Structure of PDE3A–SLFN12 complex and structure-based design for a potent apoptosis inducer of tumor cells
| Autor: | Jie Chen, Nan Liu, Yinpin Huang, Yuanxun Wang, Yuxing Sun, Qingcui Wu, Dianrong Li, Shuanhu Gao, Hong-Wei Wang, Niu Huang, Xiangbing Qi, Xiaodong Wang |
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| Jazyk: | angličtina |
| Rok vydání: | 2021 |
| Předmět: | |
| Zdroj: | Nature Communications, Vol 12, Iss 1, Pp 1-11 (2021) |
| Druh dokumentu: | article |
| ISSN: | 2041-1723 37776398 |
| DOI: | 10.1038/s41467-021-26546-8 |
| Popis: | Anagrelide, nauclefine and DNMDP induce apoptosis by forming complexes with phosphodiesterase 3A (PDE3A) and Schlafen 12 protein (SLFN12). Here, the authors present the cryo-EM structures of PDE3A-SLFN12 complexes with these compounds as molecular glues. Based on the complex structure, they developed an anagrelide analog that shows a higher potency in inducing apoptosis in cultured cells and also promotes tumor growth inhibition in tumor xenografts, which is of interest for cancer drug development. |
| Databáze: | Directory of Open Access Journals |
| Externí odkaz: |
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