科学与创新
2024
- Luo, Z., Lin, C., Yu, C., Yuan, C., Wu, W., Xu, X., … & Xie, C. Targeted Degradation of SOS1 Exhibits Potent Anticancer Activity and Overcomes Resistance in KRAS-Mutant Tumors and BCR-ABL-Positive Leukemia. Cancer Research. 2024. doi: 10.1158/0008-5472.CAN-24-1093. PMID: 39437162.
- Zhang, X, Tao, Y, Xu, Z, Jiang, B, Yang, X, Huang, T, & Tan, W. Sorafenib and SIAIS361034, a novel PROTAC degrader of BCL-xL, display synergistic antitumor effects on hepatocellular carcinoma with minimal hepatotoxicity. Biochemical Pharmacology. 2024:116542. doi: 0.1016/j.bcp.2024.116542. PMID: 39284500.
- Zhu X, Li Y, Liu H, Wang Y, Sun R, Jiang Z, Hou C, Hou X, Huang S, Zhang H, Wang H, Jiang B, Yang X*, Xu B*, Fan G*. NAMPT-targeting PROTAC and nicotinic acid co-administration elicit safe and robust anti-tumor efficacy in NAPRT-deficient pan-cancers. Cell Chem Biol. 2024 Jun 20;31(6):1203-1218.e17. doi: 10.1016/j.chembiol.2024.05.007. PMID: 38906111.
- Liu L*, Sun R, Liu H, Ren C, Zhou Y, Qiu X, Kong Y, Jiang B*, Yang X*. Design, synthesis and biological evaluation of novel quinazolinone derivatives as CRBN E3 ligase modulators. Eur J Med Chem. 2023 Feb 5;247:115016. doi: 10.1016/j.ejmech.2022.115016. Epub 2022 Dec 16. PMID: 36577219.
- Zhang Y, Xiong X, Sun R, Zhu X, Wang C, Jiang B, Yang X*, Li D*, Fan G*. Development of the nonreceptor tyrosine kinase FER-targeting PROTACs as a potential strategy for antagonizing ovarian cancer cell motility and invasiveness. J Biol Chem. 2023 Jun;299(6):104825. doi: 10.1016/j.jbc.2023.104825. Epub 2023 May 16. PMID: 37196766.
- Gao J, Yang L, Lei S, Zhou F, Nie H, Peng B, Xu T, Chen X, Yang X, Sheng C, Rao Y, Pu K, Jin J, Xu Z*, Yu H*. Stimuli-activatable PROTACs for precise protein degradation and cancer therapy. Sci Bull (Beijing). 2023 May 30;68(10):1069-1085. doi: 10.1016/j.scib.2023.04.028. Epub 2023 Apr 26. PMID: 37169612.
- Liu H, Ren C, Sun R, Wang H, Zhan Y, Yang X*, Jiang B*, Chen H*. Reactive oxygen species-responsive Pre-PROTAC for tumor-specific protein degradation. Chem Commun (Camb). 2022 Sep 8;58(72):10072-10075. doi: 10.1039/d2cc03367d. PMID: 35993284.
- Zhu X, Liu H, Chen L, Wu C, Liu X, Cang Y, Jiang B*, Yang X*, Fan G*. Addressing the Enzyme-independent tumor-promoting function of NAMPT via PROTAC-mediated degradation. Cell Chem Biol. 2022 Nov 17;29(11):1616-1629.e12. doi: 10.1016/j.chembiol.2022.10.007. Epub 2022 Nov 1. PMID: 36323324.
- Zhang S, Chen Y, Xu Z, Yang J, Sun R, Wang J, Sun Y, Jiang B*, Yang X*, Tan W*. The PROTAC selectively degrading Bcl-xL represents a novel Hedgehog pathway inhibitor with capacity of combating resistance to Smoothened inhibitors while sparing bone growth. Theranostics. 2022 Oct 24;12(17):7476-7490. doi: 10.7150/thno.75421. PMID: 36438482.
- Liu H, Mi Q, Ding X, Lin C, Liu L, Ren C, Shen S, Shao Y, Chen J, Zhou Y, Ji L, Zhang H, Bai F*, Yang X*, Yin Q*, Jiang B*. Discovery and characterization of novel potent BCR-ABL degraders by conjugating allosteric inhibitor. Eur J Med Chem. 2022 Dec 15;244:114810. doi: 10.1016/j.ejmech.2022.114810. Epub 2022 Oct 4. PMID: 36306539.
- Li F, Hu Q, Zhang X, Sun R, Liu Z, Wu S, Tian S, Ma X, Dai Z, Yang X*, Gao S*, Bai F*. DeepPROTACs is a deep learning-based targeted degradation predictor for PROTACs. Nat Commun. 2022 Nov 21;13(1):7133. doi: 10.1038/s41467-022-34807-3. PMID: 36414666.
- Ren C, Sun N, Liu H, Kong Y, Sun R, Qiu X, Chen J, Li Y, Zhang J, Zhou Y, Zhong H, Yin Q, Song X*, Yang X*, Jiang B*. Discovery of a Brigatinib Degrader SIAIS164018 with Destroying Metastasis-Related Oncoproteins and a Reshuffling Kinome Profile. J Med Chem. 2021 Jul 8;64(13):9152-9165. doi: 10.1021/acs.jmedchem.1c00373. Epub 2021 Jun 17. PMID: 34138566.
- Ren C, Sun N, Kong Y, Qu X, Liu H, Zhong H, Song X*, Yang X*, Jiang B*. Structure-based discovery of SIAIS001 as an oral bioavailability ALK degrader constructed from Alectinib. Eur J Med Chem. 2021 May 5;217:113335. doi: 10.1016/j.ejmech.2021.113335. Epub 2021 Mar 11. PMID: 33751979.
- Qu X, Liu H, Song X*, Sun N, Zhong H, Qiu X, Yang X*, Jiang B*. Effective degradation of EGFRL858R+T790M mutant proteins by CRBN-based PROTACs through both proteosome and autophagy/lysosome degradation systems. Eur J Med Chem. 2021 Jun 5;218:113328. doi: 10.1016/j.ejmech.2021.113328. Epub 2021 Mar 7. PMID: 33773286.
- Liu H, Ding X, Liu L, Mi Q, Zhao Q, Shao Y, Ren C, Chen J, Kong Y, Qiu X, Elvassore N, Yang X*, Yin Q*, Jiang B*. Discovery of novel BCR-ABL PROTACs based on the cereblon E3 ligase design, synthesis, and biological evaluation. Eur J Med Chem. 2021 Nov 5;223:113645. doi: 10.1016/j.ejmech.2021.113645. Epub 2021 Jun 25. PMID: 34217059.
- Liu H, Sun R, Ren C, Qiu X, Yang X*, Jiang B*. Construction of an IMiD-based azide library as a kit for PROTAC research. Org Biomol Chem. 2021 Jan 6;19(1):166-170. doi: 10.1039/d0ob02120b. PMID: 33226388.
- Sun N, Ren C, Kong Y, Zhong H, Chen J, Li Y, Zhang J, Zhou Y, Qiu X, Lin H*, Song X*, Yang X*, Jiang B*. Development of a Brigatinib degrader (SIAIS117) as a potential treatment for ALK positive cancer resistance. Eur J Med Chem. 2020 May 1;193:112190. doi: 10.1016/j.ejmech.2020.112190. Epub 2020 Feb 29. PMID: 32179332.
- Zhao Q, Ren C, Liu L, Chen J, Shao Y, Sun N, Sun R, Kong Y, Ding X, Zhang X, Xu Y, Yang B, Yin Q*, Yang X*, Jiang B*. Discovery of SIAIS178 as an Effective BCR-ABL Degrader by Recruiting Von Hippel-Lindau (VHL) E3 Ubiquitin Ligase. J Med Chem. 2019 Oct 24;62(20):9281-9298. doi: 10.1021/acs.jmedchem.9b01264. Epub 2019 Oct 2. PMID: 31539241.
- Qiu X, Sun N, Kong Y, Li Y, Yang X*, Jiang B*. Chemoselective Synthesis of Lenalidomide-Based PROTAC Library Using Alkylation Reaction. Org Lett. 2019 May 17;21(10):3838-3841. doi: 10.1021/acs.orglett.9b01326. Epub 2019 May 8. PMID: 31066567.