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Receptors as Drug Targets

Abstract Table of Contents Figures Literature Cited Abstract Receptors, located on both the cell surface and within the cell, are the molecular targets through which drugs produce their beneficial effects in various disease states. Recepto

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Disulfide Conjugation of Peptides to Oligonucleotides and Their Analogs

Abstract Table of Contents Materials Figures Literature Cited Abstract Peptide conjugation of oligonucleotides and their analogs is being studied widely towards improving the delivery of oligonucleotides

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Mapping Chromatin Interactions by Chromosome Conformation Capture

Abstract Table of Contents Materials Figures Literature Cited Abstract Chromosome conformation capture (3C) is one of the only techniques that allows for analysis of an intermediate level of chromosome st

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Practical Aspects of Radioligand Binding

Abstract Table of Contents Figures Literature Cited Abstract Radioligand binding has been used for many years to identify new binding sites, characterize receptors, and identify novel ligands. Although various techniques have been develope

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Methoxyoxalamido Chemistry in the Synthesis of Tethered Phosphoramidites and Functionalized Oligonucleotides

Abstract Table of Contents Materials Figures Literature Cited Abstract A general approach to phosphoramidites tethered with single and multiple linkers through the use of methoxyoxalamido (MOX) chemistry

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Studies of the Ubiquitin Proteasome System

Abstract Table of Contents Materials Figures Literature Cited Abstract A concept that has arisen over the last decade is that proteins can, in general, be covalently modified by poly

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Using Biacore to Measure the Binding Kinetics of an Antibody‐Antigen Interaction

Abstract Table of Contents Materials Figures Literature Cited Abstract The optical phenomenon of surface plasmon resonance (SPR) used by Biacore systems enables the detection and measurement of protein?pr

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Overview of Biacore Systems and Their Applications

Abstract Table of Contents Literature Cited Abstract Surface plasmon resonance (SPR) allows for the investigation of the functional nature of binding interactions and provides detailed kinetic information across a wide range of molecular weights, including small molecules,

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Fluorescence Quenching Methods to Study Lipid‐Protein Interactions

Abstract Table of Contents Materials Figures Literature Cited Abstract This unit describes how fluorescence quenching methods can be used to determine binding constants for phospholipids binding to intrin

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Rational Design and Evaluation of FRET Experiments to Measure Protein Proximities in Cells

Abstract Table of Contents Figures Literature Cited Abstract Fluorescence resonance energy transfer (FRET) refers to the nonradiative transfer of energy from one fluorescent molecule (the donor) to another fluorescent molecule (the accepto

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Quantitative Determination of Protein Stability and Ligand Binding by Pulse Proteolysis

Abstract Table of Contents Materials Figures Literature Cited Abstract Pulse proteolysis exploits the difference in proteolytic susceptibility between folded and unfolded proteins for facile but quantitat

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Circular Dichroism to Study Protein Interactions

Abstract Table of Contents Figures Literature Cited Abstract Circular dichroism (CD) is a powerful technique for studying the structures of proteins in solution, as well as structural changes that may occur when proteins bind to ligands. C

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Identifying Small‐Molecule Modulators of Protein‐Protein Interactions

Abstract Table of Contents Materials Figures Literature Cited Abstract This unit outlines methods for identifying cyclic peptides that inhibit protein?protein interactions. Proteins of interest are cloned

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Benzodiazepine Binding to GABAA Receptors

Abstract Table of Contents Materials Figures Literature Cited Abstract This unit describes ligand binding assays for the characterization of the benzodiazepine (BZ) site of GABAA receptors in the central ne

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Preparation of 2′‐Deoxy‐2′‐Methylseleno‐Modified Phosphoramidites and RNA

Abstract Table of Contents Materials Figures Literature Cited Abstract The derivatization of nucleic acids with selenium is a useful approach to facilitate phase determination during three?dimensional str

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Identification and Analysis of Multiprotein Complexes Through Chemical Crosslinking

Abstract Table of Contents Materials Figures Literature Cited Abstract Chemical crosslinking provides information about protein?protein interactions in the context of intact protein complexes; therefore,

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Determination of Protein Contacts by Chemical Cross‐Linking With EDC and Mass Spectrometry

Abstract Table of Contents Materials Figures Literature Cited Abstract This unit describes a method for analyzing protein complexes by chemically cross?linking closely positioned amino acids. The cross?li

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Characterization of Dopamine Receptors

Abstract Table of Contents Materials Figures Literature Cited Abstract Dopamine receptors are the principal targets of drugs used for the treatment of neuropsychiatric disorders such as schizophrenia and

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Characterization of Adrenoceptors

Abstract Table of Contents Materials Figures Literature Cited Abstract Norepinephrine and epinephrine are important neurotransmitters in both the peripheral and the central nervous systems. The actions of

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Characterization of Histaminergic Receptors

Abstract Table of Contents Materials Figures Literature Cited Abstract This unit describes radioligand binding protocols for histamine H1, H2, H3, and H4 receptors. Because these rec

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