Search Results - "van der Lee, Miranda M. C"
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Design, Synthesis, and Evaluation of Linker-Duocarmycin Payloads: Toward Selection of HER2-Targeting Antibody–Drug Conjugate SYD985
Published in Molecular pharmaceutics (01-06-2015)“…Antibody–drug conjugates (ADCs) that are currently on the market or in clinical trials are predominantly based on two drug classes: auristatins and…”
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A Platform for the Generation of Site-Specific Antibody–Drug Conjugates That Allows for Selective Reduction of Engineered Cysteines
Published in Bioconjugate chemistry (16-09-2020)“…Engineering cysteines at specific sites in antibodies to create well-defined ADCs for the treatment of cancer is a promising approach to increase the…”
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SYD985, a Novel Duocarmycin-Based HER2-Targeting Antibody-Drug Conjugate, Shows Antitumor Activity in Uterine Serous Carcinoma with HER2/Neu Expression
Published in Molecular cancer therapeutics (01-08-2016)“…Uterine serous carcinoma (USC) is an aggressive form of endometrial cancer. Up to 35% of USC may overexpress the HER2/neu oncogene at strong (i.e., 3+) levels…”
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4
Chemokine cooperativity is caused by competitive glycosaminoglycan binding
Published in The Journal of immunology (1950) (15-04-2014)“…Chemokines comprise a family of secreted proteins that activate G protein-coupled chemokine receptors and thereby control the migration of leukocytes during…”
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Nonpeptidergic allosteric antagonists differentially bind to the CXCR2 chemokine receptor
Published in The Journal of pharmacology and experimental therapeutics (01-05-2009)“…The chemokine receptor CXCR2 is involved in different inflammatory diseases, like chronic obstructive pulmonary disease, psoriasis, rheumatoid arthritis, and…”
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β-Arrestin-biased signaling of PTH analogs of the type 1 parathyroid hormone receptor
Published in Cellular signalling (01-02-2013)“…Parathyroid hormone (PTH) is an anabolic agent that mediates bone formation through activation of the Gαs-, Gαq- and β-arrestin-coupled parathyroid hormone…”
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The Preclinical Profile of the Duocarmycin-Based HER2-Targeting ADC SYD985 Predicts for Clinical Benefit in Low HER2-Expressing Breast Cancers
Published in Molecular cancer therapeutics (01-03-2015)“…SYD985 is a HER2-targeting antibody-drug conjugate (ADC) based on trastuzumab and vc-seco-DUBA, a cleavable linker-duocarmycin payload. To evaluate the…”
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Pharmacological characterization of receptor redistribution and beta-arrestin recruitment assays for the cannabinoid receptor 1
Published in Journal of biomolecular screening (01-08-2009)“…Receptor redistribution and beta-arrestin recruitment assays provide a G-protein-subtype-independent method to measure ligand-stimulated activation of…”
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Preclinical Profile of BYON3521 Predicts an Effective and Safe MET Antibody-Drug Conjugate
Published in Molecular cancer therapeutics (01-06-2023)“…MET, the cell-surface receptor for the hepatocyte growth factor/scatter factor, which is widely overexpressed in various solid cancer types, is an attractive…”
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Unraveling the Interaction between Carboxylesterase 1c and the Antibody-Drug Conjugate SYD985: Improved Translational PK/PD by Using Ces1c Knockout Mice
Published in Molecular cancer therapeutics (01-11-2018)“…Carboxylesterase 1c (CES1c) is responsible for linker-drug instability and poor pharmacokinetics (PK) of several antibody-drug conjugates (ADC) in mice, but…”
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Discovery of SYD5115, a novel orally active small molecule TSH-R antagonist
Published in Bioorganic & medicinal chemistry (15-04-2023)“…[Display omitted] •Discovery of a novel class of thyrotropin receptor antagonists.•A highly potent compound with oral efficacy was identified.•Risk of…”
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β-Arrestin Recruitment and G Protein Signaling by the Atypical Human Chemokine Decoy Receptor CCX-CKR
Published in The Journal of biological chemistry (08-03-2013)“…Chemokine receptors form a large subfamily of G protein-coupled receptors that predominantly activate heterotrimeric Gi proteins and are involved in immune…”
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beta-Arrestin recruitment assay for the identification of agonists of the sphingosine 1-phosphate receptor EDG1
Published in Journal of biomolecular screening (01-12-2008)“…beta-Arrestin recruitment assays provide a generic assay platform for drug discovery on G-protein-coupled receptors (GPCRs). The PathHunter assay technology…”
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1160 Phosphonate-antibody-drug conjugates: a novel immunostimulatory class of ADCs driving inside-out activation of Vγ9Vδ2 T cells leading to selective tumor cell killing
Published in Journal for immunotherapy of cancer (01-11-2023)“…BackgroundGamma delta (γδ) T cells are cytotoxic effector cells that can recognize and kill tumor cells in a major histocompatibility complex (MHC)-independent…”
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Enzyme fragment complementation binding assay for p38alpha mitogen-activated protein kinase to study the binding kinetics of enzyme inhibitors
Published in Assay and drug development technologies (01-08-2006)“…The majority of protein kinase assays used in drug discovery research are enzyme activity assays. These assays are based on the measurement of phosphorylated…”
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