title: Bioreactive Tethers.
abstract: Ion channel complexes are challenging to study by traditional biochemical methods due to their membranous lipid environment and large size. Bioreactive tethers are specialized chemical probes that have been used in electrophysiological experiments to provide unique insight into ion channel structure and function. Because bioreactive tethers are small molecular probes, they can be used to manipulate ion channel function in heterologous expression systems, native cells and animal models. This chapter covers three classes of tethers: photoswitchable, molecular rulers, and chemically reactive. The modular nature of bioreactive tethers enables the facile synthesis of next generation reagents with enhanced functionalities to interrogate and control ion channels in novel and multifarious ways.
authors.affiliation: Department of Chemical and Systems Biology, 269 Campus Drive, CCSR 3150, 94305, Stanford, CA, USA. kmruk@stanford.edu.
authors.forename: Karen
authors.initials: K
authors.lastname: Mruk
authors.affiliation: Department of Biochemistry and Molecular Pharmacology, University of Massachusetts Medical School, 364 Plantation Street, 01605-2324, Worcester, MA, USA. william.kobertz@umassmed.edu.
authors.forename: William R
authors.initials: WR
authors.lastname: Kobertz
mesh_terms: D000818:Animals; D001665:Binding Sites; D006801:Humans; D015640:Ion Channel Gating; D007473:Ion Channels / Q000737:chemistry / Q000378:metabolism*; D017136:Ion Transport; D008564:Membrane Potentials; D008958:Models, Molecular; D015336:Molecular Probe Techniques; D015335:Molecular Probes / Q000737:chemistry / Q000378:metabolism*; D011485:Protein Binding; D011487:Protein Conformation; D013329:Structure-Activity Relationship
chemical_list: D007473:Ion Channels; D015335:Molecular Probes
keywords: Azobenzene; Cysteine chemistry; Ion channel blockers; Ligands; Protein derivatization; Quaternary ammonium compounds