Molecular Targets of Minor Cannabinoids in Breast Cancer: In Silico and In Vitro Studies

• Type: Article in International Scientific Journal
• Date: 2024

Authors

Almeida, CF (Author) Other; Palmeira, A (Author) FFUP; Valente, MJ (Author) Other; Georgina Correia da Silva (Author) FFUP; Vinggaard, AM (Author) Other; Emilia Sousa (Author) FFUP; Teixeira, N (Author) Other; Amaral, C (Author) Other

Journal

Title: Pharmaceuticals

Vol. 17

Final page: 1245

ISSN: 1424-8247

Publisher: MDPI

Indexing

ISI Web of Knowledge - 0 Citations

Scopus - 0 Citations

Other information

Authenticus ID: P-017-4EN

DOI: 10.3390/ph17091245

Abstract (EN): Background: Breast cancer therapy has been facing remarkable changes. Classic treatments are now combined with other therapies to improve efficacy and surpass resistance. Indeed, the emergence of resistance demands the development of novel therapeutic approaches. Due to key estrogen signaling, estrogen receptor-positive (ER+) breast cancer treatment has always been focused on aromatase inhibition and ER modulation. Lately, the effects of phytocannabinoids, mainly Delta 9-tetrahydrocannabinol (THC) and cannabidiol (CBD), have been evaluated in different cancers, including breast. However, Cannabis sativa contains more than 120 phytocannabinoids less researched and understood. Methods: Here, we evaluated, both in silico and in vitro, the ability of 129 phytocannabinoids to modulate important molecular targets in ER+ breast cancer: aromatase, ER, and androgen receptor (AR). Results: In silico results suggested that some cannabinoids may inhibit aromatase and act as ER alpha antagonists. Nine selected cannabinoids showed, in vitro, potential to act either as ER antagonists with inverse agonist properties, or as ER agonists. Moreover, these cannabinoids were considered as weak aromatase inhibitors and AR antagonists with inverse agonist action. Conclusions: Overall, we present, for the first time, a comprehensive analysis of the actions of the phytocannabinoids in targets of ER+ breast tumors, pointing out their therapeutic potential in cancer and in other diseases.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 31