Faculty

Tomasz Cierpicki

Assistant Professor of Pathology

Ph.D., University of Wroclaw, Poland
Postdoctoral Fellow, University of Virginia

Research Focus: Structural biology, Development of small molecules targeting protein-protein interactions, Development of NMR techniques for drug discovery

Phone: 734.615.9324
E-mail: tomaszc@umich.edu
Fax: 734.615.0688

The research in Dr Cierpicki’s laboratory is focused on structural and chemical biology of proteins in cancer. We are interested in understanding the molecular basis leading to acute leukemia and in development of small molecules which could reverse the effect of leukemia oncoproteins. One of the current projects in my laboratory is development of small molecule inhibitors targeting BMI-1 oncoprotein. We are using broad range of biochemical, biophysical and structural biology methods (NMR and X-ray crystallography) in combination with medicinal chemistry to support development of potent inhibitors. In collaboration with Dr. Jolanta Grembecka we are developing small molecules targeting menin-MLL interaction to reverse the oncogenic potential of MLL fusion oncoproteins.

We are applying NMR fragment-based screening approach to identify small molecules targeting challenging proteins. Laboratory of Dr. Cierpicki is equipped in state-of-the art NMR spectrometer with automatic sample changer allowing for programmed running of NMR experiments as well as in robotic system for automatic sample preparation. Our goal is to develop small molecule inhibitors and chemical probes targeting proteins with validated activity in cancer.

 

Representative Publications

  1. Grembecka J, He S, Shi A, Purohit T, Muntean AG, Sorenson RJ, Showalter HD, Murai, M, Belcher A, Hartley T, Hess JL, Cierpicki T. (2012) Menin-MLL Inhibitors Reverse Oncogenic Activity of MLL Fusion Proteins in Leukemia. Nature Chem. Biol, 8, 277-284.

  2. Shi A, Murai MJ, He S, Lund G, Hartley T, Purohit T, Reddy G, Chruszcz M, Grembecka, J and Cierpicki T. (2012) Structural insights into inhibition of the bivalent menin-MLL interaction by small molecules in leukemia. Blood.120, 4461

  3. Gray FL, Murai MJ, Grembecka J, Cierpicki T. (2012) Detection of disordered regions in globular proteins using (13) C-detected NMR. Protein Science. 21, 1954

  4. George Lund, Sergii Dudkin, Dmitry Borkin, Wendi Ni, Jolanta Grembecka and Tomasz Cierpicki. (2014). Inhibition of CDC25B Phosphatase Through Disruption of Protein-Protein Interaction. ACS Chemical Biology, 10(2):390-394

  5. Borkin D, He S, Miao H, Kempinska K, Pollock J, Chase J, Purohit T, Malik B, Zhao T, Wang J, Wen B, Zong H, Jones M, Danet-Desnoyers G, Guzman ML, Talpaz M, Bixby DL, Sun D, Hess JL, Muntean AG, Maillard I, Cierpicki T and Grembecka J.(2015). Pharmacologic inhibition of the menin-MLL interaction blocks progression of MLL leukemia in vivo . Cancer Cell, 27(4):589-602

 

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