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MR Molecular Imaging of Prostate Cancer with a Small Molecular CLT1 Peptide Targeted Contrast Agent
Published on: September 3, 2013
Prospects for prostate cancer imaging and therapy using high-affinity TRPM8 activators
Benjamin Beck1, Gabriel Bidaux, Alexis Bavencoffe
1Inserm, U800, Equipe Labellisée par la Ligue Contre le Cancer, Villeneuve d'Ascq F-59650, France.
Cell Calcium
|September 5, 2006
Summary
Researchers identified novel, high-affinity ligands for the TRPM8 channel, a key player in prostate cancer. One compound, WS-12, shows significantly greater affinity than menthol, offering potential for cancer diagnosis and therapy.
Area of Science:
- Molecular biology
- Pharmacology
- Oncology
Background:
- Transient receptor potential melastatin 8 (TRPM8) channels are activated by cold and cooling agents.
- TRPM8 is implicated in prostate cancer pathophysiology, with increased expression and involvement in apoptosis.
- TRPM8 serves as a potential tumor marker and therapeutic target for prostate cancer.
Purpose of the Study:
- To investigate the action of "WS" compounds on TRPM8 channels.
- To identify novel TRPM8-specific ligands with high affinity.
- To compare the affinity of new ligands to menthol and icilin.
Main Methods:
- Screening of "WS" compounds for TRPM8 channel activity.
- Affinity comparison of identified ligands with menthol and icilin.
- Assessment of a fluorinated WS-12 analog's activity.
Main Results:
- Identification of new TRPM8 agonists from the "WS" compound series.
- WS-12 demonstrated significantly higher affinity than menthol (EC50 approx. 2000 times lower).
- A fluorinated WS-12 derivative retained 75% of the parent compound's activity.
Conclusions:
- WS-12 is the highest-affinity TRPM8 ligand identified to date.
- Novel TRPM8 ligands hold potential for prostate cancer diagnosis and therapy.
- Radiohalogen incorporation into these ligands could facilitate imaging and treatment strategies.
