Search Results - "Meijer, Femke A"
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Characterization and small-molecule stabilization of the multisite tandem binding between 14-3-3 and the R domain of CFTR
Published in Proceedings of the National Academy of Sciences - PNAS (01-03-2016)“…Cystic fibrosis is a fatal genetic disease, most frequently caused by the retention of the CFTR (cystic fibrosis transmembrane conductance regulator) mutant…”
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Ligand Dependent Switch from RXR Homo- to RXR-NURR1 Heterodimerization
Published in ACS chemical neuroscience (20-09-2017)“…Retinoid X receptors (RXRs) play key roles in many physiological processes in both the periphery and central nervous system. In addition, RXRs form…”
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Orthosteric and Allosteric Dual Targeting of the Nuclear Receptor RORγt with a Bitopic Ligand
Published in ACS chemical biology (19-03-2021)“…The RORγt nuclear receptor (NR) is of critical importance for the differentiation and proliferation of T helper 17 (Th17) cells and their production of the…”
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Allosteric small molecule modulators of nuclear receptors
Published in Molecular and cellular endocrinology (05-04-2019)“…Nuclear Receptors (NRs) are multi-domain proteins, whose natural regulation occurs via ligands for a classical, orthosteric, binding pocket and via intra- and…”
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Cooperativity between the orthosteric and allosteric ligand binding sites of RORγt
Published in Proceedings of the National Academy of Sciences - PNAS (09-02-2021)“…Cooperative ligand binding is an important phenomenon in biological systems where ligand binding influences the binding of another ligand at an alternative…”
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Ligand-Based Design of Allosteric Retinoic Acid Receptor-Related Orphan Receptor γt (RORγt) Inverse Agonists
Published in Journal of medicinal chemistry (09-01-2020)“…Retinoic acid receptor-related orphan receptor γt (RORγt) is a nuclear receptor associated with the pathogenesis of autoimmune diseases. Allosteric inhibition…”
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Structure–Activity Relationship Studies of Trisubstituted Isoxazoles as Selective Allosteric Ligands for the Retinoic-Acid-Receptor-Related Orphan Receptor γt
Published in Journal of medicinal chemistry (08-07-2021)“…The inhibition of the nuclear receptor retinoic-acid-receptor-related orphan receptor γt (RORγt) is a promising strategy in the treatment of autoimmune…”
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Characterization of Coding/Noncoding Variants for SHROOM3 in Patients with CKD
Published in Journal of the American Society of Nephrology (01-05-2018)“…Interpreting genetic variants is one of the greatest challenges impeding analysis of rapidly increasing volumes of genomic data from patients. For example, is…”
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Inhibition of 14-3-3/Tau by Hybrid Small-Molecule Peptides Operating via Two Different Binding Modes
Published in ACS chemical neuroscience (21-11-2018)“…Current molecular hypotheses have not yet delivered marketable treatments for Alzheimer’s disease (AD), arguably due to a lack of understanding of AD biology…”
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Elucidation of an Allosteric Mode of Action for a Thienopyrazole RORγt Inverse Agonist
Published in ChemMedChem (03-04-2020)“…The demand for allosteric targeting of nuclear receptors is high, but examples are limited, and structural information is scarce. The retinoic acid‐related…”
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Covalent Occlusion of the RORγt Ligand Binding Pocket Allows Unambiguous Targeting of an Allosteric Site
Published in ACS medicinal chemistry letters (08-04-2021)“…The nuclear receptor RORγt is a key positive regulator in the differentiation and proliferation of T helper 17 (Th17) cells and the production of…”
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