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
Join Our Team
Position Title
Research Fellow in Cancer Biology
University of Michigan, Ann Arbor
Description
Postdoctoral position is available in Prof. Jolanta Grembecka laboratory, University of Michigan, Ann Arbor, to carry out an interdisciplinary project to study the effect of small molecules in in vitro and in vivo models of cancers and to pursue target validation studies using genetic approaches. We are seeking for a highly motivated postdoctoral fellow with extensive experience in cancer cell biology. The research will be focused on evaluation of the activity and the mechanism of action of novel small molecules blocking epigenetic proteins in cancer. This position requires the expertise in cell biology and molecular biology techniques, including PCR, qRT-PCR, Western Blotting, co-Immunoprecipitation, ChIP, ChIPSeq, flow cytometry, fluorescence microscopy, immunostaining. Prior work experience with animals such as transgenic mice and xenograft models of cancer would be desired. Successful candidate will be a part of an interdisciplinary team focused on development and pre-clinical evaluation of novel anti-cancer drug candidates.
Requirements
Applicant must have PhD in biology or related field. The candidates must be a first author on at least 2-3 publications. This position requires extensive experience in cell and molecular biology techniques. Furthermore, excellent oral and written communication skills in English are required as well as the ability to conduct independent scientific investigations.
How to apply
Please submit cover letter, CV, and contact information for 2-3 references combined into one PDF file by e-mail to: jolantag@umich.edu.
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Contact: Jolanta Grembecka, PhD, Associate Professor
Department of Pathology, University of Michigan
Ann Arbor, MI, 48109, USA
e-mail: jolantag@umich.edu
Relevant publications
1. Borkin, D. et al., Grembecka, J., Pharmacologic inhibition of the menin-MLL interaction blocks progression of MLL leukemia in vivo, Cancer Cell, 2015, 27 (4), 589-602.
2. He S, Grembecka J., Menin-MLL inhibitors block oncogenic transformation by MLL fusion proteins in a fusion partner independent manner. Leukemia. 2016 Feb;30(2):508-13.
Position title
Postdoctoral Research Fellow in Medicinal Chemistry for Cancer Drug Discovery
University of Michigan, Ann Arbor
Job Description
Postdoctoral position is available in the laboratory of Prof. Tomasz Cierpicki, University of Michigan, Ann Arbor, to develop small molecule inhibitors for targeted therapies in cancer. We are seeking for highly motivated synthetic organic chemists and medicinal chemists to join a comprehensive drug discovery program. Dr. Cierpicki’s lab. is conducting highly interdisciplinary research focused on pre-clinical development of novel anti-cancer drugs, which covers medicinal chemistry, structural biology, biochemical and biophysical assays, biological and animal studies. We have a strong team of synthetic chemists to support our drug-discovery efforts. The successful candidate will be involved in designing and synthesis of small molecule inhibitors targeting proteins as potential anti-cancer agents with a major focus on synthesis of heterocyclic compounds targeting protein-protein interactions relevant to cancer. The duties will include design and synthesis of new analogues of existing leads to develop biologically active compounds for testing in cancer cells and animals. The candidate must be independent in designing synthetic routes, solving challenging synthetic problems, efficient in synthesizing targeted molecules, including multi-step synthesis.
Requirements
Applicant must have PhD in synthetic organic chemistry or medicinal chemistry and be a first author on at least 2-3 publications. This position requires extensive experience in designing synthetic routes for new classes of compounds, solving challenging synthetic problems, SAR analysis. Applicant needs an expertise in using HPLC, NMR and MS for organic chemistry applications. Excellent oral and written communication skills in English are required.
How to apply
Please submit cover letter, CV, and contact information for 2-3 references combined into one PDF file by e-mail to: tomaszc@umich.edu.
—
Contact: Tomasz Cierpicki, PhD, Associate Professor
Department of Pathology, University of Michigan
Ann Arbor, MI, 48109, USA
e-mail: tomaszc@umich.edu
Relevant publications:
1. Borkin D. et al, Property Focused Structure-Based Optimization of Small Molecule Inhibitors of the Protein-Protein Interaction between Menin and Mixed Lineage Leukemia (MLL). J Med Chem. 2016, 59(3): 892-913.
2. Borkin, D. et al., Pharmacologic inhibition of the menin-MLL interaction blocks progression of MLL leukemia in vivo, Cancer Cell, 2015, 27 (4), 589-602.
3. Pollock JW, et al, Rational design of orthogonal multipolar interactions with fluorine in protein-ligand complexes. J. Med. Chem., 2015, 58 (18): 7465-74.
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