Teng Lab Publications

†contributed equally, *corresponding author

On-demand modular assembly for expedited PROTAC development.
Ayan Mukherjee,† Vilas D. Kadam,† Qi Miao,† Wanheng Zhang, Kevin R. MacKenzie, Zhi Tan,* Mingxing Teng.* Expert Opin. Drug Discov. 2024, 19, 769-772.

Unlocking DCAFs to catalyze degrader development: an arena for innovative approaches.
Qi Miao,† Vilas D. Kadam,† Ayan Mukherjee, Zhi Tan, Mingxing Teng.* J. Med. Chem. 2023, 66, 13369-13383.

The rise of degrader drugs.
Mingxing Teng,* Nathanael S. Gray.* Cell Chem. Biol. 2023, 30, 864-878.

The pursuit of enzyme activation: a snapshot of the gold rush.
Mingxing Teng,* Damian W. Young, Zhi Tan. J. Med. Chem. 2022, 65, 14289-14304.

Exploration of the tunability of BRD4 degradation by DCAF16 trans-labelling covalent glues.
Muhammad Murtaza Hassan,† Yen-Der Li,† Michelle W. Ma,† Mingxing Teng, Woong Sub Byun, Kedar Puvar, Ryan Lumpkin, Brittany Sandoval, Justine C. Rutter, Cyrus Y. Jin, Michelle Y. Wang, Shawn Xu, Anna M. Schmoker, Hakyung Cheong, Brian J. Groendyke, Jun Qi, Eric S. Fischer,* Benjamin L. Ebert,* Nathanael S. Gray.* Eur. J. Med. Chem. 2024, 280, online ahead of print.

Template-assisted covalent modification of DCAF16 underlies activity of BRD4 molecular glue degraders.
Yen-Der Li,† Michelle W. Ma,† Muhammad Murtaza Hassan,† Moritz Hunkeler, Mingxing Teng, Kedar Puvar, Justine C. Rutter, Ryan J. Lumpkin, Brittany Sandoval, Cyrus Y. Jin, Anna M. Schmoker, Scott B. Ficarro, Hakyung Cheong, Rebecca J. Metivier, Michelle Y. Wang, Shawn Xu, Brian J. Groendyke, Inchul You, Logan H. Sigua, Isidoro Tavares, Charles Zou, Jonathan M. Tsai, Paul M. C. Park, Hojong Yoon, Felix C. Majewski, Haniya T. Sperling, Jarrod A. Marto, Jun Qi, Radosław P. Nowak, Katherine A. Donovan, Mikołaj Słabicki, Nathanael S. Gray,* Eric S. Fischer,* Benjamin L. Ebert.* Nat. Chem. Biol. 2024, 20, online ahead of print.

Reversible male contraception by targeted inhibition of serine/threonine kinase 33.
Angela F. Ku, Kiran L. Sharma,† Hai Minh Ta,† Courtney M. Sutton,† Kurt M. Bohren, Yong Wang, Srinivas Chamakuri, Ruihong Chen, John M. Hakenjos, Ravikumar Jimmidi, Katarzyna Kent, Feng Li, Jian-Yuan Li, Lang Ma, Chandrashekhar Madasu, Murugesan Palaniappan, Stephen S. Palmer, Xuan Qin, Matthew B. Robers, Banumathi Sankaran, Zhi Tan, Yasmin M. Vasquez, Jian Wang, Jennifer Wilkinson, Zhifeng Yu, Qiuji Ye, Damian W. Young, Mingxing Teng, Choel Kim, Martin M. Matzuk.* Science 2024, 384, 885-890.

CYP3A mediates an unusual C(sp2)-C(sp3) bond cleavage via ipso-addition of oxygen in drug metabolism.
Xuan Qin, Yong Wang, Qiuji Ye, John M. Hakenjos, Jin Wang, Mingxing Teng, Lei Guo, Zhi Tan, Damian W. Young, Kevin R. Mackenzie, Feng Li.* Angew. Chem. Int. Ed. Engl. 2024, 63, e202405197.

Advancing ASMS with LC-MS/MS for the discovery of novel PDCL2 ligands from DNA-encoded chemical library selections.
Qiuji Ye, Hassane Belabed, Yong Wang, Zhifeng Yu, Murugesan Palaniappan, Jian-Yuan Li, Stacey A. Kalovidouris, Kevin R. MacKenzie, Mingxing Teng, Damian W. Young, Yoshitaka Fujihara,* Martin M. Matzuk.* Andrology 2023, 11, 808-815.

Discovery of potent BET bromodomain 1 stereoselective inhibitors using DNA-encoded chemical library selections.
Ram K. Modukuri,† Zhifeng Yu,† Zhi Tan,† Hai Minh Ta,† Melek Nihan Ucisik, Zhuang Jin, Justin L. Anglin, Kiran L. Sharma, Pranavanand Nyshadham, Feng Li, Kevin Riehle, John C. Faver, Kevin Duong, Sureshbabu Nagarajan, Nicholas Simmons, Stephen S. Palmer, Mingxing Teng, Damian W. Young, Joanna S. Yi, Choel Kim, Martin M. Matzuk.* Proc. Natl. Acad. Sci. U. S. A. 2022, 119, e2122506119.

• Primary publications

Targeting the dark lipid kinase PIP4K2C with a potent and selective binder and degrader.
Mingxing Teng,† Jie Jiang,† Eric S. Wang, Qixiang Geng, Sean T. Toenjes, Katherine A. Donovan, Nada Mageed, Hong Yue, Radosław P. Nowak, Jinhua Wang, Theresa D. Manz, Eric S. Fischer, Lewis C. Cantley, Nathanael S. Gray.* Angew. Chem. Int. Ed. Engl. 2023, 62, e202302364.

The dawn of allosteric BCR-ABL1 drugs: from a phenotypic screening hit to an approved drug.
Mingxing Teng, Marlise R. Luskin, Sandra W. Cowan-Jacob, Qiang Ding, Doriano Fabbro, Nathanael S. Gray.* J. Med. Chem. 2022, 65, 7581-7594.

Development of PDE6D and CK1α degraders through chemical derivatization of FPFT-2216.
Mingxing Teng,† Wenchao Lu,† Katherine A. Donovan, Jialin Sun, Noah M. Krupnick, Radosław P. Nowak, Yen-Der Li, Adam S. Sperling, Tinghu Zhang, Benjamin L. Ebert, Eric S. Fischer,* Nathanael S. Gray.* J. Med. Chem. 2022, 65, 747-756.

Exploring ligand-directed N‑Acyl‑N‑alkylsulfonamide-based acylation chemistry for potential targeted degrader development.
Mingxing Teng,† Jie Jiang,† Scott B. Ficarro,† Hyuk-Soo Seo, Jae Hyun Bae, Katherine A. Donovan, Eric S. Fischer, Tinghu Zhang, Sirano Dhe-Paganon, Jarrod A. Marto,* Nathanael S. Gray.* ACS. Med. Chem. Lett. 2021, 12, 1302-1307.

Rationally designed covalent BCL6 inhibitor that targets a tyrosine residue in the homodimer interface.
Mingxing Teng, Scott B. Ficarro, Hojong Yoon, Jianwei Che, Jing Zhou, Eric S. Fischer, Jarrod A. Marto, Tinghu Zhang,* Nathanael S. Gray.* ACS. Med. Chem. Lett. 2020, 11, 1269-1273.

Development of CDK2 and CDK5 dual degrader TMX-2172.
Mingxing Teng,† Jie Jiang,† Zhixiang He, Nicholas P. Kwiatkowski, Katherine A. Donovan, Caitlin E. Mills, Chiara Victor, John M. Hatcher, Eric S. Fischer, Peter K. Sorger, Tinghu Zhang,* Nathanael S. Gray.* Angew. Chem. Int. Ed. Engl. 2020, 59, 13865-13870.

The discovery of tetrahydropyridine analogs as hNav1.7 selective inhibitors for analgesia.
Mingxing Teng, Wentao Wu,* Zhixiang Li, Guangwen Yang, Jian Qin, Yikai Wang, Zhijing Hu, Haiheng Dong, Lijuan Hou, Guoping Hu, Liang Shen, Yang Zhang,* Jian Li, Shuhui Chen, Jingwei Tian,* Liang Ye, Jianzhao Zhang, Hongbo Wang. Bioorg. Med. Chem. Lett. 2017, 27, 4979-4984.

Total synthesis of the monoterpenoid indole alkaloid (±)-aspidophylline A.
Mingxing Teng, Weiwei Zi, Dawei Ma.* Angew. Chem. Int. Ed. Engl. 2014, 53, 1814-1817.

• Co-authored publications

Targeting transcription cycles in cancer.
Stephin J. Vervoort,† Jennifer R. Devlin,† Nicholas Kwiatkowski,† Mingxing Teng, Nathanael S. Gray,* Ricky W. Johnstone.* Nat. Rev. Cancer 2022, 22, 5-24.

Targeting oncoproteins with a positive selection assay for protein degraders.
Vidyasagar Koduri,† Leslie Duplaquet,† Benjamin L. Lampson, Adam C. Wang, Amin H. Sabet, Mette Ishoey, Joshiawa Paulk, Mingxing Teng, Isaac S. Harris, Jennifer E. Endress, Xiaoxi Liu, Ethan Dasilva, Joao A. Paolo, Kimberly J. Briggs, John G. Doench, Christopher J. Ott, Tinghu Zhang, Katherine A. Donovan, Eric S. Fischer, Steven P. Gygi, Nathanael S. Gray, James Bradner, Jeffrey A. Medin, Sara J. Buhrlage, Matthew G. Oser,* William G. Kaelin, Jr.* Sci. Adv. 2020, 7, eabd6263.

Mapping the degradable kinome: resource for expedited degrader development.
Katherine A. Donovan,† Fleur M. Ferguson,† Jonathan W. Bushman, Nicholas A. Eleuteri, Debabrata Bhunia, SeongShick Ryu, Li Tan, Kun Shi, Hong Yue, Xiaoxi Liu, Dennis Buckley, Dennis Dobrovolsky, Baishan Jiang, Jinhua Wang, Mingfeng Hao, Inchul You, Minxing Teng, Yanke Liang, John Hatcher, Zhengnian Li, Theresa Manz, Brian Groendyke, Yunju Nam, Sandip Sengupta, Hanna Cho, Injae Shin, Jianwei Che, Sara J. Buhrlage, Taebo Sim, Nathanael S. Gray,* Eric S. Fischer.* Cell 2020, 183, 1714-1731.

Recent advances in selective and irreversible covalent ligand development and validation.
Tinghu Zhang, John M. Hatcher, Mingxing Teng, Nathanael S. Gray,* Milka Kostic.* Cell Chem. Biol. 2019, 26, 1486-1500.

The discovery of tetrahydropyridine analogs as hNav1.7 selective inhibitors for analgesia.
Wentao Wu, Zhixiang Li, Guangwen Yang, Mingxing Teng, Jian Qin, Zhijing Hu, Lijuan Hou, Liang Shen, Haiheng Dong, Yang Zhang,* Jian Li, Shuhui Chen, Jingwei Tian,* Jianzhao Zhang, Liang Ye. Bioorg. Med. Chem. Lett. 2017, 27, 2210-2215.