Identification of a potent sodium hydrogen exchanger isoform 1 (NHE1) inhibitor with a suitable profile for chronic dosing and demonstrated cardioprotective effects in …

JD Huber, J Bentzien, SJ Boyer, J Burke…

Index: Huber, John D.; Bentzien, Joerg; Boyer, Stephen J.; Burke, Jennifer; De Lombaert, Stephane; Eickmeier, Christian; Guo, Xin; Haist, James V.; Hickey, Eugene R.; Kaplita, Paul; Karmazyn, Morris; Kemper, Raymond; Kennedy, Charles A.; Kirrane, Thomas; Madwed, Jeffrey B.; Mainolfi, Elizabeth; Nagaraja, Nelamangara; Soleymanzadeh, Fariba; Swinamer, Alan; Eldrup, Anne B. Journal of Medicinal Chemistry, 2012 , vol. 55, # 16 p. 7114 - 7140

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Citation Number: 14

Abstract

Sodium–hydrogen exchanger isoform 1 (NHE1) is a ubiquitously expressed transmembrane ion channel responsible for intracellular pH regulation. During myocardial ischemia, low pH activates NHE1 and causes increased intracellular calcium levels and aberrant cellular processes, leading to myocardial stunning, arrhythmias, and ultimately cell damage and death. The role of NHE1 in cardiac injury has prompted interest in the development of ...