Search Results - "Dokter, Wim"
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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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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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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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Therapy-Induced Senescence Enhances the Efficacy of HER2-Targeted Antibody-Drug Conjugates in Breast Cancer
Published in Cancer research (Chicago, Ill.) (16-12-2022)“…Antibody-drug conjugates (ADC) are antineoplastic agents recently introduced into the antitumor arsenal. T-DM1, a trastuzumab-based ADC that relies on…”
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5
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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Acute and 2-week exposure to prednisolone impair different aspects of β-cell function in healthy men
Published in European journal of endocrinology (01-04-2010)“…ObjectiveGlucocorticoids (GCs), such as prednisolone, are associated with adverse metabolic effects, including glucose intolerance and diabetes. In contrast to…”
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The Second Generation Antibody-Drug Conjugate SYD985 Overcomes Resistances to T-DM1
Published in Cancers (13-03-2020)“…Trastuzumab-emtansine (T-DM1) is an antibody-drug conjugate (ADC) approved for the treatment of HER2 (human epidermal growth factor receptor 2)-positive breast…”
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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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Preclinical profile of the HER2-targeting ADC SYD983/SYD985: introduction of a new duocarmycin-based linker-drug platform
Published in Molecular cancer therapeutics (01-11-2014)“…A linker-drug platform was built on the basis of a cleavable linker-duocarmycin payload for the development of new-generation antibody-drug conjugates (ADC). A…”
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11
Glucose kinetics in the collagen-induced arthritis model: an all-in-one model to assess both efficacy and metabolic side effects of glucocorticoids
Published in PloS one (02-09-2014)“…Prednisolone and other glucocorticoids (GCs) are potent anti-inflammatory drugs, but chronic use is hampered by metabolic side effects. Therefore, there is an…”
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12
Prednisolone-induced differential gene expression in mouse liver carrying wild type or a dimerization-defective glucocorticoid receptor
Published in BMC genomics (05-06-2010)“…Glucocorticoids (GCs) control expression of a large number of genes via binding to the GC receptor (GR). Transcription may be regulated either by binding of…”
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13
A comparison of anti-HER2 IgA and IgG1 in vivo efficacy is facilitated by high N-glycan sialylation of the IgA
Published in mAbs (01-01-2016)“…Monomeric IgA has been proposed as an alternative antibody format for cancer therapy. Here, we present our studies on the production, purification and…”
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14
Activation of Proteinase 3 Contributes to Nonalcoholic Fatty Liver Disease and Insulin Resistance
Published in Molecular medicine (Cambridge, Mass.) (01-01-2016)“…Activation of inflammatory pathways is known to accompany development of obesity-induced nonalcoholic fatty liver disease (NAFLD), insulin resistance and type…”
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Identification of gene signatures for prednisolone-induced metabolic dysfunction in collagen-induced arthritic mice
Published in Pharmacogenomics (01-04-2014)“…Prednisolone is a potent anti-inflammatory glucocorticoid (GC) but chronic use is hampered by metabolic side effects. Little is known about the long-term…”
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Synthesis and Evaluation of a Series of Long-Acting Glucagon-Like Peptide-1 (GLP-1) Pentasaccharide Conjugates for the Treatment of Type 2 Diabetes
Published in ChemMedChem (01-08-2015)“…The present study details the development of a family of novel D‐Ala8 glucagon‐like peptide‐1 (GLP‐1) peptide conjugates by site specific conjugation to an…”
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Prednisolone-induced beta cell dysfunction is associated with impaired endoplasmic reticulum homeostasis in INS-1E cells
Published in Cellular signalling (01-11-2011)“…Glucocorticoids (GCs), such as prednisolone (PRED), are widely prescribed anti-inflammatory drugs, but their use may induce glucose intolerance and diabetes…”
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BYON4228 is a pan-allelic antagonistic SIRPα antibody that potentiates destruction of antibody-opsonized tumor cells and lacks binding to SIRPγ on T cells
Published in Journal for immunotherapy of cancer (01-04-2023)“…BackgroundPreclinical studies have firmly established the CD47-signal-regulatory protein (SIRP)α axis as a myeloid immune checkpoint in cancer, and this is…”
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Org 214007-0: a novel non-steroidal selective glucocorticoid receptor modulator with full anti-inflammatory properties and improved therapeutic index
Published in PloS one (12-11-2012)“…Glucocorticoids (GCs) such as prednisolone are potent immunosuppressive drugs but suffer from severe adverse effects, including the induction of insulin…”
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20
Assessing the metabolic effects of prednisolone in healthy volunteers using urine metabolic profiling
Published in Genome medicine (30-11-2012)“…Glucocorticoids, such as prednisolone, are widely used anti-inflammatory drugs, but therapy is hampered by a broad range of metabolic side effects including…”
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