Novel adenosine 5′-triphosphate-sensitive potassium channel ligands: a patent overview (2005 – 2010)

Abstract

Introduction: ATP-sensitive potassium channels are important metabolic regulators that link cellular metabolism to excitability. Their wide distribution in various tissues and organs makes them significant and topical targets in a large number of diseases.

Areas covered: This review summarizes the current understanding of the molecular biology and pharmacology of K_ATP channels, and the pathological states that result from aberrant expression or function of these proteins. In particular, relevant research, patents and patent applications of the past 5 years are discussed.

Expert opinion: The tissue-specific K_ATP channel modulation reflects an early discovery stage in drug design. The wide distribution of K_ATP channels lets us consider them as valid targets for several pathologies, but on other hand the ubiquitous nature is a relevant drawback in developing an effective therapy because of the onset of side effects related to the lack of selectivity. On this basis, further investigations on both the structures and the localization of each receptor subtype should be carried out either exploring the structure–activity relationship of the already existing K_ATP ligands or developing new selective fluorescent probes. To date, this research area still strives to design new tissue-targeted ligands that could pave the way to the development of innovative and effective drugs for clinical use.

Keywords::

• ATP-sensitive potassium channel
• K_ATP blocker
• K_ATP channel ligands
• K_ATP channel modulator
• KCOs
• mito-K_ATP channel opener

Notes

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