Fulvio Loiodice

TL;DR: The x-ray crystal structures of the PPARγ ligand binding domain complexed with the R- and the S-enantiomer shows that the different degree of stabilization of the helix 12 induced by the ligand determines its behavior as full or partial agonist.

TL;DR: The hypothesis that resveratrol and its metabolites control aspects of PPAR transcriptional activity through direct interaction with PPARs is addressed and it is proposed that res veratrol acts as a PPAR antagonist through its direct interactionwith PPARγ and PPARα.

TL;DR: The data allow the hypothesis that the chloride channel of skeletal muscle membrane could also have a stereospecific binding site (or receptor) regulating chloride ion flux, like other ion channels present in various biological systems.

TL;DR: Betulinic acid (BA), a compound already known for its anti-inflammatory, anti-tumour and antidiabetic properties, is identified as a PPARγ and PPARα antagonist and indicates a unique binding mode of this antagonist type.

TL;DR: Evaluation of the sensitivity of CLC-Ka to derivatives of NFA and FFA together with a modeling study of these ligands allow us to conclude that one major characteristic of activating compounds is the coplanarity of the two rings of the molecules, whereas block requires a noncoplanar configuration.