Conformation-Sensitive Assay Detection for Accelerated Drug Discovery Research
Scot R. Weinberger
Monday, March 30, 2015
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Chapters
Introduction
Back-Scattering Interferometry
Drug Discovery Services
TruBind™ System 100
Back-Scattering Interferometry
Back-Scattering Interferometry Signal Processing
Back-scattering Interferometry Sample Preparation and Analysis
BSI and pH Dependent Conformational Change: Bovine Serum Albumin Experiment
Ligand Induce BACE1 Conformational Change: X-ray Crystallographic Data
Polarity Correlates with BACE1 Conformation: Closed or Open Flap
BSI Analysis of Complex Protein Targets: Range of Targets Analyzed
Bcr-Abl Kinase Inhibitor Study
Imatinib Binding experiments
Comparison to combined Cell-based Assay and literature Data
Integral Membrane Protein Targets
Chimeric KcsA-Kv1.3 Ion Channel Nanodisc
Allosterism in GPCRs: Affinity vs Efficacy MOA
Orthosteric & Allosteric Binding: GPCR Targets
M4 Acetylcholine Receptor: Class A Muscarinic GPCR Receptor
M4 – Acetylcholine Binding Assay: Target Engagement and Direct Kd Determination
VU0152100 Effects M4 – Ach Binding: Positive Allosteric Modulator
Summary of M4 Allostery Study
Binding Cooperativity mGluR5 Allosteric Modifier Study
Contractile Protein Complexes: Cardiac and Skeletal Muscle
Binding of B to Contractile Complex Receptor: Positive Modulator A
Protein-Protein Interactions: Small molecule interruption
Small Molecule P-P Interaction Inhibition
Neuro-Fibril Aggregates: Alzheimer’s Research
Fibril Aggregation Effects: Fast-aggregating mutant monomer with small molecule and peptide ligands
Acknowledgements
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