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Showing 25 to 36 of 135 entries
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A Back-to-Front Fragment-Based Drug Design Search Strategy Targeting the DFG-Out Pocket of Protein Tyrosine Kinases.

ACS medicinal chemistry letters

Iwata H, Oki H, Okada K, Takagi T, Tawada M, Miyazaki Y, Imamura S, Hori A, Lawson JD, Hixon MS, Kimura H, Miki H.
PMID: 24900475
ACS Med Chem Lett. 2012 Feb 28;3(4):342-6. doi: 10.1021/ml3000403. eCollection 2012 Apr 12.

We present a straightforward process for the discovery of novel back pocket-binding fragment molecules against protein tyrosine kinases. The approach begins by screening against the nonphosphorylated target kinase with subsequent counterscreening of hits against the phosphorylated enzyme. Back pocket-binding...

Atypical Teratoid Rhabdoid Tumour : From Tumours to Therapies.

Journal of Korean Neurosurgical Society

Richardson EA, Ho B, Huang A.
PMID: 29742888
J Korean Neurosurg Soc. 2018 May;61(3):302-311. doi: 10.3340/jkns.2018.0061. Epub 2018 May 01.

Atypical teratoid rhabdoid tumours (ATRTs) are the most common malignant central nervous system tumours in children ≤1 year of age and represent approximately 1-2% of all pediatric brain tumours. ATRT is a primarily monogenic disease characterized by the bi-allelic...

Phase I clinical trial combining imatinib mesylate and IL-2 in refractory cancer patients: IL-2 interferes with the pharmacokinetics of imatinib mesylate.

Oncoimmunology

Pautier P, Locher C, Robert C, Deroussent A, Flament C, Le Cesne A, Rey A, Bahleda R, Ribrag V, Soria JC, Vassal G, Eggermont A, Zitvogel L, Chaput N, Paci A.
PMID: 23525192
Oncoimmunology. 2013 Feb 01;2(2):e23079. doi: 10.4161/onci.23079.

Imatinib mesylate (IM) is a small molecule inhibitor of protein tyrosine kinases. In addition to its direct effect on malignant cells, it has been suggested IM may activate of natural killer (NK) cells, hence exerting immunomodulatory functions. In preclinical...

Tyrosine kinases in rheumatoid arthritis.

Journal of inflammation (London, England)

Okamoto H, Kobayashi A.
PMID: 21861931
J Inflamm (Lond). 2011 Aug 24;8:21. doi: 10.1186/1476-9255-8-21.

Rheumatoid arthritis (RA) is an inflammatory, polyarticular joint disease. A number of cellular responses are involved in the pathogenesis of rheumatoid arthritis, including activation of inflammatory cells and cytokine expression. The cellular responses involved in each of these processes...

Moving on up: Second-Line Agents as Initial Treatment for Newly-Diagnosed Patients with Chronic Phase CML.

Clinical Medicine Insights. Oncology

Shieh MP, Mitsuhashi M, Lilly M.
PMID: 21792346
Clin Med Insights Oncol. 2011;5:185-99. doi: 10.4137/CMO.S6416. Epub 2011 Jun 23.

The treatment of chronic myelogenous leukemia (CML) was revolutionized by the development of imatinib mesylate, a small molecule inhibitor of several protein tyrosine kinases, including the ABL1 protein tyrosine kinase. The current second generation of FDA-approved ABL tyrosine kinase...

Lysophosphatidic acid induces protein tyrosine phosphorylation in the absence of phospholipase C activation in human platelets.

Platelets

[No authors listed]
PMID: 16793648
Platelets. 1997 Apr;8(2):181-8. doi: 10.1080/09537109777456.

Lysophosphatidic acid is a biologically active phospholipid able to induce cell proliferation and platelet aggregation. In this study we investigated the biochemical mechanisms of platelet activation by lysophosphatidic acid. We found that lysophosphatidic acid stimulated 4-azidoanilido-{ alpha 32P}GTP to...

JAKs and STATs branch out.

Trends in cell biology

Briscoe J, Kohlhuber F, Müller M.
PMID: 15157430
Trends Cell Biol. 1996 Sep;6(9):336-40. doi: 10.1016/0962-8924(96)10028-3.

The JAK-STAT signal-transduction pathway is utilized by a wide range of cytokines to regulate gene expression. Cytokines activate members of the JAK family o f protein tyrosine kinases, which in turn activate, by tyrosine phosphorylation, one or more STAT...

The use of erythrocytic and animal models in the study of protein phosphorylation.

Environmental toxicology and pharmacology

Bordin L, Coleman MD, Clari G.
PMID: 21783652
Environ Toxicol Pharmacol. 2006 Feb;21(2):148-52. doi: 10.1016/j.etap.2005.07.005. Epub 2005 Aug 15.

Phosphorylation processes are common post-transductional mechanisms, by which it is possible to modulate a number of metabolic pathways. Proteins are highly sensitive to phosphorylation, which governs many protein-protein interactions. The enzymatic activity of some protein tyrosine-kinases is under tyrosine-phosphorylation...

Critical role of Shp2 in tumor growth involving regulation of c-Myc.

Genes & cancer

Ren Y, Chen Z, Chen L, Fang B, Win-Piazza H, Haura E, Koomen JM, Wu J.
PMID: 21442024
Genes Cancer. 2010 Oct;1(10):994-1007. doi: 10.1177/1947601910395582.

Activating mutants of Shp2 protein tyrosine phosphatase, encoded by the PTPN11 gene, are linked to leukemia. In solid tumors, however, PTPN11 mutations occur at low frequencies while the wildtype Shp2 is activated by protein tyrosine kinases (PTKs) in cancer...

Lysophosphatidic acid induces protein tyrosine phosphorylation in the absence of phospholipase C activation in human platelets.

Platelets

Torti M, Festetics ET, Bertoni A, Moratti R, Balduini C, Sinigaglia F.
PMID: 20297941
Platelets. 1997;8(2):181-7. doi: 10.1080/09537109709169335.

Lysophosphatidic acid is a biologically active phospholipid able to induce cell proliferation and platelet aggregation. In this study we investigated the biochemical mechanisms of platelet activation by lysophosphatidic acid. We found that lysophosphatidic acid stimulated the binding of the...

A review on Eph/ephrin, angiogenesis and lymphangiogenesis in gastric, colorectal and pancreatic cancers.

Chinese journal of cancer research = Chung-kuo yen cheng yen chiu

Rudno-Rudzińska J, Kielan W, Frejlich E, Kotulski K, Hap W, Kurnol K, Dzierżek P, Zawadzki M, Hałoń A.
PMID: 28947862
Chin J Cancer Res. 2017 Aug;29(4):303-312. doi: 10.21147/j.issn.1000-9604.2017.04.03.

Erythroprotein-producing human hepatocellular carcinoma receptors (Eph receptors) compose a subfamily of transmembrane protein-tyrosine kinases receptors that takes part in numerous physiological and pathological processes. Eph family receptor-interacting proteins (Ephrins) are ligands for those receptors. Eph/ephrin system is responsible for...

Protein-tyrosine phosphorylation in Bacillus subtilis: a 10-year retrospective.

Frontiers in microbiology

Mijakovic I, Deutscher J.
PMID: 25667587
Front Microbiol. 2015 Jan 23;6:18. doi: 10.3389/fmicb.2015.00018. eCollection 2015.

The discovery of tyrosine-phosphorylated proteins in Bacillus subtilis in the year 2003 was followed by a decade of intensive research activity. Here we provide an overview of the lessons learned in that period. While the number of characterized kinases...

Showing 25 to 36 of 135 entries