Loading...
  • PIK3CA
  • Diverse PIK3CA mutations activate lipid kinase activity hence changing confirmation of cytosolic membranes. (biomedcentral.com)
  • BYL719 displays a favorable safety profile, and tumor regression and prolonged disease control are observed in heavily pretreated patients with various tumor types carrying PIK3CA mutation in a phase I study ( 3 , 4 ). (thno.org)
  • However, a phase Ib study with BYL719 and letrozole for therapy of ER-positive breast cancer demonstrates that the efficacy is not restricted to patients with PIK3CA mutant tumors ( 5 ). (thno.org)
  • intracellular
  • InsP 3 has the capacity to release cytosolic Ca 2+ from intracellular stores, which then activates Ca 2+ -activated Cl - channels (ClC Ca ) and membrane depolarization, required for opening of voltage-operated calcium channels (VOCC) and Ca 2+ influx. (biomedcentral.com)
  • Intracellular phosphatidylinositol intermediaries were increased upon direct measure in c.1380delA CDH1 SB.mhdgc-1 cells. (biomedcentral.com)
  • RTKs
  • Reacting to a various mobile phone stimulant drugs, like advancement factor-mediated service regarding receptor tyrosine kinases (RTKs), Ras thinks an initialized GTP-bound point out, resulting in recruitment of Raf from the cytosol for the cell membrane, wherever it becomes turned on, probably with a Src-family tyrosine kinase [20, 21 years of age, 34- (immune-source.com)
  • Aberrant activation of PI3K signaling pathway occurs frequently in breast cancer through different mechanisms such as hyper-activation of upstream receptor tyrosine kinases (RTKs), mutant RAS, mutations and/or amplifications of PI3K and downstream effector AKT, and functional loss of PTEN or INPP4B. (thno.org)
  • activate
  • Ca(2+) and DAG , in turn, activate Protein kinase C alpha ( PKC-alpha ). (bio-rad.com)
  • MEK1(MAP2K1) and MEK2(MAP2K2) in turn activate ERK1/2 [ 2 ], [ 3 ]. (bio-rad.com)
  • A point mutation in this region, K227E, blocks the GTP-dependent interaction of PI 3-kinase p110alpha with Ras in vitro and the ability of Ras to activate PI 3-kinase in intact cells. (embl.de)
  • Tissue and vascular injuries activate ECs, resulting in not only the expression of adhesion molecules including P-and E-selectins, ICAMs, and vascular cell adhesion mole-cule-1 (VCAM-1) but also the production and release of vWF, reactive oxygen species (ROS), and inflammatory cytokines [ 3 , 17 - 19 ]. (pubmedcentralcanada.ca)
  • receptors
  • There is only one class IB PI3K (p110γ) and this operates downstream of heterotrimeric GPCRs (G-protein-coupled receptors). (biochemj.org)
  • Rather, NK cells utilize an array of activating and inhibitory receptors with the latter largely detecting major histocompatibility complex (MHC) class I ligands, or in the case of 2B4, the signaling lymphocyte activation molecule (SLAM) family ligand CD48. (frontiersin.org)
  • Inhibitory Ly49 receptors expressed on NK cells recognize major histocompatibility complex class I (MHC I) molecules and inhibit NK cell killing of normal cells that express high amounts of MHC I. In addition to maintaining self-tolerance of NK cells, the Ly49:MHC I interaction is required for the functional maturation of NK cells by a process termed "NK cell licensing. (ubc.ca)
  • ERK1
  • In addition, ACM2 stimulates ERK1/2 activation in Protein kinase C (PKC) and/or Ca('2+) -dependent manner. (bio-rad.com)
  • ERK1/2 substrates include a wide variety of transcription factors, kinases and phosphatases, cytoskeletal proteins, signaling proteins, and apoptotic proteins and proteinases. (bocsci.com)
  • substrate specificity
  • On the basis of structural similarities and substrate specificity, the PI3K family can be subdivided into three classes termed I, II, and III. (abcam.com)
  • 70, The term PI3K is given to a family of lipid kinases which, in mammals, consists in eight identified PISKs that are divided into three sub-families according to their structure and their substrate specificity. (allindianpatents.com)
  • PI3K is a family of phospholipid kinase that is divided into three classes based on structure, function and substrate specificity. (biomedcentral.com)
  • activation
  • Stimulation of primary human erythroid progenitors (PEPs) with erythropoietin (Epo) leads to the activation of the mitogenic kinases (MEKs and Erks). (biomedcentral.com)
  • Furthermore, Erk activation in PEPs is insensitive to the inhibition of Raf kinases but suppressed upon PKC inhibition. (biomedcentral.com)
  • Exogenous NE and clonidine (1 μM each) activated both PI3Kγ and PKCζ, and the activation of these kinases was abolished by preincubation of tissue with the α 2 -adrenoceptor blocker yohimbine. (biomedcentral.com)
  • In addition, SDF-1α induced activation of the focal adhesion kinase (FAK) as well as the migration of breast cancer cells. (aacrjournals.org)
  • Apoptosis was documented by changes in mitochondrial membrane potential, alteration of the plasma membrane, caspase 3 activation and DNA fragmentation. (beds.ac.uk)
  • found that the TGF-β-induced activation of PI3K depends on another ubiquitin ligase-mediated mechanism and a SMAD protein but is independent of the kinase function of TβRI. (sciencemag.org)
  • Activation of the phosphatidylinositol 3-kinase (PI3K) pathway in response to MEK inhibition through a negative MEK-epidermal growth factor receptor-PI3K feedback loop was found to limit efficacy. (aacrjournals.org)
  • Leptin signaling in the hypothalamus occurs through leptin receptor, Janus kinase 2 (JAK2), and signal transducer and activator of transcription 3 (STAT3) activation. (diabetesjournals.org)
  • Also a serine kinase, IKK is induced by the activation of nuclear factor-κB (NF-κB) ( 19 ). (diabetesjournals.org)
  • Apoptosis
  • We studied the role of phosphoinositol-3-kinase (PI3K) p110γ in the regulation of in situ apoptosis, macrophage proliferation and polarization towards M1 or M2 phenotypes in atherosclerotic lesions. (nih.gov)
  • Regulation
  • The enhanced IKKε expression in adipose tissue, liver, and adipose tissue macrophages of DIO mice, together with the complex IKKε KO phenotype, indicate that this serine kinase is key to the regulation of metabolism. (diabetesjournals.org)
  • Biswas R, Basu M, Sen-Majumdar A and Das M (1985) Intrapeptide autophosphorylation of the epidermal growth factor receptor: regulation of kinase catalytic function by receptor dimerization. (springer.com)
  • epidermal
  • Boonstra J, Mummery CL, van der Saag PT and de Laat SW (1985a) Two receptor classes for epidermal growth factor on pheochromocytoma cells, distinguishable by temperature, lectins and tumour promoters. (springer.com)
  • polypeptide
  • Indeed, polypeptide growth factors such as insulin-like growth factor (IGF)-I, platelet-derived growth factor (PDGF), neuregulins, neurotrophins, and hepatocyte growth factor (HGF) have been shown to control medulloblastoma proliferation, survival, differentiation, and metastasis ( 4 - 6 ) by binding to specific receptor tyrosine kinases (RTK). (aacrjournals.org)