Nature Chem. Biol. | first PROTAC molecules to STAT5 proteins with high specificity: new in the treatment of chronic myeloid leukemia

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Recently, the first STAT5 PROTAC (AK-2292) was reported in Nature Chemical Biology by Wang Shaomeng at the University of Michigan. AK-2292 is highly specific to STAT5 protein. But there was no effect on other STAT proteins. In addition, AK-2292 blocked cell growth in chronic myeloid leukemia (CML) cell lines and induced tumor regression in two CML mouse models.

1. Represents the molecule

2. Targets and indications

◆ Target: Signal transducer and activator of transcription 5 (STAT5)
Potential indication: Chronic Myeloid Leukemia (CML)

3. Synthesis path

4. Biological activity

In vitro results showed that AK-2292 was highly specific to STAT5, but had no effect on other STAT proteins (Figure a). AK-2292 inhibited cell growth in KU812 cell line (Figure b). AK-2292 induced tumor regression in the KU812 mouse model (Figure c).

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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. Meinol is one of the first companies to deeply research and development services in the field of protein degradation in China. It has 8 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. Contact number: 0512-62837236.