allosteric activation
Allosteric activation of apicomplexan calcium-dependent protein kinases
... CDPKs are obvious therapeutic targets. Development of small molecule inhibitors against them has focused exclusively on ATP analogs, which often suffer from off-target effects against other host and parasite kinases. ...
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Allosteric activation of periplasmic HtrA proteases
... In a previous study from this lab, we noted that the side-chain rotamer of Met 319 in the PDZ domain changes between inactive DegS and OMP-bound active DegS, relieving a clash that would otherwise occur with the ...
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Mechanism of the allosteric activation of the ClpP protease machinery by substrates and active-site inhibitors
... Because the small molecular weight of the substrate used in our as- says is not an obstacle to its free diffusion into the proteolytic chamber (molecular weight of 574 Da) (30), we tested whether TtClpX binding to TtClpP ...
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Identification of allosteric inhibitors of the ecto-5'-nucleotidase (CD73) targeting the dimer interface
... Allosteric regulation has been extensively described for many enzymes, especially kinases like p21-activiated kinase 4 [ 36 ], small GTPases [ 37 ] or G-protein-coupled receptors for more than half a century [ 38 ...
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A Conserved Activation Cluster Is Required for Allosteric Communication in HtrA-Family Proteases
... trimer. Allosteric activation over this distance is partially explained by remodeling of the protease-domain L3 loop, which is spatially adjacent to bound OMP peptide ...
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Allosteric regulation of DegS protease subunits through a shared energy landscape
... of allosteric activation by OMP peptides, here we generate and study the enzymatic properties of asymmetric DegS trimers that lack one or two PDZ ...the allosteric conformations and thus the ...
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Allosteric nanobodies uncover a role of hippocampal mGlu2 receptor homodimers in contextual fear consolidation
... mGlu2 activation by quantifying presynaptic calcium transients evoked by electrical stimulation of mossy fibers, using photometric measurements of the fluorescent Ca 2+ sensitive dye, magnesium green-AM 38 ...
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Activation des lymphocytes T gamma delta dans les cancers
... their activation which is thus only induced here by PAg and not by other activator ...T activation ( 9 , 24 ...weak activation of Vγ9Vδ2 T cells, we focused on RHOB inside the ...T activation ...
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Activation chimique du métakaolin dans une matrice cimentaire
... L’analyse paramétrique nous a également permis de définir des dosages en MK (25% de substitution massique au ciment) et en NS (4% du poids de liant) qui, tout en assurant une activation significative aux jeunes ...
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Allosteric nanobodies uncovered a role of hippocampal mGlu2 receptor homodimers in contextual fear consolidation.
... nanobody to the receptor is then measured by a TR-FRET signal. b) Specific TR-FRET binding data obtained with the indicated mGlu receptor and either DN1, DN10, DN13 or a control irrelev[r] ...
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Analysis of allosteric effect of pathologic variants at the light of local protein conformations
... Analysis of allosteric effect of pathologic variants at the light of local protein conformations6. Belgrade BioInformatics Conference – BelBi 2018, Jun 2018, Belgrade, Serbia.?[r] ...
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Allosteric inhibition of VIMs metallo-β-lactamases by a camelid single-domain antibody fragment.
... This work was supported by FRIA (FNRS) and the Belgian Science Policy. ligand in the active-site (Salsbury et al, 2009). Binding of CA1838 could prevent such a dynamic flip, thereby acting as an allosteric ...
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Activation des cellules dendritiques par des composantes de bioaérosols
... BMDC activation can stratify the air quality status of different groups of occupational settings, which in this case, are all classified among the high bacterial concentration and high total organic dust category ...
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Allosteric Inhibition of Human Ribonucleotide Reductase by dATP Entails the Stabilization of a Hexamer
... of allosteric inhibition for the class Ia RNRs, in which dATP is the only e ffector that favors stabilization of a single conformation, one in which β 2 likely has limited access to the active sites of α 6 ...
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Isomérisation du lactose en lactulose par électro-activation
... 27 Lobyshev, 2001). L’activation de l’eau et son passage à un stade non équilibré thermodynamiquement peut se faire par voie chimique, physique ou biologique. L’eau activée est caractérisée par une activité ...
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Immune activation and chronic inflammation
... immune activation and inflammation from cryopreserved sera, using ultrasensitive techniques (Luminex & Simoa) to identify whether biomarkers were associated with ...
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Targeting Degradation of EGFR through the Allosteric Site Leads to Cancer Cell Detachment-Promoted Death
... Another important issue in our study is the identification of a putative molecular switch for EGFR endocytic degradation. The structure-activity relationship analysis strongly suggests that receptor degradation is a ...
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DESIGN OF HIGH-AFFINITY LIGANDS FOR THE BENZOTHIADIAZINE ALLOSTERIC BINDING SITE OF THE AMPA RECEPTORS
... -‐45.4065 Based on the cristallographic data obtained with molecule (4) in the allosteric pocket, docking experiments were achieved by C. Bouckaert (NAMEDIC). This study confirmed in silico that the envisaged ...
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Deep Learning of Activation Energies
... The idea behind constructing difference fingerprints is to subtract out the effects of atoms that do not change significantly in the reaction, and, therefore, do not contribute much to the activation energy ...
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Connectivity-informed fMRI Activation Detection
... Each dataset consisted of 10 subjects. Each subject’s data comprised 100 regions with the first 20 regions set to be mutually correlated and activated across all subjects. The next 20 regions were set to be mutually ...
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