Targeting the inward-rectifier potassium channel ROMK in cardiovascular disease.
The kidney plays a critical role in blood pressure homeostasis as a result of the integrated activity of different mechanisms that ensure proper salt and water reabsorption. Diuretics, developed more than four decades ago, are used to treat hypertension and/or congestive heart failure, although there are therapeutic issues that limit their use. Human and rodent genetic studies provide a large body of evidence which suggests that inhibitors of the kidney potassium channel, ROMK, will represent novel diuretics for the treatment of hypertension. The search for potent and selective ROMK inhibitors has recently yielded compounds that display efficacy in animal models, providing the first pharmacological validation of ROMK as a novel diuretic target.
Kanalis Consulting, L.L.C., 5 Ashbrook Drive, Edison, NJ 08820, USA. Electronic address: mlgarciagarcia@optonline.net.
Maria L
ML
Garcia
Kanalis Consulting, L.L.C., 5 Ashbrook Drive, Edison, NJ 08820, USA.
Gregory J
GJ
Kaczorowski
D000818:Animals; D002318:Cardiovascular Diseases / Q000188:drug therapy* / Q000378:metabolism; D057166:High-Throughput Screening Assays / Q000379:methods; D006801:Humans; D058990:Molecular Targeted Therapy; D026902:Potassium Channel Blockers / Q000494:pharmacology*; D024661:Potassium Channels, Inwardly Rectifying / Q000037:antagonists & inhibitors* / Q000378:metabolism; D054852:Small Molecule Libraries / Q000494:pharmacology
D026902:Potassium Channel Blockers; D024661:Potassium Channels, Inwardly Rectifying; D054852:Small Molecule Libraries