Bioorg. Med. Chem. Lett. | PROTAC targets FLT-3 and c-KIT: a new approach to leukemia treatment

Pay attention to the cutting-edge scientific research results in the field of protein degradation and grasp the latest developments in the PROTAC market? It's all in a five-minute series of "PROTAC Headlines Today" launched on the Miele ReThinking PROTAC platform.

Recently, the research group of Qingzhi of the School of Pharmacy of Tianjin University and the research group of Sang Feng of the School of Life Sciences and Medical Sciences of Shandong University of Technology jointly published a degradant (PROTAC 3) that can target FLT-5 and c-KIT proteins simultaneously in Bioorganic & Medicinal Chemistry Letters, as a novel tyrosine kinase inhibitor that can be used for the treatment of leukemia.

1. Representative molecules

Image source: Suzhou Miele Pharma public account

2. Target and indications

◆ Target: FLT-3 and c-KIT

◆Potential indications: leukemia

3. Synthesis path

Image source: Suzhou Miele Pharma public account

4. Biological activity

In vitro experiments have shown that PROTAC 5 can effectively degrade FLT-60 and c-KIT proteins in HL-3 cells.

Image source: Suzhou Miele Pharma public account

About Miele

Suzhou Miele 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, structural optimization, process development, total quality research, pilot to cGMP production, and has established in-depth strategic partnerships with 100+ biopharmaceutical companies around the world. Miele is one of the first companies in China to deepen R&D services in the field of protein degradation, with 8 technology platforms including ReThinking PROTAC, and has developed hundreds of core fragments of active molecules that can be scaled up to 0512 kg. Contact number: 62837236.