Publications by authors named "Jeanne A Stuckey"

77Publications

Discovery of Potent Small-Molecule Inhibitors of MLL Methyltransferase.

ACS Med Chem Lett 2020 Jun 14;11(6):1348-1352. Epub 2020 May 14.

Department of Medicinal Chemistry, Department of Internal Medicine, Department of Pharmacology, Department of Pathology, and Life Sciences Institute, University of Michigan, Ann Arbor, Michigan 48109, United States.

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http://dx.doi.org/10.1021/acsmedchemlett.0c00229DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7294728PMC
June 2020

A Potent and Selective Small-Molecule Degrader of STAT3 Achieves Complete Tumor Regression In Vivo.

Cancer Cell 2019 11;36(5):498-511.e17

Rogel Cancer Center, University of Michigan, Ann Arbor, MI 48109, USA; Department of Internal Medicine, University of Michigan, Ann Arbor, MI 48109, USA; Department of Pharmacology, University of Michigan, Ann Arbor, MI 48109, USA; Department of Medicinal Chemistry, University of Michigan, Ann Arbor, MI 48109, USA. Electronic address:

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http://dx.doi.org/10.1016/j.ccell.2019.10.002DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6880868PMC
November 2019

How Outer Coordination Sphere Modifications Can Impact Metal Structures in Proteins: A Crystallographic Evaluation.

Chemistry 2019 May 25;25(27):6773-6787. Epub 2019 Apr 25.

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

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http://dx.doi.org/10.1002/chem.201806040DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6510599PMC
May 2019

Structure-Based Design of N-(5-Phenylthiazol-2-yl)acrylamides as Novel and Potent Glutathione S-Transferase Omega 1 Inhibitors.

J Med Chem 2019 03 22;62(6):3068-3087. Epub 2019 Feb 22.

Key Laboratory of Drug Targeting and Drug Delivery System of Ministry of Education, West China School of Pharmacy , Sichuan University , No. 17 People's South Road , Chengdu 610041 , P. R. China.

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http://pubs.acs.org/doi/10.1021/acs.jmedchem.8b01960
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http://dx.doi.org/10.1021/acs.jmedchem.8b01960DOI Listing
March 2019

Design, Synthesis, and Biological Evaluation of 4-Quinoline Carboxylic Acids as Inhibitors of Dihydroorotate Dehydrogenase.

J Med Chem 2018 06 14;61(12):5162-5186. Epub 2018 May 14.

Life Sciences Institute and Department of Biological Chemistry , University of Michigan , Ann Arbor , Michigan 48109 , United States.

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http://dx.doi.org/10.1021/acs.jmedchem.7b01862DOI Listing
June 2018

Discovery of a Highly Potent, Cell-Permeable Macrocyclic Peptidomimetic (MM-589) Targeting the WD Repeat Domain 5 Protein (WDR5)-Mixed Lineage Leukemia (MLL) Protein-Protein Interaction.

J Med Chem 2017 06 12;60(12):4818-4839. Epub 2017 Jun 12.

Department of Medicinal Chemistry, ‡Department of Internal Medicine, §Comprehensive Cancer Center, ∥Department of Pathology, ⊥Howard Hughes Medical Institute, #Department of Biological Chemistry, ∇Department of Pharmaceutical Sciences, ○Department of Pharmacology, and ¶Life Sciences Institute, University of Michigan , Ann Arbor, Michigan 48109, United States.

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http://dx.doi.org/10.1021/acs.jmedchem.6b01796DOI Listing
June 2017

d-Cysteine Ligands Control Metal Geometries within De Novo Designed Three-Stranded Coiled Coils.

Chemistry 2017 Jun 26;23(34):8232-8243. Epub 2017 May 26.

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

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http://dx.doi.org/10.1002/chem.201700660DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5518473PMC
June 2017

Buried Hydrogen Bond Interactions Contribute to the High Potency of Complement Factor D Inhibitors.

ACS Med Chem Lett 2016 Dec 13;7(12):1092-1096. Epub 2016 Sep 13.

Departments of Internal Medicine and Biological Chemistry and Life Sciences Institute, University of Michigan , Ann Arbor, Michigan 48109, United States.

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http://dx.doi.org/10.1021/acsmedchemlett.6b00299DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5151139PMC
December 2016

Molecular Mechanism for Isoform-Selective Inhibition of Acyl Protein Thioesterases 1 and 2 (APT1 and APT2).

ACS Chem Biol 2016 12 31;11(12):3374-3382. Epub 2016 Oct 31.

Program in Chemical Biology, ‡Department of Chemistry, §Department of Biophysics, and ∥Life Sciences Institute, University of Michigan , 930 N. University Ave., Ann Arbor, Michigan 48109, United States.

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http://dx.doi.org/10.1021/acschembio.6b00720DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5359770PMC
December 2016

D3R grand challenge 2015: Evaluation of protein-ligand pose and affinity predictions.

J Comput Aided Mol Des 2016 09 30;30(9):651-668. Epub 2016 Sep 30.

Drug Design Data Resource, Center for Research in Biological Systems, University of California, San Diego, 9500 Gilman Drive, La Jolla, CA, 92093, USA.

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http://dx.doi.org/10.1007/s10822-016-9946-8DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5562487PMC
September 2016

Mechanistic evaluation and transcriptional signature of a glutathione S-transferase omega 1 inhibitor.

Nat Commun 2016 10 5;7:13084. Epub 2016 Oct 5.

Department of Pharmacology and Pharmaceutical Sciences, School of Pharmacy, University of Southern California, 1985 Zonal Avenue, Los Angeles, California 90033, USA.

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http://dx.doi.org/10.1038/ncomms13084DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5059489PMC
October 2016

High-resolution crystal structures of Colocasia esculenta tarin lectin.

Glycobiology 2017 01 24;27(1):50-56. Epub 2016 Aug 24.

Department of Biological Chemistry, University of Michigan, 1150 W. Medical Center Drive, Ann Arbor, MI 48109, USA

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http://dx.doi.org/10.1093/glycob/cww083DOI Listing
January 2017

A Crystallographic Examination of Predisposition versus Preorganization in de Novo Designed Metalloproteins.

J Am Chem Soc 2016 09 2;138(36):11979-88. Epub 2016 Sep 2.

Department of Chemistry, ‡Biophysics Program, and §Life Sciences Institute, University of Michigan , Ann Arbor, Michigan 48109, United States.

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http://dx.doi.org/10.1021/jacs.6b07165DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5242185PMC
September 2016

CSAR 2014: A Benchmark Exercise Using Unpublished Data from Pharma.

J Chem Inf Model 2016 06 17;56(6):1063-77. Epub 2016 May 17.

Department of Medicinal Chemistry, College of Pharmacy, University of Michigan , 428 Church St., Ann Arbor, Michigan 48109-1065, United States.

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http://dx.doi.org/10.1021/acs.jcim.5b00523DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5228621PMC
June 2016

KRAS Engages AGO2 to Enhance Cellular Transformation.

Cell Rep 2016 Feb 4;14(6):1448-1461. Epub 2016 Feb 4.

Michigan Center for Translational Pathology, University of Michigan, Ann Arbor, MI 48109, USA; Department of Pathology, University of Michigan, Ann Arbor, MI 48109, USA; Howard Hughes Medical Institute, University of Michigan, Ann Arbor, MI 48109, USA; Comprehensive Cancer Center, University of Michigan, Ann Arbor, MI 48109, USA; Department of Urology, University of Michigan, Ann Arbor, MI 48109, USA. Electronic address:

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http://dx.doi.org/10.1016/j.celrep.2016.01.034DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4758864PMC
February 2016

Conformational Sampling and Binding Site Assessment of Suppression of Tumorigenicity 2 Ectodomain.

PLoS One 2016 6;11(1):e0146522. Epub 2016 Jan 6.

Ministry of Education Key Laboratory of Protein Science, Center for Structural Biology, School of Life Sciences, Tsinghua University, Beijing 100084, China.

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http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0146522PLOS
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4703388PMC
July 2016

Structure-Based Design of γ-Carboline Analogues as Potent and Specific BET Bromodomain Inhibitors.

J Med Chem 2015 Jun 16;58(12):4927-39. Epub 2015 Jun 16.

†Departments of Medicinal Chemistry, ‡Internal Medicine, §Pharmacology, and ∥Biological Chemistry, ⊥Life Sciences Institute, and #Comprehensive Cancer Center, University of Michigan, Ann Arbor, Michigan 48109, United States.

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http://dx.doi.org/10.1021/acs.jmedchem.5b00613DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5474678PMC
June 2015

Structural analysis and binding properties of isoforms of tarin, the GNA-related lectin from Colocasia esculenta.

Biochim Biophys Acta 2015 Jan 23;1854(1):20-30. Epub 2014 Oct 23.

Instituto de Química, Universidade Federal do Rio de Janeiro (UFRJ), Rio de Janeiro 21941-909, Brazil. Electronic address:

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http://dx.doi.org/10.1016/j.bbapap.2014.10.013DOI Listing
January 2015

Crystal structure of patatin-17 in complex with aged and non-aged organophosphorus compounds.

PLoS One 2014 23;9(9):e108245. Epub 2014 Sep 23.

Life Sciences Institute and Department of Biological Chemistry, University of Michigan, Ann Arbor, Michigan, United States of America.

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http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0108245PLOS
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4172759PMC
December 2015

Insights into substrate and metal binding from the crystal structure of cyanobacterial aldehyde deformylating oxygenase with substrate bound.

ACS Chem Biol 2014 Nov 15;9(11):2584-93. Epub 2014 Sep 15.

Department of Chemistry, ‡Life Sciences Institute, and §Department of Biological Chemistry, University of Michigan , Ann Arbor, Michigan 48109, United States.

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http://dx.doi.org/10.1021/cb500343jDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4245163PMC
November 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

Mechanistic characterization and crystal structure of a small molecule inactivator bound to plasminogen activator inhibitor-1.

Proc Natl Acad Sci U S A 2013 Dec 2;110(51):E4941-9. Epub 2013 Dec 2.

Departments of Pathology and Internal Medicine, Division of Cardiovascular Medicine, University of Michigan Medical School, Ann Arbor, MI 48109.

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http://dx.doi.org/10.1073/pnas.1216499110DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3870673PMC
December 2013

CSAR data set release 2012: ligands, affinities, complexes, and docking decoys.

J Chem Inf Model 2013 Aug 10;53(8):1842-52. Epub 2013 May 10.

Department of Medicinal Chemistry, University of Michigan, 428 Church St., Ann Arbor, Michigan 48109-1065, USA.

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http://dx.doi.org/10.1021/ci4000486DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3753885PMC
August 2013

CSAR benchmark exercise 2011-2012: evaluation of results from docking and relative ranking of blinded congeneric series.

J Chem Inf Model 2013 Aug 10;53(8):1853-70. Epub 2013 May 10.

Department of Medicinal Chemistry, University of Michigan, Ann Arbor, Michigan 48109-1065, USA.

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http://dx.doi.org/10.1021/ci400025fDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3753884PMC
August 2013

Ordering a dynamic protein via a small-molecule stabilizer.

J Am Chem Soc 2013 Mar 22;135(9):3363-6. Epub 2013 Feb 22.

Program in Chemical Biology, University of Michigan, Ann Arbor, Michigan 48109, United States.

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http://dx.doi.org/10.1021/ja3122334DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3607081PMC
March 2013

Structure-based discovery of BM-957 as a potent small-molecule inhibitor of Bcl-2 and Bcl-xL capable of achieving complete tumor regression.

J Med Chem 2012 Oct 2;55(19):8502-14. Epub 2012 Oct 2.

Comprehensive Cancer Center, University of Michigan, 1500 East Medical Center Drive, Ann Arbor, MI 48109-0934, USA.

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http://dx.doi.org/10.1021/jm3010306DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3495162PMC
October 2012

Structure-based design of potent Bcl-2/Bcl-xL inhibitors with strong in vivo antitumor activity.

J Med Chem 2012 Jul 2;55(13):6149-61. Epub 2012 Jul 2.

Comprehensive Cancer Center and Departments of Internal Medicine, Pharmacology and Medicinal Chemistry, University of Michigan, Ann Arbor, MI 48109-0934, USA.

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http://dx.doi.org/10.1021/jm300608wDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3417242PMC
July 2012

Design of Bcl-2 and Bcl-xL inhibitors with subnanomolar binding affinities based upon a new scaffold.

J Med Chem 2012 May 10;55(10):4664-82. Epub 2012 May 10.

Comprehensive Cancer Center and Department of Internal Medicine, University of Michigan , 1500 East Medical Center Drive, Ann Arbor, Michigan 48109-0934, United States.

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http://pubs.acs.org/doi/10.1021/jm300178u
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http://dx.doi.org/10.1021/jm300178uDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3397176PMC
May 2012

Structural basis for the enhanced stability of highly fluorinated proteins.

Proc Natl Acad Sci U S A 2012 Mar 12;109(13):4810-5. Epub 2012 Mar 12.

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

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http://dx.doi.org/10.1073/pnas.1120112109DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3324029PMC
March 2012

Hydrolytic catalysis and structural stabilization in a designed metalloprotein.

Nat Chem 2011 Nov 27;4(2):118-23. Epub 2011 Nov 27.

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

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http://dx.doi.org/10.1038/nchem.1201DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3270697PMC
November 2011

CSAR benchmark exercise of 2010: selection of the protein-ligand complexes.

J Chem Inf Model 2011 Sep 22;51(9):2036-46. Epub 2011 Jul 22.

Department of Medicinal Chemistry, University of Michigan, Ann Arbor, Michigan 48109-1065, United States.

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http://dx.doi.org/10.1021/ci200082tDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3180202PMC
September 2011

A dual-readout F2 assay that combines fluorescence resonance energy transfer and fluorescence polarization for monitoring bimolecular interactions.

Assay Drug Dev Technol 2011 Aug 11;9(4):382-93. Epub 2011 Mar 11.

Department of Pharmacology and Emory Chemical Biology Discovery Center, Emory University School of Medicine, Atlanta, Georgia, USA.

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http://dx.doi.org/10.1089/adt.2010.0292DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3148108PMC
August 2011

Structural bases for the different anti-fibrillatory effects of chloroquine and quinidine.

Cardiovasc Res 2011 Mar 13;89(4):862-9. Epub 2011 Jan 13.

Center for Arrhythmia Research, University of Michigan, 5025 Venture Dr., Ann Arbor, MI 48108, USA.

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http://dx.doi.org/10.1093/cvr/cvr008DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3039250PMC
March 2011

High-resolution x-ray structure and functional analysis of the murine norovirus 1 capsid protein protruding domain.

J Virol 2010 Jun 24;84(11):5695-705. Epub 2010 Mar 24.

Department of Microbiology and Immunology, University of Michigan Medical School, Ann Arbor, Michigan 48109, USA.

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http://dx.doi.org/10.1128/JVI.00316-10DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2876589PMC
June 2010

Tyrosines 868, 966, and 972 in the kinase domain of JAK2 are autophosphorylated and required for maximal JAK2 kinase activity.

Mol Endocrinol 2010 May 19;24(5):1062-76. Epub 2010 Mar 19.

Department of Molecular and Integrative Physiology, The University of Michigan Medical School, Ann Arbor, Michigan 48109-5622, USA.

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http://dx.doi.org/10.1210/me.2009-0355DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2870937PMC
May 2010

The tail of KdsC: conformational changes control the activity of a haloacid dehalogenase superfamily phosphatase.

J Biol Chem 2009 Oct 2;284(44):30594-603. Epub 2009 Sep 2.

Department of Medicinal Chemistry, College of Pharmacy, University of Michigan, Ann Arbor, Michigan 48109, USA.

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http://dx.doi.org/10.1074/jbc.M109.012278DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2781614PMC
October 2009

Switching the chirality of the metal environment alters the coordination mode in designed peptides.

Angew Chem Int Ed Engl 2009 ;48(40):7371-4

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

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http://dx.doi.org/10.1002/anie.200902166DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3014729PMC
December 2009

Conserved residues in the HAMP domain define a new family of proposed bipartite energy taxis receptors.

J Bacteriol 2009 Jan 24;191(1):375-87. Epub 2008 Oct 24.

Department of Microbiology and Immunology, University of Michigan, Ann Arbor, Michigan, USA.

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http://dx.doi.org/10.1128/JB.00578-08DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2612422PMC
January 2009

Interaction of a cyclic, bivalent smac mimetic with the x-linked inhibitor of apoptosis protein.

Biochemistry 2008 Sep 22;47(37):9811-24. Epub 2008 Aug 22.

Department of Internal Medicine, Comprehensive Cancer Center, University of Michigan, 1500 East Medical Center Drive, Ann Arbor, Michigan 48109, USA.

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http://dx.doi.org/10.1021/bi800785yDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2784912PMC
September 2008

LplA1-dependent utilization of host lipoyl peptides enables Listeria cytosolic growth and virulence.

Mol Microbiol 2007 Nov 1;66(3):758-70. Epub 2007 Oct 1.

Department of Microbiology and Immunology, University of Michigan Medical School, 1150 W. Medical Center Drive, 5641 Medical Sciences II, Ann Arbor, MI 48109-0620, USA.

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http://doi.wiley.com/10.1111/j.1365-2958.2007.05956.x
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http://dx.doi.org/10.1111/j.1365-2958.2007.05956.xDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2367003PMC
November 2007

Identifying important structural characteristics of arsenic resistance proteins by using designed three-stranded coiled coils.

Proc Natl Acad Sci U S A 2007 Jul 3;104(29):11969-74. Epub 2007 Jul 3.

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

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http://dx.doi.org/10.1073/pnas.0701979104DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1924535PMC
July 2007

Laboratory evolution of one disulfide isomerase to resemble another.

Proc Natl Acad Sci U S A 2007 Jul 3;104(28):11670-5. Epub 2007 Jul 3.

Medical Scientist Training Program, University of Michigan, Ann Arbor, MI 48109, USA.

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http://dx.doi.org/10.1073/pnas.0704692104DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1906722PMC
July 2007

Modeling the tertiary structure of the patatin domain of neuropathy target esterase.

Protein J 2007 Apr;26(3):165-72

Toxicology Program, Department of Environmental Health Sciences, The University of Michigan, Ann Arbor, MI 48109, USA.

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http://dx.doi.org/10.1007/s10930-006-9058-8DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6643263PMC
April 2007

Crystal structure of banana lectin reveals a novel second sugar binding site.

Glycobiology 2005 Oct 8;15(10):1033-42. Epub 2005 Jun 8.

Life Sciences Institute, University of Michigan, Ann Arbor, MI, USA.

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http://dx.doi.org/10.1093/glycob/cwi088DOI Listing
October 2005

Two substrate-targeting sites in the Yersinia protein tyrosine phosphatase co-operate to promote bacterial virulence.

Mol Microbiol 2005 Mar;55(5):1346-56

Department of Molecular Genetics and Microbiology and Center for Infectious Diseases, State University of New York at Stony Brook, Stony Brook, NY 11794-5222, USA.

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http://dx.doi.org/10.1111/j.1365-2958.2005.04477.xDOI Listing
March 2005

Development and optimization of a binding assay for the XIAP BIR3 domain using fluorescence polarization.

Anal Biochem 2004 Sep;332(2):261-73

University of Michigan Comprehensive Cancer Center, Departments of Internal Medicine and Medicinal Chemistry, University of Michigan, 1500 E. Medical Center Drive, Ann Arbor, MI 48109-0934, USA.

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http://linkinghub.elsevier.com/retrieve/pii/S000326970400494
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http://dx.doi.org/10.1016/j.ab.2004.05.055DOI Listing
September 2004

Function of His185 in Aquifex aeolicus 3-deoxy-D-manno-octulosonate 8-phosphate synthase.

J Mol Biol 2002 Nov;324(2):205-14

Department of Biochemistry and Molecular Biology, Wayne State University School of Medicine, Detroit, MI 48201, USA.

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http://dx.doi.org/10.1016/s0022-2836(02)01096-3DOI Listing
November 2002

Cloning, expression, and characterization of the Galalpha 1,3Gal high affinity lectin from the mushroom Marasmius oreades.

J Biol Chem 2002 Apr 8;277(17):15002-5. Epub 2002 Feb 8.

Department of Biological Chemistry, University of Michigan, Ann Arbor, Michigan 48109-0606, USA.

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http://dx.doi.org/10.1074/jbc.M200165200DOI Listing
April 2002

A unique carbohydrate binding domain targets the lafora disease phosphatase to glycogen.

J Biol Chem 2002 Jan 5;277(4):2377-80. Epub 2001 Dec 5.

Life Sciences Institute and Department of Biological Chemistry, and the Biophysics Research Division, University of Michigan, Ann Arbor, Michigan 48109-0606, USA.

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http://www.jbc.org/lookup/doi/10.1074/jbc.C100686200
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http://dx.doi.org/10.1074/jbc.C100686200DOI Listing
January 2002