• Mechanism of Act
  • Determine the impact of genetic differences in proteins involved in drug response (transport, metabolism, and mechanism of action) on clinical response and adverse events associated with gemcitabine in these patients. (bioportfolio.com)
  • potent
  • SMARCB1 is a core protein subunit of the 15 subunit SWI/SNF (or BAF) complex involved in regulating the nucleosome architecture of our genome and has been shown to be a potent tumor suppressor gene, meaning that its primary role is to control cell division and to even halt division under appropriate circumstances (i.e. signals to over-replicate). (wikipedia.org)
  • peptide
  • Additional structures (3G60 and 3G61) of P-gp were also solved revealing the binding site(s) of two different cyclic peptide substrate/inhibitors. (wikipedia.org)
  • residues
  • The results supported the proposed function of the enzyme, as the amount of abnormal L-aspartate residues increased when cells were treated with the indirect inhibitor, adenosine dialdehyde. (wikipedia.org)
  • When PIMT is not present in cells, the abnormal aspartyl residues accumulate, creating abnormal proteins that have been known to cause fatal progressive epilepsy in mice. (wikipedia.org)
  • encode
  • However, ETV6 is also an anti-oncogene or tumor suppressor gene in that mutations in it that encode for a truncated and therefore inactive protein are also associated with certain types of cancers. (wikipedia.org)
  • These fusion genes encode fusion proteins that continuously stimulate cell growth, proliferation, prolonged survival, and/or differentiation. (wikipedia.org)
  • Therapeutics
  • Accordingly, our data provide valuable information for the further development of therapeutics targeting Lyn and the important Src-family of kinases. (edu.au)
  • genistein
  • This treatment did not alter the inhibitory effect of genistein, although it did result in irreversible protein kinase A-dependent regulation of the Ca 2+ current. (aspetjournals.org)
  • Bath application of lavendustin A, a PTK inhibitor that is structurally unrelated to genistein, did not affect the Ca 2+ current amplitude. (aspetjournals.org)
  • selective
  • Subsequent studies have confirmed that SU6656 is relatively selective for Src family kinases but some additional biochemical activities have been identified including: BRSK2, AMPK, Aurora C, Aurora B, CaMKKβ. (wikipedia.org)
  • In 2009 he was awarded the Lasker Clinical Award and in 2012 the Japan Prize for the development of Gleevec, a selective BCR-ABL inhibitor for the treatment of chronic myeloid leukaemia (CML), which converted a fatal cancer into a manageable chronic condition. (wikipedia.org)
  • sensitivity
  • Rsf-1 Influences the Sensitivity of Non-Small Cell Lung Cancer to Paclitaxel by Regulating NF-κB Pathway and Its Downstream Proteins. (bioportfolio.com)
  • Based on their association with eosinophils, unique genetic mutations, and known or potential sensitivity to tyrosine kinase inhibitors or other specific drug therapies, they are now in the process of being classified together under the term clonal hypereosinophilia or clonal eosinophilia. (wikipedia.org)
  • 2016
  • In this report, the United States Protein Kinase Inhibitor market is valued at USD XX million in 2016 and is expected to reach USD XX million by the end of 2022, growing at a CAGR of XX% between 2016 and 2022. (reportsnreports.com)
  • stimulate
  • The mutations cause these proteins to be continuously active and thereby to stimulate growth in an uncontrolled and continuous manner. (wikipedia.org)
  • activity
  • Although several Src-family inhibitors are available, the development of Lyn-specific inhibitors, or inhibitors with reduced off-target activity to Lyn, has been hampered by the lack of structural data on the Lyn kinase. (edu.au)
  • One such inhibitor, the p.o. active ZD1839 (Iressa), has pronounced antiproliferative activity against human tumor xenografts. (aacrjournals.org)
  • A 2015 review of polymorphisms in ABCB1 found that "the effect of ABCB1 variation on P-glycoprotein expression (messenger RNA and protein expression) and/or activity in various tissues (e.g. the liver, gut and heart) appears to be small. (wikipedia.org)
  • With the discovery of the uncontrolled tyrosine kinase activity of this disorder and the use of tyrosine kinase inhibitors. (wikipedia.org)
  • cells
  • Cells were harvested 18 h after transfection and lysed at 4 C in a Dounce homogenizer in 250 mm sucrose, 20 mm TrisHCl, 1 mm CaCl2, 1 mm MgCl2, cOmplete protease inhibitor cocktail (Roche Applied Science), pH 8. (molecularcircuit.com)
  • P-glycoprotein 1 (permeability glycoprotein, abbreviated as P-gp or Pgp) also known as multidrug resistance protein 1 (MDR1) or ATP-binding cassette sub-family B member 1 (ABCB1) or cluster of differentiation 243 (CD243) is an important protein of the cell membrane that pumps many foreign substances out of cells. (wikipedia.org)
  • As these proteins accumulate, they begin to form plaques that interfere with signaling between cells of the nervous system found within the brain. (wikipedia.org)
  • In treated cells the inhibitor blocks downstream cellular signalling (JAK-STAT) leading to suppression of proliferation and induction of apoptosis. (wikipedia.org)
  • dialdehyde
  • Increase of malonic dialdehyde (MDA) by 89% and protein carbonyl groups (PCG) by 60% and decrease of superoxide dismutase (SOD) by 40% were also observed. (hindawi.com)
  • regulates
  • The ETV6 protein regulates the development and growth of diverse cell types, particularly those of hematological tissues. (wikipedia.org)
  • Initially
  • SU6656 was initially identified as a Src kinase inhibitor by virtue of its ability to reverse an effect that an activated mutant form of Src (hu SRC Y530F) has on the actin cytoskeleton, namely the formation of podosome rosettes, otherwise known as invadopodia. (wikipedia.org)
  • diseases
  • A 1989 in vitro study found that piceatannol blocked LMP2A, a viral protein-tyrosine kinase implicated in leukemia, non-Hodgkin's lymphoma and other diseases associated with Epstein-Barr virus. (wikipedia.org)
  • Fedratinib (TG101348;SAR302503) is an orally available inhibitor of Janus kinase 2 (JAK-2) developed for the treatment of patients with myeloproliferative diseases including myelofibrosis. (wikipedia.org)
  • substrates
  • This protein functions as a multispecific organic anion transporter, with oxidized glutathione, cysteinyl leukotrienes, and activated aflatoxin B1 as substrates. (wikipedia.org)