... a specific inhibitor of protein kinase named staurosporine; a proteasome inhibitor named lactacystin; a fatty acid biosynthesis ... Tomoyasu Hirose; Toshiaki Sunazuka; Satoshi Omura (1 January 2010). "Recent development of two chitinase inhibitors, Argifin ... 30 years since the discovery of staurosporine". The Journal of Antibiotics. 62 (1): 17-26. doi:10.1038/JA.2008.4. ISSN 0021- ... inhibitor named cerulenin; Furthermore, compounds having a unique structure and biological activity discovered by Omura are ...

Lee SK, Stern PH (October 2000). "Divergent effects of protein kinase C (PKC) inhibitors staurosporine and bisindolylmaleimide ... The protein kinase C inhibitor bis(indolyl)maleimide inhibitor BIM1 is clearly seen in the structure of PKCiota (residue 574- ... protein kinase C inhibitor bisindolyl maleimide 2 binds with reversed orientations to different conformations of protein kinase ... and BIM-8 are bisindolylmaleimide-based protein kinase C (PKC) inhibitors. These inhibitors also inhibit PDK1 explaining the ...

It is structurally similar to staurosporine, but does not show any inhibitory activity against protein kinases. It shows ... Rebeccamycin (NSC 655649) is a weak topoisomerase I inhibitor isolated from Nocardia sp. ... Topoisomerase inhibitors, Halogen-containing alkaloids, All stub articles, Antineoplastic and immunomodulating drug stubs). ...

"Novel Effects on The Gonyaulax Circadian System Produced by the Protein Kinase Inhibitor Staurosporine". J. Biol. Rhythms. 14 ( ... This work has now been expanded to other proteins in the cell. On the other hand, short pulses of inhibitors of synthesis of ... Taylor, W.R.; Dunlap, J.C.; Hastings, J.W. (1982). "Inhibitors of protein synthesis on 80s ribosomes phase shift the Gonyaulax ... At still another level, protein phosphorylation inhibitors also influence the period of the rhythm. Other luminescent systems: ...

... is in the non-halogenated class. Staurosporine is the precursor of the novel protein kinase inhibitor midostaurin ... Staurosporine is a prototypical ATP-competitive kinase inhibitor in that it binds to many kinases with high affinity, though ... The main biological activity of staurosporine is the inhibition of protein kinases through the prevention of ATP binding to the ... an inhibitor of protein kinases, on the cell cycle and chromatin structure of normal and leukemic lymphocytes". Cancer Research ...

Staurosporine, a nonspecific protein kinase C inhibitor can induce squamous metaplasia in breast tissue while other known PKC ... ISBN 978-0-323-03758-7. Heffelfinger SC, Miller MA, Gear R, Devoe G (1998). "Staurosporine-induced versus spontaneous squamous ... inhibitors did not show this effect. cAMP stimulation can also induce squamous metaplasia. Multiple imaging modalities may be ...

... such as staurosporine-like bisindole inhibitors of protein kinases. 5-Methylindole ChemExper Chemical Directory. Accessed 1 ...

... is a kinase inhibitor with specificity towards protein kinase A. It is a semi-synthetic derivative of K252a and analog ... of staurosporine. Makarevich, A. V.; Sirotkin, A. V.; Rafay, J. (2010). "Comparison of Effects of Protein Kinase A, Mitogen- ... Protein kinase inhibitors, Indolocarbazoles, All stub articles, Biochemistry stubs). ... activated Protein Kinase, and Cyclin-dependent Kinase Blockers on Rabbit Ovarian Granulosa Cell Functions". Hormone and ...

... one Staurosporine Drug developments for kinase inhibitors are started from kinase assays, the lead compounds are usually ... Hunter T (1991). "Protein kinase classification". Protein Phosphorylation Part A: Protein Kinases: Assays, Purification, ... One very important group of protein kinases are the MAP kinases (acronym from: "mitogen-activated protein kinases"). Important ... Hanks SK, Hunter T (May 1995). "Protein kinases 6. The eukaryotic protein kinase superfamily: kinase (catalytic) domain ...

Protein kinase inhibitors, Breakthrough therapy, Orphan drugs). ... a staurosporine-like inhibitor which blocks c-Met. K252a was ... c-Met inhibitors are a class of small molecules that inhibit the enzymatic activity of the c-Met tyrosine kinase, the receptor ... Targeting the ATP binding site of c-Met by small molecules inhibitors is one strategy for inhibition of the tyrosine kinase. ... The structure of tivantinib in complex with the c-Met kinase domain shows that the inhibitor binds a conformation that is ...

Staurosporine, Methylene blue and other kinase inhibitors can pass the blood brain barrier and inhibit MARK which consequently ... It is suspected that at a threonine (Thr175 ), kinases such as GSK3β and MARK hyper-phosphorylate the mutant tau protein ... Also researcher have linked to NFT survive (mutant tau protein maintenance) to heat shock protein 90 (HSP90) since HSP90 ... Transformation in tau gene on chromosome 17 can be linked to PART due to the fact that the tau protein analyzed from PART NFTs ...

The number of protein kinases thought to exist in the human genome exceeds six hundred, making a nanomolar inhibitor such as ... Staurosporine as the main". Kagaku to Seibutsu. 32: 463-469. doi:10.1271/kagakutoseibutsu1962.32.463. Pereira E. R., Fabre S., ... cyclin-dependent kinases, G-protein coupled receptor kinases, tyrosine kinase, and cytomegalovirus pUL97 protein. Topoisomerase ... a broad protein kinase inhibitor. The next landmark discovery came with the detection of rebeccamycin (REB) in a sample of ...

CYP2D6 inhibitors, CYP3A4 inducers, Protein kinase inhibitors, Alkaloids, Lactams, Indolocarbazoles). ... It is a semi-synthetic derivative of staurosporine, an alkaloid from the bacterium Streptomyces staurosporeus. The U.S. Food ... Midostaurin, sold under the brand name Rydapt & Tauritmo both by Novartis, is a multi-targeted protein kinase inhibitor that ... June 2002). "Inhibition of mutant FLT3 receptors in leukemia cells by the small molecule tyrosine kinase inhibitor PKC412". ...

"Inhibitory activity and selectivity of staurosporine derivatives towards protein kinase C". Bioorganic & Medicinal Chemistry ... Protein kinase inhibitors). ... to improve the selective inhibition of protein kinase C as a ... 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 ...

This staurosporine analog is a highly potent cell permeable inhibitor of CaM kinase and phosphorylase kinase (IC50 = 1.8 and ... At higher concentrations it is also an efficient inhibitor of serine/threonine protein kinases (IC50 of 10 to 30 nmol/L). K252a ... Protein kinase inhibitors, TrkB antagonists, Tertiary alcohols, Methyl esters, All stub articles, Biochemistry stubs). ... has been shown to block the neuronal differentiation of rat pheochromocytoma PC12 cells by inhibition of trk tyrosine kinase ...

... coli Effector Protein NleF Is a Caspase Inhibitor". PLOS ONE. 8 (3): e58937. Bibcode:2013PLoSO...858937B. doi:10.1371/journal. ... Clark, Christina S.; Maurelli, Anthony T. (May 2007). "Shigella flexneri Inhibits Staurosporine-Induced Apoptosis in Epithelial ... "The assembly of a GTPase-kinase signalling complex by a bacterial catalytic scaffold". Nature. 469 (7328): 107-111. doi:10.1038 ... Mattoo, Seema; Lee, Yvonne M; Dixon, Jack E (August 2007). "Interactions of bacterial effector proteins with host proteins". ...

It is a potent inhibitor of the serine/threonine kinases protein kinase A (PKA) and protein kinase C (PKC), binding in a ... with an inhibition profile similar to that of staurosporine. Balanol prevents functioning by binding competitively to the ... June 2003). "Mutants of protein kinase A that mimic the ATP-binding site of protein kinase B (AKT)". Journal of Molecular ... Gustafsson AB, Brunton LL (August 1999). "Differential and selective inhibition of protein kinase A and protein kinase C in ...

"Heat shock protein 72 suppresses apoptosis by increasing the stability of X-linked inhibitor of apoptosis protein in renal ... "Hsc70 regulates accumulation of cyclin D1 and cyclin D1-dependent protein kinase". Molecular and Cellular Biology. 23 (5): 1764 ... staurosporine, and doxorubicin. This role leads to its involvement in many pathological processes, such as oncogenesis, ... Heat shock 70 kDa protein 8 also known as heat shock cognate 71 kDa protein or Hsc70 or Hsp73 is a heat shock protein that in ...

"Heat shock protein 72 suppresses apoptosis by increasing the stability of X-linked inhibitor of apoptosis protein in renal ... double-stranded RNA-dependent protein kinase-mediated death signaling pathway requires the Fanconi anemia protein, FANCC". J. ... staurosporine, and doxorubicin. This role leads to its involvement in many pathological processes, such as oncogenesis, ... This protein is a member of the Hsp70 family. In conjunction with other heat shock proteins, this protein stabilizes existing ...

The limitations of kinase inhibitors include the facts that they only inhibit kinase-dependent MET activation, and that none of ... The protein possesses tyrosine kinase activity. The primary single chain precursor protein is post-translationally cleaved to ... K252a (Fermentek Biotechnology) is a staurosporine analogue isolated from Nocardiopsis sp. soil fungi, and it is a potent ... Kinase inhibitors are low molecular weight molecules that prevent ATP binding to MET, thus inhibiting receptor ...

... activates its receptor c-Met which activates mitogen-activated protein/extracellular signal-regulated kinase kinase (MEK) and ... For example, QSulf1 reduces specific HS 6-O sulfation which releases Noggin, an inhibitor of bone morphogenetic protein (BMP), ... In extension, Sulf1 mediated HCC cell apoptotic sensitivity to cisplatin and staurosporine. As a review, HGF, or scatter factor ... which then leads to induction of the mitogen-activated protein kinase (MAPK) pathway (in addition to other pathways). This ...

"Ruthenium half-sandwich complexes as protein kinase inhibitors: derivatization of the pyridocarbazole pharmacophore ligand". ... Inhibitor acts as ATP mimetic in ATP binding pocket Staurosporine and Ruthenium Compound 12 General Structure of ... making it an attractive target for potent small-molecule PIM kinase inhibitors. Many inhibitors are often more selective for ... Serine/threonine-protein kinase Pim-2 is an enzyme that in humans is encoded by the PIM2 . PIM2 or Proviral Integrations of ...

... via the inhibition of protein kinases). S. hygroscopicus and S. viridochromogenes produce the natural herbicide bialaphos. ... Staurosporine (from S. staurosporeus) also has a range of activities from antifungal to antineoplastic ( ... October 2012). "Molecular insights into the biosynthesis of guadinomine: a type III secretion system inhibitor". Journal of the ... Expression of eukaryotic proteins in E. coli may be problematic. Sometimes, proteins do not fold properly, which may lead to ...

K01-0509), inhibitors of the type III secretion system. Non-Streptomyces actinomycetes, filamentous fungi, and non-filamentous ... KP6107 by screening based on adenylate kinase assay". Journal of Basic Microbiology. 53 (7): 581-9. doi:10.1002/jobm.201200045 ... Streptomyces coelicolor has shown useful for the heterologous expression of proteins. Methods like "ribosome engineering" have ... staurosporine (precursor to stauprimide and midostaurin), neothramycin, aclarubicin, tomaymycin, sibiromycin, and mazethramycin ...

... protease inhibitor - protein kinase C - proteoglycan - proteomic profile - proteomics - proton beam radiation therapy - proton ... staurosporine - stavudine - stellate - stem cell - stem cell factor - stem cell transplantation - stent - stereotactic biopsy ... tyrosine kinase inhibitor - TZT-1027 ubiquinone - UCN-01 - UGT1A1 - ultrasonogram - ultrasonography - ultrasound-guided biopsy- ... fusion protein G-CSF - gabapentin - Gail model - gallium nitrate - gallium scan - gamma knife - gamma ray - ganciclovir - ...