Novel Chemical Tools to Study Ion Channel Biology (Advances in Experimental Medicine and Biology)
74 M. Priest and F. Bezanilla Osteen JD, Barro-Soria R, Robey S, Sampson KJ, Kass RS, Larsson HP (2012) Allosteric gating mechan ...
Functional Site-Directed Fluorometry 75 Sesti F, Rajan S, Gonzalez-Colaso R, Nikolaeva N, Goldstein SAN (2003) Hyperpolarization ...
76 M. Priest and F. Bezanilla Wang Q, Lynch JW (2011) Activation and desensitization induce distinct conformational chang- es at ...
77 W. R. Kobertz () Department of Biochemistry and Molecular Pharmacology, University of Massachusetts Medical School, 364 Plan ...
78 K. Mruk and W. R. Kobertz These reagents have been traditionally bifunctional: containing two “targeting” moieties that assoc ...
Bioreactive Tethers 79 firing. The first bioreactive tether (Bartels et al. 1971 ) used the acetylcholine receptor agonist, tran ...
80 K. Mruk and W. R. Kobertz 2 Approach Bioreactive tethers have three components: two targeting moieties linked together via a ...
81 Linker synthesis: The linker is the most synthetically tunable component of a bioreactive tether; thus, most of the creativi ...
82 K. Mruk and W. R. Kobertz 45 Å (7 glycines) are both much harder to synthesize and purify; however, contract research organiz ...
83 Tether Targeting moieties Ion channels Application/Results Refs. CleavableDithiocarbamate Charybdotoxin (CTX) Maleimide Kv7.1 ...
84 K. Mruk and W. R. Kobertz Tether Targeting moieties Ion channels Application/Results Refs. PhotoreversibleAzobenzene Glutamat ...
85 enables the modification of endogenous channels; however, it can be challenging to unequivocally demonstrate whether and wher ...
86 K. Mruk and W. R. Kobertz Channels can also be expressed in cell culture and channel function monitored by whole cell patch c ...
87 The first example of a photoswitchable ion channel was demonstrated with wild- type nicotinic acetylcholine receptors (nAChR) ...
88 K. Mruk and W. R. Kobertz mutant containing an extracellular cysteine, blocked channel current that could be reversed after u ...
89 the simultaneous control and recording of activity in cultured cells (Wang et al. 2007 ), paving the way for in vivo studies ...
90 K. Mruk and W. R. Kobertz Photoisomerizable bioreactive tethers offer several advantages over other op- togenetic and optopha ...
91 At the time, the PLD tethered approach was particularly remarkable because there was no high-resolution structural informatio ...
92 K. Mruk and W. R. Kobertz revealed that the top of the S3 transmembrane domain is farthest away from the center of the pore, ...
93 These distances were consistent with computational resting-state models proposed by Jensen et al., solidifying the understand ...
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