FLTX2: A Novel Tamoxifen Derivative Endowed with Antiestrogenic, Fluorescent, and Photosensitizer Properties

  1. Canerina-Amaro, Ana
  2. Mesa-Herrera, Fátima 1
  3. Lobo, Fernando 1
  4. Lahoz, Fernando 1
  5. Hernández, Dácil
  6. Marín, Raquel 1
  7. Estévez-Braun, Ana 1
  8. Díaz, Mario
  9. Valdés-Baizabal, Catalina 1
  10. Soler, Kevin 1
  11. Boto, Alicia
  12. Amesty, Ángel 1
  1. 1 Universidad de La Laguna
    info

    Universidad de La Laguna

    San Cristobal de La Laguna, España

    GRID grid.10041.34

Journal:
International Journal of Molecular Sciences

ISSN: 1422-0067

Year of publication: 2021

Volume: 22

Issue: 10

Pages: 5339

Type: Article

Export: RIS
DOI: 10.3390/ijms22105339 GOOGLE SCHOLAR lock_openOpen access editor
Author's full text: lockOpen access editor

Metrics

Cited by

  • Scopus Cited by: 0 (13-10-2021)

JCR (Journal Impact Factor)

(Indicator corresponding to the last year available on this portal, year 2020)
  • Year 2020
  • Journal Impact Factor: 5.923
  • Best Quartile: Q1
  • Area: BIOCHEMISTRY & MOLECULAR BIOLOGY Quartile: Q1 Rank in area: 67/297 (Ranking edition: SCIE)
  • Area: CHEMISTRY, MULTIDISCIPLINARY Quartile: Q2 Rank in area: 49/178 (Ranking edition: SCIE)

SCImago Journal Rank

(Indicator corresponding to the last year available on this portal, year 2020)
  • Year 2020
  • SJR Journal Impact: 1.455
  • Best Quartile: Q1
  • Area: Computer Science Applications Quartile: Q1 Rank in area: 62/2196
  • Area: Inorganic Chemistry Quartile: Q1 Rank in area: 6/68
  • Area: Medicine (miscellaneous) Quartile: Q1 Rank in area: 271/2448
  • Area: Organic Chemistry Quartile: Q1 Rank in area: 15/179
  • Area: Physical and Theoretical Chemistry Quartile: Q1 Rank in area: 16/167
  • Area: Spectroscopy Quartile: Q1 Rank in area: 5/78
  • Area: Catalysis Quartile: Q2 Rank in area: 17/60
  • Area: Molecular Biology Quartile: Q2 Rank in area: 131/402

CiteScore

(Indicator corresponding to the last year available on this portal, year 2020)
  • Year 2020
  • CiteScore of the Journal : 5.7
  • Area: Inorganic Chemistry Percentile: 83
  • Area: Spectroscopy Percentile: 79
  • Area: Computer Science Applications Percentile: 78
  • Area: Physical and Theoretical Chemistry Percentile: 78
  • Area: Organic Chemistry Percentile: 77
  • Area: Molecular Biology Percentile: 61
  • Area: Catalysis Percentile: 55

Journal Citation Indicator (JCI)

(Indicator corresponding to the last year available on this portal, year 2020)
  • Year 2020
  • Journal Citation Indicator (JCI): 0.71
  • Best Quartile: Q2
  • Area: BIOCHEMISTRY & MOLECULAR BIOLOGY Quartile: Q2 Rank in area: 157/311
  • Area: CHEMISTRY, MULTIDISCIPLINARY Quartile: Q2 Rank in area: 65/218

Abstract

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.

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