1. CDK12/13 dual inhibitors are potential therapeutics for acute myeloid leukemia.
- Author
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Savoy, Lindsey, Long, Nicola, Lee, Hyunjung, Chen, Reid, Allen, Basil, Lin, Hsin‐Yun, Tognon, Cristina, V. Malhotra, Sanjay, Tyner, Jeffrey W., and Zhang, Haijiao
- Subjects
ACUTE myeloid leukemia ,THERAPEUTICS ,GENE expression ,DNA repair ,OVARIAN cancer ,PROTEIN kinases ,CYCLIN-dependent kinases ,SERINE/THREONINE kinases ,PROSTATE cancer - Abstract
Interestingly, THZ531 area under the curve (AUC) values exhibited a strong negative correlation with Venetoclax (Figure 1C), suggesting that CDK12/CDK13 inhibitors may be effective in the cases refractory/resistant to Venetoclax-based treatments. Strikingly, THZ531 and SR-4835 were sensitive in all three samples tested (Figure 1F), further validating that CDK12/CDK13 inhibitors can overcome Venetoclax resistance. The presented data highlights the contrasting sensitivities of THZ531 and Venetoclax in leukaemia samples and proposes the potential of THZ531 to overcome drug resistance associated with Venetoclax-based therapy. [Extracted from the article]
- Published
- 2023
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