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Synthesis and pharmacological characterization of mitochondrial K

Authors :
Lara, Testai
Simona, Sestito
Alma, Martelli
Era, Gorica
Lorenzo, Flori
Vincenzo, Calderone
Simona, Rapposelli
Source :
Bioorganic chemistry. 107
Publication Year :
2020

Abstract

Mitochondria play a key role for deciding fate of cells and thus are considered an attractive target for pharmacological interventions focused on containment of myocardial ischemia/reperfusion (I/R) injury. Notably, the activation of mitochondrial potassium (mitoK) channels produces a mild depolarization of mitochondrial membrane, that contributes to reduce the driving force to calcium uptake and prevents the formation of mitochondrial transition membrane pore (MPTP); these events underlie anti-ischemic cardioprotection. However, an ideal mitoK channel opener should possess the fundamental requirement to be delivered at mitochondrial level; therefore, to improve the mitochondrial delivery of a previously characterized spirocyclic benzopyrane F81, new compounds have been developed. The three original triphenylphosphonium (TPP

Details

ISSN :
10902120
Volume :
107
Database :
OpenAIRE
Journal :
Bioorganic chemistry
Accession number :
edsair.pmid..........bedaa5da759ac252cc05736f8be87b79