  • Human
  • Based on the natural high affinity of folate for the folate receptor protein (FR), which is commonly expressed on the surface of many human cancers, folate-drug conjugates also bind tightly to the FR and trigger cellular uptake via endocytosis. (wikipedia.org)
  • Specifically, despite the human body's endogenous receptors, hormones, and other neurotransmitters, pharmacologists utilize assays in order to create drugs that are selective, or mimic, the endogenously found cellular components. (wikipedia.org)
  • chemistry
  • As a direct result of these monumental findings, researchers have continued the advancement of ligand binding assays in many facets in the fields of biology, chemistry, and the like. (wikipedia.org)
  • binds
  • Mytomycin C (MC), an antibiotic produced by S. lavendulae, exhibits cytotoxicity when the activated drug covalently binds complementary strands of DNA. (wikipedia.org)
  • The second locus (mrd) binds with MC as a complex which prevents drug activation. (wikipedia.org)
  • Yeast three-hybrid assays have shown that this protein binds to the stem loops within the 3'UTR of the POLB mRNA, however the exact mechanism in how this protein regulates gene expression is still to be determined. (wikipedia.org)
  • chemical
  • Using a chemical complementation assay, we found that NSC 663284 blocked cellular Erk dephosphorylation caused by ectopic Cdc25A expression. (pitt.edu)
  • Screening of chemical libraries for AR blockers led to the discovery of the first antiandrogen, cyproterone. (wikipedia.org)
  • Therefore, in order to be sure what process or processes are producing the measured heat flow, great care must be taken in both experimental design and in the initial use of related chemical, physical and biologic assays. (wikipedia.org)
  • Evaluation
  • MHC tetramers are used in studies of pathogen immunity and vaccine development, in evaluation of antitumor responses, in allergy monitoring and desensitization studies, and in autoimmunity. (wikipedia.org)
  • involves
  • Modern drug discovery is thus usually a capital-intensive process that involves large investments by pharmaceutical industry corporations as well as national governments (who provide grants and loan guarantees). (wikipedia.org)
  • Discovering drugs that may be a commercial success, or a public health success, involves a complex interaction between investors, industry, academia, patent laws, regulatory exclusivity, marketing and the need to balance secrecy with communication. (wikipedia.org)
  • Combination chemotherapy involves treating a patient with a number of different drugs simultaneously. (wikipedia.org)
  • Proteins
  • The foundations for which ligand binding assay have been built are a result of Karl Landsteiner, in 1945, and his work on immunization of animals through the production of antibodies for certain proteins. (wikipedia.org)
  • time
  • As a flow-cytometry-based application, tetramers are also easy to use and have a short assay time, similar to Antibody-based flow cytometry studies. (wikipedia.org)
  • cell
  • Treatment with RA caused an increase in the cytotoxicity of all 3 drugs to the 2 RA-sensitive cell lines. (uni-regensburg.de)
  • Crizotinib received accelerated approval for the treatment of patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) that is ALK-positive as detected by a test approved by the U.S. Food and Drug Administration (FDA). (wikipedia.org)
  • development
  • Such advances provide researchers with the ability not only to quantify hormones and hormone receptors, but also to contribute important pharmacological information in drug development and treatment plans. (wikipedia.org)
  • Type
  • Testing patients' blood or bone marrow to find out if their type of cancer may be sensitive to a specific drug may help doctors choose more effective treatments. (clinicaltrials.gov)
  • treatment
  • In 1989 the United States Food and Drug Administration (FDA) approved it for use the treatment of prostate cancer. (wikipedia.org)
  • Induction chemotherapy is the first line treatment of cancer with a chemotherapeutic drug. (wikipedia.org)
  • This was approved by the U.S. Food and Drug Administration in January 2005 for the treatment of breast cancer after failure of combination chemotherapy for metastatic disease or relapse within six months of adjuvant chemotherapy. (wikipedia.org)