Potent and selective chemical probe of hypoxic signalling downstream of HIF-α hydroxylation via VHL inhibition

Potent and selective chemical probe of hypoxic signalling downstream of HIF-α hydroxylation via VHL inhibition

Small molecule probes used to trigger hypoxic response by activating hypoxia inducible factors (HIFs) often lack specificity. Here the authors report a potent small molecule inhibitor that induces hypoxic response by blocking VHL:HIF interactions, providing a selective route to probe hypoxic signall...

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Detalles Bibliográficos
Autores principales: Julianty Frost, Carles Galdeano, Pedro Soares, Morgan S. Gadd, Katarzyna M. Grzes, Lucy Ellis, Ola Epemolu, Satoko Shimamura, Marcus Bantscheff, Paola Grandi, Kevin D. Read, Doreen A. Cantrell, Sonia Rocha, Alessio Ciulli
Formato: article
Lenguaje:EN
Publicado: Nature Portfolio 2016
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Science
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Acceso en línea:https://doaj.org/article/3040359d09be44dd8ac2502767cf24e9
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Sumario:Small molecule probes used to trigger hypoxic response by activating hypoxia inducible factors (HIFs) often lack specificity. Here the authors report a potent small molecule inhibitor that induces hypoxic response by blocking VHL:HIF interactions, providing a selective route to probe hypoxic signalling.

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