Search Results - "Collins, Jon"
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Ube3a unsilencer for the potential treatment of Angelman syndrome
Published in Nature communications (08-07-2024)“…Deletion of the maternal UBE3A allele causes Angelman syndrome (AS) ; because paternal UBE3A is epigenetically silenced by a long non-coding antisense (…”
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ApoE Promotes the Proteolytic Degradation of Aβ
Published in Neuron (Cambridge, Mass.) (12-06-2008)“…Apolipoprotein E is associated with age-related risk for Alzheimer's disease and plays critical roles in Aβ homeostasis. We report that ApoE plays a role in…”
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Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120)
Published in Bioorganic & medicinal chemistry letters (15-07-2014)“…The exploration of a diarylsulfonamide series of free fatty acid receptor 4 (FFA4/GPR120) agonists is described. This work led to the identification of…”
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4
Recruitment of FBXO22 for targeted degradation of NSD2
Published in Nature chemical biology (04-07-2024)“…Targeted protein degradation (TPD) is an emerging therapeutic strategy that would benefit from new chemical entities with which to recruit a wider variety of…”
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The Nuclear Receptor Superfamily and Drug Discovery
Published in ChemMedChem (12-05-2006)“…Targeting the nuclear receptors: The ligand‐binding domain of the glucocorticoid receptor (ribbon) bound with the ligand, dexamethasone (space‐filling) is just…”
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Inhibition of apical sodium-dependent bile acid transporter as a novel treatment for diabetes
Published in American journal of physiology: endocrinology and metabolism (01-01-2012)“…Bile acids are recognized as metabolic modulators. The present study was aimed at evaluating the effects of a potent Asbt inhibitor (264W94), which blocks…”
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Population pharmacokinetics of belantamab mafodotin, a BCMA‐targeting agent in patients with relapsed/refractory multiple myeloma
Published in CPT: pharmacometrics and systems pharmacology (01-08-2021)“…Belantamab mafodotin (belamaf) is an antibody–drug conjugate (ADC) targeting B‐cell maturation antigen (BCMA). Nonlinear mixed‐effects models were developed to…”
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Direct and Indirect Mechanisms for Regulation of Fatty Acid Synthase Gene Expression by Liver X Receptors
Published in The Journal of biological chemistry (29-03-2002)“…The nuclear receptors LXRα and LXRβ have been implicated in the control of lipogenesis and cholesterol homeostasis. Ligand activation of these receptors in…”
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Ligand activation of LXR beta reverses atherosclerosis and cellular cholesterol overload in mice lacking LXR alpha and apoE
Published in The Journal of clinical investigation (01-08-2007)“…Liver X receptors (LXRs) alpha and beta are transcriptional regulators of cholesterol homeostasis and potential targets for the development of…”
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Divalproex, lithium and suicide among Medicaid patients with bipolar disorder
Published in Journal of affective disorders (01-04-2008)“…Abstract Background Suicide completion and attempted suicide are major concerns for people with bipolar disorder. Studies in the private sector have suggested…”
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Synthetic LXR Ligand Inhibits the Development of Atherosclerosis in Mice
Published in Proceedings of the National Academy of Sciences - PNAS (28-05-2002)“…The nuclear receptors LXRα and LXRβ have been implicated in the control of cholesterol and fatty acid metabolism in multiple cell types. Activation of these…”
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Activation of Liver X Receptor Improves Glucose Tolerance through Coordinate Regulation of Glucose Metabolism in Liver and Adipose Tissue
Published in Proceedings of the National Academy of Sciences - PNAS (29-04-2003)“…The control of lipid and glucose metabolism is closely linked. The nuclear receptors liver X receptor (LXR)α and LXRβ have been implicated in gene expression…”
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13
GSK4112, a Small Molecule Chemical Probe for the Cell Biology of the Nuclear Heme Receptor Rev-erbα
Published in ACS chemical biology (15-10-2010)“…The identification of nonporphyrin ligands for the orphan nuclear receptor Rev-erbα will enable studies of its role as a heme sensor and regulator of metabolic…”
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Longitudinal efficacy and safety modeling and simulation framework to aid dose selection of belantamab mafodotin for patients with multiple myeloma
Published in CPT: pharmacometrics and systems pharmacology (01-10-2023)“…Belantamab mafodotin, a monomethyl auristatin F (MMAF)-containing monoclonal antibody-drug conjugate (ADC), demonstrated deep and durable responses in the…”
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Identification of a Novel Human Constitutive Androstane Receptor (CAR) Agonist and Its Use in the Identification of CAR Target Genes
Published in The Journal of biological chemistry (09-05-2003)“…The orphan nuclear constitutive androstane receptor (CAR) is proposed to play a central role in the response to xenochemical stress. Identification of CAR…”
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Exploration of phenylpropanoic acids as agonists of the free fatty acid receptor 4 (FFA4): Identification of an orally efficacious FFA4 agonist
Published in Bioorganic & medicinal chemistry letters (01-03-2017)“…[Display omitted] The long chain free fatty acid receptor 4 (FFA4/GPR120) has recently been recognized as lipid sensor playing important roles in nutrient…”
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Crystal structure of the PXR–T1317 complex provides a scaffold to examine the potential for receptor antagonism
Published in Bioorganic & medicinal chemistry (01-03-2007)“…The crystal structure of the nuclear xenobiotic receptor PXR in complex with T0901317 leads to the synthesis of agonists specific to PXR relative to the…”
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Discovery of Tertiary Sulfonamides as Potent Liver X Receptor Antagonists
Published in Journal of medicinal chemistry (22-04-2010)“…Tertiary sulfonamides were identified in a HTS as dual liver X receptor (LXR, NR1H2, and NR1H3) ligands, and the binding affinity of the series was increased…”
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The Human Nuclear Xenobiotic Receptor PXR: Structural Determinants of Directed Promiscuity
Published in Science (American Association for the Advancement of Science) (22-06-2001)“…The human nuclear pregnane X receptor (hPXR) activates cytochrome P450-3A expression in response to a wide variety of xenobiotics and plays a critical role in…”
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Structural Disorder in the Complex of Human Pregnane X Receptor and the Macrolide Antibiotic Rifampicin
Published in Molecular endocrinology (Baltimore, Md.) (01-05-2005)“…The human nuclear xenobiotic receptor, pregnane X receptor (PXR), detects a variety of structurally distinct endogenous and xenobiotic compounds and controls…”
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