Recently, Inhee Choi's group at the Pasteur Institute in Korea reported in the Journal of Enzyme Inhibition and Medicinal Chemistry a novel PROTAC degrader (compound 45) targeting the AIMP2-DX2 protein. The experimental data confirmed that compound 45 overcomes the disadvantage of the low activity of the original small molecule inhibitor by targeting binding to degrade the AIMP2-DX2 protein, and offers a new opportunity for the treatment of lung cancer.
1, Representative molecules
2,Targets and indications
Target: AIMP2-DX2 target protein
Potential indications: lung cancer
3,Synthesis pathway
4,Biological activity
In vitro experiments have shown that compound 45 significantly degrades AIMP2-DX2 protein at concentrations above 3 μM (see left below) and that compound 45-mediated anti-proliferative efficacy of AIMP2-DX2 is dependent on Siah1 levels, and that compound 45-mediated degradation of the target protein is lost when Siah1 is knocked out of the cells (see right below).
About Meno
Suzhou Meno Pharmaceutical Technology Co., Ltd. is a platform company focusing on small molecule drug discovery and development. Founded in 2008 as one of the first CROs/CDMOs in China to focus on protein degradation, the company has grown over the past 14 years and now has 8 technology platforms including ReThinking PROTAC, a protein degradation drug development platform, and has successfully developed dozens of core fragments (100 kg scale) for stable production.
We provide integrated services from drug synthesis, structure optimization, process development, comprehensive quality studies, pilot testing to cGMP production for global biopharmaceutical companies and have established deep strategic partnerships with 100+ biopharmaceutical companies worldwide.
