*  Plus it
Tyrosine kinase domain mutations are a common cause of acquired clinical resistance to tyrosine kinase inhibitors (TKI) used to ... Following kinase activation, the FLT3 protein was incubated with 100 μmol/L quizartinib for 1 hour at room temperature. The ... Multiple BCR-ABL kinase domain mutations confer polyclonal resistance to the tyrosine kinase inhibitor imatinib (STI571) in ... Structural mechanism of the Pan-BCR-ABL inhibitor ponatinib (AP24534): lessons for overcoming kinase inhibitor resistance. Chem ...
  http://cancerdiscovery.aacrjournals.org/content/5/6/668
*  Abstract C93: The design and synthesis of a novel fluorogenic probe targeting inactive forms of Burton's tyrosine kinase for...
Targeting inactive conformations of kinase is an attractive approach for drug discovery to develop a selective kinase inhibitor ... As expected, the NBD-labeled CGI1746 probe showed strong fluorescence when it mixied with Btk protein but quenched by adding of ... The Burton's tyrosine kinase (Btk) is a member of the Tec family of cytoplasmic tyrosine kinase and plays a crucial role in the ... Therefore inhibitors of Btk are considered as potential therapeutic agents for the treatment of B cell lymphoma, chronic ...
  http://mct.aacrjournals.org/content/10/11_Supplement/C93
*  Dovitinib - AdisInsight
... an oral multi-targeted receptor tyrosine kinase inhibitor, for the treatment of cancer. Dovitinib strongly ... Fms-like tyrosine kinase 3 inhibitors; Platelet-derived growth factor beta receptor antagonists; Proto oncogene protein c-kit ... Alternative Names: CHIR-258; Dovitinib lactate; GFKI-258; Growth factor kinase inhibitor 258; TKI 258 Latest Information Update ... inhibitors; Type 3 fibroblast growth factor receptor antagonists; Vascular endothelial growth factor receptor antagonists ...
  http://adisinsight.springer.com/drugs/800019244?error=cookies_not_supported&code=f9baf102-28b3-4938-adb3-5af360056640
*  PDB 1qpc citation summary ‹ Protein Data Bank in Europe (PDBe) ‹ EMBL-EBI
Structural analysis of the lymphocyte-specific kinase Lck in complex with non-selective and Src family selective kinase ... a potent but non-selective protein kinase inhibitor); and PP2 (a potent Src family selective protein tyrosine kinase inhibitor ... Can MM-PBSA calculations predict the specificities of protein kinase inhibitors? Page CS, Bates PA. J Comput Chem 27 1990-2007 ... Structural biology in drug design: selective protein kinase inhibitors. Scapin G. Drug Discov. Today 7 601-611 (2002) ...
  http://www.ebi.ac.uk/pdbe/entry/pdb/1qpc/citations
*  Plus it
A novel ALK secondary mutation and EGFR signaling cause resistance to ALK kinase inhibitors. Cancer Res 2011;71:6051-60. ... 2A and B). All four shRNA vectors decreased NF1 mRNA and 3 of 4 had an appreciable effect on protein level (Fig. 2A and B). We ... Loss of NF1 has recently been reported to drive resistance to tyrosine kinase inhibitors in a number of settings including BRAF ... Dasatinib is an FDA-approved oral tyrosine kinase inhibitor, which has been studied in several trials of patients with lung ...
  http://mct.aacrjournals.org/content/13/2/475
*  CID 11654378 | FMS receptor tyrosine kinase inhibitor | FMS inhibitor compound 8 | FMS inhibitor compound 1b | CID11654378 |...
FMS inhibitor compound 8 , FMS inhibitor compound 1b , CID11654378 , CID-11654378 , CAS [885704-21-2] , Axon 2061 , Axon Ligand ... Selective DDR1 receptor tyrosine kinase (RTK) inhibitor €95.00 2571 GW 2580 Orally bioavailable inhibitor of cFMS kinase and ... Potent FMS kinase inhibitor Chemical name. 4-cyano-N-(4-(4-methylpiperazin-1-yl)-2-(4-methylpiperidin-1-yl)phenyl)-1H-pyrrole-2 ... A highly potent FMS kinase inhibitor (IC50 = 0.8 nM); a proof-of-concept candidate in a collagen-induced model of arthritis in ...
  https://www.axonmedchem.com/product/2061
*  ChemistryOpen hot off the press! | Wiley Open Access
Eric Meggers, Holger Steuber and co-workers present an organometallic inhibitor scaffold for Pim kinases. These are interesting ... Usually kinase inhibitors are ATP competitive. However, as shown in… ... The current Issue of ChemistryOpen includes an exciting Communication on a Non-ATP-Mimetic Organometallic Protein Kinase ... current Issue of ChemistryOpen includes an exciting Communication on a Non-ATP-Mimetic Organometallic Protein Kinase Inhibitor ...
  https://wileyopenaccess.wordpress.com/2014/01/24/chemistryopen-hot-off-the-press/
*  Good Growth Opportunities in Kinase Inhibitors For Cancer Treatment Market Till 2026
Kinase Inhibitors are specific enzymes which oppose the process of cell division and growth in cancerous cells. It comes handy ... normally a protein with an important role in tumor development or growth. This methodology differs from the more observed ... Kinase Inhibitors for Cancer Treatment Market: Key Players. Some of the key participating global players in kinase inhibitors ... Kinase Inhibitors for Cancer Treatment Market: Overview. The global market for kinase inhibitors for cancer treatmentis ...
  https://theglobalhealthnews.com/kinase-inhibitors-cancer-treatment-market/
*  Improved tyrosine kinase inhibitor (TKI) selectively activates in tumor tissue, minimizing side effects in patients - ONA
... by an interdisciplinary team of researchers aims to reduce the side effects connected to use of tyrosine kinase inhibitors ( ... The action of tyrosine kinase inhibitors is based on the specific inhibition of proteins overactivated in cancer cells, driving ... Improved tyrosine kinase inhibitor (TKI) selectively activates in tumor tissue, minimizing side effects in patients. Share this ... So far no comparable strategy exists to reduce the severe side effects of tyrosine kinase inhibitors. It is hoped that this ...
  http://www.oncologynurseadvisor.com/web-exclusives/improved-tyrosine-kinase-inhibitor-tki-selectively-activates-in-tumor-tissue-minimizing-side-effects-in-patients/article/379032/
*  Chordomas - DrugBank
Imatinib is a small molecule kinase inhibitor used to treat certain types of cancer. It is currently marketed by Novartis as ... Multidrug resistance protein 1. transporter. DB00877. Sirolimus. Solute carrier organic anion transporter family member 1B1. ... It is the first member of a new class of agents that act by inhibiting particular tyrosine kinase enzymes, instead of non- ...
  https://www.drugbank.ca/indications/DBCOND0042698
*  Anti-Inflammatory Effects of Protein Kinase Inhibitor Pyrrol Derivate
... Halyna M. Kuznietsova, Maryna S. Yena, Iryna P. Kotlyar ... In our previous studies we showed antitumor and anti-inflammatory activities of protein kinases inhibitor pyrrol derivate 1-(4- ... Increase of malonic dialdehyde (MDA) by 89% and protein carbonyl groups (PCG) by 60% and decrease of superoxide dismutase (SOD ...
  https://www.hindawi.com/journals/tswj/2016/2145753/abs/
*  Anti-Inflammatory Effects of Protein Kinase Inhibitor Pyrrol Derivate
MI-1 was synthesized as protein kinases inhibitor [8]. It was tested on 32 protein kinases for determination of inhibitory ... Anti-Inflammatory Effects of Protein Kinase Inhibitor Pyrrol Derivate. Halyna M. Kuznietsova, Maryna S. Yena, Iryna P. Kotlyar ... Protein kinase inhibitor pyrrol derivate 1-(4-Cl-benzyl)-3-Cl-4-(CF3-fenylamino)-1Н-pyrrol-2,5-dione (MI-1) (Figure 1) has been ... G. G. Dubinina, O. O. Chupryna, M. O. Platonov et al., "In silico design of protein kinase inhibitors: successes and failures ...
  https://www.hindawi.com/journals/tswj/2016/2145753/
*  Pharmaceuticals | Free Full-Text | cGMP-Dependent Protein Kinase Inhibitors in Health and Disease | Notes
Various inhibitors of PKG were developed directed against diverse functional regions of the kinase. These inhibitors of PKG ... The review article will summarize these different inhibitors regarding their specificity and their present applications in ... which expresses the membrane associated PKG-II protein. The enzyme kinetics, the localization and the substrates of these PKG ... cGMP-dependent protein kinases (PKG) exhibit diverse physiological functions in the mammalian system e.g., in vascular and ...
  http://www.mdpi.com/1424-8247/6/2/269/notes
*  United States Protein Kinase Inhibitor Market Report 2017 : ReportsnReports
In this report, the United States Protein Kinase Inhibitor market... ... 96 Pages Report] Check for Discount on United States Protein Kinase Inhibitor Market Report 2017 report by QYResearch Group. ... 1.2.3 Serine/Threonine Protein Kinase Inhibitors. 1.2.4 Tyrosine Protein Kinase Inhibitor. 1.3 United States Protein Kinase ... 1 Protein Kinase Inhibitor Overview. 1.1 Product Overview and Scope of Protein Kinase Inhibitor. 1.2 Classification of Protein ...
  http://www.reportsnreports.com/reports/897534-united-states-protein-kinase-inhibitor-market-report-2017.html
*  Inhibition of Nucleoside Transport by Protein Kinase Inhibitors | Journal of Pharmacology and Experimental Therapeutics
Inhibition of Nucleoside Transport by Protein Kinase Inhibitors. Min Huang, Yanhong Wang, Susan B. Cogut, Beverly S. Mitchell ... Inhibition of Nucleoside Transport by Protein Kinase Inhibitors. Min Huang, Yanhong Wang, Susan B. Cogut, Beverly S. Mitchell ... Inhibition of Nucleoside Transport by Protein Kinase Inhibitors. Min Huang, Yanhong Wang, Susan B. Cogut, Beverly S. Mitchell ... Inhibition of Nucleoside Transport by Protein Kinase Inhibitors Message Subject (Your Name) has forwarded a page to you from ...
  http://jpet.aspetjournals.org/content/304/2/753
*  RCSB PDB - Protein Feature View - cAMP-dependent protein kinase inhibitor alpha - P63248 (IPKA MOUSE)
The PDB archive contains information about experimentally-determined structures of proteins, nucleic acids, and complex ... Extremely potent competitive inhibitor of cAMP-dependent protein kinase activity, this protein interacts with the catalytic ... This protein in other organisms (by gene name): P63248 - Mus musculus 22 * P61926 - Oryctolagus cuniculus 21 ... Protein disorder predictions are based on JRONN (Troshin, P. and Barton, G. J. unpublished), a Java implementation of RONN * ...
  http://www.rcsb.org/pdb/protein/P63248
*  RCSB PDB - Protein Feature View - cAMP-dependent protein kinase inhibitor alpha - P63249 (IPKA RAT)
The PDB archive contains information about experimentally-determined structures of proteins, nucleic acids, and complex ... Extremely potent competitive inhibitor of cAMP-dependent protein kinase activity, this protein interacts with the catalytic ... This protein in other organisms (by gene name): P63249 - Rattus norvegicus 5 * P61926 - Oryctolagus cuniculus 20 ... Protein disorder predictions are based on JRONN (Troshin, P. and Barton, G. J. unpublished), a Java implementation of RONN * ...
  http://www.rcsb.org/pdb/protein/P63249
*  Development of sirtuin and calmodulin-dependent protein kinase inhibitors as anti-cancer therapeutics
... identifying more selective sirtuin inhibitors and more potent calmodulin-dependent protein kinase inhibitors.The sirtuins are a ... Small molecule inhibitors of the human sirtuins and calmodulin-dependent protein kinases have shown promising anti-cancer ... Development of sirtuin and calmodulin-dependent protein kinase inhibitors as anti-cancer therapeutics. ... an inhibitor of the calmodulin-dependent protein kinases (CaMKs), enhances the terminal differentiation of retinoic acid ...
  https://digital.lib.washington.edu/researchworks/handle/1773/8491
*  Protein kinase inhibitors selectively block phorbol ester- or forskolin- induced changes in excitability of Aplysia neurons |...
Protein kinase inhibitors selectively block phorbol ester- or forskolin- induced changes in excitability of Aplysia neurons. PJ ... Protein kinase inhibitors selectively block phorbol ester- or forskolin- induced changes in excitability of Aplysia neurons ... Protein kinase inhibitors selectively block phorbol ester- or forskolin- induced changes in excitability of Aplysia neurons ... Protein kinase inhibitors selectively block phorbol ester- or forskolin- induced changes in excitability of Aplysia neurons ...
  http://www.jneurosci.org/content/9/2/473
*  Effects of HA1077, a protein kinase inhibitor, on myosin phosphorylation and tension in smooth muscle. | Sigma-Aldrich
Effects of HA1077, a protein kinase inhibitor, on myosin phosphorylation and tension in smooth muscle.. [M Seto, Y Sasaki, H ... We examined the effects of HA1077, a potent inhibitor of protein kinases in vitro, on the relationship between tension and ... observations indicate that the relationship between tension and MLC20 phosphorylation involves inhibition of protein kinases by ...
  https://www.sigmaaldrich.com/catalog/papers/1874276
*  Protein kinase inhibitor - Wikipedia
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 ...
  https://en.wikipedia.org/wiki/Protein_kinase_inhibitor
*  Protein Kinase inhibitors for the treatment of thyroid cancer: molecular mechanisms of resistance - fedOA
Magesh, Muthu (2011) Protein Kinase inhibitors for the treatment of thyroid cancer: molecular mechanisms of resistance. [Tesi ... Protein Kinase inhibitors for the treatment of thyroid cancer: molecular mechanisms of resistance. ... protein kinase small molecule inhibitors (PKI) have been considered as promising novel agents for the treatment of thyroid ... Mechanisms of resistance, thyroid cancer, kinase inhibitors. Settori scientifico-disciplinari del MIUR:. Area 06 - Scienze ...
  http://www.fedoa.unina.it/8777/
*  Mitogen activated protein kinase inhibitors: where are we now and where are we going? | Annals of the Rheumatic Diseases
Mitogen activated protein kinase inhibitors: where are we now and where are we going? ... Mitogen activated protein kinase inhibitors: where are we now and where are we going? ... The mitogen activated protein (MAP) kinases are especially attractive because they regulate both cytokine production and ... These approaches might permit effective use of MAP kinase inhibitors for the treatment of rheumatic and immune-mediated ...
  http://ard.bmj.com/content/65/suppl_3/iii83
*  Marine Drugs | Free Full-Text | Marine Derived Hamacanthins as Lead for the Development of Novel PDGFRβ Protein Kinase...
... competitive protein kinase inhibitors with implications as anti-cancer drugs. Initially, we identified the pyrazin-2(1H)-one ... by Molecular Modeling studies as core binding motif in the ATP pocket of receptor tyrosine kinases (RTK), which are validated ... ones showing interesting properties as lead for their further development towards potent PDGFR-inhibitors. ...
  http://www.mdpi.com/1660-3397/11/9/3209/notes
*  Randomized Phase II Study of AZD6244 (Mitogen-activated Protein Kinase Inhibitor) MEK-Inhibitor With Erlotinib in KRAS Wild...
Randomized Phase II Study of AZD6244 (Mitogen-activated Protein Kinase Inhibitor) MEK-Inhibitor With Erlotinib in KRAS Wild ... Protein Kinase Inhibitors. Antineoplastic Agents. Enzyme Inhibitors. Molecular Mechanisms of Pharmacological Action. ... Previous MEK (methyl ethyl ketone) inhibitor or prior treatment with EGFR TKI (tyrosine kinase inhibitor). ... mitogen-activated protein) kinase pathway) that causes some lung cancer cells to grow. The MAP kinase pathway could be ...
  https://clinicaltrials.gov/ct2/show/NCT01229150?term=AZD6244%2FErlotinib%3A+NSCLC&rank=1