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*  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
*  LiveDNA: Publications of Johann Hofmann
The protein kinase C inhibitor CGP 41251, a staurosporine derivative with antitumor activity, reverses multidrug resistance. ... Detection of activity of P-glycoprotein in human tumour samples using rhodamine 123. Br. J. Haematol., 82: 161-168.. CrossRef ... Activity of P-glycoprotein in B-cell chronic lymphocytic leukemia determined by a flow cytometric assay. J. Natl. Cancer Inst ... Low incidence of activity of P-glycoprotein (P-170) in de novo acute lymphoblastic leukemia determined by a flow cytometric ...
  http://livedna.net/?dna=43.6033
*  GSK-3: tricks of the trade for a multi-tasking kinase | Journal of Cell Science
Apoptotic stimuli such as staurosporine treatment or neurotrophic factor withdrawal increase GSK-3 activity and tyrosine ... Analysis of the in vitro kinase activity of GSK-3β2 revealed reduced activity towards the microtubule-associated protein tau, ... The enzyme retains activity. Also, the S9-phosphorylated pseudosubstrate is no longer capable of inactivating the enzyme. As a ... Chen, G., Huang, L. D., Jiang, Y. M. and Manji, H. K. (1999). The mood-stabilizing agent valproate inhibits the activity of ...
  http://jcs.biologists.org/content/116/7/1175?ijkey=aa5e6bf5983d0c651923d106d68885856536fc6a&keytype2=tf_ipsecsha
*  Plus it
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
*  Frontiers | VDAC1 as Pharmacological Target in Cancer and Neurodegeneration: Focus on Its Role in Apoptosis | Chemistry
2006). Antitumor activity of plant cannabinoids with emphasis on the effect of cannabidiol on human breast carcinoma. J. ... 2008). DIDS attenuates staurosporine-induced cardiomyocyte apoptosis by PI3K/Akt signaling pathway: activation of eNOS/NO and ... In AD, the activity of GSK3β is significantly enhanced, resulting in a cascade events which include VDAC1 phosphorylation, ... 2010). Swapping of the N-terminus of VDAC1 with VDAC3 restores full activity of the channel and confers anti aging features to ...
  https://www.frontiersin.org/articles/10.3389/fchem.2018.00108/full
*  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
*  Plus it
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
*  G2 checkpoint abrogators as anticancer drugs | Molecular Cancer Therapeutics
It shows as much variety in activities as caffeine does (55). Due to this broad range of effects, it is fair to say that ... Tam SW, Schlehel R. Staurosporine overrides checkpoints for mitotic onset in BHK cells. Cell Growth & Differ, 1992;3:811-7. ... Its G2 abrogating activity was found much later and is the first published paper which shows that G2 checkpoint abrogation is ... All of these show much less inhibitory activity against PKC, and Go6976 and ICP-1 have been reported not to have the human ...
  http://mct.aacrjournals.org/content/3/4/513.full
*  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
*  Adhesion to type V collagen enhances staurosporine-induced apoptosis of adrenocortical cancer cells | SpringerLink
... on growth and hormonal activity of human adrenocortical carcinoma cell line (H295R) in vitro. Cell Tissue Res. 2010;340(2):371- ... and type I-III collagens didn't modify staurosporine-induced apoptosis. Staurosporine-treated H295R cells showed an increase of ... Yet, staurosporine induced Akt and Erk activation on H295R cells: the adhesion on type V collagen didn't modify Akt activation ... Adrenocortical cancer Type V collagen Apoptosis Staurosporine This is a preview of subscription content, log in to check access ...
  https://link.springer.com/article/10.1007/s13277-014-2281-6
*  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
*  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
*  Plus it
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
*  Plus it
... which is the basis for its contraceptive activity. In our studies, we found that RU486 antagonized the protective activities of ... In vitro, we demonstrated that MP attenuates oligodendrocyte apoptosis induced by AMPA and staurosporine, whereas neuronal ... A, B, In addition, caspase-3 activity (B) and DNA fragmentation (C) were measured. D, Cell death was assessed using an LDH ... Both GR siRNAs resulted in an attenuation of the protective activity of MP (Fig. 2B), concomitant with knockdown of GR mRNA ( ...
  http://www.jneurosci.org/content/28/12/3141
*  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
*  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