التفاصيل البيبلوغرافية
| العنوان: |
A photoswitchable antimetabolite for targeted photoactivated chemotherapy |
| المؤلفون: |
C. Matera, A. Gomila-Juaneda, N. Camarero, M. Libergoli, C. Soler, P. Gorostiza |
| المساهمون: |
C. Matera, A. Gomila-Juaneda, N. Camarero, M. Libergoli, C. Soler, P. Gorostiza |
| سنة النشر: |
2018 |
| المجموعة: |
The University of Milan: Archivio Istituzionale della Ricerca (AIR) |
| مصطلحات موضوعية: |
Settore CHIM/08 - Chimica Farmaceutica |
| الوصف: |
The efficacy and tolerability of systemically administered anticancer agents are limited by their off-target effects. Precise spatiotemporal control over their cytotoxic activity would allow improving chemotherapy treatments, and light-regulated drugs are well suited to this purpose. We have developed phototrexate, the first photoswitchable inhibitor of the human dihydrofolate reductase (DHFR), as a photochromic analog of methotrexate, a widely prescribed chemotherapeutic drug to treat cancer and psoriasis. Quantification of the light-regulated DHFR enzymatic activity, cell proliferation, and in vivo effects in zebrafish show that phototrexate behaves as a potent antifolate in its photoactivated cis configuration, and that it is nearly inactive in its dark-relaxed trans form. Thus, phototrexate constitutes a proof-of-concept to design light-regulated cytotoxic small molecules, and a step forward to develop targeted anticancer photochemotherapies with localized efficacy and reduced adverse effects.[1] Reference 1. Matera, C.; Gomila-Juaneda, A.; Camarero, N.; Libergoli, M.; Soler, C.; Gorostiza, P. J. Am. Chem. Soc., DOI:10.1021/jacs.8b08249. |
| نوع الوثيقة: |
conference object |
| اللغة: |
English |
| Relation: |
International Symposium on Photopharmacology (ISPP); http://hdl.handle.net/2434/770301 |
| الاتاحة: |
http://hdl.handle.net/2434/770301 |
| Rights: |
info:eu-repo/semantics/openAccess |
| رقم الانضمام: |
edsbas.CFD6C71B |
| قاعدة البيانات: |
BASE |