Search Results - "Hilberg, Frank"
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Design, Synthesis, and Evaluation of Indolinones as Triple Angiokinase Inhibitors and the Discovery of a Highly Specific 6-Methoxycarbonyl-Substituted Indolinone (BIBF 1120)
Published in Journal of medicinal chemistry (23-07-2009)“…Inhibition of tumor angiogenesis through blockade of the vascular endothelial growth factor (VEGF) signaling pathway is a new treatment modality in oncology…”
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2
Epigenetic SMAD3 Repression in Tumor-Associated Fibroblasts Impairs Fibrosis and Response to the Antifibrotic Drug Nintedanib in Lung Squamous Cell Carcinoma
Published in Cancer research (Chicago, Ill.) (15-01-2020)“…The tumor-promoting fibrotic stroma rich in tumor-associated fibroblasts (TAF) is drawing increased therapeutic attention. Intriguingly, a trial with the…”
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Therapeutic impact of Nintedanib with paclitaxel and/or a PD-L1 antibody in preclinical models of orthotopic primary or metastatic triple negative breast cancer
Published in Journal of experimental & clinical cancer research (11-01-2019)“…Triple negative breast cancer (TNBC) is an aggressive malignancy with poor prognosis, in part because of the current lack of any approved molecularly targeted…”
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4
Nintedanib and a bi-specific anti-VEGF/Ang2 nanobody selectively prevent brain metastases of lung adenocarcinoma cells
Published in Clinical & experimental metastasis (01-12-2020)“…Brain metastases (BM) are an ever-increasing challenge in oncology, threatening quality of life and survival of many cancer patients. The majority of BM…”
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Nintedanib Is Active in Malignant Pleural Mesothelioma Cell Models and Inhibits Angiogenesis and Tumor Growth In Vivo
Published in Clinical cancer research (01-08-2018)“…Malignant pleural mesothelioma (MPM) is an aggressive thoracic tumor type with limited treatment options and poor prognosis. The angiokinase inhibitor…”
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Enhancing gastric cancer conventional chemotherapy effects by triple angiokinase inhibitor nintedanib in preclinical models
Published in Frontiers in oncology (10-05-2023)“…Gastric adenocarcinoma (GAC) is the fourth leading cause of cancer death worldwide. Systemic chemotherapy is a preferred treatment option for advanced and…”
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CD44 Suppresses TLR-Mediated Inflammation
Published in The Journal of immunology (1950) (15-03-2008)“…The cell adhesion molecule CD44, which is the major hyaluronan receptor, has been implicated in the binding, endocytosis, and metabolism of hyaluronan…”
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Functions of c-Jun in Liver and Heart Development
Published in The Journal of cell biology (31-05-1999)“…Mice lacking the AP-1 transcription factor c-Jun die around embryonic day E13.0 but little is known about the cell types affected as well as the cause of…”
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Bortezomib, Dexamethasone, and Fibroblast Growth Factor Receptor 3–Specific Tyrosine Kinase Inhibitor in t(4;14) Myeloma
Published in Clinical cancer research (15-01-2009)“…Purpose: Novel drugs including targeted approaches have changed treatment paradigms for multiple myeloma (MM) and may also have therapeutic potential in the…”
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CD44 is a determinant of inflammatory bone loss
Published in The Journal of experimental medicine (21-03-2005)“…Chronic inflammation is a major trigger of local and systemic bone loss. Disintegration of cell-matrix interaction is a prerequisite for the invasion of…”
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Growth inhibition and induction of apoptosis in acute myeloid leukemia cells by new indolinone derivatives targeting fibroblast growth factor, platelet-derived growth factor, and vascular endothelial growth factor receptors
Published in Molecular cancer therapeutics (01-12-2006)“…In acute myeloid leukemia (AML), receptor tyrosine kinase ligands promote growth and survival and contribute to AML-associated marrow neoangiogenesis. We have…”
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Nintedanib: From Discovery to the Clinic
Published in Journal of medicinal chemistry (12-02-2015)“…Nintedanib (BIBF1120) is a potent, oral, small-molecule tyrosine kinase inhibitor, also known as a triple angiokinase inhibitor, inhibiting three major…”
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Abstract 1043: Enhancing cytotoxic chemotherapy effects by nintedanib in gastric cancer preclinical models
Published in Cancer research (Chicago, Ill.) (01-07-2021)“…Abstract Background: Gastric adenocarcinoma (GAC) remains the 3rd most common cause of cancer mortality in the world. Systemic chemotherapy is a preferred…”
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Drug resistance profiles of mutations in the RET kinase domain
Published in British journal of pharmacology (01-09-2018)“…Background and Purpose Alterations in the tyrosine kinase enzyme RET are found in thyroid and lung cancer. While RET TK inhibitors (TKIs) are used to treat…”
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Abstract 2869: Nintedanib abrogates the activation and tumor-promoting effects of fibroblasts from lung adenocarcinoma patients
Published in Cancer research (Chicago, Ill.) (01-07-2018)“…Abstract Nintedanib is a clinically-approved multikinase receptor inhibitor that, in combination with docetaxel, provides clinical benefits to advanced lung…”
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Structural basis of resistance of mutant RET protein-tyrosine kinase to its inhibitors nintedanib and vandetanib
Published in The Journal of biological chemistry (05-07-2019)“…RET is a transmembrane growth factor receptor. Aberrantly activated RET is found in several types of human cancer and is a target for treating RET…”
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Abstract 2982: Unraveling the antifibrotic mode of action of nintedanib against the TGF-β pathway in tumor-associated fibroblasts in non-small cell lung cancer
Published in Cancer research (Chicago, Ill.) (15-08-2020)“…Abstract Non-small cell lung cancer (NSCLC) is the leading cause of cancer related death, and its major histotypes are lung adenocarcinoma (ADC) and squamous…”
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BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy
Published in Cancer research (Chicago, Ill.) (15-06-2008)“…Inhibition of tumor angiogenesis through blockade of the vascular endothelial growth factor (VEGF) signaling pathway is a novel treatment modality in oncology…”
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Tumour-infiltrating neutrophils counteract anti-VEGF therapy in metastatic colorectal cancer
Published in British journal of cancer (08-01-2019)“…Background Immune infiltration is implicated in the development of acquired resistance to anti-angiogenic cancer therapy. We therefore investigated the…”
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Abstract B09: Nintedanib inhibits tumor and vessel growth and leads to vascular normalization in A549-NSCLC-xenografts
Published in Molecular cancer therapeutics (01-12-2015)“…Abstract Angiogenesis plays a major role in the growth and progression of non-small-cell lung cancer (NSCLC). The triple angiokinase inhibitor nintedanib is a…”
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