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Kinase, kinases inhibitors

Kurold, M. and O Flaherty, J.T. (1997). Differential effects of a mitogen-activated protein kinase kinase inhibitor on human neutrophil responses to chemotactic factors. Biochem. Biophys. Res. Commun. 232, 474 77. [Pg.391]

Neurotoxicity induced by oxidised low-density-lipoprotein in cultures of embryonic mouse striatal neurones was neither reduced nor enhanced by inhibiting extracellular signal-regulated kinases 1/2 activation with mitogen-activated protein kinase kinase inhibitors, suggesting that this cascade is unlikely to be involved in either oxidised low-density-lipoprotein toxicity or the protective effects of flavonoids (SCHROETER etal. 2001). [Pg.510]

Hur E, Chang KY, Lee E, Lee S-K, Park H. Mitogen-activated protein kinase kinase inhibitor PD98059 blocks the trans-activation hut not the stabilization or DNA hinding ability of h3q>oxia-inducible factor-la. Mol Pharmacol 2001 59 1216-1224. [Pg.106]

The cyclization with a,p-unsaturated nitriles has proven effective for the synthesis of 3-aminothiophene 14, a key intermediate for the synthesis of p38 kinase inhibitors."... [Pg.186]

The fact that the aliosterically preferred conformation may be relatively rare in the library of conformations available to the receptor may have kinetic implications. Specifically, if the binding site for the modulator appears only when the preferred conformation is formed spontaneously, then complete conversion to alios terically modified receptor may require a relatively long period of equilibration. For example, the allosteric p38 MAP kinase inhibitor BIRB 796 binds to a conformation of MAP kinase requiring movement of a Phe residue by 10 angstroms (so-called out conformation). The association rate for this modulator is 8.5 x 105 M-1 s-1, 50 times slower than that required for other inhibitors (4.3 x 107 M 1 s-1). The result is that while other inhibitors reach equilibrium within 30 minutes, BIRB 376 requires 2 full hours of equilibration time [8],... [Pg.129]

Kunkel, E. J., Plavec, L, Nguyen, D., Melrose, J., Rosier, E. S., Kao, L. T., Wang, Y., Hytopoulos, E., Bishop, A. C., Bateman, R., et al. (2004). Rapid structure-activity and selectivity analysis of kinase inhibitors by Bio Map analysis in complex human primary cell-based models. ASSAY Drug Dev. Technol. 2 431-441. [Pg.197]

Tyrosine Kinase Inhibitors/Receptor Associated Tyrosine Kinase Inhibitors (RTK-I)... [Pg.156]

P70S6 Kinase Inhibitors (Slrollmus, Everollmus, Temslrollmus)... [Pg.619]

BCR-ABL tyrosine kinase that is essential for malignant transformation. Cytogenetic responses to IFN-a therapy were seen in 30-40% of the treated patients with complete responses in about 10%. Long term survival can therefore be expected in these patients. In 2000, the BCR-ABL tyrosine kinase inhibitor Imatinib has been introduced for CML therapy and meanwhile has proven more efficient than IFN-a therapy. [Pg.645]

Changelian PS, Flanagan ME, Ball DJ et al (2003) Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor. Science 302 875-878... [Pg.669]

Tyrosine Kinase Inhibitors Protein Kinase Inhibitors... [Pg.673]

Kinase Inhibitors Mechanism of Action Biological Consequences... [Pg.743]

The most extensive development of pharmacological inhibitors of MAPK cascades members has been for p38 (Table 1) [3]. Small-molecule inhibitors have been developed for two p38 isoforms (a and (3). Pyridinyl imidazole compounds have been known to block inflammation since the early 1970s. Structural analyses have revealed that p38 kinase inhibitors binds to the ATP-binding pocket of p38 thereby acting as competitive inhibitors. The p38 kinase inhibitor SB202190 is able to bind both the low-activity nonphosphorylated... [Pg.744]

Protein Kinase Inhibitors. Figure 1 Major mechanism by which inhibitors can prevent the activity of protein kinases. [Pg.1009]


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See also in sourсe #XX -- [ Pg.200 ]




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2,4-diamino pyrimidine kinase inhibitors

AKT kinase inhibitors

Activated Protein (MAP) Kinase Inhibitors

Active Inhibitor-insensitive Kinase Mutants (Orthogonal Protein Kinases)

Adenosine kinase inhibitor

Adenosine triphosphate -competitive kinase inhibitor

Aurora kinase inhibitor

Bcr-Abl kinase inhibitors

Bcr-Abl-tyrosine kinase inhibitor

Beyond kinase inhibitors

Binding Modes for Early Kinase Inhibitors

Binding kinase inhibitors

Bisubstrate tyrosine kinase inhibitors

Breast Cancer Human Epidermal Growth Factor Tyrosine Kinase Inhibitors

C-Kit kinases inhibitors

CKIs (cyclin-dependent kinase inhibitors

Cancer chemotherapy tyrosine kinase inhibitors

Cancer, treatment using tyrosine kinase inhibitors

Cancer, treatment using tyrosine kinase receptor inhibitors

Cell cycle cyclin-dependent kinase inhibitors

Checkpoint kinase-1 inhibitors

Chemotherapy tyrosine kinase inhibitors

Choline kinase inhibitors

Creatine kinase inhibitors

Cyclin dependent kinase inhibitors

Cyclin dependent kinase inhibitors synthesis

Cyclin kinase inhibitors

Cyclin-dependant kinase inhibitor

Cyclin-dependent kinase 4 , inhibitor activity against

Cyclin-dependent kinase inhibitor p21Wafl

Cyclin-dependent kinase inhibitors cell cycle regulation

Cydin kinase inhibitors

Drug kinase inhibitors

EFGR tyrosine kinase inhibitor

EGFR tyrosine kinase inhibitor

Focal adhesion kinase inhibitor

Glycogen synthase kinase inhibitors

Guanylate kinase, inhibitors

Histidine kinases inhibitors

Imidazoles tyrosine kinase inhibitor

Inhibitor-insensitive kinase

Inhibitors, spleen tyrosine kinase

Insulin receptor kinase inhibitor

Irreversible kinase inhibitors

Janus kinase 2 inhibitors

Jun N-terminal kinase inhibitor

K-252c protein kinase inhibitor

KDR kinase inhibitors

Kinase Growth Factor VEGFR-2 and FGFR-1 Inhibitors

Kinase Inhibitor Scaffolds

Kinase Inhibitors - Stabilizing Inactive Enzyme Conformations

Kinase Inhibitors Designed to Crate Floppy Regions

Kinase domain receptor inhibitors

Kinase inhibition, inhibitors

Kinase inhibitors

Kinase inhibitors

Kinase inhibitors hinge binding

Kinase inhibitors ligands

Kinase inhibitors targeting with small molecule

Kinase inhibitors types

Kinase orthogonal inhibitors

Kinase, kinases inhibitor-insensitive

Kinase, kinases irreversible inhibitors

Kinase-inhibitor-likeness

Library kinase inhibitor

Light Chain Kinase Inhibitors

Macrocyclic kinase inhibitors

Macrocyclic kinase inhibitors CDKs)

Macrocyclic kinase inhibitors macrocycle design

Macrocyclic kinase inhibitors synthesis

Microxine as Cdc2 kinase inhibitor

Mitogen-activated protein kinase inhibitors

Multi-kinase inhibitors

Multi-target kinase inhibitors

Multiple tyrosine kinase inhibitor

Natural tyrosine kinase inhibitor

Nucleoside kinase transcriptase inhibitors

Of tyrosine kinase inhibitor

P38 MAP kinase inhibitors

P38 kinase inhibitors

PI3 kinase inhibitors

Phosphatidylinositol-3-kinases inhibitors

Pirn kinase inhibitors

Polo-like kinases inhibitors

Protein Kinase Inhibitor History

Protein kinase A inhibitors

Protein kinase B inhibitors

Protein kinase C inhibitors

Protein kinase family inhibitor selectivity

Protein kinase inhibitors

Protein kinase inhibitors design/discovery

Protein kinase inhibitors signal transduction

Protein kinase inhibitors, for cancer

Protein kinase-bisubstrate analog inhibitors

Protein kinases inhibitors/drug targets

Protein-tyrosine Kinase Inhibitors

Raf kinase inhibitor protein

Raf kinase inhibitor, sorafenib

Raf kinase inhibitors

Receptor tyrosine kinase inhibitor

Rho kinase inhibitor

SIFt and the Analysis of Protein Kinase - Inhibitor Complexes

Sphingosine kinases inhibitors

Structural Aspects of Kinase Inhibitors

Structural Aspects of Kinases and Their Inhibitors

The Mechanisms and Kinetics of Protein Kinase Inhibitors

Thymidine Kinase Substrates and Inhibitors

Thymidine kinase inhibitors

Tie2 tyrosine kinase inhibitor

Treatment mitogen-activated protein kinase inhibitors

Tumor suppressor genes cyclin dependent kinase inhibitors

Tyrosine kinase inhibitor therapy

Tyrosine kinase inhibitors

Tyrosine kinase inhibitors Philadelphia chromosome

Tyrosine kinase inhibitors biological activity

Tyrosine kinase inhibitors imatinib mesylate

Tyrosine kinase inhibitors in cancer therapy

Tyrosine kinase inhibitors molecular modeling

Tyrosine kinase plant-derived inhibitors

Tyrosine-specific kinase inhibitor

Uniquely Inhibitable Kinases inhibitor

VEGF receptor tyrosine kinase inhibitors

Vascular endothelial growth factor tyrosine kinase inhibitors

Will P. falciparum Kinase Inhibitors Work as Anti-Malarial Drugs

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