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Tyrosine Phosphorylation of Mitochondrial Pyruvate Dehydrogenase Kinase 1 Is Important for Cancer Metabolism

Molecular cell, 2011-12, Vol.44 (6), p.864-877

2011

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Tyrosine phosphorylation inhibits PKM2 to promote the Warburg effect and tumor growth

Science signaling, 2009-11, Vol.2 (97), p.ra73

2009

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Mechanisms of resistance to imatinib mesylate in gastrointestinal stromal tumors and activity of the PKC412 inhibitor against imatinib-resistant mutants

Gastroenterology (New York, N.Y. 1943), 2005-02, Vol.128 (2), p.270-279

2005

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Clinical resistance to the kinase inhibitor PKC412 in acute myeloid leukemia by mutation of Asn-676 in the FLT3 tyrosine kinase domain

Blood, 2006-01, Vol.107 (1), p.293-300

2006

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Fibroblast Growth Factor Receptor 3 Associates with and Tyrosine Phosphorylates p90 RSK2, Leading to RSK2 Activation That Mediates Hematopoietic Transformation

Molecular and Cellular Biology, 2009-04, Vol.29 (8), p.2105-2117

2009

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PKC412 Inhibits the Zinc Finger 198-Fibroblast Growth Factor Receptor 1 Fusion Tyrosine Kinase and Is Active in Treatment of Stem Cell Myeloproliferative Disorder

Proceedings of the National Academy of Sciences - PNAS, 2004-10, Vol.101 (40), p.14479-14484

2004

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Uniform sensitivity of FLT3 activation loop mutants to the tyrosine kinase inhibitor midostaurin

Blood, 2007-12, Vol.110 (13), p.4476-4479

2007

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Investigation into CYP3A4-mediated drug–drug interactions on midostaurin in healthy volunteers

Cancer chemotherapy and pharmacology, 2013-12, Vol.72 (6), p.1223-1234

2013

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Comparison of the Kinase Profile of Midostaurin (Rydapt) with That of Its Predominant Metabolites and the Potential Relevance of Some Newly Identified Targets to Leukemia Therapy

Biochemistry (Easton), 2018-09, Vol.57 (38), p.5576-5590

2018

Volltextzugriff (PDF)

Comparison of the Profile of the AML Drug Midostaurin (Rydapt®) As a Kinase Inhibitor with Those of Its Predominant Primary Human Metabolites

Blood, 2017-12, Vol.130, p.1383-1383

2017

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Target interaction profiling of midostaurin and its metabolites in neoplastic mast cells predicts distinct effects on activation and growth

Leukemia, 2016-02, Vol.30 (2), p.464-472

2016

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Plasma inhibitory activity (PIA): a pharmacodynamic assay reveals insights into the basis for cytotoxic response to FLT3 inhibitors

Blood, 2006-11, Vol.108 (10), p.3477-3483

2006

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[(Alkylamino)methyl]acrylophenones: Potent and Selective Inhibitors of the Epidermal Growth Factor Receptor Protein Tyrosine Kinase

Journal of medicinal chemistry, 1995-06, Vol.38 (13), p.2441-2448

1995

Volltextzugriff (PDF)

Aromatic Interactions with Phenylalanine 691 and Cysteine 828: A Concept for FMS-like Tyrosine Kinase-3 Inhibition. Application to the Discovery of a New Class of Potential Antileukemia Agents

Journal of medicinal chemistry, 2006-07, Vol.49 (15), p.4451-4454

2006

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The Midostaurin (PKC412) Metabolite CGP52421 Shows Little Growth-Inhibitory Activity Against Against Neoplastic Mast Cells but Retains Inhibitory Effects on IgE-Dependent Activation and Histamine Release

Blood, 2011-11, Vol.118 (21), p.1417-1417

2011

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Fingolimod (FTY720) Inhibits BCR-ABL Signaling Allosterically by Binding to the Myristate Binding Site

Blood, 2011-11, Vol.118 (21), p.2746-2746

2011

Volltextzugriff (PDF)

Markers of tumor angiogenesis and proteolysis independently define high- and low-risk subsets of node-negative breast cancer patients

Journal of clinical oncology, 1998-09, Vol.16 (9), p.3129-3136

1998

Volltextzugriff (PDF)

Abstract 5371: A pooled apoptome shRNA screen to identify pathways that enhance NVP-BEZ235-induced apoptosis

Cancer research (Chicago, Ill.), 2011-04, Vol.71 (8_Supplement), p.5371-5371

2011

Volltextzugriff (PDF)

Novel Spirodihydrobenzofuranlactams as Antagonists of Endothelin and as Inhibitors of HIV-1 Protease Produced by Stachybotrys sp: I. Fermentation, Isolation and Biological Activity

The Journal of Antibiotics, 1996/01/25, Vol.49(1), pp.13-19

1996

Volltextzugriff (PDF)

Antileukemic Effects of Novel First- and Second-Generation FLT3 Inhibitors: Structure-Affinity Comparison

Genes & cancer, 2010-10, Vol.1 (10), p.1021-1032

2010

Volltextzugriff (PDF)

Sulfonylbenzoyl-nitrostyrenes: Potential bisubstrate type inhibitors of the EGF-receptor tyrosine protein kinase

Journal of medicinal chemistry, 1991-08, Vol.34 (8), p.2328-2337

1991

Volltextzugriff (PDF)

Abstract A140: Evaluation of prediction of in vivo activity from in vitro combinations: Examples using a MEK1/2 inhibitor combined with docetaxel in NSCLC models

Molecular cancer therapeutics, 2013-11, Vol.12 (11_Supplement), p.A140-A140

2013

Volltextzugriff (PDF)

Abstract 1257: Tyrosine phosphorylation of mitochondrial pyruvate dehydrogenase kinase 1 is important for cancer metabolism

Cancer research (Chicago, Ill.), 2011-04, Vol.71 (8_Supplement), p.1257-1257

2011

Volltextzugriff (PDF)

Abstract 2798: Tyrosine phosphorylation of LDH-A is important for cancer cell redox homeostasis and tumor growth

Cancer research (Chicago, Ill.), 2011-04, Vol.71 (8_Supplement), p.2798-2798

2011

Volltextzugriff (PDF)

Entry into a New Class of Potent Proteasome Inhibitors Having High Antiproliferative Activity by Structure-Based Design

Journal of medicinal chemistry, 2004-09, Vol.47 (20), p.4810-4813

2004

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Tyrosine Phosphorylation of Mitochondrial Pyruvate Dehydrogenase Kinase 1 Is Important for Cancer Metabolism

Tyrosine phosphorylation inhibits PKM2 to promote the Warburg effect and tumor growth

Mechanisms of resistance to imatinib mesylate in gastrointestinal stromal tumors and activity of the PKC412 inhibitor against imatinib-resistant mutants

Clinical resistance to the kinase inhibitor PKC412 in acute myeloid leukemia by mutation of Asn-676 in the FLT3 tyrosine kinase domain

Fibroblast Growth Factor Receptor 3 Associates with and Tyrosine Phosphorylates p90 RSK2, Leading to RSK2 Activation That Mediates Hematopoietic Transformation

PKC412 Inhibits the Zinc Finger 198-Fibroblast Growth Factor Receptor 1 Fusion Tyrosine Kinase and Is Active in Treatment of Stem Cell Myeloproliferative Disorder

Uniform sensitivity of FLT3 activation loop mutants to the tyrosine kinase inhibitor midostaurin

Investigation into CYP3A4-mediated drug–drug interactions on midostaurin in healthy volunteers

Comparison of the Kinase Profile of Midostaurin (Rydapt) with That of Its Predominant Metabolites and the Potential Relevance of Some Newly Identified Targets to Leukemia Therapy

Comparison of the Profile of the AML Drug Midostaurin (Rydapt®) As a Kinase Inhibitor with Those of Its Predominant Primary Human Metabolites

Target interaction profiling of midostaurin and its metabolites in neoplastic mast cells predicts distinct effects on activation and growth

Plasma inhibitory activity (PIA): a pharmacodynamic assay reveals insights into the basis for cytotoxic response to FLT3 inhibitors

[(Alkylamino)methyl]acrylophenones: Potent and Selective Inhibitors of the Epidermal Growth Factor Receptor Protein Tyrosine Kinase

Aromatic Interactions with Phenylalanine 691 and Cysteine 828: A Concept for FMS-like Tyrosine Kinase-3 Inhibition. Application to the Discovery of a New Class of Potential Antileukemia Agents

The Midostaurin (PKC412) Metabolite CGP52421 Shows Little Growth-Inhibitory Activity Against Against Neoplastic Mast Cells but Retains Inhibitory Effects on IgE-Dependent Activation and Histamine Release

Fingolimod (FTY720) Inhibits BCR-ABL Signaling Allosterically by Binding to the Myristate Binding Site

Markers of tumor angiogenesis and proteolysis independently define high- and low-risk subsets of node-negative breast cancer patients

Abstract 5371: A pooled apoptome shRNA screen to identify pathways that enhance NVP-BEZ235-induced apoptosis

Novel Spirodihydrobenzofuranlactams as Antagonists of Endothelin and as Inhibitors of HIV-1 Protease Produced by Stachybotrys sp: I. Fermentation, Isolation and Biological Activity

Antileukemic Effects of Novel First- and Second-Generation FLT3 Inhibitors: Structure-Affinity Comparison

Sulfonylbenzoyl-nitrostyrenes: Potential bisubstrate type inhibitors of the EGF-receptor tyrosine protein kinase

Abstract A140: Evaluation of prediction of in vivo activity from in vitro combinations: Examples using a MEK1/2 inhibitor combined with docetaxel in NSCLC models

Abstract 1257: Tyrosine phosphorylation of mitochondrial pyruvate dehydrogenase kinase 1 is important for cancer metabolism

Abstract 2798: Tyrosine phosphorylation of LDH-A is important for cancer cell redox homeostasis and tumor growth

Entry into a New Class of Potent Proteasome Inhibitors Having High Antiproliferative Activity by Structure-Based Design

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