The present invention concerns Glabrescione B and derivatives thereof that selectively inhibit the activity of the Hedgehog (Hh) pathway, and processes for their preparation. Compounds of the present invention are therefore useful in treating Hh-dependent tumors, such as medulloblastoma (MB), and many other cancers. The present invention also provides methods for the identification of compounds capable of binding and antagonizing the serpentine Smoothened (SMO)/Hh receptor and/or antagonizing Gli1-mediated transcription, which constitute the final step in the Hh pathway activation.
Multitarget hedgehog pathway inhibitors and uses thereof / Botta, Bruno; Gulino, Alberto; Botta, M.; Mori, M.; DI MARCOTULLIO, Lucia; Infante, P.; Ghirga, Francesca; Toscano, Sara; Ingallina, Cinzia; Alfonsi, Romina. - (2013).
Multitarget hedgehog pathway inhibitors and uses thereof
BOTTA, Bruno;GULINO, Alberto;DI MARCOTULLIO, LUCIA;P. Infante;GHIRGA, FRANCESCA;TOSCANO, SARA;INGALLINA, CINZIA;ALFONSI, ROMINA
2013
Abstract
The present invention concerns Glabrescione B and derivatives thereof that selectively inhibit the activity of the Hedgehog (Hh) pathway, and processes for their preparation. Compounds of the present invention are therefore useful in treating Hh-dependent tumors, such as medulloblastoma (MB), and many other cancers. The present invention also provides methods for the identification of compounds capable of binding and antagonizing the serpentine Smoothened (SMO)/Hh receptor and/or antagonizing Gli1-mediated transcription, which constitute the final step in the Hh pathway activation.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
