Is there any correlation between binding and functional effects at the translocator protein (TSPO) (18 kDa)?

Current Molecular Medicine
A M ScarfM Kassiou

Abstract

The translocator protein (TSPO) is a potential drug target for the treatment of CNS diseases, with TSPO ligands being able to modulate steroidogenesis, apoptosis, and cell proliferation. While there exist multiple TSPO binding sites, the nature of these sites--either overlapping or allosterically linked--remains largely uncharacterized. Furthermore, while evidence suggests that microglial activation and polymerization result in changes to TSPO binding sites, these changes are poorly understood. While current pharmacophoric models can be used to synthesize TSPO ligands with high affinity and selectivity, these models are unable to predict ligands with desirable functional effects. Better characterization of TSPO binding sites in health and disease may provide insight into particular sites which mediate promising therapeutic profiles, thus refining the TSPO pharmacophore.

Citations

Jan 12, 2016·Scientific Reports·Barbara CostaClaudia Martini
Nov 22, 2014·Apoptosis : an International Journal on Programmed Cell Death·Barbara CostaClaudia Martini
Jun 9, 2016·International Journal of Molecular Sciences·Leo VeenmanMoshe Gavish
Jul 2, 2016·International Journal of Molecular Sciences·Eleonora Da PozzoClaudia Martini
Apr 14, 2016·Biochemistry·Fei LiShelagh Ferguson-Miller

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