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Apoptosis Therapy in Cancer: The First Single-molecule Co-activating p53 and the Translocator Protein in Glioblastoma.

Al's Comment:

 Exciting approach. Not done in people yet, but I will be watching this one.

Posted on: 04/26/2014

Sci Rep. 2014 Apr 23;4:4749. doi: 10.1038/srep04749.
Apoptosis Therapy in Cancer: The First Single-molecule Co-activating p53 and the Translocator Protein in Glioblastoma.
Daniele S1, Taliani S1, Da Pozzo E1, Giacomelli C1, Costa B1, Trincavelli ML1, Rossi L2, La Pietra V3, Barresi E1, Carotenuto A3, Limatola A3, Lamberti A4, Marinelli L3, Novellino E3, Da Settimo F1, Martini C1.
Author information: 
1Department of Pharmacy, University of Pisa, Pisa, Italy.
2Department of Clinical and Experimental Medicine, University of Pisa, Italy.
3Department of Pharmacy, University of Naples Federico II, Italy.
4Dipartimento di Scienze Motorie, University of Naples "Parthenope", Naples, Italy.
In the complex scenario of cancer, treatment with compounds targeting multiple cell pathways has been emerging. In Glioblastoma Multiforme (GBM), p53 and Translocator Protein (TSPO), both acting as apoptosis inducers, represent two attractive intracellular targets. On this basis, novel indolylglyoxylyldipeptides, rationally designed to activate TSPO and p53, were synthesized and biologically characterized. The new compounds were able to bind TSPO and to reactivate p53 functionality, through the dissociation from its physiological inhibitor, murine double minute 2 (MDM2). In GBM cells, the new molecules caused Δψm dissipation and inhibition of cell viability. These effects resulted significantly higher with respect to those elicited by the single target reference standards applied alone, and coherent with the synergism resulting from the simultaneous activation of TSPO and p53. Taken together, these results suggest that TSPO/MDM2 dual-target ligands could represent a new attractive multi-modal opportunity for anti-cancer strategy in GBM. 
 PMID: 24756113 [PubMed - in process] 
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