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Target-mediated drug disposition model for drugs with N > 2 binding sites that bind to a target with one binding site
The paper extended the TMDD model to drugs with more than two ( N > 2) identical binding sites (N-to-one TMDD). The quasi-steady-state (N-to-one QSS),...
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Inactivation of cell-free HIV-1 by designing potent peptides based on mutations in the CD4 binding site
Human immunodeficiency virus type 1 (HIV-1) is a major global health problem, with over 38 million people infected worldwide. Current anti-HIV-1...
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Rifabutin but not rifampicin can partly out-balance P-glycoprotein induction by concurrent P-glycoprotein inhibition through high affinity binding to the inhibitory site
Physiology-based pharmacokinetic modeling suggests that rifabutin can out-balance P-glycoprotein (P-gp) induction by concurrent P-gp inhibition....
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Mutation in the TRKB Cholesterol Recognition Site that blocks Antidepressant Binding does not Influence the Basal or BDNF-Stimulated Activation of TRKB
Brain-derived neurotrophic factor (BDNF) acting upon its receptor Neurotrophic tyrosine kinase receptor 2 (NTRK2, TRKB) plays a central role in the...
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Radioligand Binding at Muscarinic Receptors
Five subtypes of muscarinic acetylcholine receptors denoted M1 through M5 mediate a wide array of physiological functions. Therefore, impairment of...
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Allosteric Modulation of Ligand Binding to Muscarinic Receptors
Allosteric ligands bind to a site on the receptor different from the primary (orthosteric) site. They modulate the binding and function of muscarinic...
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Specific Mutations in the Cholesterol-Binding Site of APP Alter Its Processing and Favor the Production of Shorter, Less Toxic Aβ Peptides
Excess brain cholesterol is strongly implicated in the pathogenesis of Alzheimer’s disease (AD). Here we evaluated how the presence of a...
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Investigating the ATP-binding pocket of CX3CL1-binding protein 2 using in silico approach
Plasmodium falciparum (Pf) causes the most fatal form of malaria owing to its ability to cytoadhere in the microvasculature of various organs in the...
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Structural basis of tolvaptan binding to the vasopressin V2 receptor
The vasopressin V 2 receptor (V 2 R) is a validated therapeutic target for autosomal dominant polycystic kidney disease (ADPKD), with tolvaptan being...
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Conventional Receptor Radioligand Binding Techniques Applied to the Study of Monoamine Oxidase
Designed to measure binding interactions between small molecules and receptor proteins, radioligand binding approaches may also be applied to...
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Basic Theoretical Description of Sensor-Target Binding
Quantitative measures are highly needed in fluorescence sensing. In this Chapter the reader finds discussion on parameters that have to be optimized...
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Study of Modification of Drug Binding Site I of Human Serum Albumin by Sodium Hypochlorite by Time Resolved Fluorescent Spectroscopy
Abstract —The kinetics of fluorescence decay of the K-35 probe and the tryptophan amino acid residue were measured after the addition of sodium...
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Characterization of the substrate binding site of an iron detoxifying membrane transporter from Plasmodium falciparum
BackgroundPlasmodium species are entirely dependent upon their host as a source of essential iron. Although it is an indispensable micronutrient,...
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An insertion variant of MGMT disrupts a STAT1 binding site and confers susceptibility to glioma
BackgroundO 6 -methylguanine-DNA methyltransferase (MGMT) is a pivotal enzyme for repairing DNA alkylation damage. Epigenetic modification of MGMT has...
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Exploring Muscarinic Acetylcholine Receptor Binding Kinetics with Fluorescence Anisotropy
Many different assays are available for measuring ligand binding to muscarinic acetylcholine receptors. Each has advantages and throwbacks, making...
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Characterization of Linear IgE-Binding Epitopes in Food Allergens
An IgE epitope is a part of an allergen that is capable of binding to IgE antibodies and eliciting an immune response. Identifying and characterizing...
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KDeep: a new memory-efficient data extraction method for accurately predicting DNA/RNA transcription factor binding sites
This paper addresses the crucial task of identifying DNA/RNA binding sites, which has implications in drug/vaccine design, protein engineering, and...
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Solid-Phase Binding Assay for Ganglioside Binding of Human Respiroviruses
Human parainfluenza virus types 1 (hPIV-1) and 3 (hPIV-3) belong to the family Paramyxoviridae, subfamily Paramyxoviridae, and genus Respirovirus....