Bifunctional degraders of BRPF1 that retain the antiproliferative phenotype

Utilizing our Integrated Drug Discovery Platform consisting of in-house PROTAC synthetic capabilities, ability in PROTAC ADME characterization, and biological screening capabilities in haematological malignancies, we disclose our initial investigations into the role of BRPF1 in Acute Myeloid Leukemia (AML). We have designed a series of BRPF1 PROTACs to test the hypothesis that small-molecule degraders of BRPF1 will have profound antiproliferative effects in AML cell lines that harbor MLL translocations. In addition to their potential as new medicines, PROTACs are a powerful tool in the arsenal of techniques available for target validation.

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