Results 1 to 10 of about 3,511,004 (317)

Genome-wide binding potential and regulatory activity of the glucocorticoid receptor’s monomeric and dimeric forms

Nature Communications, 2021
Glucocorticoid receptors (GR) are thought to bind DNA as dimers or monomers, to regulate different transcription pathways. Here, the authors perform genome-wide studies on GRs with mutations that impair dimerization and provide evidence that monomeric ...
Thomas A. Johnson, Ville Paakinaho, Sohyoung Kim, Gordon L. Hager, Diego M. Presman   +4 more
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Targeting IFN activity to both B cells and plasmacytoid dendritic cells induces a robust tolerogenic response and protection against EAE

Scientific Reports, 2021
Type I Interferon (IFN) was the very first drug approved for the treatment of Multiple Sclerosis (MS), and is still frequently used as a first line therapy. However, systemic IFN also causes considerable side effects, affecting therapy adherence and dose
Anje Cauwels, Sandra Van Lint, Elke Rogge, Annick Verhee, Bram Van Den Eeckhout, Shengru Pang, Marco Prinz, Niko Kley, Gilles Uzé, Jan Tavernier   +9 more
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Residue 6.43 defines receptor function in class F GPCRs

Nature Communications, 2021
The class Frizzled of G protein-coupled receptors (GPCRs) consist of ten Frizzled (FZD1-10) subtypes and Smoothened (SMO). Here the Schulte laboratory demonstrates that FZDs differ substantially from SMO in receptor activation-associated conformational ...
Ainoleena Turku, Hannes Schihada, Pawel Kozielewicz, Carl-Fredrik Bowin, Gunnar Schulte   +4 more
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Carboxylic Acid Bioisosteres in Medicinal Chemistry: Synthesis and Properties

Journal of Chemistry, 2022
Lead optimization represents the tedious process of fine-tuning lead compounds from biologically active hits to suitable drug candidates for clinical trials.
Kato Bredael, Silke Geurs, Dorien Clarisse, Karolien De Bosscher, Matthias D’hooghe   +4 more
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Bioengineering of Extracellular Vesicles: Exosome-Based Next-Generation Therapeutic Strategy in Cancer

Bioengineering, 2021
Extracellular nano vesicles and exosomes hold compelling evidence in intercellular communication. Exosomal intracellular signal transduction is mediated by the transfer of cargo proteins, lipids, micro (mi)RNAs, long noncoding (lnc)RNAs, small ...
Priyanka Saha, Suchisnigdha Datta, Sukanya Ghosh, Anurima Samanta, Paramita Ghosh, Dona Sinha   +5 more
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Structural insights into the activation of human calcium-sensing receptor

eLife, 2021
Human calcium-sensing receptor (CaSR) is a G-protein-coupled receptor that maintains Ca2+ homeostasis in serum. Here, we present the cryo-electron microscopy structures of the CaSR in the inactive and agonist+PAM bound states.
Xiaochen Chen, Lu Wang, Qianqian Cui, Zhanyu Ding, Li Han, Yongjun Kou, Wenqing Zhang, Haonan Wang, Xiaomin Jia, Mei Dai, Zhenzhong Shi, Yuying Li, Xiyang Li, Yong Geng   +13 more
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Compound A influences gene regulation of the Dexamethasone-activated glucocorticoid receptor by alternative cofactor recruitment

Scientific Reports, 2017
The glucocorticoid receptor (GR) is a transcription factor of which the underlying gene regulatory mechanisms are complex and incompletely understood. The non-steroidal anti-inflammatory Compound A (CpdA), a selective GR modulating compound in various ...
S. J. Desmet, N. Bougarne, L. Van Moortel, L. De Cauwer, J. Thommis, M. Vuylsteke, D. Ratman, R. Houtman, J. Tavernier, K. De Bosscher   +9 more
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Structural insights into the peptide selectivity and activation of human neuromedin U receptors

Nature Communications, 2022
Neuromedin U receptors (NMURs) are potential drug targets for obesity and inflammatory disorders. Here, the authors report structural basis for neuromedin recognition and activation mechanism of NMURs.
Chongzhao You, Yumu Zhang, Peiyu Xu, Sijie Huang, Wanchao Yin, H. Eric Xu, Yi Jiang   +6 more
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Glucocorticoid Receptor-mediated transactivation is hampered by Striatin-3, a novel interaction partner of the receptor

Scientific Reports, 2017
The transcriptional activity of the glucocorticoid receptor (GR) is co-determined by its ability to recruit a vast and varying number of cofactors. We here identify Striatin-3 (STRN3) as a novel interaction partner of GR that interferes with GR’s ligand ...
Ioanna Petta, Nadia Bougarne, Jolien Vandewalle, Lien Dejager, Sofie Vandevyver, Marlies Ballegeer, Sofie Desmet, Jonathan Thommis, Lode De Cauwer, Sam Lievens, Claude Libert, Jan Tavernier, Karolien De Bosscher   +12 more
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Pathway selectivity in Frizzleds is achieved by conserved micro-switches defining pathway-determining, active conformations

Nature Communications, 2023
The class Frizzled of G protein-coupled receptors (GPCRs), consisting of ten Frizzled (FZD1-10) paralogs and Smoothened, remains one of the most enigmatic GPCR families.
Lukas Grätz, Maria Kowalski-Jahn, Magdalena M. Scharf, Pawel Kozielewicz, Michael Jahn, Julien Bous, Nevin A. Lambert, David E. Gloriam, Gunnar Schulte   +8 more
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