Premium
Bridging Pharmaceutical Chemistry with Drug and Nanoparticle Targeting to Investigate the Role of the 18‐kDa Translocator Protein TSPO
Author(s) -
Iacobazzi Rosa Maria,
Lopalco Antonio,
Cutrignelli Annalisa,
Laquintana Valentino,
Lopedota Angela,
Franco Massimo,
Denora Nunzio
Publication year - 2017
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201700322
Subject(s) - translocator protein , nanocarriers , mitochondrion , chemistry , mitochondrial permeability transition pore , drug delivery , drug , prodrug , biochemistry , microbiology and biotechnology , biophysics , biology , pharmacology , programmed cell death , apoptosis , medicine , disease , pathology , organic chemistry , neuroinflammation
An interesting mitochondrial biomarker is the 18‐kDa mitochondrial translocator protein (TSPO). Decades of study have shown that this protein plays an important role in a wide range of cellular functions, including opening of the mitochondrial permeability transition pore as well as programmed cell death and proliferation. Variations in TSPO expression have been correlated to different diseases, from tumors to endocrine and neurological disorders. TSPO has therefore become an appealing target for both early diagnosis and selective mitochondrial drug delivery. The number of structurally different TSPO ligands examined has increased over time, highlighting the scientific community′s growing understanding of the roles of TSPO in normal and pathological conditions. However, only few TSPO ligands are characterized by the presence of groups that are potentially derivatizable; therefore only few such ligands are well suited for the preparation of targeted prodrugs or nanocarriers able to deliver therapeutics and/or diagnostic agents to mitochondria. This review provides an overview of the very few examples of drug delivery systems characterized by moieties that target TSPO.