Publications by authors named "Ethan Whipp"
Acute myeloid leukemia (AML) is a highly aggressive hematologic cancer with poor survival across a broad range of molecular subtypes. Development of efficacious and well-tolerable therapies encompassing the range of mutations that can arise in AML remains an unmet need. The bromo- and extra-terminal domain (BET) family of proteins represents an attractive therapeutic target in AML due to their crucial roles in many cellular functions, regardless of any specific mutation.
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- Richter's Transformation (RT) is a dangerous progression of chronic lymphocytic leukemia (CLL) that appears as diffuse large B-cell lymphoma, with a key role suspected for protein arginine methyltransferase 5 (PRMT5).
- Research shows that PRMT5 is consistently overexpressed in patients developing RT and that mice with increased levels of PRMT5 face a higher death risk and develop aggressive B-cell diseases similar to RT.
- The study also introduces PRT382, a new and selective inhibitor of PRMT5, suggesting its potential for targeted treatment in aggressive cases of CLL and RT, highlighting the need for clinical trials.
Chronic lymphocytic leukemia (CLL) is effectively treated with targeted therapies including Bruton tyrosine kinase inhibitors and BCL2 antagonists. When these become ineffective, treatment options are limited. Positive transcription elongation factor complex (P-TEFb), a heterodimeric protein complex composed of cyclin dependent kinase 9 (CDK9) and cyclin T1, functions to regulate short half-life transcripts by phosphorylation of RNA Polymerase II (POLII).
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