Key result
DIDS hydrolyzes and multimerizes in aqueous solution to form polythioureas that inhibit chloride channels 3-200 times more potently than DIDS itself.
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DIDS multimers formed in aqueous solution are significantly more potent inhibitors of chloride channels than DIDS itself, potentially acting as tethered blockers.
4,4'-Diisothiocyanatostilbene-2,2'-disulfonic acid (DIDS) has been used as an inhibitor of anion transporters and channels since the early 1970s. A study in this issue shows that DIDS hydrolyzes in aqueous solution and then multimerizes to di-, tri-, tetra-, and pentameric polythioureas, which inhibit both the bacterial ClC-ec1 Cl(-)/H(+) exchanger and the mammalian ClC-Ka chloride channel 3-200 times more potently than DIDS itself. The DIDS tetra- and pentamer could potentially act as tethered blockers that simultaneously obstruct both chloride pathways in the dimeric CLC proteins.
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Heike Wulff (2008) reported an editorial. DIDS multimerized polythioureas vs. DIDS itself was evaluated on Inhibition of bacterial ClC-ec1 Cl(-)/H(+) exchanger and mammalian ClC-Ka chloride channel (3-200 times more potent). DIDS hydrolyzes and multimerizes in aqueous solution to form polythioureas that inhibit chloride channels 3-200 times more potently than DIDS itself.
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