Search Results - "Gottardis, Marco M."
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Castration-Resistant Prostate Cancer: Locking Up the Molecular Escape Routes
Published in Clinical cancer research (15-05-2009)“…The understanding of the key role that androgens play on the normal and pathological physiology of the prostate guided the development of different therapies…”
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2
Insulin-Mediated Acceleration of Breast Cancer Development and Progression in a Nonobese Model of Type 2 Diabetes
Published in Cancer research (Chicago, Ill.) (15-01-2010)“…Epidemiologic studies suggest that type 2 diabetes (T2D) increases breast cancer risk and mortality, but there is limited experimental evidence supporting this…”
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3
BMS-754807, a small molecule inhibitor of insulin-like growth factor-1R/IR
Published in Molecular cancer therapeutics (01-12-2009)“…BMS-754807 is a potent and reversible inhibitor of the insulin-like growth factor 1 receptor/insulin receptor family kinases (Ki, <2 nmol/L). It is currently…”
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Constitutively Active Type I Insulin-Like Growth Factor Receptor Causes Transformation and Xenograft Growth of Immortalized Mammary Epithelial Cells and Is Accompanied by an Epithelial-to-Mesenchymal Transition Mediated by NF-κB and Snail
Published in Molecular and Cellular Biology (01-04-2007)“…Article Usage Stats Services MCB Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley…”
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Drug safety is a barrier to the discovery and development of new androgen receptor antagonists
Published in The Prostate (01-04-2011)“…BACKGROUND Androgen receptor (AR) antagonists are part of the standard of care for prostate cancer. Despite the almost inevitable development of resistance in…”
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6
HER receptor signaling confers resistance to the insulin-like growth factor-I receptor inhibitor, BMS-536924
Published in Molecular cancer therapeutics (01-09-2008)“…We have reported previously the activity of the insulin-like growth factor-I (IGF-IR)/insulin receptor (InsR) inhibitor, BMS-554417, in breast and ovarian…”
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Discovery of a 2,4-Disubstituted Pyrrolo[1,2-f][1,2,4]triazine Inhibitor (BMS-754807) of Insulin-like Growth Factor Receptor (IGF-1R) Kinase in Clinical Development
Published in Journal of medicinal chemistry (10-12-2009)“…This report describes the biological activity, characterization, and SAR leading to 9d (BMS-754807) a small molecule IGF-1R kinase inhibitor in clinical…”
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ETV6-NTRK3―Mediated Breast Epithelial Cell Transformation Is Blocked by Targeting the IGF1R Signaling Pathway
Published in Cancer research (Chicago, Ill.) (01-02-2011)“…The insulin-like growth factor (IGF) 1 receptor (IGF1R) is an important therapeutic target under study in many cancers. Here, we describe a breast cancer model…”
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9
Molecular markers for novel therapies in neuroendocrine (carcinoid) tumors
Published in Endocrine-related cancer (01-09-2010)“…Neuroendocrine (carcinoid) tumors (NETs) are endocrine neoplasms occurring most frequently in gastrointestinal and bronchopulmonary (BP) systems. The majority…”
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Combined Inhibition of IGF-1R/IR and Src family kinases enhances antitumor effects in prostate cancer by decreasing activated survival pathways
Published in PloS one (26-12-2012)“…Treatment of metastatic prostate cancer (PCa) with single agents has shown only modest efficacy. We hypothesized dual inhibition of different pathways in PCa…”
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BMS-536924 Reverses IGF-IR-Induced Transformation of Mammary Epithelial Cells and Causes Growth Inhibition and Polarization of MCF7 Cells
Published in Clinical cancer research (01-01-2009)“…Purpose: This study aimed to test the ability of a new insulin-like growth factor receptor ( IGF-IR ) tyrosine kinase inhibitor, BMS-536924, to reverse the…”
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12
A fibronectin scaffold approach to bispecific inhibitors of epidermal growth factor receptor and insulin-like growth factor-I receptor
Published in mAbs (01-01-2011)“…Engineered domains of human fibronectin (Adnectins™) were used to generate a bispecific Adnectin targeting epidermal growth factor receptor (EGFR) and…”
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Discovery of the Selective CYP17A1 Lyase Inhibitor BMS-351 for the Treatment of Prostate Cancer
Published in ACS medicinal chemistry letters (14-01-2016)“…Efforts to identify a potent, reversible, nonsteroidal CYP17A1 lyase inhibitor with good selectivity over CYP17A1 hydroxylase and CYPs 11B1 and 21A2 for the…”
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14
GREB1 is a novel androgen-regulated gene required for prostate cancer growth
Published in The Prostate (01-06-2006)“…BACKGROUND Gene regulated in breast cancer 1 (GREB1) is a novel estrogen‐regulated gene shown to play a pivotal role in hormone‐stimulated breast cancer…”
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15
Discovery of JNJ-63576253: A Clinical Stage Androgen Receptor Antagonist for F877L Mutant and Wild-Type Castration-Resistant Prostate Cancer (mCRPC)
Published in Journal of medicinal chemistry (28-01-2021)“…Persistent androgen receptor (AR) activation drives therapeutic resistance to second-generation AR pathway inhibitors and contributes to the progression of…”
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The discovery of BMS-737 as a potent, CYP17 lyase-selective inhibitor for the treatment of castration-resistant prostate cancer
Published in Bioorganic & medicinal chemistry letters (01-11-2022)“…[Display omitted] We report herein, the discovery of BMS-737 (compound 33) as a potent, non-steroidal, reversible small molecule inhibitor demonstrating…”
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Phase I Trial of Weekly Paclitaxel and BMS-214662 in Patients with Advanced Solid Tumors
Published in Clinical cancer research (15-06-2007)“…Purpose: To assess the maximum tolerated dose (MTD), dose-limiting toxicity (DLT), pharmacodynamics, and antitumor activity of continuous weekly-administered…”
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Differential Mechanisms of Acquired Resistance to Insulin-like Growth Factor-I Receptor Antibody Therapy or to a Small-Molecule Inhibitor, BMS-754807, in a Human Rhabdomyosarcoma Model
Published in Cancer research (Chicago, Ill.) (15-09-2010)“…Agents targeting insulin-like growth factor-I receptor (IGF-IR), including antibodies and small-molecule inhibitors, are currently in clinical development for…”
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Discovery of JNJ-63576253, a Next-Generation Androgen Receptor Antagonist Active Against Wild-Type and Clinically Relevant Ligand Binding Domain Mutations in Metastatic Castration-Resistant Prostate Cancer
Published in Molecular cancer therapeutics (01-05-2021)“…Numerous mechanisms of resistance arise in response to treatment with second-generation androgen receptor (AR) pathway inhibitors in metastatic…”
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High IGF-IR Activity in Triple-Negative Breast Cancer Cell Lines and Tumorgrafts Correlates with Sensitivity to Anti-IGF-IR Therapy
Published in Clinical cancer research (15-04-2011)“…We previously reported an insulin-like growth factor (IGF) gene expression signature, based on genes induced or repressed by IGF-I, which correlated with poor…”
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