Results 11 to 20 of about 3,521,155 (317)

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

Lipoxin Receptors [PDF]

open access: yesThe Scientific World JOURNAL, 2007
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
openaire   +4 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

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

NAADP Receptors [PDF]

open access: yesCold Spring Harbor Perspectives in Biology, 2010
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 ...
openaire   +5 more sources

Receptors | Angiotensin Receptors

open access: yes, 2021
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.
openaire   +1 more source

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

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

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

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