Výsledky vyhledávání - "Ulrich Graedler"

Abstract 1482: M4645 is a potent and highly selective inhibitor of disease relevant cKIT mutations for the treatment of metastatic or recurrent GIST

Autor: Dieter Dorsch, Nina Glaser, Eva Sherbetjian, Ulrich Graedler, Andreas Blum, Michael Busch, Nina Linde, Carl Petersson, Christina Esdar, Aaron Ruff

Publikováno v: Cancer Research. 81:1482-1482

Oncogenic mutations in cKIT in exons 9 and 11 are the main driver of gastrointestinal stromal tumors (GIST). Imatinib is standard of care in 1L in unresectable metastatic or recurrent GIST, yet secondary resistance mutations in exons 13/14 and 17/18

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::f127f8d8c63cdc63bbc6c35d9082c956
https://doi.org/10.1158/1538-7445.am2021-1482

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Abstract 3500: Highly potent and selective ATM kinase inhibitor M4076: A clinical candidate drug with strong anti-tumor activity in combination therapies

Autor: Kai Schiemann, Daniel Kuhn, Andree Blaukat, Frank Zenke, Holger Kubas, Astrid Zimmermann, Ulrich Graedler, Thomas Fuchss, Heike Dahmen

Publikováno v: Cancer Research. 79:3500-3500

M4076 is an ATP-competitive inhibitor of the Ataxia telangiectasia mutated (ATM) kinase (IC50 < 1 nM), which targets tumor cell survival and growth by inhibiting double-strand break (DSB) repair as well as checkpoint control. DSB repair is crucial fo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::0b321d12df5a2e640c697669f96a3fd6
https://doi.org/10.1158/1538-7445.am2019-3500

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Discovery and structure–activity relationships of pentanedioic acid diamides as potent inhibitors of 11β-hydroxysteroid dehydrogenase type I

Autor: Eric Valeur, Marc Lecomte, Christine Charon, Caroline Leriche, Franck F. Lepifre, Liliane Doare, Fabien Schmidlin, Denis Carniato, Serge Christmann-Franck, Didier Roche, Ulrich Graedler, Sophie Bozec

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 19:2674-2678

Benzylamides of pentanedioic acid were identified as inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) by high-throughput screening. Optimisation to 2-adamantyl amides yielded inhibitors with single digit nanomolar IC(50)s on the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8c61e2cc60b1bdbbd6439650150da2e9
https://doi.org/10.1016/j.bmcl.2009.03.140

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Abstract 2786: Identification and preclinical characterization of EMD 1204831 – A selective c-Met kinase inhibitor in clinical phase 1

Autor: Christine Knuehl, Friedhelm Bladt, Manja Friese-Hamim, Michael Meyring, Oliver Schadt, Claus Fittschen, Andree Blaukat, Dieter Dorsch, Frank Stieber, Ulrich Graedler

Publikováno v: Cancer Research. 71:2786-2786

The involvement of the mesenchymal endothelial transition factor (c-Met) in the primary event of oncogenic transformation and the secondary ability to mediate metastatic spread has been convincingly demonstrated in preclinical and early clinical sett

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::002bd092bd26b23ead8ee2f1178d5484
https://doi.org/10.1158/1538-7445.am2011-2786

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Abstract 3622: Preclinical characterization of EMD1214063, a potent and highly selective inhibitor of the c-Met kinase in Phase I clinical trials

Autor: Oliver Schadt, Wilfried Rautenberg, Andree Blaukat, Michael Meyring, Claus Fittschen, Frank Stieber, Ulrich Graedler, Dieter Dorsch, Manja Friese-Hamim, Friedhelm Bladt

Publikováno v: Cancer Research. 70:3622-3622

c-Met, the receptor for hepatocyte growth factor (HGF), is a well characterized receptor tyrosine kinase, which is crucial for cell functions, such as survival, proliferation, motility and migration. Activating point mutations of c-Met have been iden

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::decf900c515047ab79f5633ba14de0b0
https://doi.org/10.1158/1538-7445.am10-3622

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Abstract 5777: EMD 1214063, an exquisitely selective c-Met kinase inhibitor in clinical phase 1

Autor: Ulrich Graedler, Andree Blaukat, Frank Stieber, Claus Fittschen, Oliver Schadt, Michael Meyring, Claudia Wilm, Wilfried Rautenberg, Dieter Dorsch, Friedhelm Bladt, Manja Friese-Hamim

Publikováno v: Cancer Research. 70:5777-5777

The role of the receptor tyrosin kinase c-Met in tumor progression, metastasis and aggressiveness has been convincingly demonstrated in preclinical and early clinical settings. Several compounds with different selectivity profiles inhibiting c-Met ar

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::5b7c32d94508b7b4bfa0561a37026384
https://doi.org/10.1158/1538-7445.am10-5777

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Abstract B252: Identification of a new class of highly potent and selective c-Met kinase inhibitors

Autor: Wilfried Rautenberg, Ulrich Graedler, Friedhelm Bladt, Claus Fittschen, Frank Stieber, Dieter Dorsch, Andree Blaukat, Manja Friese-Hamim, Oliver Schadt, Michael Meyring

Publikováno v: Molecular Cancer Therapeutics. 8:B252-B252

The role of the receptor tyrosin kinase c-Met in tumor progression and metastasis has been shown in preclinical studies and in early clinical settings. Several c-Met inhibitors with different selectivity profiles are currently in preclinical/clinical

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::f6595a3d47eadae1f1db299fbc279be4
https://doi.org/10.1158/1535-7163.targ-09-b252

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