Bingbing Li, M.D., Ph.D.

  • Research Assistant Professor of Chemical Physiology and Biochemistry, School of Medicine


Dr. Bingbing Li is interested in the interface between biology and chemistry to use innovative chemical tools to dissect the complexity of cancer biology with a goal to identify novel cancer therapeutics. In one project, she focuses on the molecular understanding of clear cell sarcoma of soft tissue (CCSST) driven by EWSR1-ATF1/CREB fusion and identification of novel therapeutics for CCSST. The fusion protein EWS-ATF1/CREB is constitutively driving CREB/ATF1-dependent gene transcription. She recently discovered a potent CREB/ATF1 inhibitor called 666-15 and is now investigating its therapeutic potential in CCSST. She is also taking an unbiased proteomics screening approach to discover other druggable proteins for CCSST.

In another project, she is using a combination of chemical biology and cell biology to investigate the nuclear envelope. The nuclear envelope is not only important for separating nucleus from cytosol, but also important for numerous signaling pathways involved in cancer and aging. She recently discovered the first small molecule called LBL1 that binds to nuclear lamins, which are type V intermediate filament proteins lying underneath inner nuclear membrane. She capitalizes this discovery to investigate the nuclear lamina-ome composition under physiologically relevant conditions using LBL1 and its chemical probes.

Education and training

    • M.D., 1998, Henan Medical University
    • M.S., 2002, Shanghai Medical College of Fudan University
    • Ph.D., 2007, Purdue University

Areas of interest

  • Chemical Biology
  • Cancer Biology
  • Cancer Pharmacology


Selected publications

  • Xiao, X.; Li, B. X. “Identification of Lamins as the Molecular Targets of LBL1 using a clickable photoaffinity probe” Methods Enzymol., 2020, 633, 185-201.
  • Li, B. X.; Xiao, X. “A suite of bioassays to evaluate CREB inhibitors” Methods Enzymol., 2020, 633, 169-184.
  • Xie, F.; Fan, Q.; Li, B. X.; Xiao, X. “Discovery of a Synergistic Inhibitor of cAMP-Response Element Binding Protein (CREB)-mediated Gene Transcription with 666-15” J. Med. Chem., 2019, 62, 11423-11429.
  • Li, B. X.; Chen, J.; Chao, B.; Zheng, Y; Xiao, X. “A Lamin-Binding Ligand Inhibits Homologous Recombination Repair of DNA Double-Strand Breaks” ACS Cent. Sci., 2018, 4, 1201-1210.
  • Li, B. X.; Chen, J.; Chao, B.; David, L; Xiao, X. “A lamin-binding ligand LBL1 targets nuclear lamins” ACS Chem. Biol., 2018, 8, 1380-1387
  • Xie, F.; Li, B. X.; Xiao, X. “Design, Synthesis and Biological Evaluation of Regioisomers of 666-15 as Inhibitors of CREB-mediated Gene Transcription” Bioorg. Med. Chem. Lett., 2017, 27, 994-998
  • Li, B. X.; Gardner, R.; Xue, C.; Qian, D. Z.; Xie, F.; Thomas, G.; Kazmierczak, S. C.; Habecker, B. A.; Xiao, X. “Systemic Inhibition of CREB is Well-tolerated in vivo” Scientific Reports, 2016, 6, 34513.
  • Xie, F.; Li, B. X.; Kassenbrock, A.; Xue, C.; Wang, X.; Qian, D. Z.; Sears, R. C.; Xiao, X. “Identification of a Potent Inhibitor of CREB-Mediated Gene Transcription with Efficacious in Vivo Anticancer Activity” J. Med. Chem., 2015, 58, 5075–5087. (Highlighted in Biocentury Innovations (formerly SciBX), Labbase News)
  • Chen, J.; Kassenbrock, A.; Li, B. X.; Xiao, X. “Discovery of a Potent Anti-tumor Agent through Regioselective Mono-N-acylation of 7H-Pyrrolo[3,2-f]quinazoline-1,3-diamine” MedChemComm, , 2013, 4, 1275-1282
  • Li, B. X.; Xiao, X. “Discovery of a Small Molecule Inhibitor of KIX-KID Interaction” ChemBioChem 2009, 10, 2721-2724.


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