*  Protein kinase C
... inhibitors, such as ruboxistaurin, may potentially be beneficial in peripheral diabetic nephropathy. ... membrane-bound receptor for activated protein kinase C proteins). The protein kinase C enzymes are known for their long-term ... Protein kinase C, commonly abbreviated to PKC (EC 2.7.11.13), is a family of protein kinase enzymes that are involved in ... The consensus sequence of protein kinase C enzymes is similar to that of protein kinase A, since it contains basic amino acids ...
*  Protein kinase inhibitor
A protein kinase inhibitor is a type of enzyme inhibitor that blocks the action of one or more protein kinases. Protein kinases ... and protein kinase inhibitors can be used to treat diseases due to hyperactive protein kinases (including mutant or ... Some of the kinase inhibitors used in treating cancer are inhibitors of tyrosine kinases. The effectiveness of kinase ... PC = Pregnancy category PC = Pregnancy category Tyrosine kinase inhibitor "Definition of tyrosine kinase inhibitor - NCI ...
*  Raf kinase inhibitor protein
The Raf kinase inhibitor protein (RKIP) is a kinase inhibitor protein, that regulates many signaling pathways within the cell. ... Lorenz K, Lohse MJ, Quitterer U (2003): Protein kinase C switches the Raf kinase inhibitor from Raf-1 to GRK-2. Nature 426: 574 ... RKIP has also been shown to inhibit G protein coupled receptor kinases (GRK) when phosphorylated by protein kinase C. Via this ... Odabaei, G.; Chatterjee, D.; Jazirehi, A. R.; Goodglick, L.; Yeung, K.; Bonavida, B. (2004). "Raf-1 Kinase Inhibitor Protein: ...
*  Cyclin-dependent kinase inhibitor protein
A cyclin-dependent kinase inhibitor protein is a protein which inhibits cyclin-dependent kinase. Several function as tumor ... Cyclin-Dependent Kinase Inhibitor Proteins at the US National Library of Medicine Medical Subject Headings (MeSH). ... suppressor proteins. Cell cycle progression is negatively controlled by cyclin-dependent kinases inhibitors (called CDIs, CKIs ... "Crystal structure of the p27Kip1 cyclin-dependent-kinase inhibitor bound to the cyclin A-Cdk2 complex". Nature. 382 (6589): 325 ...
*  Calcium/calmodulin dependent protein kinase II inhibitor 1
... is a protein that in humans is encoded by the CAMK2N1 gene. GRCh38: ... Calcium/calmodulin dependent protein kinase II inhibitor 1". Retrieved 2017-09-09. Wang C, Li N, Liu X, Zheng Y, Cao X (2008 ... "A novel endogenous human CaMKII inhibitory protein suppresses tumor growth by inducing cell cycle arrest via p27 stabilization ...
*  Tyrosine kinase 2
Thompson JE (June 2005). "JAK protein kinase inhibitors". Drug News Perspect. 18 (5): 305-10. doi:10.1358/dnp.2005.18.5.904198 ... This gene encodes a member of the tyrosine kinase and, to be more specific, the Janus kinases (JAKs) protein families. This ... Non-receptor tyrosine-protein kinase TYK2 is an enzyme that in humans is encoded by the TYK2 gene. Tyk2 was the first member of ... Velazquez L, Fellous M, Stark GR, Pellegrini S (July 1992). "A protein tyrosine kinase in the interferon alpha/beta signaling ...
*  Mubritinib
Protein kinase inhibitor McCormick, Frank; Doriano Fabbro (2005). Protein Tyrosine Kinases: From Inhibitors to Useful Drugs ( ... Mubritinib (TAK-165) is a protein kinase inhibitor which was under development by Takeda for the treatment of cancer. It ...
*  Rottlerin
... a novel protein kinase inhibitor". Biochem Biophys Res Commun. 199 (1): 93-8. doi:10.1006/bbrc.1994.1199. Davies, SP; Reddy, H ... Caivano, M; Cohen, P (2001). "Specificity and mechanism of action of some commonly used protein kinase inhibitors". Biochem. J ... but some studies showed it did not block PKCδ activity and did block other kinase and non-kinase proteins in vitro. Rottlerin ... It was found to reduce ATP levels, activate 5'-AMP-activated protein kinase and affect mitochondrial production of reactive ...
*  Betaenone B
Patrick, D.; Heimbrook, D (1996). "Protein kinase inhibitors for the treatment of cancer". Drug Discovery Today. 1: 325-330. ... The compounds were found to inhibit a variety of protein kinases signifying a possible role in cancer treatment. The structure ... betaenone C has been shown to inhibit RNA and protein synthesis. Most of the major work on betaenone B, including the initial ... "Specific inhibitors of eukaryotic DNA synthesis and DNA polymerase α, 3-deoxyaphidicolin and aphidicolin-17-monoacetate". ...
*  Betaenone
Patrick, D.; Heimbrook, D (1996). "Protein kinase inhibitors for the treatment of cancer". Drug Discovery Today. 1: 325-330. ... Novel Inhibitors of Protein Kinases". Journal of Natural Products. 63: 739-745. doi:10.1021/np9905259. PMID 10869191. ... The compounds were found to inhibit a variety of protein kinases. Betaenone A Betaenone B Betaenone C Two further betaenones ...
*  Ceritinib
Others examine the composition of protein kinase inhibitors. The most recent patents are specific the methodologies of using ... Ceritinib is a selective and potent inhibitor of anaplastic lymphoma kinase (ALK). In normal physiology, ALK functions as a key ... Ceritinib is an aplastic lymphoma kinase (ALK)-positive inhibitor primarily used for the treatment of metastatic NSCLC. ... Finally, ceritinib is both a substrate and potent inhibitor of the enzyme CYP3A4, so medications should be monitored carefully ...
*  Safingol
... is a lyso-sphingolipid protein kinase inhibitor. It has the molecular formula C18H39NO2 and is a colorless solid. ... Potentiation of apoptosis by treatment with the protein kinase C-specific inhibitor safingol in mitomycin C-treated gastric ... Safingol is also a putative inhibitor of sphingosine kinase 1 (SphK), which catalyzes the production of sphingosine 1-phosphate ... Safingol competitively competes with phorbol dibutyrate at regulatory domains of the protein kinase C family, inhibiting the ...
*  SU6656
2007). "The selectivity of protein kinase inhibitors: a further update". Biochem J. 408 (3): 297-315. doi:10.1042/BJ20070797. ... 2-INDOLINONE PROTEIN TYROSINE KINASE INHIBITORS Blake, R. A., M. A. Broome; et al. (2000). "SU6656, a selective src family ... SU6656 was initially identified as a Src kinase inhibitor by virtue of its ability to reverse an effect that an activated ... SU6656 is a Src family kinase inhibitor developed by the biotechnology company SUGEN Inc (a subsidiary of Pharmacia) in 2000. ...
*  Ralimetinib
It is a p38 mitogen-activated protein kinase inhibitor. A phase II trial for treatment of ovarian cancer is expected to be ...
*  Metastatic breast cancer
Experimental medications: sorafenib a combined Tyrosine protein kinases inhibitor. Scheduling of drug treatments and ... kinases. Heparanase cleaves heparin sulfate chains of HSPGs, which have an extensive network with several proteins on the cell ... The ECM protein tenascin C (TNC) is up-regulated in metastatic breast cancer. TNC is an adhesion-modulating extracellular ... Some of these proteins are discussed here in relation to breast-cancer metastasis. Fibronectin is an extracellular glycoprotein ...
*  Fasudil
Shibuya M, Suzuki Y (Sep 1993). "[Treatment of cerebral vasospasm by a protein kinase inhibitor AT 877]". Nō to Shinkei = Brain ... Fasudil (INN) is a potent Rho-kinase inhibitor and vasodilator. Since it was discovered, it has been used for the treatment of ... Nagumo H, Sasaki Y, Ono Y, Okamoto H, Seto M, Takuwa Y (Jan 2000). "Rho kinase inhibitor HA-1077 prevents Rho-mediated myosin ... Fasudil (HA-1077) is a selective RhoA/Rho kinase (ROCK) inhibitor. ROCK is an enzyme that plays an important role in mediating ...
*  Nilotinib
2010). "Extended kinase profile and properties of the protein kinase inhibitor nilotinib". Biochimica et Biophysica Acta. 1804 ... Nilotinib is a selective Bcr-Abl kinase inhibitor that is 10-30 fold more potent than imatinib in inhibiting Bcr-Abl tyrosine ... Bcr-Abl tyrosine-kinase inhibitor#Nilotinib (AMN107) re development and resistance "Tasigna (nilotinib) dosing, indications, ... Breccia, M.; Alimena, G. (2010). "Nilotinib: a second-generation tyrosine kinase inhibitor for chronic myeloid leukemia". ...
*  Staurosporine
1989) Staurosporine, K-252 and UCN-01: potent but nonspecific inhibitors of protein kinases. Trends in Pharmacological Science ... Staurosporine is the precursor of the novel protein kinase inhibitor midostaurin (PKC412). Besides midostaurin, staurosporine ... Staurosporine is a prototypical ATP-competitive kinase inhibitor in that it binds to many kinases with high affinity, though ... an inhibitor of protein kinases, on the cell cycle and chromatin structure of normal and leukemic lymphocytes. Cancer Res 52: ...
*  PIM2 (gene)
"Ruthenium half-sandwich complexes as protein kinase inhibitors: derivatization of the pyridocarbazole pharmacophore ligand". ... making it an attractive target for potent small-molecule PIM kinase inhibitors. Interestingly, many inhibitors are often more ... Serine/threonine-protein kinase Pim-2 is an enzyme that in humans is encoded by the PIM2 . PIM2 or Proviral Integrations of ... While PIM kinase to autophosphorylate, the functional consequences are not known. Inhibitor acts as ATP mimetic in ATP binding ...
*  Sunitinib
The drug was discovered at SUGEN, a biotechnology company which pioneered protein kinase inhibitors. It was the third in a ... This concept led to the invention of many small-molecule tyrosine kinase inhibitors, including Gleevec, Sutent, Tarceva and ... "Phase II study of SU11248, a multi-targeted tyrosine kinase inhibitor in patients with previously treated metastatic breast ... Sunitinib blocks the tyrosine kinase activities of KIT, PDGFR, VEGFR2 and other tyrosine kinases involved in the development of ...
*  SUGEN
... (Sugen) was a drug discovery company focused on development of protein kinase inhibitors. It was founded in 1991, and ... Sugen developed small-molecule inhibitors of protein kinases, key enzymes in signal transduction and cellular decision-making. ... leading to protein kinases being the second most active area of drug development, largely based on ATP-competitive inhibitors. ... after pioneering protein kinases as therapeutic targets and developing the successful cancer therapy sunitinib (Sutent). Sugen ...
*  John Woodland Hastings
Comolli, J.; Hastings, J. W. (1999). "Novel Effects on The Gonyaulax Circadian System Produced by the Protein Kinase Inhibitor ... 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: ...
*  Tyrosine-kinase inhibitor
Bcr-Abl tyrosine-kinase inhibitor Protein kinase inhibitor Yaish P, Gazit A, Gilon C, Levitzki A (1988). "Blocking of EGF- ... A tyrosine kinase inhibitor (TKI) is a pharmaceutical drug that inhibits tyrosine kinases. Tyrosine kinases are enzymes ... 2013). "ATP-competitive inhibitors block protein kinase recruitment to the Hsp90-Cdc37 system". Nture Chem Biol. 9 (5): 307-312 ... which do not inhibit protein kinases that phosphorylate serine or threonine residues and can discriminate between the kinase ...
*  H-89
... is a protein kinase inhibitor with greatest effect on protein kinase A (PKA). H-89, derived from H-8 (N-[2-(methylamino) ... novel and potent inhibitors of cyclic nucleotide dependent protein kinase and protein kinase C". Biochemistry. 23 (21): 5036- ... Marunaka, Yoshinori; Niisato, Naomi (2003). "H89, an inhibitor of protein kinase A (PKA), stimulates Na+ transport by ... neurite outgrowth and protein phosphorylation by a newly synthesized selective inhibitor of cyclic AMP-dependent protein kinase ...
*  P38 mitogen-activated protein kinases
Zhou, Z (2017). "Retention of normal glia function by an isoform-selective protein kinase inhibitor drug candidate that ... P38 mitogen-activated protein kinases are a class of mitogen-activated protein kinases (MAPKs) that are responsive to stress ... a novel p38 mitogen-activated protein kinase inhibitor: preclinical analysis of efficacy and selectivity". J. Pharmacol. Exp. ... p38 MAP Kinase (MAPK), also called RK or CSBP (Cytokinin Specific Binding Protein), is the mammalian orthologue of the yeast ...
*  G1 phase
Once the required proteins and growth are complete, the cell enters the next phase of the cell cycle, S phase. The duration of ... Biochemical triggers known as cyclin-dependent kinases (Cdks) switch on cell cycles events at the corrected time and in the ... and a high concentration of Cdk inhibitors is found during G1 phase. The restriction point (R) in the G1 phase is different ... In these cases where the G1 phase is affected, it is generally because gene regulatory proteins of the E2F family have become ...
*  BIM-1
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 ... Page CS, Bates PA (December 2006). "Can MM-PBSA calculations predict the specificities of protein kinase inhibitors?". J Comput ...