Search Results - "ORTON, Darren"
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The Small Molecule IMR-1 Inhibits the Notch Transcriptional Activation Complex to Suppress Tumorigenesis
Published in Cancer research (Chicago, Ill.) (15-06-2016)“…In many cancers, aberrant Notch activity has been demonstrated to play a role in the initiation and maintenance of the neoplastic phenotype and in cancer stem…”
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2
Pyrvinium Attenuates Hedgehog Signaling Downstream of Smoothened
Published in Cancer research (Chicago, Ill.) (01-09-2014)“…The Hedgehog (HH) signaling pathway represents an important class of emerging developmental signaling pathways that play critical roles in the genesis of a…”
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3
Repurposing the FDA-approved pinworm drug pyrvinium as a novel chemotherapeutic agent for intestinal polyposis
Published in PloS one (08-07-2014)“…Mutations in the WNT-pathway regulator ADENOMATOUS POLYPOSIS COLI (APC) promote aberrant activation of the WNT pathway that is responsible for APC-associated…”
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4
An allosteric potentiator of M4 mAChR modulates hippocampal synaptic transmission
Published in Nature chemical biology (2008)“…Muscarinic acetylcholine receptors (mAChRs) provide viable targets for the treatment of multiple central nervous system disorders. We have used cheminformatics…”
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5
Targeting the Wnt pathway in synovial sarcoma models
Published in Cancer discovery (01-11-2013)“…Synovial sarcoma is an aggressive soft-tissue malignancy of children and young adults, with no effective systemic therapies. Its specific oncogene, SYT-SSX…”
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The antihelmintic drug pyrvinium pamoate targets aggressive breast cancer
Published in PloS one (27-08-2013)“…WNT signaling plays a key role in the self-renewal of tumor initiation cells (TICs). In this study, we used pyrvinium pamoate (PP), an FDA-approved…”
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7
SU11248 (Sunitinib) Sensitizes Pancreatic Cancer to the Cytotoxic Effects of Ionizing Radiation
Published in International journal of radiation oncology, biology, physics (01-07-2008)“…Purpose SU11248 (sunitinib) is a small-molecule tyrosine kinase inhibitor which targets VEGFR and PDGFR isoforms. In the present study, the effects of SU11248…”
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8
Discovery and characterization of novel allosteric potentiators of M1 muscarinic receptors reveals multiple modes of activity
Published in Molecular pharmacology (01-03-2009)“…Activators of M(1) muscarinic acetylcholine receptors (mAChRs) may provide novel treatments for schizophrenia and Alzheimer's disease. Unfortunately, the…”
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Pharmacological Disruption of the Notch1 Transcriptional Complex Inhibits Tumor Growth by Selectively Targeting Cancer Stem Cells
Published in Cancer research (Chicago, Ill.) (15-06-2021)“…In many human cancers, deregulation of the Notch pathway has been shown to play a role in the initiation and maintenance of the neoplastic phenotype. Aberrant…”
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10
Small-molecule inhibition of Wnt signaling through activation of casein kinase 1α
Published in Nature chemical biology (01-11-2010)“…A Xenopus laevis two-reporter screen identifies the antihelminthic drug pyrvinium as an inhibitor of the Wnt/β-catenin signaling pathway that works by…”
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11
A CK1α Activator Penetrates the Brain and Shows Efficacy Against Drug-resistant Metastatic Medulloblastoma
Published in Clinical cancer research (15-02-2019)“…Although most children with medulloblastoma are cured of their disease, Sonic Hedgehog (SHH) subgroup medulloblastoma driven by mutations is essentially…”
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Differential abundance of CK1α provides selectivity for pharmacological CK1α activators to target WNT-dependent tumors
Published in Science signaling (27-06-2017)“…Constitutive WNT activity drives the growth of various human tumors, including nearly all colorectal cancers (CRCs). Despite this prominence in cancer, no WNT…”
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13
An allosteric potentiator of M 4 mAChR modulates hippocampal synaptic transmission
Published in Nature chemical biology (01-01-2008)Get full text
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14
Context-dependent pharmacology exhibited by negative allosteric modulators of metabotropic glutamate receptor 7
Published in Molecular pharmacology (01-03-2010)“…Phenotypic studies of mice lacking metabotropic glutamate receptor subtype 7 (mGluR7) suggest that antagonists of this receptor may be promising for the…”
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Biology Contribution: SU11248 (Sunitinib) Sensitizes Pancreatic Cancer to the Cytotoxic Effects of Ionizing Radiation
Published in International journal of radiation oncology, biology, physics (01-07-2008)“…Purpose: SU11248 (sunitinib) is a small-molecule tyrosine kinase inhibitor which targets VEGFR and PDGFR isoforms. In the present study, the effects of SU11248…”
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16
Asymmetric Synthesis of the Putative Structure of (−)-Oryzoxymycin
Published in Organic letters (06-02-2003)“…A short asymmetric synthesis of (2‘S,5R,6R)-2‘-[6-amino-5-hydroxy-1,3-cyclohexadiene-1-carbonyloxy]propionic acid, the enantiomer of the reported structure of…”
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A biochemical screen for identification of small-molecule regulators of the Wnt pathway using Xenopus egg extracts
Published in Journal of biomolecular screening (01-10-2011)“…Misregulation of the Wnt pathway has been shown to be responsible for a variety of human diseases, most notably cancers. Screens for inhibitors of this pathway…”
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18
Structure–activity relationships of anthranilamide-based factor Xa inhibitors containing piperidinone and pyridinone P4 moieties
Published in Bioorganic & medicinal chemistry letters (01-05-2008)“…Introduction of the phenyl piperidinone and phenyl pyridinone P4 moieties in the anthranilamide scaffold led to potent, selective, and orally bioavailable…”
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Small-molecule inhibition of Wnt signaling through activation of casein kinase 1[alpha]
Published in Nature chemical biology (01-11-2010)“…Wnt/b-catenin signaling is critically involved in metazoan development, stem cell maintenance and human disease. Using Xenopus laevis egg extract to screen for…”
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The Antihelmintic Drug Pyrvinium Pamoate Targets Aggressive Breast Cancer: e71508
Published in PloS one (01-08-2013)“…WNT signaling plays a key role in the self-renewal of tumor initiation cells (TICs). In this study, we used pyrvinium pamoate (PP), an FDA-approved…”
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