ACS Med. Chem. Lett. | PROTAC targeted FLT3 - ITD proteins: new therapy of acute myeloid leukemia

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Recently, Medicinal Chemistry in ACS by Nobumichi Ohoka and Mikihiko Naito of the National Institute of Health Sciences in Japan Letters jointly published a novel PROTAC depressant (CRBN(FLT3)-8) based on gilteritinib targeting Flt3-itD protein, which provides a new therapeutic idea for patients with acute myeloid leukemia.

1. Represents the molecule

2. Targets and indications
◆ Target: FLT3-ITD
◆ Potential indication: acute myeloid leukemia (AML)

3. Synthesis path

4. Biological activity

In vitro experiments showed that, compared with gilteritinib, CRBN(FLT3-8) could significantly inhibit the proliferation of FLT3-ITD mutant AML cells, and showed obvious targeted degradation of FLT3-ITD.

Reference materials:
Ohoka N, Suzuki M, Uchida T, et al. Development of Gilteritinib-Based Chimeric Small Molecules that Potently Induce Degradation of FLT3-ITD Protein[J]. ACS Med. Chem. Lett. 2022, 13(12): 1885-1891.
https://doi.org/10.1021/acsmedchemlett.2c00402

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About Meno
Suzhou Meinuo Pharmaceutical Technology Co., Ltd. is a platform enterprise focusing on small molecule drug CRO/CDMO. Founded in 2008, the company aims to provide global biopharmaceutical companies with integrated services from drug synthesis, structure optimization, process development, total quality research, pilot test to cGMP production. It has established deep strategic partnership with global 100+ biopharmaceutical companies. Minuo is one of the first companies to deeply develop research and development services in the field of protein degradation in China. It has eight technology platforms including ReThinking PROTAC (protein degradation drug Development Platform), and has developed hundreds of active molecular core fragments that can be scaled up to 100 kg.