Litcius/Paper detail

Targeting the Translocator Protein (18 kDa) in Cardiac Diseases: State of the Art and Future Opportunities

Emma Baglini, Valeria Poggetti, Chiara Cavallini, Debora Petroni, Francesca Forini, Giuseppina Nicolini, Elisabetta Barresi, Silvia Salerno, Barbara Costa, Patricia Iozzo, Danilo Neglia, Luca Menichetti, Sabrina Taliani, Federico Da Settimo

2023Journal of Medicinal Chemistry11 citationsDOIOpen Access PDF

Abstract

Mitochondria dysfunctions are typical hallmarks of cardiac disorders (CDs). The multiple tasks of this energy-producing organelle are well documented, but its pathophysiologic involvement in several manifestations of heart diseases, such as altered electromechanical coupling, excitability, and arrhythmias, is still under investigation. The human 18 kDa translocator protein (TSPO) is a protein located on the outer mitochondrial membrane whose expression is altered in different pathological conditions, including CDs, making it an attractive therapeutic and diagnostic target. Currently, only a few TSPO ligands are employed in CDs and cardiac imaging. In this Perspective, we report an overview of the emerging role of TSPO at the heart level, focusing on the recent literature concerning the development of TSPO ligands used for fighting and imaging heart-related disease conditions. Accordingly, targeting TSPO might represent a successful strategy to achieve novel therapeutic and diagnostic strategies to unravel the fundamental mechanisms and to provide solutions to still unanswered questions in CDs.

Topics & Concepts

Translocator proteinMitochondrionNeuroscienceChemistryOrganelleDiseasePathologicalCell biologyBioinformaticsMedicinePathologyBiochemistryPsychologyBiologyNeuroinflammationMitochondrial Function and PathologyCardiac Ischemia and ReperfusionCardiac electrophysiology and arrhythmias