| Autor: |
Sabin Llona-Minguez, Annika Jenmalm Jensen, Artin Ghassemian, Shabnam Fayezi, José Manuel Calderón-Montaño, André Mateus, Thomas Helleday, Cindy Cazares-Körner, Matthieu Desroses, Elisee Wiita, Masoud Darabi, Pawel Baranczewski, Tobias Koolmeister, Ann-Sofie Jemth, Amir Mehdizadeh, Olga Loseva, Per Artursson, Estefanía Burgos Morón, Martin Scobie, Ulrika Warpman Berglund, Kristmundur Sigmundsson, Evert Homan, Ingrid Almlöf, Nicholas C.K. Valerie, Andreas Höglund, Kumar Sanjiv, Thomas Lundbäck |
| Rok vydání: |
2017 |
| Předmět: |
|
| Zdroj: |
Journal of Medicinal Chemistry. 60:4279-4292 |
| ISSN: |
1520-4804
0022-2623 |
| Popis: |
The dCTP pyrophosphatase 1 (dCTPase) is a nucleotide pool "housekeeping" enzyme responsible for the catabolism of canonical and noncanonical nucleoside triphosphates (dNTPs) and has been associated with cancer progression and cancer cell stemness. We have identified a series of piperazin-1-ylpyridazines as a new class of potent dCTPase inhibitors. Lead compounds increase dCTPase thermal and protease stability, display outstanding selectivity over related enzymes and synergize with a cytidine analogue against leukemic cells. This new class of dCTPase inhibitors lays the first stone toward the development of drug-like probes for the dCTPase enzyme. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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