Results 11 to 20 of about 3,521,155 (317)
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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Lipoxins (LXs) represent a class of arachidonic acid (AA) metabolites that carry potent immunoregulatory and anti-inflammatory properties, LXA4and LXB4being the main components of this series. LXs are generated by cooperation between 5-lipoxygenase (LO) and 12- or 15-LO during cell-cell interactions or by single cell types. LX epimers at carbon 15, the
ROMANO, Mario +2 more
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Residue 6.43 defines receptor function in class F GPCRs
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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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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Carboxylic Acid Bioisosteres in Medicinal Chemistry: Synthesis and Properties
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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Of the established Ca2+-mobilizing messengers, NAADP is arguably the most tantalizing. It is the most potent, often efficacious at low nanomolar concentrations, and its receptors undergo dramatic desensitization. Recent studies have identified a new class of calcium-release channel, the two-pore channels (TPCs), as the likely targets for NAADP ...
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Receptors | Angiotensin Receptors
The renin-angiotensin-aldosterone system (RAS) is a vital hormone-receptor system that regulates cardiovascular and renal functions. In this article, we discuss exciting new findings in the RAS field. Recently solved active state crystal structures of Angiotensin II type 1 (AT1R) and type 2 receptor (AT2R) helped in understanding receptor activation ...
Pardhi, Triveni R., Karnik, Sadashiva S.
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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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Structural insights into the activation of human calcium-sensing receptor
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
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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 +9 more
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