Zobrazeno 1 - 10 of 49 pro vyhledávání: '"Stuart, Ince"'
1
Changing for the Better: Discovery of the Highly Potent and Selective CDK9 Inhibitor VIP152 Suitable for Once Weekly Intravenous Dosing for the Treatment of Cancer
Autor: Franz von Nussbaum, Ulrich Lücking, Dirk Kosemund, Stuart Ince, Hans Briem, Philip Lienau, Martina Schäfer, Arne Scholz, Ulf Bömer, Dominik Mumberg, Stuart Hwang, Niels Böhnke, Gerhard Siemeister, Karsten Denner, Ildiko Terebesi, Rolf Bohlmann, Raquel Izumi
Publikováno v: Journal of Medicinal Chemistry. 64:11651-11674
Selective inhibition of exclusively transcription-regulating positive transcription elongation factor b/CDK9 is a promising new approach in cancer therapy. Starting from atuveciclib, the first selective CDK9 inhibitor to enter clinical development, l
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::801ed520b97118562e070f0649f13e62
https://doi.org/10.1021/acs.jmedchem.1c01000
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2
Rogaratinib: A potent and selective pan‐FGFR inhibitor with broad antitumor activity in FGFR‐overexpressing preclinical cancer models
Autor: Holger Hess-Stumpp, Marie-Pierre Collin, Stuart Ince, Oliver Politz, Uwe Thuss, Sebastian Bender, Klemens Lustig, Dieter Zopf, Christoph Kneip, Peter Ellinghaus, Dominik Mumberg, Sylvia Grünewald, Ulf Boemer, Charlotte Kopitz, Mélanie Héroult, Karl Ziegelbauer
Publikováno v: International Journal of Cancer
Aberrant activation in fibroblast growth factor signaling has been implicated in the development of various cancers, including squamous cell lung cancer, squamous cell head and neck carcinoma, colorectal and bladder cancer. Thus, fibroblast growth fa
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c8b248e95ce00f38e560a438cac15a23
https://doi.org/10.1002/ijc.32224
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3
BAY 1125976, a selective allosteric AKT1/2 inhibitor, exhibits high efficacy on AKT signaling-dependent tumor growth in mouse models
Autor: Ningshu Liu, Franziska Siegel, Lars Bärfacker, Franz von Nussbaum, Karl Ziegelbauer, Ulf Bömer, William J. Scott, Stuart Ince, Amaury Ernesto Fernandez-Montalvan, Dominik Mumberg, Kirstin Meyer, Roland Neuhaus, Martin Michels, Oliver Politz, Andrea Hägebarth
Publikováno v: International Journal of Cancer. 140:449-459
The PI3K-AKT-mTOR signaling cascade is activated in the majority of human cancers, and its activation also plays a key role in resistance to chemo and targeted therapeutics. In particular, in both breast and prostate cancer, increased AKT pathway act
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::5ce2c1e9fe2894b3e55ba673689a4f45
https://doi.org/10.1002/ijc.30457
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4
Abstract A099: Safety, tolerability, pharmacokinetics, and efficacy of pan-fibroblast growth factor receptor inhibitor rogaratinib in Japanese patients with refractory, locally advanced metastatic solid tumors selected with a novel, mRNA-based patient selection strategy
Autor: Changliang Zhang, Hendrik Nogai, Matthias Ocker, Stuart Ince, Makoto Tahara, Shunji Takahashi, Fumiyoshi Sei, Peter Ellinghaus
Publikováno v: Molecular Cancer Therapeutics. 17:A099-A099
Background: Fibroblast growth factor receptor (FGFR)-mediated pathways are considered to be promising anticancer therapy targets. There are several types of genetic evidence that support an oncogenic function of FGFRs: identification of gene amplific
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::cec29927ed635f2360c7e0c834d1ac2f
https://doi.org/10.1158/1535-7163.targ-17-a099
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6
Abstract 3738: Use of tumor mRNA expression for patient selection in a phase I study of the pan-fibroblast growth factor receptor inhibitor BAY 1163877
Autor: Christoph Kneip, Peter Ellinghaus, Stuart Ince, Martin Schuler, Matthias Ocker, Sebastian Bender, Markus Joerger
Publikováno v: Cancer Research. 77:3738-3738
BAY 1163877 is a potent and selective, oral, small molecule pan-FGFR inhibitor with anti-tumor activity in a wide range of cancer types. In vivo profiling in xenograft models identified tumor FGFR mRNA levels as a predictor of drug efficacy. Anti-tum
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::122054ecd25f5c73b86c95a52cd45c64
https://doi.org/10.1158/1538-7445.am2017-3738
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7
Abstract 984: Identification of potent and highly selective PTEFb inhibitor BAY 1251152 for the treatment of cancer: from p.o. to i.v. application via scaffold hops
Autor: Dirk Kosemund, Franz von Nussbaum, Gerhard Siemeister, Ulrich Luecking, Katja Prelle, Kirstin Meyer, Philip Lienau, Stuart Ince, Hans Briem, Michael Brands, Ildiko Terebesi, Karl Ziegelbauer, Rolf Bohlmann, Arne Scholz, Ray Valencia, Dominik Mumberg
Publikováno v: Cancer Research. 77:984-984
PTEFb/CDK9 mediated transcription of short-lived anti-apoptotic survival proteins like Mcl-1 and Myc plays a critical role in cancer cell growth and survival in various tumor entities including AML. In addition, these survival proteins play important
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::0617740777de36cd422ecedc3ad7cd7b
https://doi.org/10.1158/1538-7445.am2017-984
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8
BAY 1125976, a selective allosteric AKT1/2 inhibitor, exhibits high efficacy on AKT signaling-dependent tumor growth in mouse models
Autor: Oliver, Politz, Franziska, Siegel, Lars, Bärfacker, Ulf, Bömer, Andrea, Hägebarth, William J, Scott, Martin, Michels, Stuart, Ince, Roland, Neuhaus, Kirstin, Meyer, Amaury Ernesto, Fernández-Montalván, Ningshu, Liu, Franz, von Nussbaum, Dominik, Mumberg, Karl, Ziegelbauer
Publikováno v: International journal of cancer. 140(2)
The PI3K-AKT-mTOR signaling cascade is activated in the majority of human cancers, and its activation also plays a key role in resistance to chemo and targeted therapeutics. In particular, in both breast and prostate cancer, increased AKT pathway act
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::4779ff9245f0f8c406ddc4715ef7e9cf
https://pubmed.ncbi.nlm.nih.gov/27699769
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10
Phase I Study of the PTEFb Inhibitor BAY 1251152 in Patients with Acute Myelogenous Leukemia
Autor: Daniel Morillo, Martin Wermke, Mark G. Frattini, Raul Cordoba, Ioannis Mantzaris, Oliver G. Ottmann, Daniel J. Lee, Michael Byrne, Arne Scholz, Fabricio Souza, Stuart Ince, Ray Valencia
Publikováno v: Blood. 132:4055-4055
Introduction: The critical role of cyclin-dependent kinases in cell division and gene transcription has made them targets for anti-cancer therapies. Positive transcription elongation factor b (PTEFb)/cyclin-dependent kinase 9 (CDK9) plays a key role
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::d8d0f8de614492401cfccae837f9886d
https://doi.org/10.1182/blood-2018-99-117257
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