TY  - JOUR
AU  - Canerina-Amaro, Ana
AU  - Mesa-Herrera, Fátima
AU  - Lobo, Fernando
AU  - Lahoz, Fernando
AU  - Hernández, Dácil
AU  - Marín, Raquel
AU  - Estévez-Braun, Ana
AU  - Díaz, Mario
AU  - Valdés-Baizabal, Catalina
AU  - Soler, Kevin
AU  - Boto, Alicia
AU  - Amesty, Ángel
KW  - Physical and Theoretical Chemistry
KW  - Inorganic Chemistry
KW  - Organic Chemistry
KW  - Spectroscopy
KW  - Molecular Biology
KW  - Catalysis
KW  - General Medicine
KW  - Computer Science Applications
T1  - FLTX2: A Novel Tamoxifen Derivative Endowed with Antiestrogenic, Fluorescent, and Photosensitizer Properties
LA  - eng
PY  - 2021
SP  - 5339
T2  - International Journal of Molecular Sciences
SN  - 1422-0067
VL  - 22
IS  - 10
AB  - Tamoxifen is the most widely used selective modulator of estrogen receptors (SERM) and the first strategy as coadjuvant therapy for the treatment of estrogen-receptor (ER) positive breast cancer worldwide. In spite of such success, tamoxifen is not devoid of undesirable effects, the most life-threatening reported so far affecting uterine tissues. Indeed, tamoxifen treatment is discouraged in women under risk of uterine cancers. Recent molecular design efforts have endeavoured the development of tamoxifen derivatives with antiestrogen properties but lacking agonistic uterine tropism. One of this is FLTX2, formed by the covalent binding of tamoxifen as ER binding core, 7-nitrobenzofurazan (NBD) as the florescent dye, and Rose Bengal (RB) as source for reactive oxygen species. Our analyses demonstrate (1) FLTX2 is endowed with similar antiestrogen potency as tamoxifen and its predecessor FLTX1, (2) shows a strong absorption in the blue spectral range, associated to the NBD moiety, which efficiently transfers the excitation energy to RB through intramolecular FRET mechanism, (3) generates superoxide anions in a concentration- and irradiation time-dependent process, and (4) Induces concentration- and time-dependent MCF7 apoptotic cell death. These properties make FLTX2 a very promising candidate to lead a novel generation of SERMs with the endogenous capacity to promote breast tumour cell death in situ by photosensitization.
DO  - 10.3390/IJMS22105339
UR  - https://portalciencia.ull.es/documentos/60af74e6a47315441ba63fb2
DP  - Dialnet - Portal de la Investigación
ER  -