| Autor: |
Oliva MA, Prota AE, Rodríguez-Salarichs J, Gu W, Bennani YL, Jimenez-Barbero J, Bargsten K, Canales A, Steinmetz MO, Diaz JF |
| Jazyk: |
angličtina |
| Rok vydání: |
2020 |
| Předmět: |
|
| Popis: |
Noscapineisanaturalalkaloidthatisusedasanantitussivemedicine.However,italsoactsasaweakanticanceragentincertaininvivomodelsthroughamechanismthatislargelyunknown.Here,weperformedstructuralstudiesandshowthatthecytotoxicagent7A-O-demethoxy-amino-noscapine(7A-aminonoscapine)bindstothecolchicinesiteoftubulin.Wesuggestthatthe7A-methoxygroupofnoscapinepreventsbindingtotubulinduetoastericclashofthecompoundwiththeT5-loopofa-tubulin.Wefurtherproposethattheanticanceractivityofnoscapinearisesfromabioactivemetabolitethatbindstothecolchicinesiteoftubu-lintoinducemitoticarrestthroughamicrotubulecytoskeleton-basedmechanism. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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