Disease Site Focus:
Breast, Leukemia/ Lymphoma, Prostate, Thoracic/ Lung
Research Focus Area:
Drug discovery, Prostate cancer, Breast cancer
Type of Research:
Research Interest Statement:
My primary research interest involves the discovery and development of novel chemical entities for the treatment of human cancers. My strategies focused on targeted therapy including targeted inhibition or degradation of oncogenes, including but not limited to kinases, epigenetic regulators, and transcription factors, etc. In addition to discovering novel drugs for cancer treatment, I’m also interested in developing novel synthetic methodologies for rapid construction of diversified compound libraries and developing/optimizing procedures for laboratory large scale synthesis of drug candidates.
Yan Y, Shao J, Ding D, [et al., including Yan W]. 3-Aminophthalic acid, a new cereblon ligand for targeted protein degradation by O'PROTAC. Chemical communications (Cambridge, England). 2022 58(14):2383-2386. PMID: 35080528.
Zhang L, Moccia M, Briggs DC, [et al., including Yan W]. Discovery of N-Trisubstituted Pyrimidine Derivatives as Type I RET and RET Gatekeeper Mutant Inhibitors with a Novel Kinase Binding Pose. Journal of medicinal chemistry. 2022 65(2):1536-1551. PMID: 35081714.
Shao J, Yan Y, Ding D, [et al., including Yan W]. Destruction of DNA-Binding Proteins by Programmable Oligonucleotide PROTAC (O'PROTAC): Effective Targeting of LEF1 and ERG. Advanced science (Weinheim, Baden-Wurttemberg, Germany). 2021 8(20):e2102555. PMID: 34397171. PMCID: PMC8529430.
Hsu CC, Zhang X, Wang G, [et al., including Yan W]. Inositol serves as a natural inhibitor of mitochondrial fission by directly targeting AMPK. Molecular cell. 2021 81(18):3803-3819.e7. PMID: 34547240. PMCID: PMC8462099.
Yan W, Zhang L, Lv F, [et al.]. Discovery of pyrazolo-thieno[3,2-d]pyrimidinylamino-phenyl acetamides as type-II pan-tropomyosin receptor kinase (TRK) inhibitors: Design, synthesis, and biological evaluation. European journal of medicinal chemistry. 2021 216:113265. PMID: 33652352.
Zhu X, Wang X, Yan W, [et al.]. Ubiquitination-mediated degradation of TRDMT1 regulates homologous recombination and therapeutic response. NAR cancer. 2021 3(1):zcab010. PMID: 33778494. PMCID: PMC7984809.
Yan W, Lakkaniga NR, Carlomagno F, [et al.]. Correction to Insights into Current Tropomyosin Receptor Kinase (TRK) Inhibitors: Development and Clinical Application. Journal of medicinal chemistry. 2020 63(17):10089. PMID: 32841014.
Moccia M, Frett B, Zhang L, [et al., including Yan W]. Bioisosteric Discovery of NPA101.3, a Second-Generation RET/VEGFR2 Inhibitor Optimized for Single-Agent Polypharmacology. Journal of medicinal chemistry. 2020 63(9):4506-4516. PMID: 32298114.
Saha D, Kharbanda A, Yan W, [et al.]. The Exploration of Chirality for Improved Druggability within the Human Kinome. Journal of medicinal chemistry. 2020 63(2):441-469. PMID: 31550151.
Qu CH, Song GT, Xu J, [et al., including Yan W]. Merging Visible Light with Cross-Coupling: The Photochemical Direct C-H Difluoroalkylation of Imidazopyridines. Organic letters. 2019 21(20):8169-8173. PMID: 31430159.
Li Y, Huang JH, Song GT, [et al., including Yan W]. Diversity-Oriented Synthesis of Imidazo-Dipyridines with Anticancer Activity via the Groebke-Blackburn-Bienaymé and TBAB-Mediated Cascade Reaction in One Pot. The Journal of organic chemistry. 2019 84(19):12632-12638. PMID: 31357859.
Yan W, Lakkaniga NR, Carlomagno F, [et al.]. Insights into Current Tropomyosin Receptor Kinase (TRK) Inhibitors: Development and Clinical Application. Journal of medicinal chemistry. 2019 62(4):1731-1760. PMID: 30188734.
Yan W, Wang X, Dai Y, [et al.]. Discovery of 3-(5'-Substituted)-Benzimidazole-5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazoles as Potent Fibroblast Growth Factor Receptor Inhibitors: Design, Synthesis, and Biological Evaluation. Journal of medicinal chemistry. 2016 59(14):6690-708. PMID: 27348537.
Yan W, Huang Z, Wang Z, [et al.]. Discovery of 1,3-Diaryl-pyridones as Potent VEGFR-2 Inhibitors: Design, Synthesis, and Biological Evaluation. Chemical biology & drug design. 2016 87(5):694-703. PMID: 26669707.