Novel Chemical Tools to Study Ion Channel Biology (Advances in Experimental Medicine and Biology)

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Tether

Targeting moieties

Ion channels

Application/Results

Refs.

CleavableDithiocarbamate

Charybdotoxin (CTX)

Maleimide

Kv7.1+KCNE1

Subunit stoichiometric determination

Morin and Kobertz (2008a

)

Disulfide

Charybdotoxin (CTX)

Maleimide

Shaker and Kv7.1+KCNE1

Chemical control of channel function/biotin delivery

Hua et

al. (

2011

)

Nitroindoline

Spermine

Acrylamide

AMPA

Traceless fluorescent labeling of AMPA receptors

Vytla et

al. (

2011

)

Ethylene glycolsAcetylcholine

Acetylcholine

Alkylbromide

nAChR

Determination of functional stoichiometry of ligand binding

Chabala and Lester (^1986

)

Triethylene glycol

Toxin

Maleimide

Kv7.1 with (KCNE1, KCNE3 and KCNE4)

Determination of currents from heteromeric complexes

Morin and Kobertz (^2007

)

Polyethylene glycols

cGMP

cGMP

Homomeric CNG channels

Potent activation and spacing between cyclic nucleotide binding sites.

Kramer and Karpen (^1998

)

Various (n

=

x-y)

Tetraethylammonim (TEA)

Fluorescent quencher

Shaker

Nanometer measurements of voltage sensor movements

Jarecki et

al. (

2013

)

PeptidoGlycines

(n

=

x-y)

Tetraethylammonim (TEA)

Maleimide

Shaker

Voltage sensor movements/radial measurements

Blaustein et

al. (

2000

)

Glycines

(n

=

x-y)

Tetraethylammonim (TEA)

Calmodulin (CaM)

Kv7.2/Kv7.3 (KCNQ2/KCNQ3)

Quaternary structural models of K+ Channel-CaM complexes

Mruk et

al. (

2012

)

Amide/Carbamate

Saxitoxin

Maleimide

Na

1.2 and NaV

1.5V

Covalent inhibitors with bioor-thogonal reactive groups

Parsons and Du Bois (^2013

)

Table 1

Bioreactive tethers

Bioreactive Tethers