Fluorescent molecular rotors as sensors for the detection of thymidine phosphorylase.

Bioorg Med Chem

CNR - Istituto per i Sistemi Biologici, Via Salaria km 29.300, 00016 Monterotondo Scalo (RM), Italy.

Published: January 2021

AI Article Synopsis

  • Three new fluorescent molecular rotors were created to detect thymidine phosphorylase, a key enzyme affected by the chemotherapy drug 5-fluorouracil used in treating solid tumors.
  • The optimal dosage of 5-fluorouracil is critical since it varies among patients, highlighting the need for a quick and simple method to measure enzyme levels.
  • The rotors differ in the length of their alkylic spacer, and their ability to emit a fluorescent signal when interacting with thymidine phosphorylase was tested through various fluorescent measurements.

Article Abstract

Three new fluorescent molecular rotors were synthesized with the aim of using them as sensors to dose thymidine phosphorylase, one of the target enzymes of 5-fluorouracil, a potent chemotherapic drug largely used in the treatment of many solid tumors, that acts by hindering the metabolism of pyrimidines. 5-Fluorouracil has a very narrowtherapeutic window, in fact, its optimal dosage is strictly related to the level of its target enzymes that vary significantly among patients, and it would be of the utmost importance to have an easy and fast method to detect and quantify them. The three molecular rotors developed as TP sensors differ in the length of the alkylic spacer joining the ligand unit, a thymine moiety, and the fluorescent molecular rotor, a [4-(1-dimethylamino)phenyl]-pyridinium bromide. Their ability to trigger an optical signal upon the interaction with thymidine phosphorylase was investigated by fluorescent measurements.

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Source
http://dx.doi.org/10.1016/j.bmc.2020.115881DOI Listing

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