Ontology highlight
ABSTRACT:
SUBMITTER: Khan S
PROVIDER: S-EPMC6898785 | biostudies-literature | 2019 Dec
REPOSITORIES: biostudies-literature
Nature medicine 20191202 12
B-cell lymphoma extra large (BCL-X<sub>L</sub>) is a well-validated cancer target. However, the on-target and dose-limiting thrombocytopenia limits the use of BCL-X<sub>L</sub> inhibitors, such as ABT263, as safe and effective anticancer agents. To reduce the toxicity of ABT263, we converted it into DT2216, a BCL-X<sub>L</sub> proteolysis-targeting chimera (PROTAC), that targets BCL-X<sub>L</sub> to the Von Hippel-Lindau (VHL) E3 ligase for degradation. We found that DT2216 was more potent again ...[more]