Abstract
Since the discovery of antitumor activity of cisplatin in the late 60's, the development of metal-based drugs has had an enormous burst with the aim of to increase the anti-cancer activity, lower side effects and promote specific accumulation to the target cells or organs. Indeed, a new discipline, called medicinal inorganic chemistry, has born where metal ions play a fundamental role. This review provides a comprehensive overview of various metal complexes targeting the Translocator Protein (TSPO), an 18 kDa high affinity cholesterol- and drug-binding protein found mostly in the outer mitochondrial membrane and formerly known as peripheral-type benzodiazepine receptor. TSPO distribution in healthy tissues varies considerably; in contrast, aberrant expression of TSPO has been noted in several pathological specimens including neurodegenerative diseases and cancers. These findings suggest that TSPO-targeted therapy and imaging may have utility in the treatment and visualization of diseases expressing high density of TSPO. In this review, potential applications in cancer diagnosis and therapy will be discussed.
| Original language | English |
|---|---|
| Pages (from-to) | 1-18 |
| Number of pages | 18 |
| Journal | Coordination Chemistry Reviews |
| Volume | 341 |
| DOIs | |
| Publication status | Published - Jun 15 2017 |
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Keywords
- Diagnosis
- Metal complexes
- Peripheral Benzodiazepine Receptor
- Therapy
- Translocator Protein 18 kDa
- TSPO
ASJC Scopus subject areas
- Chemistry(all)
Cite this
Metal complexes targeting the Translocator Protein 18 kDa (TSPO). / Denora, Nunzio; Iacobazzi, Rosa Maria; Natile, Giovanni; Margiotta, Nicola.
In: Coordination Chemistry Reviews, Vol. 341, 15.06.2017, p. 1-18.Research output: Contribution to journal › Review article
}
TY - JOUR
T1 - Metal complexes targeting the Translocator Protein 18 kDa (TSPO)
AU - Denora, Nunzio
AU - Iacobazzi, Rosa Maria
AU - Natile, Giovanni
AU - Margiotta, Nicola
PY - 2017/6/15
Y1 - 2017/6/15
N2 - Since the discovery of antitumor activity of cisplatin in the late 60's, the development of metal-based drugs has had an enormous burst with the aim of to increase the anti-cancer activity, lower side effects and promote specific accumulation to the target cells or organs. Indeed, a new discipline, called medicinal inorganic chemistry, has born where metal ions play a fundamental role. This review provides a comprehensive overview of various metal complexes targeting the Translocator Protein (TSPO), an 18 kDa high affinity cholesterol- and drug-binding protein found mostly in the outer mitochondrial membrane and formerly known as peripheral-type benzodiazepine receptor. TSPO distribution in healthy tissues varies considerably; in contrast, aberrant expression of TSPO has been noted in several pathological specimens including neurodegenerative diseases and cancers. These findings suggest that TSPO-targeted therapy and imaging may have utility in the treatment and visualization of diseases expressing high density of TSPO. In this review, potential applications in cancer diagnosis and therapy will be discussed.
AB - Since the discovery of antitumor activity of cisplatin in the late 60's, the development of metal-based drugs has had an enormous burst with the aim of to increase the anti-cancer activity, lower side effects and promote specific accumulation to the target cells or organs. Indeed, a new discipline, called medicinal inorganic chemistry, has born where metal ions play a fundamental role. This review provides a comprehensive overview of various metal complexes targeting the Translocator Protein (TSPO), an 18 kDa high affinity cholesterol- and drug-binding protein found mostly in the outer mitochondrial membrane and formerly known as peripheral-type benzodiazepine receptor. TSPO distribution in healthy tissues varies considerably; in contrast, aberrant expression of TSPO has been noted in several pathological specimens including neurodegenerative diseases and cancers. These findings suggest that TSPO-targeted therapy and imaging may have utility in the treatment and visualization of diseases expressing high density of TSPO. In this review, potential applications in cancer diagnosis and therapy will be discussed.
KW - Diagnosis
KW - Metal complexes
KW - Peripheral Benzodiazepine Receptor
KW - Therapy
KW - Translocator Protein 18 kDa
KW - TSPO
UR - http://www.scopus.com/inward/record.url?scp=85017146989&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=85017146989&partnerID=8YFLogxK
U2 - 10.1016/j.ccr.2017.03.023
DO - 10.1016/j.ccr.2017.03.023
M3 - Review article
VL - 341
SP - 1
EP - 18
JO - Coordination Chemistry Reviews
JF - Coordination Chemistry Reviews
SN - 0010-8545
ER -