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  • 1
    Online Resource
    Online Resource
    Totowa, NJ : Humana Press
    UID:
    b3kat_BV036489441
    Format: 1 Online-Ressource
    Edition: Online-Ausgabe Springer ebook collection. Medicine 2005-2008
    ISBN: 9781597453561
    Additional Edition: Erscheint auch als Druck-Ausgabe ISBN 978-1-58829-948-2
    Language: English
    Subjects: Medicine
    RVK:
    Keywords: Krebs ; Epidermaler Wachstumsfaktor-Rezeptor
    URL: Volltext  (URL des Erstveröffentlichers)
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  • 2
    Online Resource
    Online Resource
    Totowa, NJ :Humana Press,
    UID:
    almahu_BV036489441
    Format: 1 Online-Ressource.
    Edition: Online-Ausgabe Springer ebook collection. Medicine 2005-2008
    ISBN: 978-1-59745-356-1
    Additional Edition: Erscheint auch als Druck-Ausgabe ISBN 978-1-58829-948-2
    Language: English
    Subjects: Medicine
    RVK:
    Keywords: Krebs ; Epidermaler Wachstumsfaktor-Rezeptor
    URL: Volltext  (URL des Erstveröffentlichers)
    URL: Volltext  (lizenzpflichtig)
    URL: Cover
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  • 3
    Book
    Book
    New York, NY : Humana Press
    UID:
    kobvindex_ZLB14947387
    Format: XI, 393 Seiten , Ill., graph. Darst.
    ISBN: 9781588299482
    Series Statement: Cancer drug discovery and development
    Note: Text engl.
    Language: English
    Keywords: Krebs 〈Medizin〉 ; Therapie
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  • 4
    UID:
    edochu_18452_25803
    Format: 1 Online-Ressource (9 Seiten)
    ISSN: 2472-5552 , 2472-5552
    Content: There is interest in developing inhibitors of human neutral ceramidase (nCDase) because this enzyme plays a critical role in colon cancer. There are currently no potent or clinically effective inhibitors for nCDase reported to date, so we adapted a fluorescence-based enzyme activity method to a high-throughput screening format. We opted to use an assay whereby nCDase hydrolyzes the substrate RBM 14-16, and the addition of NaIO4 acts as an oxidant that releases umbelliferone, resulting in a fluorescent signal. As designed, test compounds that act as ceramidase inhibitors will prevent the hydrolysis of RBM 14-16, thereby decreasing fluorescence. This assay uses a 1536-well plate format with excitation in the blue spectrum of light energy, which could be a liability, so we incorporated a counterscreen that allows for rapid selection against fluorescence artifacts to minimize false-positive hits. The high-throughput screen of 〉650,000 small molecules found several lead series of hits. Multiple rounds of chemical optimization ensued with improved potency in terms of IC50 and selectivity over counterscreen assays. This study describes the first large-scale high-throughput optical screening assay for nCDase inhibitors that has resulted in leads that are now being pursued in crystal docking studies and in vitro drug metabolism and pharmacokinetics (DMPK).
    Content: Peer Reviewed
    Note: This publication is with permission of the rights owner freely accessible due to an alliance licence and a national licence (funded by the DFG, German Research Foundation) respectively.
    In: Los Angeles, CA : SAGE Publications, 26,1, Seiten 113-121, 2472-5552
    Language: English
    URL: Volltext  (kostenfrei)
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  • 5
    Online Resource
    Online Resource
    Totowa, NJ :Humana Press,
    UID:
    edocfu_BV036489441
    Format: 1 Online-Ressource.
    Edition: Online-Ausgabe Springer ebook collection. Medicine 2005-2008
    ISBN: 978-1-59745-356-1
    Additional Edition: Erscheint auch als Druck-Ausgabe ISBN 978-1-58829-948-2
    Language: English
    Subjects: Medicine
    RVK:
    Keywords: Krebs ; Epidermaler Wachstumsfaktor-Rezeptor
    URL: Volltext  (URL des Erstveröffentlichers)
    Library Location Call Number Volume/Issue/Year Availability
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  • 6
    Online Resource
    Online Resource
    Totowa, NJ :Humana Press,
    UID:
    edoccha_BV036489441
    Format: 1 Online-Ressource.
    Edition: Online-Ausgabe Springer ebook collection. Medicine 2005-2008
    ISBN: 978-1-59745-356-1
    Additional Edition: Erscheint auch als Druck-Ausgabe ISBN 978-1-58829-948-2
    Language: English
    Subjects: Medicine
    RVK:
    Keywords: Krebs ; Epidermaler Wachstumsfaktor-Rezeptor
    URL: Volltext  (URL des Erstveröffentlichers)
    Library Location Call Number Volume/Issue/Year Availability
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  • 7
    Online Resource
    Online Resource
    New York, NY :Humana Press,
    UID:
    edoccha_9958073594802883
    Format: 1 online resource (392 p.)
    ISBN: 1-282-03633-5 , 9786612036330 , 1-59745-356-0
    Series Statement: Cancer drug discovery and development
    Content: The epidermal growth factor (EGF) receptor and its downstream signal transduction networks have been implicated in the ontology and maintenance of tumor tissues, which has motivated the discovery and development of molecularly targeted anti-EGFR therapies. Edited by John Haley and William J. Gullick, EGFR Signaling Networks in Cancer Therapy, is separated into two sections. The first of which probes the molecular pathways and the intersection of signaling networks which are frequently deregulated in human cancers, with a view to describing EGF receptor in a tumor tissue specific context. Meanwhile, the second section illustrates the many ways in which EGF receptor contribute to abnormal survival and migration signaling in cancer cells and to epithelial to mesenchymal transition and metastasis. The book also describes the mitogenic, survival, adhesive and migratory pathways within a framework of interacting subsystems that contribute to the activity and physiological regulation of the receptor in normal and neoplastic tissues. Even though there is still much to learn, this volume explores this fascinating system with compelling information.
    Note: Description based upon print version of record. , EGFR Signaling Networks -- EGFR Receptor Family Extracellular Domain Structures and Functions -- EGFR family heterodimers in cancer pathogenesis and treatment -- Structure-function of EGFR kinase domain and its inhibitors -- Internalization and degradation of EGF receptor -- Differential dependence of EGFR and ErbB2 on the molecular chaperone Hsp90 -- Activation of STATs 3 and 5 Through the EGFR Signaling Axis -- The intersection of EGFR and the Ras signaling pathway -- PHOSPHOINOSITIDE 3-KINASE ENZYMES AS DOWNSTREAM TARGETS OF THE EGF RECEPTOR -- Convergence of EGF Receptor and Src Family Signaling Networks in Cancer -- A Molecular Crosstalk between E-cadherin and EGFR Signaling Networks -- Crosstalk Between Insulin-like Growth Factor (IGF) and Epidermal Growth Factor (EGF) Receptors -- Negative regulation of signaling by the EGFR family -- Nuclear ErbB Receptors: Pathways and Functions -- Temporal Dynamics of EGF Receptor Signaling by Quantitative Proteomics -- Computational and Mathematical Modelling of the EGF Receptor System -- EGFR in Tumorigenesis and EGFR Tyrosine Kinase Inhibitors in Cancer Therapy -- Expression and prognostic significance of the EGFR in solid tumors -- Signalling by the EGF receptor in human cancers: accentuate the positive, eliminate the negative -- EGFR signaling in invasion, angiogenesis and metastasis -- Constitutive activation of truncated EGF receptors in glioblastoma -- EGFR Mutations, Other Molecular Alterations Related To Sensitivity to EGFR Inhibitors, and Molecular Testing for EGFR-Targeted Therapies in Non-Small Cell Lung Cancer -- Crosstalk Between COX-2 and EGFR: A Potential Therapeutic Opportunity -- Cellular sensitivity to EGF receptor inhibitors -- Utilizing combinations of molecular targeted agents to sensitize tumor cells to EGFR inhibitors. , English
    Additional Edition: ISBN 1-58829-948-1
    Language: English
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