Search Results - "Prinsen, Michael"
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Targeting of αv integrin identifies a core molecular pathway that regulates fibrosis in several organs
Published in Nature medicine (01-12-2013)“…Dean Sheppard and his colleagues show that genetic or pharmacological inhibition of α v integrin signaling ameliorates fibrosis in several solid organs…”
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Identification of druggable small molecule antagonists of the Plasmodium falciparum hexose transporter PfHT and assessment of ligand access to the glucose permeation pathway via FLAG-mediated protein engineering
Published in PloS one (09-05-2019)“…Although the Plasmodium falciparum hexose transporter PfHT has emerged as a promising target for anti-malarial therapy, previously identified small-molecule…”
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Targeting VLA4 integrin and CXCR2 mobilizes serially repopulating hematopoietic stem cells
Published in The Journal of clinical investigation (01-07-2019)“…Mobilized peripheral blood has become the primary source of hematopoietic stem and progenitor cells (HSPCs) for stem cell transplantation, with a five-day…”
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4
A novel autotaxin inhibitor reduces lysophosphatidic acid levels in plasma and the site of inflammation
Published in The Journal of pharmacology and experimental therapeutics (01-07-2010)“…Autotaxin is the enzyme responsible for the production of lysophosphatidic acid (LPA) from lysophosphatidyl choline (LPC), and it is up-regulated in many…”
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Discovery of 3-Cyano- N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1 H-pyrrolo[2,3- b]pyridin-5-yl)benzamide: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonist
Published in Journal of medicinal chemistry (13-12-2018)“…The nuclear hormone receptor retinoic acid receptor-related orphan C2 (RORC2, also known as RORγt) is a promising target for the treatment of autoimmune…”
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Pharmacologic inhibition of RGD‐binding integrins ameliorates fibrosis and improves function following kidney injury
Published in Physiological reports (01-04-2020)“…Fibrosis is a final common pathway for many causes of progressive chronic kidney disease (CKD). Arginine–glycine–aspartic acid (RGD)‐binding integrins are…”
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7
Targeting CXCR4, VLA-4, and CXCR2 for hematopoietic stem cell mobilization
Published in Blood advances (26-03-2024)Get full text
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8
Evaluation of spiropiperidine hydantoins as a novel class of antimalarial agents
Published in Bioorganic & medicinal chemistry (15-08-2015)“…[Display omitted] Given the rise of parasite resistance to all currently used antimalarial drugs, the identification of novel chemotypes with unique mechanisms…”
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Discovery of 3‑Cyano‑N‑(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)‑1H‑pyrrolo[2,3‑b]pyridin-5-yl)benzamide: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonist
Published in Journal of medicinal chemistry (13-12-2018)“…The nuclear hormone receptor retinoic acid receptor-related orphan C2 (RORC2, also known as RORγt) is a promising target for the treatment of autoimmune…”
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10
Inhibitors of Arg-Gly-Asp-Binding Integrins Reduce Development of Pancreatic Fibrosis in Mice
Published in Cellular and molecular gastroenterology and hepatology (01-07-2016)“…Background & Aims Pancreatic stellate cells (PSCs) regulate the development of chronic pancreatitis (CP) and are activated by the cytokine transforming growth…”
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Pharmacologic Comparison of Clinical Neutral Endopeptidase Inhibitors in a Rat Model of Acute Secretory Diarrhea
Published in The Journal of pharmacology and experimental therapeutics (01-05-2016)“…Racecadotril (acetorphan) is a neutral endopeptidase (NEP) inhibitor with known antidiarrheal activity in animals and humans; however, in humans, it suffers…”
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Mo1233 Pharmacologic Evaluation of Clinical Neutral Endopeptidase Inhibitors in a Rat Model of Acute Secretory Diarrhea
Published in Gastroenterology (New York, N.Y. 1943) (01-04-2015)Get full text
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Evaluation of Aminohydantoins as a Novel Class of Antimalarial Agents
Published in ACS medicinal chemistry letters (09-01-2014)“…Given the threat of drug resistance, there is an acute need for new classes of antimalarial agents that act via a unique mechanism of action relative to…”
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14
Targeting of alpha(v) integrin identifies a core molecular pathway that regulates fibrosis in several organs
Published in Nature medicine (01-12-2013)“…Myofibroblasts are the major source of extracellular matrix components that accumulate during tissue fibrosis, and hepatic stellate cells (HSCs) are believed…”
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Assessment of T-Cell Receptor (TCR) Mediated T-Cell Activation in Acute Myeloid Leukemia at Diagnosis Has Implications for Risk Stratification and Response to Immune Checkpoint Inhibitors
Published in Blood (02-11-2023)“…Background Relapse in patients with acute myeloid leukemia (AML) has been, in part, attributed to the ability of leukemic blasts to escape immune surveillance…”
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Targeting CXCR4, VLA4, and CXCR2 for Hematopoietic Stem Cell Mobilization
Published in Blood (13-11-2019)“…Background: Hematopoietic stem cell (HSC) transplant is an essential treatment for a variety of blood disorders and malignancies. A key step in this procedure…”
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Targeting of [α.sub.v] integrin identifies a core molecular pathway that regulates fibrosis in several organs
Published in Nature medicine (01-12-2013)Get full text
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Targeting of [alpha]v integrin identifies a core molecular pathway that regulates fibrosis in several organs
Published in Nature medicine (01-12-2013)“…Myofibroblasts are the major source of extracellular matrix components that accumulate during tissue fibrosis, and hepatic stellate cells (HSCs) are believed…”
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Selective αv integrin depletion identifies a core, targetable molecular pathway that regulates fibrosis across solid organs
Published in Nature medicine (10-11-2013)“…Myofibroblasts are the major source of extracellular matrix components that accumulate during tissue fibrosis, and hepatic stellate cells (HSCs) are the major…”
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Journal Article -
20
Inhibitors of Arg-Gly-Asp-Binding Integrins Reduce Development of Pancreatic Fibrosis in MiceSummary
Published in Cellular and molecular gastroenterology and hepatology (01-07-2016)“…Background & Aims: Pancreatic stellate cells (PSCs) regulate the development of chronic pancreatitis (CP) and are activated by the cytokine transforming growth…”
Get full text
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