phosphatase and kinase inhibitors
Báo cáo khoa học: Principles behind the multifarious control of signal transduction ERK phosphorylation and kinase/phosphatase control potx
... 245 How kinases and phosphatases control signaling model of a simple linear pathway that consisted of a receptor and three consecutive kinase phosphatase monocycles (Fig 1) The activation and inactivation ... now, is that mutations in MAP kinases and phosphatases can differ in the extent to which they shift a cell between differentiation and proliferation If kinases and phosphatases were considered ... phosphorylates and thereby activates the rst kinase X1 (to become X1P) Through phosphorylation, this kinase can then activate the 253 How kinases and phosphatases control signaling second kinase (X2),...
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Báo cáo khoa học: The expression of retinoblastoma and Sp1 is increased by low concentrations of cyclin-dependent kinase inhibitors ppt
... the expression (transcription, mRNA and protein levels), of both Rb and Sp1 after CDK inhibition by the chemical inhibitors UCN-01, roscovitine and olomoucine, and by the intrinsic inhibitor p21 ... Rb and Sp1 protein caused by CDK inhibitors in CHO cells The increase in total levels of Rb and Sp1 proteins caused by UCN-01 may be a result of the enhanced transcription and stability of Rb and ... between Rb and Sp1, we used DHFR as a target model to study the final effects of CDK inhibitors We report that the expression of retinoblastoma and Sp1 is increased by low concentrations of CDK inhibitors...
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Báo cáo y học: "Rho kinase inhibitors Y27632 and H1152 augment neurite extension in the presence of cultured Schwann cells" pdf
... for protein kinase A, protein kinase C, or myosin light chain kinase, as well as over 20 times greater than that for two other downstream Rho effectors, citron kinase and protein kinase N [19,20] ... inhibitor of the serine/threonine kinases, PKA, PKC and MLCK The Ki values of H1152 for these kinases are about 390, 5800 and 6300 times higher than for Rho-kinases, respectively [21-23] H1152 ... Authors have read and approved the final manuscript Acknowledgements Prof K Actories and Prof D Meyer of the Institute of Experimental and Clinical Pharmacology and Toxicology, and Centre for Neuroscience,...
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Báo cáo y học: "P38 MAP kinase inhibitors as potential therapeutics for the treatment of joint degeneration and pain associated with osteoarthritis" ppsx
... the treatment of both joint degeneration and pain associated with OA Materials and methods P38 kinase inhibitors The p38 kinase inhibitors SB 203580 and VX-745 were synthesized by the chemistry ... protein kinases (ERK), the c-Jun NH2-terminal kinase (JNK) and p38 http://www.journal-inflammation.com/content/5/1/22 [17] The p38 family has four members: α and β which are 75% homologous and γ and ... inflammatory cytokines and MMPs [17] SB 203580 [19-21] and VX-745 [22] are both potent inhibitors of p38α and β but not γ or δ The specificity of a number of widely used p38 inhibitors has been...
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Tài liệu Báo cáo khoa học: EGF receptor in relation to tumor development: molecular basis of responsiveness of cancer cells to EGFR-targeting tyrosine kinase inhibitors docx
... JNK and mitogen-activated protein kinase phosphatase- 1 The activity of JNK, one of the MAPKs, is tightly controlled by both protein kinases, such as MAPK kinase (MKK4) or MAPK kinase (MKK7) and ... ⁄ and the PI3K ⁄ Akt pathways results, in turn, in the inactivation of pro-apoptotic Bcl-2 proteins (e.g PUMA, Bax, Bim and Bad), Fas, and CDK inhibitors (e.g p27KIP1, p21WAF1 and p15INK4b), and ... protein phosphatases such as MAPK phosphatase (MKP) Mitogen-activated protein kinase phosphatase1 (MKP-1) is a dual-specificity protein phosphatase, which can dephosphorylate both phosphothreonine and...
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Báo cáo khoa học: Coiled–coil interactions modulate multimerization, mitochondrial binding and kinase activity of myotonic dystrophy protein kinase splice isoforms pptx
... Fig Myotonic dystrophy protein kinase (DMPK) isoforms and truncation mutants Structural domain organization of DMPK splice isoforms A, C, E and F, and N-terminal and C-terminal truncation mutants ... homo- and heteromultimerization occurs independently of kinase activity and alternatively spliced domains To confirm that DMPK self-association indeed occurred independently of kinase activity, a kinase ... these possibilities In DMPKlike kinases, multimerization capacity is apparently a prerequisite for proper kinase activation: the kinase activity of Rho -kinase and MRCKa is also partly dependent...
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Báo cáo khoa học: Chick embryo anchored alkaline phosphatase and mineralization process in vitro Influence of Ca 2+ and nature of substrates doc
... deposit exhibited two bands located at 1122 cm)1 and 918 cm)1 bands (Fig 5A) As mentioned above, the 918 cm)1 band may correspond to HPO42– group in OCP The 1122 cm)1 band (Fig 5A) may be associated ... alkaline phosphatase: Characterization and origin in human trabecular and cortical bone J Bone Mineral Res 14, 1926–1933 Whyte, M.P (1994) Hypophosphatasia and the role of alkaline phosphatase ... about 0.37 [73] Although ADP and ATP were completely hydrolyzed by GPI-bALP and were not inhibitors of GPI-bALP, different types of mineral deposits such as OCP and HPO42– complexes of calcium...
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Báo cáo Y học: Selection of effective antisense oligodeoxynucleotides with a green fluorescent protein-based assay Discovery of selective and potent inhibitors of glutathione S-transferase Mu expression doc
... sets: GSTM1-forA and GSTM1-revA; GSTM1-forB and GSTM1-revB; GSTM2-forA and GSTM2-revA; GSTM2-forB and GSTM2-revB Products from the first two PCR reactions were combined, melted and reannealed to ... GSTM1 and/ or GSTM2 and can be used to study the influence of reduced GSTM expression on the detoxification of xenobiotics and protection against chemical-induced carcinogenesis MATERIALS AND METHODS ... melting and cooling Four different double-stranded products were obtained, one of which had the correct 5¢-EcoRI and 3¢-BamHI overhanging ends The PCR products were cloned into the EcoRI- and BamHI-digested...
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báo cáo hóa học:" Aurora kinase inhibitors synergize with paclitaxel to induce apoptosis in ovarian cancer cells" pot
... for 1A9 and PTX10 cell lines, and Merck & Co and Vertex 19 Weaver BA, Cleveland DW: Decoding the links between mitosis, cancer, and chemotherapy: The mitotic checkpoint, adaptation, and cell ... Ten random fields were sampled for each concentration and percentage of pH3S10 positive cells calculated Aurora-A, it is highly selective and effective at inhibiting Aurora family kinases and ... VE-465 inhibits the Aurora kinases VE-465 inhibits the Aurora kinases (A) Immunoblot analysis of whole cell lysates from 1A9 and PTX10 cell lines probed for Aurora-A, Aurora-B and PP2A as a loading...
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Báo cáo y học: "Drugs in development: bisphosphonates and metalloproteinase inhibitors" potx
... collagenases, and Ro32-3555 (Roche, Basel, Switzerland), which is an effective inhibitor of collagenases but has less potency against MMP-2 and MMP-3 MMP inhibitors and arthritis: animal and clinical ... osteoclast and the bone surface [20,21], to disruption of the cytoskeleton [19,22] and to loss of function Both alendronate and tildronate can inhibit several protein tyrosine phosphatases [23–25] and ... protein 1, NFκB and mitogen-activating protein kinase pathways; by activation, MMPs are secreted as inactive zymogen and require the proteolytic cleavage of the prodomain for activation; and by inhibition,...
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Báo cáo y học: "Local expression of matrix metalloproteinases, cathepsins, and their inhibitors during the development of murine antigen-induced arthritis" pps
... Many proteinases and inhibitors were very weakly expressed and resulted in an absent call Among the strongly expressed proteinases and inhibitors, some MMPs, cathepsins, TIMPs and cystatins showed ... mRNA and protein level To complete our oligonucleotide chip and PCR results, we investigated MMP expression and activity by fluorescence assays and zymography Preparation of total RNA Materials and ... IL-6 and tumor necrosis factor (TNF)-α and the anti-inflammatory cytokine IL-4 were determined by enzyme-linked immunosorbent assay (ELISA) sandwich technique (see Materials and Methods) and were...
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Báo cáo khoa học: " The ATM and ATR inhibitors CGK733 and caffeine suppress cyclin D1 levels and inhibit cell proliferation" ppsx
... interests Authors' contributions JPA and PS conceived and designed the study JPA performed the experiments JPA and PS analyzed and interpreted the data JPA and PS drafted and wrote the manuscript Acknowledgements ... determined Our findings show that single and dual ATM/ ATR kinase inhibitors are not interchangeable and may thus differentially influence cell fate in a cell type and context dependent manner KU55933 ... active kinase complexes with cyclin dependent kinase (CDK4) or CDK6 that phosphorylate and hence inactivate the retinoblastoma tumor suppressor protein (RB) (reviewed in [27]) Caffeine and CGK733...
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Báo cáo y học: "volution of an adenocarcinoma in response to selection by targeted kinase inhibitors" potx
... neck, and progressive and new lung metastases A tumor sample was removed from the metastatic skin nodule and was subjected to both WTSS and genomic sequencing There were 1,262,856,802 and 5,022,407,108 ... was done under CT guidance and multiple aspirates were obtained for analysis Results and discussion DNA sequencing and mutation detection There were 2,584,553,684 and 498,229,009 42-bp sequence ... and were validated using PCR and Sanger sequencing on germline and tumor genomic DNA Those marked as ‘Recurrence’ (remaining nine SNVs) were identified in the post-treatment secondary tumor and...
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Genetic polymorphisms of matrix metalloproteinases and their inhibitors in potentially malignant and malignant lesions of the head and neck potx
... the development and aggressiveness of HNSCC [51] Page of 13 Three novel peptidomimetic phosphonate inhibitors have been synthesized and evaluated as potential inhibitors of MMP-2 and MMP-8 Peptidomimetic ... levels Regulation of MMPs in potentially malignant and malignant head and neck lesions Polymorphism of MMPs in potentially malignant and malignant head and neck lesions The MMPs are regulated at many ... PDGF, TNF-α and TGF-β [25] The regulation of different MMPs also occurs at the protein level MMPs are secreted as latent enzymes and this process can be achieved by activators and inhibitors The...
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báo cáo khoa học: " Preclinical evaluation of KIT/PDGFRA and mTOR inhibitors in gastrointestinal stromal tumors using small animal FDG PET" ppsx
... by mutations in the KIT and PDGFRA receptors, leading to upregulated tyrosine kinase activity [1,2] Tyrosine kinase inhibitors (TKIs), imatinib and sunitinib, are the standard treatment for patients ... inhibits the kinase activity of KIT and PDGFRA receptors and also BCR-ABL, PDGFRA and KIT [8] Nilotinib has been shown to be active in a small series of patients pre-treated with imatinib and sunitinib ... Figure 2) and with PET tomography At day 13, the mean tumor volume of all animals per group was > 0.5 cm3 for imatinib alone and nilotinib alone, and < 0.5 cm3 for the combinations and for everolimus...
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Báo cáo y học: "Matrix metalloproteinases and their inhibitors: promising novel biomarkers in severe sepsi" ppt
... diagnosis and therapy in critically ill patients, and may consecutively influence the morbidity and mortality of these patients 13 The implementation of metalloproteinases and their inhibitors ... they are often nonspecific, lack adequate sensitivity and/ or are difficult to measure and to interpret accurately Metalloproteinases and their inhibitors may represent a promising new class of biomarkers ... metalloproteinases and tissue inhibitors of metalloproteinases as biomarkers in the intensive care unit Recent data and cumulative analysis indicate that biomarkers improve diagnosis of sepsis and may help...
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Báo cáo y học: "Identification of 491 proteins in the tear fluid proteome reveals a large number of proteases and protease inhibitors" pot
... digestion (1 and μl) and one-dimensional gel separation combined with MS (GeLC-MS; lanes of μl each) on a LTQ-FT, and also through GeLC-MS on a LTQ-Orbitrap The numbers indicate the bands according ... hydrolase activity or protease inhibitors It has been demonstrated that the levels of proteases and proteases inhibitors are in a constant equilibrium in tear fluid [35,36] and that imbalance in these ... all peptides and protein hits obtained in both LTQ-FT and LTQ-Orbitrap data Click here data Orbitrap data All peptides andfile Additionalfor fileprotein hits obtained in both LTQ-FT and LTQdata...
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EXPLORING THE ROLE OF PHARMACOKINETIC ALTERATIONS IN TYROSINE KINASE INHIBITORS (TKIS) ASSOCIATED TOXICITIES
... Introduction to tyrosine kinase inhibitors 1.2 Common toxicities associated with tyrosine kinase inhibitors 1.3 Inter-patient variability in exposure of tyrosine kinase inhibitors 1.4 Sources ... tyrosine kinase inhibitors 110 5.3.2 Potential effect of enzyme inducer/inhibitor on pharmacokinetics of tyrosine kinase inhibitors 113 5.3.3 Effect of tyrosine kinase inhibitors ... Understanding tyrosine kinase inhibitor associated toxicities: a focus on hepatotoxicity 132 6.1 Hepatotoxicity with tyrosine kinase inhibitors 132 6.2 Risk of tyrosine kinase...
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Functional effects of a novel BIM deletion polymorphism in mediating resistance to tyrosine kinase inhibitors in cancer
... 1.2 The role of tyrosine kinases in cancer……………………………………… 1.3 Tyrosine kinase inhibitors as therapeutic agents in cancer………………… 1.4 Clinical resistance to tyrosine kinase inhibitors ………………………… 12 ... sarcoma viral oncogene homolog (SRC) and Janus kinases (JAKs) are examples of non-receptor tyrosine kinases In an inactive state, the kinase activity of ABL1 and SRC are repressed by intramolecular ... protein kinases, in which the last kinase in this cascade is known as the MAP kinase, an example of which is extracellular signal-regulated kinase (ERK) (Figure 3)25 The activation of the MAP kinase...
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