Targeting the Translocator Protein (18 kDa) in Cardiac Diseases: State of the Art and Future Opportunities.
Emma BagliniValeria PoggettiChiara CavalliniDebora PetroniFrancesca ForiniGiuseppina NicoliniElisabetta BarresiSilvia SalernoBarbara CostaPatricia IozzoDanilo NegliaLuca MenichettiSabrina TalianiFederico Da SettimoPublished in: Journal of medicinal chemistry (2023)
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.
Keyphrases
- quantum dots
- pet imaging
- heart failure
- left ventricular
- high resolution
- binding protein
- protein protein
- systematic review
- atrial fibrillation
- endothelial cells
- amino acid
- heat shock protein
- poor prognosis
- oxidative stress
- cancer therapy
- small molecule
- cell death
- computed tomography
- drug delivery
- room temperature
- fluorescence imaging
- transcranial direct current stimulation
- ionic liquid
- congenital heart disease