Results 1 to 10 of about 2,789,540 (267)

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

open access: yesNature 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
doaj   +1 more source

Adenosine A1 receptor: Functional receptor-receptor interactions in the brain [PDF]

open access: yesPurinergic Signalling, 2007
Over the past decade, many lines of investigation have shown that receptor-mediated signaling exhibits greater diversity than previously appreciated. Signal diversity arises from numerous factors, which include the formation of receptor dimers and interplay between different receptors.
Sichardt, Kathrin, Nieber, Karen
openaire   +2 more sources

Residue 6.43 defines receptor function in class F GPCRs

open access: yesNature 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
doaj   +1 more source

Targeting IFN activity to both B cells and plasmacytoid dendritic cells induces a robust tolerogenic response and protection against EAE

open access: yesScientific 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
doaj   +1 more source

An Introduction to Receptors and Receptor Disorders

open access: yesExperimental Biology and Medicine, 1979
SummaryIn the last decade reliable methods have been introduced to quantitate and characterize receptors for hormones and other biologically interesting ligands. Applied initially to hormone receptors on malignant cells and to androgen-resistant and insulin-resistant states, these methods have led to the identification of many disease processes where ...
J. Roth   +8 more
openaire   +3 more sources

Bioengineering of Extracellular Vesicles: Exosome-Based Next-Generation Therapeutic Strategy in Cancer

open access: yesBioengineering, 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
doaj   +1 more source

Compound A influences gene regulation of the Dexamethasone-activated glucocorticoid receptor by alternative cofactor recruitment

open access: yesScientific 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   +9 more
doaj   +1 more source

Carboxylic Acid Bioisosteres in Medicinal Chemistry: Synthesis and Properties

open access: yesJournal 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
doaj   +1 more source

Structural insights into the activation of human calcium-sensing receptor

open access: yeseLife, 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

Glucocorticoid Receptor-mediated transactivation is hampered by Striatin-3, a novel interaction partner of the receptor

open access: yesScientific 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   +12 more
doaj   +1 more source

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