Drug Discovery:

Drug discovery is highly interdisciplinary and requires a broad range of skill sets. In addition to the design and synthesis of drug candidates, we develop various cell-based and biochemical assays to evaluate the pharmacological properties of the drug candidates such as potency, selectivity, and stability. We also design assays to study the detailed cellular mechanisms of action of novel small molecules we developed such as how they induce the ubiquitination, degradation, and internalization of protein targets in cells. In addition, we also develop delivery methods for the therapeutic agents we prepared through the discovery of novel ligands for cell surface receptors and transporters.

Medicinal Chemistry and Organic Synthesis:

We are interested in developing novel reactions for the synthesis of carbo- and heterocycles that are present in diverse bioactive compounds. These reactions can be used for the optimization of pharmacological properties of small molecules such as potency, selectivity, stability, and solubility. We are interested in developing novel enabling chemistry platforms that can accelerate the generation of large small molecule libraries. We are also interested in advancing glycoscience by streamlining the synthesis of carbohydrates through the development of novel technologies (e.g. site-selective functionalization, de novo synthesis of bacterial sugars, automated synthesis, electrochemical synthesis, etc.). The carbohydrates can be used for engineering the glycans on antibodies and other therapeutic reagents.

Chemical Biology:

We are interested in dissecting the complex biological pathways by novel small molecule probes. We are currently developing small molecules that can selectively modulate protein stability and epigenetic markers.

Background: Dr. Weiping Tang joined the faculty of UW-Madison in 2007. His lab focuses on various aspects of drug discovery including synthetic organic chemistry, medicinal chemistry, chemical biology, bioassay development, and mechanism of action studies for bioactive compounds in-vitro and in-vivo. Please visit his lab website (link on the left) for updated information.

Education:

• BS 1997 Chemistry - Peking University
• MS 1999 Chemistry - New York University
• PhD 2005 Organic Chemistry - Stanford University
• Postdoc 2007 Medicinal Chemistry, Chemical Biology and Drug Discovery - Harvard University

Awards and Honors:

• Boehringer Ingelheim Predoctoral Fellowship (2002)
• Amgen Predoctoral Fellowship (2003)
• HHMI Postdoctoral Fellowship (2005-2007)
• Thieme Synlett/Synthesis Journal Award (2010)
• ACS Young Academic Investigator Symposium (2011)
• Amgen Young Investigator Award (2011)
• UW-Madison Vilas Mid-Career Award (2018)
• Janis Apinis Professor (2019)
• Vilas Distinguished Achievement Professor (2022)

Medicinal Chemistry II (PharmSci 532)

Principles of Drug Discovery (PharmSci 786)

• “Development of Substituted Phenyl Dihydrouracil as the Novel Achiral Cereblon Ligands for Targeted Protein Degradation” Xie, H.; Li, C.; Tang, H.; Tandon, H.; Liao, J.; Roberts, B. L.; Zhao, Y.; Tang, W.* J. Med. Chem. 2023, 66, 2904-2917.
• “A Platform for the Rapid Synthesis of Proteolysis Targeting Chimeras (Rapid-TAC) under Miniaturized Conditions” Guo, L.‡; Zhou, Y.‡; Nie, X.‡; Zhang, Z.; Zhang, Z.; Li, C.; Wang, T.; and Tang, W.* Eur. J. Med. Chem. 2022, 236, 114317. 
• “A General Strategy for the Synthesis of Rare Sugars via Ru(II)-catalyzed and Boron-mediated Selective Epimerization of 1,2-trans-diols to 1,2-cis-diols” Li, X.; Wu, J.; and Tang, W.* J. Am. Chem. Soc. 2022, 144, 3727-3736.
• “Development of Triantennary N-Acetylgalactosamine Conjugates as Degraders for Extracellular Proteins” Zhou, Y.; Teng, P.; Montgomery, N. T.; Li, X.; and Tang, W.* ACS Cent. Sci, 2021, 7, 499-506.
• “A Cell-based Target Engagement Assay for the Identification of Cereblon E3 Ubiquitin Ligase Ligands and Their Application in HDAC6 Degraders” Yang, K.;  Zhao, Y.; Nie, X.; Wu, H.; Wang, B.; Almodovar-Rivera, C. M.; Xie, H.;* Tang, W.* Cell Chem. Biol. 2020, 27, 866-876.
• “Two-stage Strategy for Development of Proteolysis Targeting Chimeras and its Application for Estrogen Receptor Degraders” Roberts, B. L.; Ma, Z.-X.; Gao, A.; Leisten, E. D.; Yin, D.; Xu, W.; and Tang, W.* ACS Chem. Biol. 2020,  15, 1487–1496.
• “Development of Selective Histone Deacetylase 6 (HDAC6) Degraders Recruiting Von Hippel–Lindau (VHL) E3 Ubiquitin Ligase” Yang, K.; Wu, H.; Zhang, Z.; Leisten, E. G.; Nie, X.; Liu, B.; Wen, Z.; Zhang, J.; Cunningham, M. D. and Tang, W.* ACS Med. Chem. Lett. 2020, 11, 575-581.
• "Site- and Stereoselective O-Alkylation of Glycosides by Rh(II)-Catalyzed Carbenoid Insertion" Wu, J.; Li, X.; Qi, X.; Duan, X.; Cracraft, W. L.; Guizei, I. A.; Liu, P.;* and Tang, W.* J. Am. Chem. Soc. 2019, 141, 19902-19910.
• "A general strategy for diversifying complex natural products to polycyclic scaffolds with medium-sized rings" Zhao, C.; Ye, Z.; Ma, Z.-X.; Wildman, S. A.; Blaszczyk, S. A.; Hu, L.; Guizei, I. A.; Tang, W.* Nat. Commun. 2019, 10, 4015.
• "Development of Multi-Functional Histone Deacetylase 6 Degraders with Potent Anti-Myeloma Activity" Wu, H.; Yang, K.; Zhang, Z.; Leisten, E. D.; Li, Z.; Xie, H.; Liu, J.; Smith, K. A.; Novakova, Z.; Barinka, C.; and Tang, W.* J. Med. Chem. 2019, 62, 7042-7057.
• "Development of selective small molecule MDM2 degraders based on nutlin" Wang, B.; Wu, S.; Liu, J.; Yang, K.; Xie, H.; and Tang, W.* Eur. J. Med. Chem. 2019, 176, 476-491.
• "S-Adamantyl Group Directed Site-Selective Acylation and Its Applications in the Streamlined Assembly of Oligosaccharides" Blaszczyk. S. A.;  Xiao, G.; Wen, P.; Hao, H.; Wu, J.; Wang, B.; Carattino, F.; Li, Z.; Glazier, D. A.; McCarty, B. J.; Liu, P.* and Tang, W.* Angew. Chem. Int. Ed. 2019, 58, 9542-9546.
• "Intermolecular Regio- and Stereoselective Hetero-[5+2] Cycloaddition of Oxidopyrylium Ylides and Cyclic Imines" Zhao, C.; Glazier, D. A.; Yang, D.; Yin, D.; Guzei, I. A.; Aristov, M. M.; Liu, P.* and Tang, W.* Angew. Chem. Int. Ed.  2019, 58, 887-891.