Wang, Rui; Liu, Hongwei; Shao, Yingying; Wang, Kailong; Yin, Shuangshuang; Qiu, Yuling; Wu, Honghua; Liu, Erwei; Wang, Tao; Gao, Xiumei; Yu, Haiyang published the artcile< Sophoridine inhibits human colorectal cancer progression via targeting MAPKAPK2>, Reference of 6882-68-4, the main research area is sophoridine MAPKAPK colorectal cancer progression human.
Radian Sophorae flavescentis is a traditional Chinese medicine commonly used to treat cancer in China. However, its active components and underlying mechanism remain ambiguous. In this study, we have screened the pharmacokinetic parameters of the main chem. constituents of Radian Sophorae flavescentis by Traditional Chinese Medicine Systems Pharmacol. (TCMSP) Database and Anal. Platform and have found that Sophoridine is one of the best antitumor active ingredients. We have found that MAPKAPK2 is a potential target for Sophoridine by the PharmMapper and KEGG databXase anal. Moreover, we have found that Sophoridine selectively inactivates phospho-MAPKAPK2 (Thr222) and directly binds into the ATP site of MAPKAPK2 by mol. docking. Furthermore, we have found out a direct binding between MAPKAPK2 and Sophoridine by cellular thermal shift assay and drug affinity responsive targets stability assay. The inhibition effects are further confirmed by Western blot: Sophoridine significantly decreases phospho-MAPKAPK2 (Thr222) in a time-dependent manner, but there is no obvious change in its total expression in colorectal cancer cells. Clin. studies have shown that a higher level of MAPKAPK2 is associated with a poorer percent survival rate (prognosis). Furthermore, a higher level of MAPKAPK2 is pos. associated with the enrichment of downregulation of apoptosis and autophagy by gene set enrichment anal., as well as upregulation of proliferation and cell-cycle arrest. Taken together, our results suggest that the MAPKAPK2 plays a key role in Sophoridine-inhibited growth and invasion in colorectal cancers.
Molecular Cancer Research published new progress about Animal gene Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 6882-68-4 belongs to class naphthyridine, and the molecular formula is C15H24N2O, Reference of 6882-68-4.
Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem