Publications by authors named "Jolanta Grembecka"

61Publications

Covalent and noncovalent constraints yield a figure eight-like conformation of a peptide inhibiting the menin-MLL interaction.

Eur J Med Chem 2020 Dec 20;207:112748. Epub 2020 Aug 20.

Department of Bioorganic Chemistry, Faculty of Chemistry, Wrocław University of Science and Technology, Wybrzeże Wyspiańskiego 27, 50-370, Wrocław, Poland. Electronic address:

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http://dx.doi.org/10.1016/j.ejmech.2020.112748DOI Listing
December 2020

Targeting epigenetic protein-protein interactions with small-molecule inhibitors.

Future Med Chem 2020 Jul 19;12(14):1305-1326. Epub 2020 Jun 19.

Biophysics Program, University of Michigan, Ann Arbor, MI 48109, USA.

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http://dx.doi.org/10.4155/fmc-2020-0082DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7421387PMC
July 2020

Combined MAPK Pathway and HDAC Inhibition Breaks Melanoma.

Cancer Discov 2019 Apr;9(4):469-471

Department of Pathology, University of Michigan, Ann Arbor, Michigan.

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http://dx.doi.org/10.1158/2159-8290.CD-19-0069DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6446927PMC
April 2019

Distinct pathways affected by menin versus MLL1/MLL2 in MLL-rearranged acute myeloid leukemia.

Exp Hematol 2019 01 10;69:37-42. Epub 2018 Oct 10.

Department of Pediatrics, University of Colorado, Denver/Anschutz Medical Campus. Aurora, CO, USA; Department of Pharmacology, University of Colorado, Denver/Anschutz Medical Campus. Aurora, CO, USA. Electronic address:

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https://linkinghub.elsevier.com/retrieve/pii/S0301472X183085
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http://dx.doi.org/10.1016/j.exphem.2018.10.001DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6472707PMC
January 2019

GAS41 Recognizes Diacetylated Histone H3 through a Bivalent Binding Mode.

ACS Chem Biol 2018 09 17;13(9):2739-2746. Epub 2018 Aug 17.

Department of Pathology , University of Michigan , Ann Arbor , Michigan 48109 , United States.

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http://dx.doi.org/10.1021/acschembio.8b00674DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6611172PMC
September 2018

Theoretical models of inhibitory activity for inhibitors of protein-protein interactions: targeting menin-mixed lineage leukemia with small molecules.

Medchemcomm 2017 Dec 12;8(12):2216-2227. Epub 2017 Sep 12.

Department of Chemistry , Wrocław University of Science and Technology , Wyb. Wyspiańskiego 27 , 50-370 Wrocław , Poland . Email: ; Tel: +48 71 320 3200.

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http://dx.doi.org/10.1039/c7md00170cDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5774433PMC
December 2017

Gastrin Induces Nuclear Export and Proteasome Degradation of Menin in Enteric Glial Cells.

Gastroenterology 2017 12 30;153(6):1555-1567.e15. Epub 2017 Aug 30.

Department of Internal Medicine, Division of Gastroenterology, University of Michigan, Ann Arbor, Michigan; Department of Molecular and Integrative Physiology, University of Michigan, Ann Arbor, Michigan. Electronic address:

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http://dx.doi.org/10.1053/j.gastro.2017.08.038DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5705278PMC
December 2017

Stabilizing the Mixed Lineage Leukemia Protein.

N Engl J Med 2017 04;376(17):1688-1689

From the Department of Pathology, University of Michigan, Ann Arbor.

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http://dx.doi.org/10.1056/NEJMcibr1700964DOI Listing
April 2017

H3K36 methyltransferases as cancer drug targets: rationale and perspectives for inhibitor development.

Future Med Chem 2016 09 22;8(13):1589-607. Epub 2016 Aug 22.

Department of Pathology, University of Michigan, Ann Arbor, MI 48109, USA.

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http://dx.doi.org/10.4155/fmc-2016-0071DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5020427PMC
September 2016

Two Loops Undergoing Concerted Dynamics Regulate the Activity of the ASH1L Histone Methyltransferase.

Biochemistry 2015 Sep 25;54(35):5401-13. Epub 2015 Aug 25.

Department of Pathology, ‡Center for Stem Cell Biology, Life Sciences Institute, §Division of Hematology-Oncology, Department of Internal Medicine, and ∥Department of Cell and Developmental Biology, University of Michigan , Ann Arbor, Michigan 48109, United States.

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http://dx.doi.org/10.1021/acs.biochem.5b00697DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4664444PMC
September 2015

Rational Design of Orthogonal Multipolar Interactions with Fluorine in Protein-Ligand Complexes.

J Med Chem 2015 Sep 6;58(18):7465-74. Epub 2015 Sep 6.

Department of Pathology, University of Michigan , Ann Arbor, Michigan 48109, United States.

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http://dx.doi.org/10.1021/acs.jmedchem.5b00975DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4584387PMC
September 2015

Trithorax group genes in hematopoiesis.

Oncotarget 2015 Jul;6(20):17855-6

Center for Stem Cell Biology, Life Sciences Institute, University of Michigan, Ann Arbor, MI, USA.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4627213PMC
http://dx.doi.org/10.18632/oncotarget.4882DOI Listing
July 2015

Epigenetic regulation of IL-12-dependent T cell proliferation.

J Leukoc Biol 2015 Oct 9;98(4):601-13. Epub 2015 Jun 9.

*Department of Pathology, University of Michigan Medical School, Ann Arbor, Michigan, USA; Department of Immunology, Nara Medical University, Nara, Japan; and Dermatology Research, Almirall, S.A., St Feliu de Llobregat, Spain.

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http://dx.doi.org/10.1189/jlb.1A0814-375RRDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4763868PMC
October 2015

Progress towards small molecule menin-mixed lineage leukemia (MLL) interaction inhibitors with in vivo utility.

Bioorg Med Chem Lett 2015 Jul 25;25(13):2720-5. Epub 2015 Apr 25.

Department of Chemistry, Vanderbilt University, Nashville, TN 37232, USA; Vanderbilt Specialized Chemistry Center for Probe Development (MLPCN), Nashville, TN 37232, USA; Department of Pathology, University of Michigan, Ann Arbor, 1150 West Medical Center Drive, MSRBI, Room 4510D, MI 48109, USA. Electronic address:

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http://dx.doi.org/10.1016/j.bmcl.2015.04.026DOI Listing
July 2015

Targeting the MLL complex in castration-resistant prostate cancer.

Nat Med 2015 Apr 30;21(4):344-52. Epub 2015 Mar 30.

1] Michigan Center for Translational Pathology, University of Michigan, Ann Arbor, Michigan, USA. [2] Department of Pathology, University of Michigan, Ann Arbor, Michigan, USA. [3] Comprehensive Cancer Center, University of Michigan, Ann Arbor, Michigan, USA. [4] Department of Computational Medicine and Bioinformatics, University of Michigan, Ann Arbor, Michigan, USA. [5] Howard Hughes Medical Institute, University of Michigan, Ann Arbor, Michigan, USA. [6] Department of Urology, University of Michigan, Ann Arbor, Michigan, USA.

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http://www.pcf.org/atf/cf/%7B7c77d6a2-5859-4d60-af47-132fd0f
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http://www.nature.com/doifinder/10.1038/nm.3830
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http://dx.doi.org/10.1038/nm.3830DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4390530PMC
April 2015

Targeting protein-protein interactions in hematologic malignancies: still a challenge or a great opportunity for future therapies?

Immunol Rev 2015 Jan;263(1):279-301

Department of Pathology, University of Michigan, Ann Arbor, MI, USA.

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http://dx.doi.org/10.1111/imr.12244DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4457300PMC
January 2015

Inhibition of CDC25B phosphatase through disruption of protein-protein interaction.

ACS Chem Biol 2015 Feb 1;10(2):390-4. Epub 2014 Dec 1.

Department of Pathology, University of Michigan , 4510C MSRBI 1150 West Medical Center Drive, Ann Arbor, Michigan 48109-5620, United States.

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http://dx.doi.org/10.1021/cb500883hDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4340349PMC
February 2015

Challenges and opportunities in targeting the menin-MLL interaction.

Future Med Chem 2014 Mar;6(4):447-62

Department of Pathology, University of Michigan, Ann Arbor, MI, 48109, USA.

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http://dx.doi.org/10.4155/fmc.13.214DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4138051PMC
March 2014

High-affinity small-molecule inhibitors of the menin-mixed lineage leukemia (MLL) interaction closely mimic a natural protein-protein interaction.

J Med Chem 2014 Feb 6;57(4):1543-56. Epub 2014 Feb 6.

Department of Pathology, University of Michigan , Ann Arbor, 1150 West Medical Center Drive, MSRBI, Room 4510D, Michigan, 48109, United States.

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http://dx.doi.org/10.1021/jm401868dDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3983337PMC
February 2014

The role of HTS in drug discovery at the University of Michigan.

Comb Chem High Throughput Screen 2014 Mar;17(3):210-30

Center for Chemical Genomics, Life Sciences Institute, University of Michigan, Ann Arbor, MI 48109, USA.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4166557PMC
http://dx.doi.org/10.2174/1386207317666140109121546DOI Listing
March 2014

Dysregulated hematopoiesis caused by mammary cancer is associated with epigenetic changes and hox gene expression in hematopoietic cells.

Cancer Res 2013 Oct 1;73(19):5892-904. Epub 2013 Aug 1.

Authors' Affiliations: Department of Microbiology and Immunology, I3 Research Group, Life Sciences Institute, University of British Columbia, Vancouver; Trev and Joyce Deeley Research Centre, British Columbia Cancer Agency, Victoria, British Columbia, Canada; and Department of Pathology, University of Michigan, Ann Arbor, Michigan.

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http://dx.doi.org/10.1158/0008-5472.CAN-13-0842DOI Listing
October 2013

Detection of disordered regions in globular proteins using ¹³C-detected NMR.

Protein Sci 2012 Dec;21(12):1954-60

Department of Pathology, University of Michigan, Ann Arbor, Michigan 48109, USA.

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http://doi.wiley.com/10.1002/pro.2174
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http://dx.doi.org/10.1002/pro.2174DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3575925PMC
December 2012

Crystal structure of menin reveals binding site for mixed lineage leukemia (MLL) protein.

J Biol Chem 2011 Sep 13;286(36):31742-8. Epub 2011 Jul 13.

Department of Pathology, University of Michigan, Ann Arbor, Michigan 48109, USA.

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http://dx.doi.org/10.1074/jbc.M111.258186DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3173070PMC
September 2011

Molecular basis of the mixed lineage leukemia-menin interaction: implications for targeting mixed lineage leukemias.

J Biol Chem 2010 Dec 20;285(52):40690-8. Epub 2010 Oct 20.

Department of Pathology, University of Michigan, Ann Arbor, Michigan 48109, USA.

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http://dx.doi.org/10.1074/jbc.M110.172783DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3003368PMC
December 2010

Structure of the MLL CXXC domain-DNA complex and its functional role in MLL-AF9 leukemia.

Nat Struct Mol Biol 2010 Jan 13;17(1):62-8. Epub 2009 Dec 13.

Department of Molecular Physiology and Biological Physics, University of Virginia, Charlottesville, Virginia, USA.

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http://dx.doi.org/10.1038/nsmb.1714DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2908503PMC
January 2010

Plasmodium falciparum neutral aminopeptidases: new targets for anti-malarials.

Trends Biochem Sci 2010 Jan 30;35(1):53-61. Epub 2009 Sep 30.

Malaria Biology Laboratory, Queensland Institute of Medical Research, Herston, QLD 4006, Australia.

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http://dx.doi.org/10.1016/j.tibs.2009.08.004DOI Listing
January 2010

Structural basis for the inhibition of the essential Plasmodium falciparum M1 neutral aminopeptidase.

Proc Natl Acad Sci U S A 2009 Feb 5;106(8):2537-42. Epub 2009 Feb 5.

Department of Biochemistry and Molecular Biology and Australian Research Council Centre of Excellence in Structural and Functional Microbial Genomics, Monash University, Clayton, Victoria, 3800, Australia.

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http://dx.doi.org/10.1073/pnas.0807398106DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2636733PMC
February 2009

MLL protects CpG clusters from methylation within the Hoxa9 gene, maintaining transcript expression.

Proc Natl Acad Sci U S A 2008 May 15;105(21):7517-22. Epub 2008 May 15.

Oncology Institute, Molecular Biology Program, Department of Medicine, Loyola University Chicago, Maywood, IL 60153, USA.

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http://dx.doi.org/10.1073/pnas.0800090105DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2396713PMC
May 2008

Identification of phosphinate dipeptide analog inhibitors directed against the Plasmodium falciparum M17 leucine aminopeptidase as lead antimalarial compounds.

J Med Chem 2007 Nov 26;50(24):6024-31. Epub 2007 Oct 26.

Malaria Biology Laboratory, Queensland Institute of Medical Research, 300 Herston Road, Herston, Queensland 4029, Australia.

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http://dx.doi.org/10.1021/jm070733vDOI Listing
November 2007

A synthetic method for diversification of the P1' substituent in phosphinic dipeptides as a tool for exploration of the specificity of the S1' binding pockets of leucine aminopeptidases.

Bioorg Med Chem 2007 May 22;15(9):3187-200. Epub 2007 Feb 22.

Laboratory of Organic Chemistry, Department of Chemistry, University of Athens, Panepistimiopolis Zografou, 15771 Athens, Greece.

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http://dx.doi.org/10.1016/j.bmc.2007.02.042DOI Listing
May 2007

Characterization of the Plasmodium falciparum M17 leucyl aminopeptidase. A protease involved in amino acid regulation with potential for antimalarial drug development.

J Biol Chem 2007 Jan 15;282(3):2069-80. Epub 2006 Nov 15.

Institute for the Biotechnology of Infectious Diseases, University of Technology Sydney, Level 6, Building 4, Corner of Thomas and Harris Street, Ultimo, Sydney, New South Wales 2007, Australia.

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http://dx.doi.org/10.1074/jbc.M609251200DOI Listing
January 2007

The binding of the PDZ tandem of syntenin to target proteins.

Biochemistry 2006 Mar;45(11):3674-83

Department of Molecular Physiology and Biological Physics, University of Virginia School of Medicine, Charlottesville, Virginia 22908-0736, USA.

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http://dx.doi.org/10.1021/bi052225yDOI Listing
March 2006

Exploring the Sn binding pockets in gingipains by newly developed inhibitors: structure-based design, chemistry, and activity.

J Med Chem 2006 Mar;49(5):1744-53

Department of Bioorganic Chemistry, Faculty of Chemistry, Wrocław University of Technology, Wybrzeze Wyspiańskiego 27, 50-370 Wrocław, Poland.

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http://dx.doi.org/10.1021/jm0600141DOI Listing
March 2006

High resolution structure of the HDGF PWWP domain: a potential DNA binding domain.

Protein Sci 2006 Feb 29;15(2):314-23. Epub 2005 Dec 29.

Department of Chemistry, University of Virginia, Charlottesville, VA 22906, USA.

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http://doi.wiley.com/10.1110/ps.051751706
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http://dx.doi.org/10.1110/ps.051751706DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2242466PMC
February 2006

Structure-based discovery of a boronic acid bioisostere of combretastatin A-4.

Chem Biol 2005 Sep;12(9):1007-14

Department of Chemistry, University of Virginia, Charlottesville, 22904, USA.

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http://dx.doi.org/10.1016/j.chembiol.2005.06.016DOI Listing
September 2005

alpha-Aminoalkylphosphonates as a tool in experimental optimisation of P1 side chain shape of potential inhibitors in S1 pocket of leucine- and neutral aminopeptidases.

Eur J Med Chem 2005 Aug 20;40(8):764-71. Epub 2005 Apr 20.

Institute of Organic Chemistry, Biochemistry and Biotechnology, University of Technology, Wybrzeze Wyspianskiego 27, 50-370 Wroclaw, Poland.

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http://dx.doi.org/10.1016/j.ejmech.2005.02.011DOI Listing
August 2005

Origins of the activity of PAL and LAP enzyme inhibitors: toward ab initio binding affinity prediction.

J Am Chem Soc 2005 Feb;127(6):1658-9

Department of Chemistry, Wrocław University of Technology, Wyb. Wyspiańskiego 27, 50-370 Wrocław, Poland.

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http://pubs.acs.org/doi/abs/10.1021/ja042691v
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http://dx.doi.org/10.1021/ja042691vDOI Listing
February 2005

The most potent organophosphorus inhibitors of leucine aminopeptidase. Structure-based design, chemistry, and activity.

J Med Chem 2003 Jun;46(13):2641-55

Institute of Organic Chemistry, Biochemistry and Biotechnology, Wrocław University of Technology, Wybrzeze Wyspiańskiego 27, 50-370 Wrocław, Poland.

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http://dx.doi.org/10.1021/jm030795vDOI Listing
June 2003