• • • • • • Drs.Xing Qiu, Yan Xiong, Jerrel Catlett, Zhijie Deng and Jian Jin, and Their Collaborators Published a Research Article Entitled “Discovery of an LSD1 PROTAC degrader” in PNAS

The research team led by Drs. Jian Jin and Yang Shi, a Professor at Ludwig Institute for Cancer Research, University of Oxford, discovered the first-in-class LSD1 small-molecule degrader, MS9117, which potently and selectively degraded LSD1, a well-known lysine demethylase that is overexpressed in various cancers including acute myeloid leukemia (AML) pnas.2425812122 10.1073/pnas.2425812122 https://www.pnas.org/doi/10.1073/pnas.2425812122 MS9117 effectively targeted both catalytic and noncatalytic oncogenic functions of LSD1 and displayed superior antiproliferative effects in AML cells, compared to LSD1 catalytic inhibitors.

• • • • • • Drs. Chao Qian, Yan Xiong, Yue Zhong and Jian Jin, and Their Collaborators Published a Research Article Entitled “USP28-Based Deubiquitinase-Targeting Chimeras for Cancer Treatment” in Journal of the American Chemical Society

The research team led by Dr. Wenyi Wei, a Professor at Harvard Medical School, and Dr. Jian Jin has demonstrated for the first time that USP28, a deubiquitinase (DUB), can be harnessed for development of Deubiquitinase-Targeting Chimeras (DUBTACs) utilizing a non-covalent small-molecule inhibitor of USP28 (https://pubs.acs.org/doi/10.1021/jacs.5c01889). Using this technology, the team developed proof-of-concept USP28-recruiting DUBTACs that stabilize CFTR, cGAS and PPARγ, respectively..

• • • • • • Drs. Chao Qian, Yan Xiong, Yue Zhong and Jian Jin, and Their Collaborators Published a Research Article Entitled “Harnessing the Deubiquitinase USP1 for Targeted Protein Stabilization” in Journal of the American Chemical Society

The research team led by Drs. Jian Jin and Wenyi Wei, a Professor at Harvard Medical School, has demonstrated for the first time that USP1, a deubiquitinase (DUB) that is overexpressed in several human cancers, can be harnessed for targeted protein stabilization. https://pubs.acs.org/doi/10.1021/jacs.5c01662 By utilizing a non-covalent small-molecule inhibitor of USP1, the team developed the first UTX Deubiquitinase-Targeting Chimera (DUBTAC) that selectively stabilizes and activates the tumor suppressor UTX and simultaneously inhibits the oncoprotein JMJD3. This work advances the TPS field.

• • • • • • Md Kabir, Xiaoping Hu, Dmitry Pokushalov, Yue Zhong, Yan Xiong, and Prof. Jin, and their Collaborators Published a Research Article Entitled “Harnessing the TAF1 Acetyltransferase for Targeted Acetylation of the Tumor Suppressor p53” in Advanced Science.