Wei Yan

Assistant Professor/Research

Personal Statement:

Discovery and Development of Novel Chemical Entities for Human Cancer Treatment: My primary research interest lies in the exploration and advancement of innovative chemical compounds to effectively address human cancers. I specialize in targeted therapy approaches, focusing on the inhibition or degradation of oncogenes such as kinases, epigenetic regulators, and transcription factors, among others.

Efficient and Economical Synthesis of Drug Candidates: I am also passionate about developing efficient and cost-effective synthetic processes for the large-scale synthesis of drug candidates or key intermediates, making them more accessible for further research and development.

Education

B.E. - East China University of Science and Technology, Shanghai
Ph.D. - East China University of Science and Technology, Shanghai
Postdoctoral Fellowship - University of Arkansas for Medical Sciences, Little Rock, Arkansas

Research

Research Profile
Small molecule drug discovery
Cancer treatment
Kinase inhibitor Targeted protein degradation Medicinal chemistry Organic chemistry

Publications

Yan, W., Pan, B.-S., Shao, J., Lin, H.-k., Li, H-y; A feasible column chromatography free, multi-gram scale synthetic process of VH032 amine, which could enable rapid PROTAC library construction. ACS Omega, 2022, 7, 26015–26021.

Li, S.-Q., Yan, W., He, L.-J., Zhang, M., Tang, D.-Y., Li, H.-Y., Chen, Z.-Z., Xu, Z.-G. A facile one-pot synthesis of natural-product inspired spiroindolines as anti-cancer agents. Org. Chem. Front. 2022, 9, 682-686. (co-first author)

Yan, Y.; Shao, J.; Ding, D.; Pan, Y.; Tran, P.; Yan. W.; Wang, Z.; Li, H.; Huang, H. 3-Aminophthalic acid, a new cereblon ligand for targeted protein degradation by O’PROTAC. Chem. Commun., 2022, 58, 2383-2386.

Yan, W.; Zhang, L.; Lv, F.; Moccia, M.; Carlomagno, F.; Landry, C.; Santoro, M.; Gosselet, F.; Frett, B.; Li, H. Y. Discovery of thieno[3,2-d]pyrimidines as tropomyosin receptor kinase A (TRKA) inhibitors: design, synthesis, and biological evaluation. Eur. J. Med. Chem. 2021, 216: 113265

Zhu, X.L.; Wang, X.Y.; Yan, W.; Yang, H.B.; Xiang, Y.F.; Lv, F.P.; Shi, Y.; Li, H.-Y.; Lan, L. Ubiquitin-mediated degradation of TRDMT1 regulates Homologous Recombination and therapeutic response. NAR cancer. 2021, 3 (1): zcab010 (co-first author)

Zhang, L.T.; Moccia, M.; Briggs, D.C.; Bharate, J.; Lakkaniga, N.R.; Knowles, P.P.; Yan, W.; Tran, P.; Kharbanda, A.; Leung, Y.-K; Frett, B.; Santoro, M.; McDonald, N.Q.; Carlomagno, F.; Li, H.-Y. Discovery of N-trisubstituted Pyrimidine Derivatives as Type-I RET and RET Gatekeeper Mutant Inhibitors with a Novel Kinase Binding Pose. J. Med. Chem., 2021. 65, 1536-1551.

Shao, J.; Yan, Y.; Ding, D.; Wang, D.; He, Y.; Pan, Y.; Yan, W.; Kharbanda, A.; Li, H.-Y.; Huang, H. Destruction of DNA-binding proteins by programmable O’PROTAC: Oligonucleotide-based PROTAC. Adv. Sci. 2021, 8, 2102555

Hsu, C.-C.; Zhang, X.; Wang, G.H.; Zhang, W.N.; Cai, Z.; Pan, B.-S.; Gu, H.W.; Xu, C.; Jin, G.X.; Xu, X.S.; Manne, R.K.; Jin, Y.; Yan, W.; Shao, J.W.; Chen, T.J.; Lin, E.; Ketkar, A.; Eoff, R.; Xu, Z.-G.; Chen, Z.-Z. Li, H.-Y.; Lin, H.-K. Inositol serves as a natural inhibitor of mitochondrial fission by directly targeting AMPK. Mol. Cell 2021, 81, 3803–3819

Moccia, M., Frett, B., Zhang, L., Lakkaniga, N.R., Briggs, D.C., Chauhan, R., Brescia, A., Federico, G., Yan, W., Santoro, M., McDonald, N.Q., Li, H.Y., Carlomagno, F., Bioisosteric Discovery of NPA101.3, a Second-Generation RET/VEGFR2 Inhibitor Optimized for Single-Agent Polypharmacology, J. Med. Chem., 2020, 63, 4506-4516.

Saha, D.; Kharbanda, A.; Yan, W.; Lakkaniga, N. R.; Frett, B.; Li, H.-y., The Exploration of Chirality for Improved Druggability within the Human Kinome. J. Med. Chem. 2020, 63 (2), 441-469.

Yan, W.; Lakkaniga, N. R.; Carlomagno, F.; Santoro, M.; McDonald, N. Q.; Lv, F.; Gunaganti, N.; Frett, B.; Li, H. Y. Insights into Current Tropomyosin Receptor Kinase (TRK) Inhibitors: Development and Clinical Application. J. Med. Chem. 2019, 28;62(4):1731-1760.

Li, Y.; Huang, J. H.; Wang, J. L.; Song, G. T.; Tang, D. Y.; Yao, F.; Lin, H. K.; Yan, W.; Li, H. Y.; Xu, Z. G.; Chen, Z. Z. Diversity-Oriented Synthesis of Imidazo-Dipyridines with Anticancer Activity via the Groebke-Blackburn-Bienayme and TBAB-Mediated Cascade Reaction in One Pot. J. Org. Chem. 2019, 84, 12632−12638. (featured cover article)

Qu, C. H.; Song, G. T.; Xu, J.; Yan, W.; Zhou, C. H.; Li, H. Y.; Chen, Z. Z.; Xu, Z. G. Merging Visible Light with Cross-Coupling: The Photochemical Direct C-H Difluoroalkylation of Imidazopyridines. Org. Lett. 2019, 21, 8169−8173 (featured cover article)

Yan, W.; Wang, X.; Dai, Y.; Zhao, B.; Yang, X.; Fan, J.; Gao, Y.; Meng, F.; Wang, Y.; Luo, C.; Ai, J.; Geng, M.; Duan, W. Discovery of 3-(5′-Substituted)-Benzimidazole-5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazo les as Potent Fibroblast Growth Factor Receptor Inhibitors: Design, Synthesis, and Biological Evaluation. J. Med. Chem. 2016, 59, 6690-6708.