Výsledky vyhledávání - "Jürgen Mestan"

Data from In vitro Activity of Bcr-Abl Inhibitors AMN107 and BMS-354825 against Clinically Relevant Imatinib-Resistant Abl Kinase Domain Mutants

Autor: Brian J. Druker, Michael W.N. Deininger, Michael C. Heinrich, Francis Y. Lee, Sandra W. Cowan-Jacob, Jürgen Mestan, Paul W. Manley, Taiping Jia, Eric P. Stoffregen, Denise K. Walters, Thomas O'Hare

Imatinib, a Bcr-Abl tyrosine kinase inhibitor, is a highly effective therapy for patients with chronic myelogenous leukemia (CML). Despite durable responses in most chronic phase patients, relapses have been observed and are much more prevalent in pa

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::42fd1a2e5cff20d17b66aaeb1d9f2594
https://doi.org/10.1158/0008-5472.c.6493898

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Phosphorylation of Tyr245 in the open-inhibited state of Abelson kinase does not induce downstream signaling

Autor: Daniel D'Orazio, Wolfgang Jahnke, Lukasz Skora, Jürgen Mestan, Dominique Kempf

Publikováno v: European Journal of Haematology. 96:502-506

Binding of tyrosine kinase inhibitors such as imatinib was shown to induce a novel open-inhibited conformation of BCR-ABL, in which Tyr245 is exposed and prone to phosphorylation. To evaluate whether this leads to priming of the kinase in cellular sy

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8813d719231e225ebab22010cbf21e4a
https://doi.org/10.1111/ejh.12627

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Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib

Autor: Jürgen Mestan, Marion Wiesmann, Sandra W. Cowan-Jacob, Neil Gallagher, Susan Kaufman, Richard C. Woodman, Nikolaus Stiefl, Markus Wartmann, Paul W. Manley

Publikováno v: Bioorganic & Medicinal Chemistry. 18:6977-6986

Although orphan drug applications required by the EMEA must include assessments of similarity to pre-existing products, these can be difficult to quantify. Here we illustrate a paradigm in comparing nilotinib to the prototype kinase inhibitor imatini

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a6f68c79bd6444f07e8d29c8fb2c4536
https://doi.org/10.1016/j.bmc.2010.08.026

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Binding or Bending: Distinction of Allosteric Abl Kinase Agonists from Antagonists by an NMR-Based Conformational Assay

Autor: Simona Cotesta, André Strauss, Jürgen Mestan, Xavier Pelle, Sandra W. Cowan-Jacob, Andreas Marzinzik, Wolfgang Jahnke, Pascal Furet, Robert Martin Grotzfeld, Doriano Fabbro, Gabriele Fendrich

Publikováno v: Journal of the American Chemical Society. 132:7043-7048

Allosteric inhibitors of Bcr-Abl have emerged as a novel therapeutic option for the treatment of CML. Using fragment-based screening, a search for novel Abl inhibitors that bind to the myristate pocket was carried out. Here we show that not all myris

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1a5378ceec275951c3a7bd90fd92842d
https://doi.org/10.1021/ja101837n

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Inhibitors of the Abl kinase directed at either the ATP- or myristate-binding site

Autor: Francisco Adrian, Janis Liebetanz, André Strauss, Sandra W. Cowan-Jacob, Andreas Marzinzik, Xavier Pelle, Pascal Furet, Frederic Berst, Jürgen Mestan, Paul W. Manley, Gabriele Fendrich, Robert Martin Grotzfeld, Nathanael S. Gray, Markus Warmuth, Doriano Fabbro, Jianming Zhang, Alexandra Szyttenholm, Wolfgang Jahnke

Publikováno v: Biochimica et Biophysica Acta (BBA) - Proteins and Proteomics. 1804:454-462

The ATP-competitive inhibitors dasatinib and nilotinib, which bind to catalytically different conformations of the Abl kinase domain, have recently been approved for the treatment of imatinib-resistant CML. These two new drugs, albeit very efficient

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5cb61c5abe9c391126e4268635db9538
https://doi.org/10.1016/j.bbapap.2009.12.009

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Tracing pathway activities with kinase inhibitors and reverse phase protein arrays

Autor: Doriano Fabbro, Daniel Rechsteiner, Hans Voshol, Jürgen Mestan, Jan van Oostrum, Claudio Calonder, Markus Ehrat

Publikováno v: PROTEOMICS - CLINICAL APPLICATIONS. 3:412-422

Controlling aberrant protein kinase activity is a promising strategy for a variety of diseases, particularly cancer. Hence, the development of kinase inhibitors is currently a focal point for pharmaceutical research. In this study we utilize a chip-b

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fae7cc49dc6457765678bbda22064fbf
https://doi.org/10.1002/prca.200800070

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Identification of BCR-ABL point mutations conferring resistance to the Abl kinase inhibitor AMN107 (nilotinib) by a random mutagenesis study

Autor: Sandra W. Cowan-Jacob, James D. Griffin, Jürgen Mestan, Arghya Ray, Paul W. Manley

Publikováno v: Blood. 109:5011-5015

Patients with advanced stages of chronic myeloid leukemia (CML) often manifest imatinib mesylate resistance associated with point mutations in BCR-ABL. AMN107 is a new higher-potency inhibitor of BCR-ABL. To identify mutations in BCR-ABL that could r

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::868a6a1f1eac062e7ff182af5678d7c8
https://doi.org/10.1182/blood-2006-01-015347

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