Results 1 to 10 of about 6,186,932 (263)
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 +4 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 +4 more
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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 +9 more
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Actin cytoskeleton-dependent regulation of corticotropin-releasing factor receptor heteromers [PDF]
, 2017 Stress responses are highly nuanced and variable, but how this diversity is achieved by modulating receptor function is largely unknown. Corticotropin-releasing factor receptors (CRFRs), class B G protein–coupled receptors, are pivotal in mediating ...
Bhargava, Aditi +7 more
core +1 more source
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 +4 more
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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 +5 more
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The role of ECL2 in CGRP receptor activation: a combined modelling and experimental approach [PDF]
, 2013 The calcitonin gene-related peptide (CGRP) receptor is a complex of a calcitonin receptor-like receptor (CLR), which is a family B G-protein-coupled receptor (GPCR) and receptor activity modifying protein 1.
Alex C. Conner +13 more
core +2 more sources
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 +13 more
doaj +1 more source
KLHL12 promotes non-lysine ubiquitination of the dopamine receptors D-4.2 and D-4.4, but not of the ADHD-associated D-4.7 variant [PDF]
, 2015 Dopamine D-4 Receptor Polymorphism : The dopamine D-4 receptor has an important polymorphism in its third intracellular loop that is intensively studied and has been associated with several abnormal conditions, among others, attention deficit ...
Lintermans, Béatrice +3 more
core +4 more sources
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 +6 more
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