Publications
24. Pierri, M., Liu, X., (co-first author) Kroupova, A., Rutter, Z., Hallatt, A. J., Ciulli, A.*, Stereochemical inversion at a 1, 4-cyclohexyl PROTAC linker fine-tunes conformation and binding affinity. Bioorg. Med. Chem Lett. 2024, 110, 129861.
23. Zhang, X., He, Y., Liu, X., Zhang, X., Shi, P., Wang, Y., Zhou, D., Zheng, G.*, Design and Optimization of Piperlongumine Analogs as Potent Senolytics. Bioorg. Med. Chem Lett. 2024, 98, 129593.
22. Liu, X., and Ciulli, A.*, Proximity-based modalities for biology and medicine. ACS Cent. Sci. 2023, 9, (7):1269–1284. invited outlook. DOI: 10.1021/acscentsci.3c00395. Listed as 1st Most Read Article in the journal (Aug 2023)
21. Pei, J., Xiao, Y., Liu, X. (co-first author), Hu, W., Sohb, A., Yuan, Y., Zhou, S., Hua, N. Mackintosh, S.G., Zhang, X., Basso, K.B., Kamat, M., Yang, Q., Licht, J.D., Zheng, G.*, Zhou, D.*, Lv, D.* Piperlongumine conjugates induce targeted protein degradation. Cell Chem. Biol., 2023, 30(2):203-213.e17. DOI: org/10.1016/j.chembiol.2023.01.004.
20. Liu, X., Kalogeropulou, A. F. (co-first author), Domingos, S., Makukhin, N., Nirujogi, R. S., Singh, F., Shpiro, N., Saalfrank, A., Sammler, E., Ganley, I. G., Moreira, R., Alessi, D. R.*, Ciulli., A.*, Discovery of XL01126: A Potent, Fast, Cooperative, Selective, Orally Bioavailable, and Blood–Brain Barrier Penetrant PROTAC Degrader of Leucine-Rich Repeat Kinase 2. J. Am. Chem. Soc, 2022, 144, 37, 16930–16952. DOI:10.1021/jacs.2c05499. Listed as 3rd Most Read Article in the journal (1-month timeframe, Sept 2022; Listed as one of the Most Read Articles in the journal within the 12-month timeframe (July 2023).
19. Liu, X., Ciulli, A.*, DUB be good to me. Nat. Chem. Biol., 2022, 18 (4), 358-359. DOI: 10.1038/s41589-022-00978-9.
18. Lv, D., Pal, P., Liu, X., Jia, Y., Thummuri, D., Zhang, P., Hu, W., Pei, J., Zhang, Q., Zhou, S., Khan, S., Zhang, X., Hua, N., Yang, Q., Arango, S., Zhang, W., Nayak, D., Olsen, S.K., Weintraub, S.T., Hromas, R., Konopleva, M., Yuan, Y., Zheng, G.*, Zhou, D.* Development of a BCL-xL and BCL-2 dual degrader with improved anti-leukemic activity. Nat. Commun. 2021, 12 (1), 6896. DOI: 10.1038/s41467-021-27210-x
17. Pal, P., Thummuri, D., Lv, D., Liu, X., Zhang, P., Hu, W., Poddar, S., Hua, N., Khan, S., Yuan, Y., Zhang, X., Zhou, D., Zheng, G.* Discovery of a novel BCL-XL PROTAC degrader with enhanced BCL-2 inhibition. J. Med. Chem, 2021. DOI: 10.1021/acs.jmedchem.1c00517
16. Zhang, P., Zhang, X., Liu, X., Khan, S., Zhou, D., Zheng, G.*, PROTACs are effective in addressing the platelet toxicity associated with BCL-XL inhibitors. Explor. Target Antitumor Ther. 2020, 1:259-272. DOI: 10.37349/etat.2020.00017.
15. Liu, X.; Zhang, X., Lv, D.; Yuan, Y.; Zheng, G.; Zhou, D.*; Assays and Technologies for Developing Proteolysis Targeting Chimera. Future Med. Chem. 2020, 12(12), 1155-1179. DOI: 10.4155/fmc-2020-0073. Listed as one of the most-read articles on this journal.
14. He, Y., Khan, S., Huo, Z., Lv, D., Zhang, X., Liu, X., Yuan, Y., Hromas, R., Xu, M., Zheng, G., Zhou, D.*; Proteolysis targeting chimeras (PROTACs) are emerging therapeutics for hematologic malignancies. J. Hematol. Oncol. 2020 13 (1), 103. DOI: 10.1186/s13045-020-00924-z.
13. Liu, X., Gao, Z., Fu, Q., Song, L., Hendrickson, H., Crooks, P., Zhang, P., Zhang, X., Zhou, D., Zheng, G.*, Deuteration of farnesyl terminal methyl groups of δ-tocotrienol and its effects on the metabolic stability and ability of inducing G-CSF production. Bioorg. Med. Chem. 2020, 28 (11), 11548. DOI: 10.1016/j.bmc.2020.115498. Deuteration was used as a medicinal chemistry strategy to improve the metabolic stability of δ-tocotrienol.
12. He, Y.; Zhang, X.; Chang, J.; Kim, H-N.; Zhang, P.; Wang, Y.; Khan, S.; Liu, X.; Zhang, X.; Lv, D.; Li, W.; Thummuri, D.; Yuan, Y.; Elisseeff, J. H.; Campisi, J.; Almeida, M.; Zheng, G.*; Zhou, D.* Using proteolysis targeting chimera technology to overcome ABT263 on-target platelet toxicity and improve its senolytic activity. Nat. Commun. 2020, 11 (1), 1996. DOI: 10.1038/s41467-020-15838-0.
11. Zhang, X.; Thummuri, D.; Liu, X.; Khan, S.; He, Y.; Zhang, P.; Hu, W.; Yuan, Y.; Zhou, D.; Zheng, G.* Discovery of PROTAC BCL-XL degraders as potent anticancer agents with low on-target platelet toxicity. Eur. J. Med. Chem. 2020, 192, 112186. DOI: 10.1016/j.ejmech.2020.112186.
10. Liu, X.; Poddar, S.; Song, L.; Hendrickson, H.; Zhang, X., Yuan, Y.; Zhou, D.; Zheng, G.* Synthesis and Liver Microsomal Metabolic Stability Studies of a Fluoro-Substituted δ-Tocotrienol Derivative. ChemMedChem 2020, 15 (6), 506-516. DOI: 10.1002/cmdc.201900676. An example shows that fluorine substitutions failed to improve the metabolic stability of a compound.
9. Zhang, X.; Liu, X.; Zhou, D.; Zheng, G.* Targeting anti-apoptotic BCL-2 family proteins for cancer treatment. Future Med. Chem. 2020, 12(7), 563-565. DOI: 10.4155/fmc-2020-0004.
8. Khan, S.; Zhang, X.; Lv, D.; Zhang, Q.; He, Y.; Zhang, P.; Liu, X.; Thummuri, D.; Yuan, Y.; Wiegand, J.; Pei, J.; Zhang, W.; Sharma, A.; McCurdy, C.R.; Kuruvilla, V.M.; Baran, N.; Ferrando, A.A.; Kim, Y.; Rogojina, A.; Houghton, P.J.; Huang, G.; Hromas, R.; Konopleva, M.; Zheng, G.*, Zhou, D.*, A selective BCL-XL PROTAC degrader achieves safe and potent antitumor activity. Nat. Med. 2019, 25 (12), 1938-1947. DOI: 10.1038/s41591-019-0668-z.
7. Zhang, X.; Thummuri, D.; He, Y.; Liu X.; Zhang, P.; Zhou, D.; Zheng G.* Utilizing PROTAC technology to address the on-target platelet toxicity associated with inhibition of BCL-XL. Chem. Commun. 2019, 55 (98), 14765-14768. DOI: 10.1039/c9cc07217a.
6. Zhang, X.; Zhang, S.; Liu, X.; Wang, Y.; Chang, J.; Zhang, X.; Mackintosh, SG.; Tackett, AJ.; He, Y.; Lv, D.; Laberge, RM.; Campisi, J.; Wang, J.; Zheng, G.*; Zhou, D.* Oxidation resistance 1 is a novel senolytic target. Aging cell 2018, 17 (4), e12780. DOI: 10.1111/acel.12780. The target identification for the senolytic agent we discovered.
5. Liu, X.; Wang, Y.; Zhang, X.; Gao, Z; Zhang, S., Shi, P., Zhang, X., Song, L.; Hendrickson, H.; Zhou, D., Zheng, G.*, Senolytic activity of piperlongumine analogues: Synthesis and biological evaluation. Bioorg. Med. Chem. 2018, 26 (14), 3925-3938. DOI: 10.1016/j.bmc.2018.06.013.
4. Che, R.; Liu, X. (Co-first author); Lu, W.* Synthesis of 1,3,4,6-Tetra-O-Acetyl-l-Gulose. Chin. J. Chem. 2017, 35 (2), 237–241. DOI: 10.1002/cjoc.201600658.
3. Liu, X.; Gujarathi, S.; Zhang, X.; Shao, L.; Boerma, M.; Compadre, C. M.; Crooks, P. A.; Hauer-Jensen, M.; Zhou, D.; Zheng, G.* Synthesis of (2R,8′S,3′E)-δ-Tocodienol, a Tocoflexol Family Member Designed to Have a Superior Pharmacokinetic Profile Compared to δ-Tocotrienol. Tetrahedron 2016, 72 (27), 4001–4006. DOI: 10.1016/j.tet.2016.05.028.
2. Wang, Y.; Chang, J.; Liu, X.; Zhang, X.; Zhang, S.; Zhang, X.; Zhou, D.*; Zheng, G.* Discovery of Piperlongumine as a Potential Novel Lead for the Development of Senolytic Agents. Aging (Albany NY) 2016, 8 (11), 2915–2926. DOI: 10.18632/aging.101100.
1. Gujarathi, S.; Liu, X.; Song, L.; Hendrickson, H.; Zheng, G.* A Mild and Efficient AgSbF6-Catalyzed Synthesis of Fully Substituted Pyrroles through a Sequential Propargylation/Amination/Cycloisomerization Reaction. Tetrahedron 2014, 70 (34), 5267–5273. DOI: 10.1016/j.tet.2014.05.073.