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ligand binding

Application of BRET to monitor ligand binding to GPCRs

Application of BRET to monitor ligand binding to GPCRs

... fluorescent ligands, which was inhibited by agonist isoprenaline, and antagonists propranolol, ICI 118551 and CGP 12177. Therefore Nluc has a substantial dynamic range compatible with excitation wavelengths of both ...

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Modeling enzyme-ligand binding in drug discovery

Modeling enzyme-ligand binding in drug discovery

... combines ligand binding site comparison analysis, pro- tein–ligand docking and electrostatic potential calcula- tion to identify possible promiscuous protein–ligand interactions throughout the ...

8

A ligand-binding pocket in the dengue virus envelope glycoprotein

A ligand-binding pocket in the dengue virus envelope glycoprotein

... Fig. 1. Dengue E protein and its ligand-binding pocket. (A) Domain definition of dengue E. Domain I is red, domain II is yellow, and domain III is blue. (B) The dengue E protein dimer, colored as in A, in ...

7

Structure and ligand binding properties of abnormal human albumins

Structure and ligand binding properties of abnormal human albumins

... The ligand binding properties of metal ions, bilirubin, palmitate and warfarin were assessed and it was shown that Albumin Carlisle has increased warfarin binding but decreased bilirubin[r] ...

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Human Cytomegalovirus US28 Ligand Binding Activity Is Required for Latency in CD34+ Hematopoietic Progenitor Cells and Humanized NSG Mice

Human Cytomegalovirus US28 Ligand Binding Activity Is Required for Latency in CD34+ Hematopoietic Progenitor Cells and Humanized NSG Mice

... US28 ligand binding promoted higher levels of FLT3 phosphorylation than that without ligands ...of ligand, and possibly constitutive activity, promotes the formation of a cell type that is capable of ...

16

Ligand binding and homology modelling of insect odorant-binding proteins

Ligand binding and homology modelling of insect odorant-binding proteins

... study ligand–OBP interactions, as well as to research ‘super-ligands’ for insect behavioural ...their binding affinity to OBPs, as an interesting approach for using these chemicals in pest man- ...proteins. ...

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A multiple ligand binding radioimmunoassay of diiodotyrosine

A multiple ligand binding radioimmunoassay of diiodotyrosine

... adjuvant. Sera were screened for their ability to bind trace amounts of [125I]DIT. A serum that bound 40% of the tracer at a final dilution of 1:1,750 was used in the assay. Assay specificity was improved by the use of ...

8

PocketPicker: analysis of ligand binding-sites with shape descriptors

PocketPicker: analysis of ligand binding-sites with shape descriptors

... For the sake of completeness we tested PocketPicker on a test set of 210 complexes compiled by Huang and Schröder [17]. This test set also contained multimeric structures. Success rates of PocketPicker predictions for ...

17

The Unique C Termini of Orthopoxvirus Gamma Interferon Binding Proteins Are Essential for Ligand Binding

The Unique C Termini of Orthopoxvirus Gamma Interferon Binding Proteins Are Essential for Ligand Binding

... Together, these data suggest that the IFN- ␥ BP is assembled into higher-ordered structures that are dependent upon the full-length CTD and its ␣ -helical secondary structure. The assembly of these oligomers is ...

8

Protein nanoparticles with ligand-binding and enzymatic activities

Protein nanoparticles with ligand-binding and enzymatic activities

... specific binding of antibodies with the BSA-RhoB protein and the corresponding fluorescent NP were comparable with the wide range of anti-BSA antibodies dilution from 1:10 to 1:10,000 and exceeded those of non- ...

10

Selectin and selectin ligand binding: a bittersweet attraction

Selectin and selectin ligand binding: a bittersweet attraction

... selectin ligand activity can be achieved by antagonizing specific gly- cosyltransferases with small mole- cules and leads to anti-inflammatory effects in ...

5

Dynamics of ligand binding to a rigid glycosidase

Dynamics of ligand binding to a rigid glycosidase

... (75-105 ppm) in which the protein shows no resonances. Upon addition of BCX-E78Q, the resonances of many X6 resonances shift and broaden beyond detection, even at a BCX-E78Q:X6 ratio of 0.2:1 (Fig. S2D), in line with the ...

9

Protein Dynamics and Entropy: Implications for Protein-Ligand Binding

Protein Dynamics and Entropy: Implications for Protein-Ligand Binding

... compounds [49]. Recently, Freire and colleagues demonstrated a framework for lead optimization that allows one to semi-rationally overcome the barrier of enthalpy-entropy compensation [50]. In their approach, both the ...

186

Effect of dacarbazine on CD44 in live melanoma cells as measured by atomic force microscopy-based nanoscopy

Effect of dacarbazine on CD44 in live melanoma cells as measured by atomic force microscopy-based nanoscopy

... CD44 ligand binding and reduces the stability of the CD44 ligand–receptor complexes in DTIC-treated cell membranes, but does not completely inhibit the binding of the CD44 ligand to its ...

20

Structure-guided discovery of a single-domain antibody agonist against human apelin receptor

Structure-guided discovery of a single-domain antibody agonist against human apelin receptor

... in binding to APJ at the orthosteric site (29). The binding of JN241-9 or AMG3054 to APJ further resembles the binding of angiotensin II analog S1I8 to AT2R (angiotensin II receptor type II) (30) or ...

10

Comparative analysis between the protein mcp 1 and neurotrophins involved in alopecia areata

Comparative analysis between the protein mcp 1 and neurotrophins involved in alopecia areata

... 5. Ligand binding site in Neurotrophins protein family PDB ID 1SG1 Three ligand binding sites were found in PDB ID 1DOK of protein MCP-1, out of which 1 was selected for further docking ...

12

A Review on Clustering Techniques and Optimization Algorithms for Molecular Docking and DNA Nanotechnology

A Review on Clustering Techniques and Optimization Algorithms for Molecular Docking and DNA Nanotechnology

... protein binding pockets and their ...Protein-Ligand Binding sites for structure based drug design and virtual ligand ...a ligand binding site to modulate function. Binding ...

8

A Comparative Study of Binding of Different Drugs on gp120: Insight from Molecular Dynamics Simulation Study

A Comparative Study of Binding of Different Drugs on gp120: Insight from Molecular Dynamics Simulation Study

... upon ligand binding, respectively, and -TΔS is the entropy contribution arising from changes in the degrees of freedom of the solute molecules, which we reconsidered here to obtain ΔG bind ; therefore, our ...

9

Novel drugs that target the estrogen-related receptor alpha: their therapeutic potential in breast cancer

Novel drugs that target the estrogen-related receptor alpha: their therapeutic potential in breast cancer

... the ligand-binding domains of estrogen receptor alpha and estrogen-related receptor alpha, their ability to bind estrogens, phytoestrogens, and synthetic ligands, and the effects of ligand agonists, ...

28

Phosphite binding by the HtxB periplasmic binding protein depends on the protonation state of the ligand

Phosphite binding by the HtxB periplasmic binding protein depends on the protonation state of the ligand

... the ligand binding domain (residues 95–204) from D206N HtxB with WT HtxB ...the ligand binding site in the mutant protein, rotated ...no ligand binding could be detected for this ...

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