Structure-guided design of 7-azaindole DNMT1 inhibitors active against hypomethylating agent-resistant acute myeloid leukemia.
New drugs designed to overcome resistance in hard-to-treat leukemia showed activity in lab models, addressing a major clinical challenge.
Scientists designed new drugs that selectively block the DNMT1 enzyme, overcoming resistance to existing hypomethylating agents in AML. These 7-azaindole compounds showed activity against treatment-resistant AML in laboratory models, addressing a major clinical challenge.
What the study was
- Study design
- Preclinical (structure-guided drug design, in vitro and in vivo models)
- Population
- HMA-resistant AML cell lines and models
- Category
- Drug Development
- Maturity
- Exploratory
- Journal
- Proceedings of the National Academy of Sciences of the United States of America
Why it surfaced
Novel selective DNMT1 inhibitors for HMA-resistant AML published in PNAS. High novelty but preclinical only.
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