Search Results - "de Vries, Rens M.J.M"
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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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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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Structural interface between LRRK2 and 14-3-3 protein
Published in Biochemical journal (01-04-2017)“…Binding of 14-3-3 proteins to leucine-rich repeat protein kinase 2 (LRRK2) is known to be impaired by many Parkinson's disease (PD)-relevant mutations…”
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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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Indazole MRL-871 interacts with PPARγ via a binding mode that induces partial agonism
Published in Bioorganic & medicinal chemistry (15-08-2022)“…[Display omitted] The nuclear receptor peroxisome proliferator-activated receptor gamma (PPARγ) plays a central role in metabolic processes. PPARγ full…”
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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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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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