Title : A Nimbolide-Based Kinase Degrader Preferentially Degrades Oncogenic BCR-ABL.

Pub. Date : 2020 Jul 17

PMID : 32568522






5 Functional Relationships(s)
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1 A Nimbolide-Based Kinase Degrader Preferentially Degrades Oncogenic BCR-ABL. nimbolide ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens
2 We demonstrate that a PROTAC linking nimbolide to the kinase and BCR-ABL fusion oncogene inhibitor dasatinib, BT1, selectively degrades BCR-ABL over c-ABL in leukemia cancer cells, compared to previously reported cereblon or VHL-recruiting BCR-ABL degraders that show opposite selectivity or in some cases inactivity. nimbolide ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens
3 We demonstrate that a PROTAC linking nimbolide to the kinase and BCR-ABL fusion oncogene inhibitor dasatinib, BT1, selectively degrades BCR-ABL over c-ABL in leukemia cancer cells, compared to previously reported cereblon or VHL-recruiting BCR-ABL degraders that show opposite selectivity or in some cases inactivity. nimbolide ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens
4 We demonstrate that a PROTAC linking nimbolide to the kinase and BCR-ABL fusion oncogene inhibitor dasatinib, BT1, selectively degrades BCR-ABL over c-ABL in leukemia cancer cells, compared to previously reported cereblon or VHL-recruiting BCR-ABL degraders that show opposite selectivity or in some cases inactivity. nimbolide ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens
5 We demonstrate that a PROTAC linking nimbolide to the kinase and BCR-ABL fusion oncogene inhibitor dasatinib, BT1, selectively degrades BCR-ABL over c-ABL in leukemia cancer cells, compared to previously reported cereblon or VHL-recruiting BCR-ABL degraders that show opposite selectivity or in some cases inactivity. nimbolide ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens