Chemotherapy is one of the most common treatments for cancer. However, its therapeutic potential is in many cases seriously unsatisfactory due to the nonspecific drug distribution and off-target effects. Innovative chemotherapeutic treatments based on nanomedicine can increase therapeutic efficiency while reducing side effects to normal tissues. One emerging approach is photopharmacology, which relies on light-controlled nanoscale changes in the structure of a drug to turn its pharmacological activity “on” and “off” on demand. We have designed and developed the first photoswitchable inhibitor of the human dihydrofolate reductase and named it Phototrexate. Preliminary studies in vitro and in zebrafish demonstrated that Phototrexate behaves as a potent antifolate after illumination with UVA light and that it is nearly inactive in its dark-relaxed form. Moreover, early safety screenings revealed that it can be considered reasonably safe for further studies in animal models of disease. Overall, Phototrexate is emerging as a new drug candidate towards the development of high precision photochemotherapy.

Precision Chemotherapy with a Photoswitchable Drug / C. Matera, N. Camarero, A. Gomila, M. Libergoli, C. Soler, P. Gorostiza - In: Firts CA17140 cost conference : Book of Abstracts[s.l] : COST, 2019. - pp. 92-92 (( convegno Cancer Nanomedicine : from the Bench to the Bedside tenutosi a Riga nel 2019.

Precision Chemotherapy with a Photoswitchable Drug

C. Matera;
2019

Abstract

Chemotherapy is one of the most common treatments for cancer. However, its therapeutic potential is in many cases seriously unsatisfactory due to the nonspecific drug distribution and off-target effects. Innovative chemotherapeutic treatments based on nanomedicine can increase therapeutic efficiency while reducing side effects to normal tissues. One emerging approach is photopharmacology, which relies on light-controlled nanoscale changes in the structure of a drug to turn its pharmacological activity “on” and “off” on demand. We have designed and developed the first photoswitchable inhibitor of the human dihydrofolate reductase and named it Phototrexate. Preliminary studies in vitro and in zebrafish demonstrated that Phototrexate behaves as a potent antifolate after illumination with UVA light and that it is nearly inactive in its dark-relaxed form. Moreover, early safety screenings revealed that it can be considered reasonably safe for further studies in animal models of disease. Overall, Phototrexate is emerging as a new drug candidate towards the development of high precision photochemotherapy.
Settore CHIM/08 - Chimica Farmaceutica
Settore BIO/14 - Farmacologia
European Cooperation in Science and Technology - COST Action CA17140 (Nano2Clinic)
https://www.nano2clinic.eu/sites/default/files/downloads/CA1740COnference_BOA_0.pdf
Book Part (author)
File in questo prodotto:
File Dimensione Formato  
CA1740COnference_BOA.pdf

accesso aperto

Tipologia: Publisher's version/PDF
Dimensione 7.99 MB
Formato Adobe PDF
7.99 MB Adobe PDF Visualizza/Apri
Pubblicazioni consigliate

Caricamento pubblicazioni consigliate

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/2434/861352
Citazioni
  • ???jsp.display-item.citation.pmc??? ND
  • Scopus ND
  • ???jsp.display-item.citation.isi??? ND
social impact