Loading...
  • HER2
  • verification needed] Phase II results for breast cancer that over-expresses the protein human epidermal growth factor receptor 2 (Her2-positive breast cancer) were described as promising by the authors, with 19 of 41 patients achieving benefit from afatinib. (wikipedia.org)
  • specific inhibitor
  • Herein we describe the discovery by high-throughput screening and the characterization of NVP-231, a diamino-benzothiazole derivative that competes with ceramide and acts as a potent and specific inhibitor of CerK. (aspetjournals.org)
  • The protein kinase C inhibitor bis(indolyl)maleimide inhibitor BIM1 is clearly seen in the structure of PKCiota (residue 574-turn motif), need to be phosphorylated towards a PKCbeta-specific inhibitor site-directed mutagenesis of the compound for its full activation and co-crystallized as an asymmetric pair which is mediated by 3-phosphoinositide-dependent protein kinase-1 (PDK1) are downstream characteristics of PKCs and PKB/AKT. (wikipedia.org)
  • enzyme
  • IMATINIB & NILOTINIB: bind to a segment of the kinase domain that fixes the enzyme in a closed or nonfunctional state, in which the protein is unable to bind its substrate/phosphate donor, ATP. (slideshare.net)
  • Ceramide kinase (CerK) produces the bioactive lipid ceramide-1-phosphate (C1P) and appears as a key enzyme for controlling ceramide levels. (aspetjournals.org)
  • genistein
  • 2. A method according to claim 1 , wherein the GAG synthesis inhibitor is/are genistein, NaVO 3 or staurosporine, or combinations thereof. (google.com)
  • reversible
  • In this study, we discovered and characterized adamantane-1-carboxylic acid (2-benzoylamino-benzothiazol-6-yl)amide (NVP-231), a potent, specific, and reversible CerK inhibitor that competitively inhibits binding of ceramide to CerK. (aspetjournals.org)
  • pharmaceutically acceptable
  • 1. A method for the treatment of corneal haze which comprises administering to a human patient prior to, during or after corneal laser surgery, or combinations thereof, one or more compositions comprising an effective amount of one or more GAG synthesis inhibitor(s) and a pharmaceutically acceptable vehicle. (google.com)
  • The present invention relates to compounds of the Formula I, the pharmaceutically acceptable salts and stereoisomers thereof, which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent. (google.com)
  • extracellular
  • Full length human M-CSF transcripts encode a 522 amino acid (aa) type I transmembrane (TM) protein with a 464 aa extracellular region, a 21 aa TM domain, and a 37 aa cytoplasmic tail that forms a 140 kDa covalent dimer. (rndsystems.com)
  • activity
  • Kinases with activity toward all three residues. (slideshare.net)
  • In this way, protein kinases can therefore alter the function and activity of proteins and therefore cells. (news-medical.net)
  • Both Ca2+ uptake and Ca2+-ATPase activity was maximally stimulated about 2-fold by addition of cAMP-dependent protein kinase. (eurekamag.com)
  • IKK-α is sulfenylated at a conserved cysteine residue in the kinase domain, which correlated with derepression of EGF promoter activity and increased EGF expression, indicating that IKK-α stimulatea migration through dynamic interactions with the EGF promoter depending on the redox state within cells. (wikipedia.org)
  • These calphostins have cytotoxic activity due to their ability to inhibit protein kinase C activity. (wikipedia.org)
  • CX-4945 was originated by now-defunct Cylene Pharmaceuticals of San Diego, California, as the culmination of a lengthy process of rational, structure-based molecular modification of a lead compound known to have PARP inhibitor activity. (wikipedia.org)
  • Sodium
  • Sodium dodecyl sulfate/polyacrylamide gel electrophoresis (SDS/PAGE) on 3--16% gels revealed the presence of two large proteoglycan core proteins which migrated more slowly than the 200-kDa marker protein and two small proteoglycan core proteins which migrated slightly slower than the 46-kDa marker. (jove.com)
  • compounds
  • Among a large series of compounds built around a benzo[c]-[2,aphthyridine-8-carboxylic acid scaffold, CX-4945 was chosen for its high potency and selectivity as an inhibitor of CK2. (wikipedia.org)
  • synthesis
  • The compositions and methods are particularly directed to the use of GAG synthesis inhibitors in the treatment of corneal haze. (google.com)
  • cellular
  • Recent studies have focused on the role of nucleolar proteins in cellular stress responses, including that induced by reactive oxygen species. (stanford.edu)
  • human
  • In another study, researchers found that inhibiting IKK-β prevented kidney and wasting diseases in an animal model used to study wasting diseases of human AIDS sufferers. (wikipedia.org)
  • bind
  • Taxifolin is found to bind at the ATP-binding site on VEGFR-2 kinase with large value of binding energy and act as type I competitive inhibitor. (adooq.com)
  • The value of such calculations lies in understanding a variant was designed which showed improved binding characteristics of configurationally stable atropisomeric bisindolylmaleimides where the two kinase domains, and two different inhibitor conformers bind in different orientations, the hinge region of staurosporine-Pim-1 resembles co-crystallized as an asymmetric pair of biosynthetically 'related' indolocarbazole analogs. (wikipedia.org)