共 117 条
Small-molecule modulators of inward rectifier K+ channels: recent advances and future possibilities
被引:37
作者:

Bhave, Gautam
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机构:
Vanderbilt Univ, Med Ctr, Dept Anesthesiol, Nashville, TN 37232 USA
Vanderbilt Univ, Med Ctr, Div Nephrol, Nashville, TN 37232 USA Vanderbilt Univ, Med Ctr, Dept Anesthesiol, Nashville, TN 37232 USA

Lonergan, Daniel
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h-index: 0
机构:
Vanderbilt Univ, Med Ctr, Dept Anesthesiol, Nashville, TN 37232 USA Vanderbilt Univ, Med Ctr, Dept Anesthesiol, Nashville, TN 37232 USA

Chauder, Brian A.
论文数: 0 引用数: 0
h-index: 0
机构:
Vanderbilt Univ, Med Ctr, Dept Pharmacol, Nashville, TN 37232 USA Vanderbilt Univ, Med Ctr, Dept Anesthesiol, Nashville, TN 37232 USA

Denton, Jerod S.
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h-index: 0
机构:
Vanderbilt Univ, Med Ctr, Dept Anesthesiol, Nashville, TN 37232 USA
Vanderbilt Univ, Med Ctr, Dept Pharmacol, Nashville, TN 37232 USA
Vanderbilt Univ, Med Ctr, Digest Dis Res Ctr, Nashville, TN 37232 USA Vanderbilt Univ, Med Ctr, Dept Anesthesiol, Nashville, TN 37232 USA
机构:
[1] Vanderbilt Univ, Med Ctr, Dept Anesthesiol, Nashville, TN 37232 USA
[2] Vanderbilt Univ, Med Ctr, Dept Pharmacol, Nashville, TN 37232 USA
[3] Vanderbilt Univ, Med Ctr, Div Nephrol, Nashville, TN 37232 USA
[4] Vanderbilt Univ, Med Ctr, Digest Dis Res Ctr, Nashville, TN 37232 USA
关键词:
RECTIFYING POTASSIUM CHANNELS;
CELLULAR CONDUCTIVE PATHWAYS;
ANTENATAL BARTTER-SYNDROME;
CORTICAL COLLECTING DUCT;
THICK ASCENDING LIMBS;
SUBUNIT KNOCKOUT MICE;
BASOLATERAL MEMBRANE;
ATRIAL-FIBRILLATION;
CRYSTAL-STRUCTURE;
GIRK CHANNELS;
D O I:
10.4155/FMC.10.179
中图分类号:
R914 [药物化学];
学科分类号:
100701 ;
摘要:
Inward rectifier potassium (Kir) channels have been postulated as therapeutic targets for several common disorders including hypertension, cardiac arrhythmias and pain. With few exceptions, however, the small-molecule pharmacology of this family is limited to nonselective cardiovascular and neurologic drugs with off-target activity toward inward rectifiers. Consequently, the actual therapeutic potential and 'drugability' of most Kir channels has not yet been determined experimentally. The purpose of this review is to provide a comprehensive summary of publicly disclosed Kir channel small-molecule modulators and highlight recent targeted drug-discovery efforts toward Kir1.1 and Kir2.1. The review concludes with a brief speculation on how the field of Kir channel pharmacology will develop over the coming years and a discussion of the increasingly important role academic laboratories will play in this progress.
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页码:757 / 774
页数:18
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