New potent and selective polyfluoroalkyl ketone inhibitors of GVIA calcium-independent phospholipase A₂
2013
Magrioti, Victoria | Nikolaou, Aikaterini | Smyrniotou, Annetta | Shah, Ishita | Constantinou-Kokotou, Violetta | Dennis, Edward A. | Kokotos, George
Group VIA calcium-independent phospholipase A₂ (GVIA iPLA₂) has recently emerged as an important pharmaceutical target. Selective and potent GVIA iPLA₂ inhibitors can be used to study its role in various neurological disorders. In the current work, we explore the significance of the introduction of a substituent in previously reported potent GVIA iPLA₂ inhibitors. 1,1,1,2,2-Pentafluoro-7-(4-methoxyphenyl)heptan-3-one (GK187) is the most potent and selective GVIA iPLA₂ inhibitor ever reported with a XI(50) value of 0.0001, and with no significant inhibition against GIVA cPLA₂ or GV sPLA₂. We also compare the inhibition of two difluoromethyl ketones on GVIA iPLA₂, GIVA cPLA₂, and GV sPLA₂.
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