Jeffrey R Simard

Jeffrey R Simard

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Jeffrey R Simard

Jeffrey R Simard

Publications by authors named "Jeffrey R Simard"

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Direct monitoring of the conformational equilibria of the activation loop in the mitogen-activated protein kinase p38α.

Chem Commun (Camb) 2018 Oct;54(85):12057-12060

Department of Chemistry and Konstanz Research School Chemical Biology, (KoRS-CB), University of Konstanz, Universitätsstraße 10, 78457 Konstanz, Germany.

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http://xlink.rsc.org/?DOI=C8CC06128A
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http://dx.doi.org/10.1039/c8cc06128aDOI Listing
October 2018

Monitoring Conformational Changes in the Receptor Tyrosine Kinase EGFR.

Chembiochem 2016 06 21;17(11):990-4. Epub 2016 Apr 21.

Technische Universität Dortmund, Fakultät für Chemie und Chemische Biologie, Otto-Hahn-Strasse 4a, 44227, Dortmund, Germany.

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http://dx.doi.org/10.1002/cbic.201600115DOI Listing
June 2016

FLiK: a direct-binding assay for the identification and kinetic characterization of stabilizers of inactive kinase conformations.

Methods Enzymol 2014 ;548:147-71

Chemical Genomics Centre of the Max Planck Society, Dortmund, Germany; Fakultät Chemie, Chemische Biologie, Technische Universität Dortmund, Dortmund, Germany. Electronic address:

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http://dx.doi.org/10.1016/B978-0-12-397918-6.00006-9DOI Listing
July 2015

Discovery of inter-domain stabilizers-a novel assay system for allosteric akt inhibitors.

ACS Chem Biol 2015 Jan 3;10(1):279-88. Epub 2014 Jul 3.

Technische Universität Dortmund , Fakultät für Chemie und Chemische Biologie, Otto-Hahn-Strasse 6, 44227 Dortmund, Germany.

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http://dx.doi.org/10.1021/cb500355cDOI Listing
January 2015

Identification of type II and III DDR2 inhibitors.

J Med Chem 2014 May 5;57(10):4252-62. Epub 2014 May 5.

Department of Chemistry and Chemical Biology, Technical University of Dortmund , Otto-Hahn-Straße 6, 44227 Dortmund, Germany.

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http://dx.doi.org/10.1021/jm500167qDOI Listing
May 2014

Overcoming compound fluorescence in the FLiK screening assay with red-shifted fluorophores.

J Am Chem Soc 2013 Jun 24;135(22):8400-8. Epub 2013 May 24.

Chemical Genomics Centre of the Max-Planck-Society , Otto-Hahn-Strasse 15, 44137 Dortmund, Germany.

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http://dx.doi.org/10.1021/ja403074jDOI Listing
June 2013

Selective detection of allosteric phosphatase inhibitors.

J Am Chem Soc 2013 May 26;135(18):6838-41. Epub 2013 Apr 26.

Chemical Genomics Centre der Max-Planck-Gesellschaft, Dortmund, Germany.

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http://dx.doi.org/10.1021/ja4030484DOI Listing
May 2013

Development and implementation of a high-throughput AlphaLISA assay for identifying inhibitors of EZH2 methyltransferase.

Assay Drug Dev Technol 2013 Apr 14;11(3):152-62. Epub 2013 Feb 14.

Amgen, Inc., Cambridge, Massachusetts 02142, USA.

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http://dx.doi.org/10.1089/adt.2012.481DOI Listing
April 2013

Targeting GSK3 from Ustilago maydis: type-II kinase inhibitors as potential antifungals.

ACS Chem Biol 2012 Jul 15;7(7):1257-67. Epub 2012 May 15.

Fakultät Chemie - Chemische Biologie, Technische Universität Dortmund, Germany.

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http://dx.doi.org/10.1021/cb300128bDOI Listing
July 2012

Direct binding assay for the detection of type IV allosteric inhibitors of Abl.

J Am Chem Soc 2012 Jun 25;134(22):9138-41. Epub 2012 May 25.

Chemical Genomics Centre of the Max-Planck-Society, Dortmund, Germany.

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http://pubs.acs.org/doi/10.1021/ja303858w
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http://dx.doi.org/10.1021/ja303858wDOI Listing
June 2012

Structure-based design, synthesis and biological evaluation of N-pyrazole, N'-thiazole urea inhibitors of MAP kinase p38α.

Eur J Med Chem 2012 Feb 18;48:1-15. Epub 2011 Nov 18.

Chemical Genomics Centre of the Max Planck Society, Otto-Hahn-Strasse 15, D-44227 Dortmund, Germany.

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http://dx.doi.org/10.1016/j.ejmech.2011.11.019DOI Listing
February 2012

Fluorescence labels in kinases: a high-throughput kinase binding assay for the identification of DFG-out binding ligands.

Methods Mol Biol 2012 ;800:95-117

Chemical Genomics Centre of the Max Planck Society, Dortmund, Germany.

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http://dx.doi.org/10.1007/978-1-61779-349-3_8DOI Listing
January 2012

Identification of Ustilago maydis Aurora kinase as a novel antifungal target.

ACS Chem Biol 2011 Sep 20;6(9):926-33. Epub 2011 Jun 20.

Chemical Genomics Centre of the Max Planck Society, Dortmund, Germany.

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http://dx.doi.org/10.1021/cb200112yDOI Listing
September 2011

Synthesis and biological evaluation of 7-substituted-1-(3-bromophenylamino)isoquinoline-4-carbonitriles as inhibitors of myosin light chain kinase and epidermal growth factor receptor.

Bioorg Med Chem 2011 Jan 10;19(1):429-39. Epub 2010 Nov 10.

Chemical Genomics Centre of the Max Planck Society, Otto-Hahn-Strasse 15, 44227 Dortmund, Germany.

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http://dx.doi.org/10.1016/j.bmc.2010.11.007DOI Listing
January 2011

Proteus in the world of proteins: conformational changes in protein kinases.

Arch Pharm (Weinheim) 2010 Apr;343(4):193-206

Chemical Genomics Centre of the Max Planck Society, Otto-Hahn-Strasse 15, D-44227 Dortmund, Germany.

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http://doi.wiley.com/10.1002/ardp.201000028
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http://dx.doi.org/10.1002/ardp.201000028DOI Listing
April 2010

Fluorophore labeling of the glycine-rich loop as a method of identifying inhibitors that bind to active and inactive kinase conformations.

J Am Chem Soc 2010 Mar;132(12):4152-60

Chemical Genomics Centre of the Max Planck Society, Otto-Hahn-Strasse 15, D-44227 Dortmund, Germany.

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http://dx.doi.org/10.1021/ja908083eDOI Listing
March 2010

Displacement assay for the detection of stabilizers of inactive kinase conformations.

J Med Chem 2010 Jan;53(1):357-67

Chemical Genomics Centre of the Max Planck Society, Otto-Hahn-Strasse 15, D-44227 Dortmund, Germany.

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http://dx.doi.org/10.1021/jm901297eDOI Listing
January 2010

Fast diffusion of very long chain saturated fatty acids across a bilayer membrane and their rapid extraction by cyclodextrins: implications for adrenoleukodystrophy.

J Biol Chem 2009 Nov 28;284(48):33296-304. Epub 2009 Sep 28.

Department of Biophysics and Physiology, Boston University School of Medicine, Boston University, Boston, Massachusetts 02118, USA.

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http://dx.doi.org/10.1074/jbc.M109.043737DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2785172PMC
November 2009

Chemical and structural biology to direct the repurposing of sulindac.

ChemMedChem 2009 Nov;4(11):1793-5

Chemical Genomics Centre of the Max-Planck-Society, Dortmund, Germany.

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http://dx.doi.org/10.1002/cmdc.200900384DOI Listing
November 2009

Development of a fluorescent-tagged kinase assay system for the detection and characterization of allosteric kinase inhibitors.

J Am Chem Soc 2009 Sep;131(37):13286-96

Chemical Genomics Centre of the Max Planck Society, Otto-Hahn-Strasse 15, D-44227 Dortmund, Germany.

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http://dx.doi.org/10.1021/ja902010pDOI Listing
September 2009

Hybrid compound design to overcome the gatekeeper T338M mutation in cSrc.

J Med Chem 2009 Jul;52(13):3915-26

Chemical Genomics Centre of the Max Planck Society, D-44227 Dortmund, Germany.

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http://dx.doi.org/10.1021/jm9002928DOI Listing
July 2009

A new screening assay for allosteric inhibitors of cSrc.

Nat Chem Biol 2009 Jun 26;5(6):394-6. Epub 2009 Apr 26.

Chemical Genomics Centre of the Max Planck Society, Dortmund, Germany.

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http://dx.doi.org/10.1038/nchembio.162DOI Listing
June 2009

Fatty acid flip-flop in a model membrane is faster than desorption into the aqueous phase.

Biochemistry 2008 Sep 12;47(35):9081-9. Epub 2008 Aug 12.

Department of Physiology and Biophysics, Boston University School of Medicine, 715 Albany Street, Boston, Massachusetts 02118, USA.

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http://dx.doi.org/10.1021/bi800697qDOI Listing
September 2008

Measuring the adsorption of Fatty acids to phospholipid vesicles by multiple fluorescence probes.

Biophys J 2008 Jun 22;94(11):4493-503. Epub 2008 Feb 22.

Departments of Physiology and Biophysics, Boston University School of Medicine, Boston, Massachusetts 02118, USA.

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http://dx.doi.org/10.1529/biophysj.107.121186DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2480657PMC
June 2008

Structural insights into how irreversible inhibitors can overcome drug resistance in EGFR.

Bioorg Med Chem 2008 Apr 20;16(7):3482-8. Epub 2008 Feb 20.

Chemical Genomics Centre of the Max-Planck-Society, Otto-Hahn-Strasse 15, 44227 Dortmund, Germany.

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https://linkinghub.elsevier.com/retrieve/pii/S09680896080017
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http://dx.doi.org/10.1016/j.bmc.2008.02.053DOI Listing
April 2008

Acrylodan-labeled intestinal fatty acid-binding protein to measure concentrations of unbound fatty acids.

Methods Mol Biol 2007 ;400:27-43

Department of Physiology, Boston University School of Medicine, MA, USA.

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http://dx.doi.org/10.1007/978-1-59745-519-0_3DOI Listing
December 2007

Fluorescence assays for measuring fatty acid binding and transport through membranes.

Methods Mol Biol 2007 ;400:237-55

Department of Physiology and Biophysics, Boston University School of Medicine, MA, USA.

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http://dx.doi.org/10.1007/978-1-59745-519-0_16DOI Listing
December 2007

Location of high and low affinity fatty acid binding sites on human serum albumin revealed by NMR drug-competition analysis.

J Mol Biol 2006 Aug 30;361(2):336-51. Epub 2006 Jun 30.

Department of Pharmacology and Experimental Therapeutics, Boston University School of Medicine, 715 Albany Street Boston, MA 02118, USA.

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http://dx.doi.org/10.1016/j.jmb.2006.06.028DOI Listing
August 2006

Role of caveolin-1 and cholesterol in transmembrane fatty acid movement.

Biochemistry 2006 Mar;45(9):2882-93

Department of Biochemistry, Boston University School of Medicine, 715 Albany Street, Boston, Massachusetts 02118, USA.

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http://dx.doi.org/10.1021/bi051999bDOI Listing
March 2006