نتایج جستجو برای: ligand binding
تعداد نتایج: 489309 فیلتر نتایج به سال:
Ligand binding to the glucocorticoid receptor (GR) results in receptor binding to glucocorticoid response elements (GREs) and the formation of transcriptional regulatory complexes. Equally important, these complexes are continuously disassembled, with active processes driving GR off GREs. We found that co-chaperone p23-dependent disruption of GR-driven transcription depended on the ligand bindi...
Binding of a family brominated benzotriazoles to the catalytic subunit human protein kinase CK2 (hCK2α) was used as model system assess contribution halogen bonding protein–ligand interaction. is constitutively active pleiotropic serine/threonine that belongs CMGC group eukaryotic kinases (EPKs). Due addiction some cancer cells, an attractive and well-characterized drug target. Halogenated act ...
Abstract Organic Cu-binding ligands have a fundamental influence on Cu distributions in the global ocean and they complex >99% of dissolved seawater. however, represent large diversity compounds with distinct sources, sinks chemical properties. This heterogeneity makes organic ligand pool difficult to study at scale. In this review, we provide an overview that compose marine Cu-ligand pool, ...
Although the NF-kappaB transcription factor tolerates significant sequence variations in its DNA binding site, NF-kappaB sites show remarkable evolutionary stability. In this issue of Cell, demonstrate that a single nucleotide change in an NF-kappaB binding site changes the dependence of the promoter on a specific coactivator without affecting NF-kappaB binding. These data suggest that binding ...
A protease-activatable collagen targeting probe (proCNA35) is synthesized by conjugation of a synthetic collagen fragment to the collagen binding protein CNA35 via a protease-cleavable linker. Cleavage of the linker by MMP1 releases the intramolecular inhibition of the collagen binding site and restores its collagen binding capacity.
Integrin-ligand interactions are regulated in a complex manner by divalent cations, and previous studies have identified ligand-competent, stimulatory, and inhibitory cation-binding sites. In collagen-binding integrins, such as 2 1, ligand recognition takes place exclusively at the subunit I domain. However, activation of the I domain depends on its interactionwith a structurally similar domain...
Members of the multiple antibiotic resistance regulator (MarR) family often regulate gene activity by responding to a specific ligand. In the absence of ligand, most MarR proteins function as repressors, while ligand binding causes attenuated DNA binding and therefore increased gene expression. Previously, we have shown that urate is a ligand for MftR (major facilitator transport regulator), wh...
RORγt is critical for the differentiation and proliferation of Th17 cells associated with several chronic autoimmune diseases. We report the discovery of a novel allosteric binding site on the nuclear receptor RORγt. Co-crystallization of the ligand binding domain (LBD) of RORγt with a series of small-molecule antagonists demonstrates occupancy of a previously unreported allosteric binding pock...
The inositol 1,4,5-trisphosphate receptor (InsP(3)R) is activated by InsP(3) binding to amino-terminal ligand binding domain (InsP(3)R-N). Recently we reported functional coupling of phosphatidylinositol (4, 5)-bisphosphate (PIP(2)) to the InsP(3)R. Specific binding of PIP(2) to InsP(3)R-N domain was postulated as a part of the InsP(3)R-PIP(2) functional coupling model. Here we utilized bacteri...
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