2008
DOI: 10.1074/jbc.m802054200
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Structural Basis of a Potent Peptide Inhibitor Designed for Kv1.3 Channel, a Therapeutic Target of Autoimmune Disease

Abstract: The potassium channel Kv1.3 is an attractive pharmacological target for immunomodulation of T cell-mediated autoimmune diseases. Potent and selective blockers of Kv1.3 are potential therapeutics for treating these diseases. 28 and His 33 of ADWX-1 locate right above the selectivity filter-S6 linker of Kv1.3. Together, our data indicate that the specific ADWX-1 peptide would be a viable lead in the therapy of T cell-mediated autoimmune diseases, and the successful design of ADWX-1 suggests that rational design… Show more

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Cited by 128 publications
(193 citation statements)
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“…Peptide Expression and Purification-ADWX-1 peptide was obtained as described previously (20). The molecular mass of the purified ADWX-1 peptide was obtained by MALDI-TOF-MS (Voyager-DESTR, Applied Biosystems).…”
Section: Methodsmentioning
confidence: 99%
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“…Peptide Expression and Purification-ADWX-1 peptide was obtained as described previously (20). The molecular mass of the purified ADWX-1 peptide was obtained by MALDI-TOF-MS (Voyager-DESTR, Applied Biosystems).…”
Section: Methodsmentioning
confidence: 99%
“…Previously, we determined that ADWX-1 targets the artificially expressed Kv1.3 channels in transfected cells and blocks the channel currents (20). Moreover, the voltage-gated Kv1.3 channels open for potassium efflux after antigen-induced depolarization, which promotes calcium influx through the calcium release-activated calcium channel (26,27).…”
Section: Ccr7mentioning
confidence: 99%
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