Novel adenosine 5'-triphosphate-sensitive potassium channel ligands: a patent overview (2005-2010).
BACKGROUND
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.


METHODS
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.


CONCLUSIONS
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.
Dipartimento di Scienze Farmaceutiche - Università di Pisa, Via Bonanno, 6, 56126 Pisa, Italy. simona.rapposelli@farm.unipi.it
Simona
S
Rapposelli
D000818:Animals; D019610:Cytoprotection; D003920:Diabetes Mellitus / Q000188:drug therapy; D006801:Humans; D054086:KATP Channels / Q000037:antagonists & inhibitors / Q000187:drug effects* / Q000502:physiology; D008024:Ligands; D009131:Muscle, Smooth, Vascular / Q000187:drug effects / Q000502:physiology; D032383:Myocytes, Cardiac / Q000502:physiology; D009765:Obesity / Q000188:drug therapy; D010179:Pancreas / Q000502:physiology; D010330:Patents as Topic
D054086:KATP Channels; D008024:Ligands