Results 11 to 20 of about 5,438,451 (166)

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

Pathway selectivity in Frizzleds is achieved by conserved micro-switches defining pathway-determining, active conformations

open access: yesNature 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   +8 more
doaj   +1 more source

Orexin-1 receptor-cannabinoid CB1 receptor heterodimerization results in both ligand-dependent and -independent coordinated alterations of receptor localization and function [PDF]

open access: yes, 2006
Following inducible expression in HEK293 cells, the human orexin-1 receptor was targeted to the cell surface but became internalized following exposure to the peptide agonist orexin A.
Canals Buj, M.   +4 more
core   +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

Structural insights into the peptide selectivity and activation of human neuromedin U receptors

open access: yesNature 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
doaj   +1 more source

Harmonic oscillator model of the insulin and IGF1 receptors’ allosteric binding and activation

open access: yesMolecular Systems Biology, 2009
The insulin and insulin‐like growth factor 1 receptors activate overlapping signalling pathways that are critical for growth, metabolism, survival and longevity.
Vladislav V Kiselyov   +3 more
doaj   +1 more source

The role of ECL2 in CGRP receptor activation: a combined modelling and experimental approach [PDF]

open access: yes, 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

Evaluation of a novel virtual screening strategy using receptor decoy binding sites [PDF]

open access: yes, 2016
Virtual screening is used in biomedical research to predict the binding affinity of a large set of small organic molecules to protein receptor targets.
Kukol, A.   +3 more
core   +2 more sources

Structural insight into small molecule action on Frizzleds

open access: yesNature Communications, 2020
WNT-Frizzled (FZD) signaling plays a critical role in embryonic development, tissue homeostasis and human disease but no small molecule drugs targeting FZD with distinct efficacy have emerged so far.
Paweł Kozielewicz   +9 more
doaj   +1 more source

Discrimination and Quantification of Glomerular Receptor Subtypes for Atrial Natriuretic Factor (Anf) [PDF]

open access: yes, 1991
Binding sites for atrial natriuretic factor (ANF) were determined on isolated rat glomeruli as well as on glomerular membranes. To define optimal conditions, binding of ANF was investigated varying incubation time, temperature and protein concentration ...
Gerbes, Alexander L.   +2 more
core   +1 more source

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