DHFR Inhibitors: Reading the Past for Discovering Novel Anticancer Agents
| Autor: | Daniela Rossi, Ornella Randazzo, Elisa Vignoni, Giampaolo Barone, Simona Collina, Mery La Franca, Maria Valeria Raimondi |
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| Přispěvatelé: | Raimondi, Maria Valeria, Randazzo, Ornella, Franca, Mery La, Barone, Giampaolo, Vignoni, Elisa, Rossi, Daniela, Collina, Simona |
| Rok vydání: | 2019 |
| Předmět: |
Antifungal
Cancer chemotherapy medicine.drug_class Drug Evaluation Preclinical dihydrofolate reductase (DHFR) enzyme Pharmaceutical Science Antineoplastic Agents Computational biology Review 01 natural sciences hybrid compounds Analytical Chemistry lcsh:QD241-441 03 medical and health sciences Structure-Activity Relationship Folic Acid lcsh:Organic chemistry heterocyclic compounds Neoplasms Dihydrofolate reductase parasitic diseases Drug Discovery medicine Animals Humans Physical and Theoretical Chemistry 030304 developmental biology 0303 health sciences Heterocyclic compound biology 010405 organic chemistry Drug discovery Organic Chemistry DHFR inhibitors as anticancer agent Settore CHIM/08 - Chimica Farmaceutica 0104 chemical sciences DHFR drug discovery Tetrahydrofolate Dehydrogenase Mechanism of action Chemistry (miscellaneous) Settore CHIM/03 - Chimica Generale E Inorganica DHFR inhibitors as anticancer agents biology.protein Molecular Medicine Folic Acid Antagonists medicine.symptom |
| Zdroj: | Molecules Molecules, Vol 24, Iss 6, p 1140 (2019) |
| ISSN: | 1420-3049 |
| Popis: | Dihydrofolate reductase inhibitors are an important class of drugs, as evidenced by their use as antibacterial, antimalarial, antifungal, and anticancer agents. Progress in understanding the biochemical basis of mechanisms responsible for enzyme selectivity and antiproliferative effects has renewed the interest in antifolates for cancer chemotherapy and prompted the medicinal chemistry community to develop novel and selective human DHFR inhibitors, thus leading to a new generation of DHFR inhibitors. This work summarizes the mechanism of action, chemical, and anticancer profile of the DHFR inhibitors discovered in the last six years. New strategies in DHFR drug discovery are also provided, in order to thoroughly delineate the current landscape for medicinal chemists interested in furthering this study in the anticancer field. |
| Databáze: | OpenAIRE |
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