Oct 2020
Combination of menin and FLT3 inhibitors is very effective in AML models. Read in Blood. Featured on the cover!
Aug 2020
We published first in class NSD1 inhibitors in Nature Chemical Biology. Highlighted in Nature Reviews in Drug Discovery.
July 2020
Here is our review on epigenetic protein-protein interactions with Brian as first author
Jan 2020
We reported MI-3454, a very potent menin inhibitor. See our JCI paper.
# news not updated
Jan 2016
We published paper "Property focused structure-based optimization of small molecule inhibitors of the protein-protein interaction between menin and Mixed Lineage Leukemia (MLL)" in the Journal of Medicinal Chemistry.
Nov 2015
We determined structure of ZMIZ1 TPR domain and published paper in collaboration with Mark Chiang: The PIAS-like Coactivator Zmiz1 Is a Direct and Selective Cofactor of Notch1 in T Cell Development and Leukemia. Published in Immunity.
Aug 2015
Our manuscript "Two loops undergoing concerted dynamics regulate activity of the ASH1L histone methyltransferase" has been published in Biochemistry.
Our study "Rational design of orthogonal multipolar interactions with fluorine in protein-ligand complexes" has been published in Journal of Medicinal Chemistry, selected as Editor's choice.
July 2015
Felicia Gray defended her PhD thesis: "Dissecting Bmi1 protein-protein interactions through chemical biology". Congratulations Felicia!
June 2015
We have published study demonstrating that menin-MLL inhibitors block activity of MLL fusion proteins in a mechanism independent on fusion partner. Published in Leukemia.
May 2015
George Lund defended his PhD dissertation: "Targeting CDC25B-CDK2/CyclinA Activity Using Chemical Biology Approaches".
Congratulations George!
April 2015
Our menin-MLL inhibitor program has been featured as cover story in BioCentury Innovations
Dr. Chinnaiyan's lab discovered role of menin and demonstrated efficacy of menin inhibitors in castrate resistant prostate cancer. Study published in Nature Medicine.
March 2015
Our team work resulted in development of potent inhibitors of menin-MLL interaction with strong efficacy in animal models of leukemia. Published in Cancer Cell.
We have licensed menin-MLL inhibitors to Kura Oncology for further development.
Feb 2015
Jola is co-author on study to develop small molecule inhibitors of CBFB-SMMHC: "A small-molecule inhibitor of the aberrant transcription factor CBFβ-SMMHC delays leukemia in mice" published in Science.
Jan 2015
We published review Targeting protein–protein interactions in hematologic malignancies: still a challenge or a great opportunity for future therapies? in Immunological Reviews
Dec 2014
Our study Inhibition of CDC25B Phosphatase Through Disruption of Protein-Protein Interaction has been published in ACS Chemical Biology.
Nov 17, 2014
Jola has been elected to the University of Michigan Medical School "League of Research Excellence". Congratulations to Jola!
Oct 2014
Our study "The same site on LEDGF IBD domain represents therapeutic target for MLL leukemia and HIV" has been published in Blood.
Apr 21, 2014
George's publication "Solution NMR studies reveal no global flexibility in the catalytic domain of CDC25B" has been published in the journal Proteins.
Congratulations to George!
Our review "Challenges and opportunities in targeting the menin-MLL interaction" has been published in Future Medicinal Chemistry
Tomasz Cierpicki
tomaszc@umich.edu
Education:
- MSc in chemistry: Department of Chemistry; Wroclaw University of Technology; Poland
- PhD in biochemistry: Department of Biochemistry and Molecular Biology; University of Wroclaw; Poland
- Postdoctoral fellow: University of Virginia, Charlottesville, VA
- Assistant Professor in the Department on Pathology, University of Michigan (2009-2016)
- Associate Professor in the Department of Pathology, University of Michigan (since 2016)
Honors:
- 1998 Award of President of Wrocław University of Technology
- 1999 Award of Polish Chemical Society
- 2001 Award of Polish Biochemical Society
- 2002 Young Scholar Award from the Foundation for Polish Science
- 2003 Award of Polish Prime Minister
- 2011 American Cancer Society Scholar
- 2016 Leukemia and Lymphoma Society Scholar
- 2018 Senior Forbes Institute Scholar
Affiliations with graduate programs:
- Molecular and Cellular Pathology program
- Biophysics program
- Chemical Biology program
Research interest:
- Structure-function studies of proteins involved in development of acute leukemia
- Developing small molecules targeting menin-MLL-LEDGF interaction in leukemia
- Targeting protein-protein interactions using small molecules
- Development of small molecule inhibitors targeting epigenetic modulators in cancer
- Development of PRC1 inhibitors
- Fragment-based drug discovery
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