Patent US6015892 - Oligonucleotide modulation of protein kinase C - Google Patents
Staurosporine, an alkaloid product of Streptomyces sp., and its analogs, are the most potent in vitro inhibitors of PKC ... 10 is a line graph showing anti-tumor activity of ISIS 3521 (SEQ ID NO:2). Each dashed line represents tumor volume in one ... Treatment of cells with phorbol esters causes an initial activation of kinase activity, followed by a down-regulation of PKC. ... Current agents which modulate the activity or metabolism of protein kinase C exhibit many unacceptable side effects due to ...http://www.google.com.au/patents/US6015892
Stauprimide - Wikipedia
"Inhibitory activity and selectivity of staurosporine derivatives towards protein kinase C". Bioorganic & Medicinal Chemistry ... Staurosporine Rebeccamycin K252a Midostaurin Caravatti, Giorgio; Meyer, Thomas; Fredenhagen, Andreas; Trinks, Uwe; Mett, Helmut ... Stauprimide is a semi-synthetic analog of the staurosporine family of indolocarbazoles. Stauprimide was first published in 1994 ... as part of an extensive structure-activity investigation to improve the selective inhibition of protein kinase C as a potential ...https://en.wikipedia.org/wiki/Stauprimide
Staurosporine - Wikipedia
The main biological activity of staurosporine is the inhibition of protein kinases through the prevention of ATP binding to the ... Staurosporine was discovered to have biological activities ranging from anti-fungal to anti-hypertensive. The interest in these ... Staurosporine is in the non-halogenated class. Staurosporine is the precursor of the novel protein kinase inhibitor midostaurin ... This is achieved through the stronger affinity of staurosporine to the ATP-binding site on the kinase. Staurosporine is a ...https://en.wikipedia.org/wiki/Staurosporine
Indolocarbazole - Wikipedia
Numerous forms have tested positive for anti-tumor activity, such as 7-hydroxy-STA and 7-oxo-STA2. Some of the strains from ... Staurosporine as the main". Kagaku Seibutsu. 32: 463-469. Pereira E. R., Fabre S., Sancelme M., Prudhomme M. (1995). " ... Over the course of the next decade, further study of the compound showed some fungi inhibition, hypotensive activity, and most ... The first isolated ICZ, dubbed staurosporine (STA) was in 1977 from a culture of Streptomyces staurosporeus found in a soil ...https://en.wikipedia.org/wiki/Indolocarbazole
The Structural Bases of CDK5 Activity | Springer for Research & Development
Zhang, B. F., Peng, F. F., Zhang, J. Z., and Wu, D. C. (2003). Staurosporine induces apoptosis in NG108-15 cells. Acta ... Musacchio A. (2008) The Structural Bases of CDK5 Activity. In: Ip N.Y., Tsai LH. (eds) Cyclin Dependent Kinase 5 (Cdk5). ... Nolen, B., Taylor, S., and Ghosh, G. (2004). Regulation of protein kinases: controlling activity through activation segment ... How tyrosine 15 phosphorylation inhibits the activity of cyclin-dependent kinase 2-cyclin A. J Biol Chem 282, 3173-3181.PubMed ...https://rd.springer.com/chapter/10.1007/978-0-387-78887-6_14
Topoisomerase activities in the siTop1 cell lines. The main steps used to produce the shRNA vectors and siRNA cell lines are ... Staurosporine is a protein kinase inhibitor and a remarkably potent and widely used inducer of apoptosis in a variety of cell ... Almouzni G, Mechali M. Assembly of spaced chromatin involvement of ATP and DNA topoisomerase activity. EMBO J 1988; 7: 4355-65. ... Analysis of the promoters and 5′-UTR of mouse Cd59 genes, and of their functional activity in erythrocytes. Genes Immun 2006; 7 ...http://cancerres.aacrjournals.org/content/67/18/8752
Transcriptional Stimulation of the eNOS Gene by the Stable Prostacyclin Analogue Beraprost Is Mediated Through cAMP-Responsive...
Li H, Forstermann U. Structure-activity relationship of staurosporine analogs in regulating expression of endothelial nitric- ... A, Luciferase activity of −1600eNOS-Luc was measured in BAECs with or without BPS treatment (10 μmol/L) for 24 hours. PKA ... Luciferase activity is expressed relative to that of −743eNOS-Luc with control vehicle, which is designated as 1.0. Data are ... Luciferase activity is expressed relative to that of the eNOS gene promoter (−1600 bp/+21 bp) with vehicle, which is designated ...http://circres.ahajournals.org/content/93/6/523
Topotecan - Wikipedia
"Recent developments in the clinical activity of topoisomerase-1 inhibitors". Update on Cancer Therapeutics. 1 (2). (Huang et al ... "Induction of a Common Pathway of Apoptosis by Staurosporine". Experimental Cell Research. 211 (2): 314-321. doi:10.1006/excr. ... Bertrand, Richard; Solary, Eric; O'Connor, Patrick; Kohn, Kurt W.; Pommier, Yves (1994-04-01). " ...https://en.wikipedia.org/wiki/Topotecan
Lycogala epidendrum - Wikipedia
Both of these polypropionate lactone glycosides are antibacterial; exhibiting growth inhibitory activity against Gram-positive ... A All of these bis-indole alkaloid compounds are chemically very similar to the broad-spectrum kinase inhibitor staurosporine. ... 2005). "New cytotoxic bisindole alkaloids with protein tyrosine kinase inhibitory activity from a myxomycete Lycogala ... 1994). "Isolation and synthesis of 3,4-bis(Indol-3-Yl)pyrrole-2,5-dicarboxylic acid-derivatives from the slime-mold Lycogala ...https://en.wikipedia.org/wiki/Lycogala_epidendrum
GRAPE: Uses, Side Effects, Interactions and Warnings - WebMD
Durak, I., Cetin, R., Devrim, E., and Erguder, I. B. Effects of black grape extract on activities of DNA turn-over enzymes in ... Protective effect of grape seed extract against oxidative stress-induced cell death in a staurosporine-differentiated retinal ... Pazos, M., Gallardo, J. M., Torres, J. L., and Medina, I. Activity of grape polyphenols as inhibitors of the oxidation of fish ... Yi, W., Fischer, J., and Akoh, C. C. Study of anticancer activities of muscadine grape phenolics in vitro. J Agric.Food Chem 11 ...https://www.webmd.com/vitamins-supplements/ingredientmono-472-Grape+Leaf++GRAPE.aspx?activeIngredientId=472&activeIngredientName=Grape+Leaf++%28GRAPE%29&source=2
Kawakami K., Futami H., Takahara J., Yamaguchi K. UCN-01, 7-hydroxyl-staurosporine, inhibits kinase activity of cyclin- ... PKC Activity Assay.. Logarithmically growing MDA-MB-231 or MCF-10A cells were incubated with 0-100 nm UCN-01 or 0-1000 nm ... The G1 arrest is dependent upon wild-type p53 activity, whereas S and G2 arrest do not require p53, so cells mutated for p53 ( ... Akinaga S., Nomura K., Gomi K., Okabe M. Enhancement of antitumor activity of mitomycin C in vitro and in vivo by UCN-01, a ...http://cancerres.aacrjournals.org/content/63/1/31
Cell Responses Initiated by Ecto-Kinases | SpringerLink
Exquisite sensitivity to staurosporine. Biochem. J. 285, 585-591.PubMedGoogle Scholar ... Kang, E. S., Gates, R. E., Chiang, T. M., and Kang, A. H. (1979) Ectoprotein kinase activity of the isolated rat adipocyte. ... Chiang, T. M., Kang, E. S., and Kang, A. H. (1979) Ecto-protein kinase activity of fibroblasts. Arch. Biochem. Biophys. 195, ... Dusenbery, K. E., Mendiola, J. R., and Skubitz, K. M. (1988) Evidence for ecto-protein kinase activity on the surface of human ...https://link.springer.com/chapter/10.1007/978-1-4612-1800-5_10
Table of Contents - May 01, 1994, 22 (2) | Biochemical Society Transactions
The activities of cathepsins B, D and H in the hearts of rats treated with ethanol TAHIR SIDDIQ, DEEPAK K. SHORI, GORDON B. ... Inhibition of insulin release by staurosporine and Ro 31-8220: a role for protein kinase C? SHANTA J. PERSAUD, PETER M. JONES ... Up-regulation of system A activity by hypertonic shock in CHO-K1 cells and an alanine-resistant mutant M. GOMEZ-ANGELATS, B. ... Immunoinhibition of protein kinase activity of PK-A catalytic subunit RACHEL A. GARDNER, ROGER A. CLEGG ...http://www.biochemsoctrans.org/content/22/2
Regulation of Endothelial Constitutive Nitric Oxide Synthase by Protein Kinase C | Hypertension
Incubation of BAEC with staurosporine increased ecNOS mRNA expression (Fig 1⇓, top). Staurosporine had minimal effects on the ... Measurement of NOS Activity by Quantification of the NO Release. NO production was evaluated by measurement of nitrite (NO2−) ... Staurosporine, K-252 and UCN-01: potent but nonspecific inhibitors of protein kinases. Trends Pharmacol Sci. 1989;10:218-220. ... Staurosporine is the most potent protein kinase inhibitor (IC50 value, 2.7 nmol/L47 ), inhibiting the catalytic domain of PKC, ...http://hyper.ahajournals.org/content/25/3/415
Previous studies have identified a number of activity-dependent and input-specific changes in the activity of dendritic voltage ... Sixty-minutes post-5 Hz stimulation PS amplitudes were potentiated to 227 ± 20% of baseline in staurosporine-treated slices ( ... a number of recent studies have found lasting activity-dependent alterations in the activity of voltage-dependent ion channels ... 2005) Activity-dependent decrease of excitability in rat hippocampal neurons through increases in I(h) Nat Neurosci 8:1542-1551 ...http://www.jneurosci.org/content/29/36/11203
KAKEN - Research Projects | Role of autocrine motility factor in fibrosarcoma (KAKENHI-PROJECT-05671198)
1994, Research Category：Grant-in-Aid for General Scientific Research (C), Research Field：Orthopaedic surgery ... Two motile activities, acidic and basic AMFs with regard to binding features on ion exchange chromatography, were purified from ... preincubation of Dunn osteosarcoma cells with both staurosporine and genistein resulted in a significant decrease in the ... We demonstrated the motility stimulating activity in the synovial fluid from three patients with RA.The ability of this ...https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-05671198/
Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target...
The cellular activity of NVP-BEZ235 translates well in in vivo models of human cancer. Thus, the compound was well tolerated, ... particularly those of the complex with staurosporine (PDB code 1E8Z), based on a standard sequence alignment. This binding mode ... The activity of NVP-BEZ235 against mTOR was confirmed using a biochemical mTOR K-LISA assay (IC50, 20.7 nmol/L; Supplementary ... Antitumor activity is expressed as %T/C (mean increase of tumor volumes of treated animals divided by the mean increase of ...http://mct.aacrjournals.org/content/7/7/1851
Antiepileptic Drugs in Non-Epilepsy Disorders | Springer for Research & Development
Sabra AF, Hallett M. Action tremor with altering activity in antagonist muscles. Neurology 1984; 34: 151-6PubMedCrossRefGoogle ... by the kinase inhibitor Staurosporine or its clinically relevant analogue UCN-01. Br J Cancer 2006; 22: 1436-45CrossRefGoogle ... Neuroprotective activities of sodium valproate in a murine model of human immunodeficiency virus-1 encephalitis. J Neurosci ... Potentiation of the anticancer effect of valproic acid, an antiepileptic agent with histone deacetylase inhibitory activity, ...https://rd.springer.com/article/10.2165/00023210-200822010-00003
A presenilin‐1/γ‐secretase cleavage releases the E‐cadherin intracellular domain and regulates disassembly of adherens...
Having both activities in the same polypeptide may represent an efficient and quick way for the formation and dissolution of ... A) A431 cells were treated for the indicated times with 1 μM of staurosporine (STS) to induce apoptosis (Steinhusen et al., ... A cadherin mutant unable to bind PS1 is not cleaved by the PS1/γ‐secretase activity. To examine whether PS1 binding to E‐ ... A PS1/γ‐secretase activity controls E‐cadherin processing. We used extracts from PS1 knock‐out mouse embryos (PS1−/−) (Baki et ...http://emboj.embopress.org/content/21/8/1948
Regulation of ABCB1/PGP1‐catalysed auxin transport by linker phosphorylation | The EMBO Journal
... staurosporine and quercetin, block PID by inhibiting its kinase activity. These data are consistent with a recent report ... expression regulates ABCB activity in an action that is dependent on its kinase activity as shown by mutational and ... Gschwendt M, Horn F, Kittstein W, Marks F (1983) Inhibition of the calcium‐ and phospholipid‐dependent protein kinase activity ... Rashotte AM, DeLong A, Muday GK (2001) Genetic and chemical reductions in protein phosphatase activity alter auxin transport, ...http://emboj.embopress.org/content/31/13/2965
Plants | Free Full-Text | Regulation by Light of Chemotaxis to Nitrite during the Sexual Life Cycle in Chlamydomonas...
Staurosporine at low concentrations is a specific inhibitor of PKC, as is chelerythrine. After addition of staurosporine or ... The peroxidase activity was detected by an enhanced chemiluminescence assay (Roche). 5. Conclusions. We have shown that ... A) Effect of staurosporine (. ■. ), chelerythrine () or SC-9 () on the loss of chemotaxis in pregametes of RNAi20 that were ... A) Effect of staurosporine (. ■. ), chelerythrine () or SC-9 () on the loss of chemotaxis in pregametes of RNAi20 that were ...http://mdpi.com/2223-7747/3/1/113/htm
These included staurosporine (a protein kinase C inhibitor with additional off-target activities), gemcitabine (a DNA synthesis ... Antitumour activity of novel taxanes that act at the same time as cytotoxic agents and P-glycoprotein inhibitors. Br J Cancer ... We analyzed MCP110 activity in NIH3T3 cells transformed by constitutively active H-Ras(G12V), K-Ras(G12V), and N-Ras(G12D). For ... In these activities, MCP110 was more potent than sorafenib, and significantly more potent than U0126 used at similar ...http://mct.aacrjournals.org/content/6/3/898
Aspirin Protects Endothelial Cells From Oxidant Damage Via the Nitric Oxide-cGMP Pathway | Arteriosclerosis, Thrombosis, and...
Li H, Förstermann U. Structure-activity relationship of staurosporine analogs in regulating expression of endothelial nitric- ... NOS Activity and Expression. Measurements of NOS activity, determined as citrulline formation, were performed in protein ... Moreover, in RFL-6 cells that are devoid of NOS activity but rich in soluble guanylyl cyclase,20,47,48⇓⇓ basal cGMP levels ... NOS Activity (Citrulline Formation). Citrulline synthesis was measured by a modification of a previously described technique.26 ...http://atvb.ahajournals.org/content/23/8/1345
PRKCQ - Wikipedia
transferase activity. • nucleotide binding. • protein kinase C activity. • metal ion binding. • kinase activity. • protein ... 1xjd: Crystal Structure of PKC-theta complexed with Staurosporine at 2A resolution ... protein serine/threonine kinase activity. • protein kinase activity. Cellular component. • cytoplasm. • cytosol. • membrane. • ... positive regulation of telomerase activity. • cell chemotaxis. • positive regulation of interleukin-17 production. • ...https://en.wikipedia.org/wiki/PKC%CE%B8
JCI - CD2AP in mouse and human podocytes controls a proteolytic program that regulates cytoskeletal structure and cellular...
D) Time course of CatL activity in the presence of CA074 in high-Tgfb1Cd2ap-/- podocytes, high-Tgfb1Cd2ap-/- podocytes infected ... Stauro, staurosporine; Actino D, actinomycin D; Angio II, angiotensin II. (I) TGF-β1-induced apoptosis was reversed by ... Cytosolic CatL activity regulates actin cytoskeleton in Cd2ap-/- cells. (A) Ctsl mRNA levels, determined by RT-PCR, in high- ... C) Time course of CatL activity in high-Tgfb1Cd2ap-/- podocytes and in high-Tgfb1Cd2ap-/- podocytes infected with lentiviruses ...https://jinshu-huishou.com.www.mobile.jci.org/articles/view/58552