Brown Cancer Center. Making tomorrow BRIGHTER for everyone.

 

NMR - Major Users and Research Projects

Jason Chesney (BCC)

Our laboratory is using an NMR-based metabolomics approach to understand the regulation of glucose metabolism in cancer cells, via the activity of iPFK-2. We are using isotopomer analyses in conjunction with molecular biology approaches (e.g. siRNA) to modulate specific enzyme activities to further test the Warburg hypothesis and examine the fate of glucose carbon in transformed versus untransformed cell types.

Selected References:
Chesney J, Mitchell R, Benigni F, Bacher M, Spiegel L, Al-Abed Y, Han JH, Metz C, Bucala R. (1999) An inducible gene product for 6-phosphofructo-2-kinase with an AU-rich instability element: Role in tumor cell glycolysis and the Warburg effect. Proc. Natl. Acad. Sci. 96, 3047-3052

Atsumi T, Chesney J, Metz C, Leng L, Donnelly S, Makita Z, Mitchell R, Bucala R. (2002) High expression of inducible 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase (iPFK-2;
PFKFB3) in human cancers Cancer Research 62, 5881-5887


Teresa Fan (Dept. Chemistry UofL)

Our laboratory is using NMR methods in three major areas. (1) metabolomics characterization of cells and their responses to mutations and environmental insults and the mechanisms of Se compounds in these processes. (2) Structural characterization of the SECIS 3’-RNA species in regulation of SeCys incorporation into critical enzymes. (3) Analysis of soil organic matter chemistry and remediation against environmental toxicants. These projects all make use of the spectral editing capabilities of partially labeled samples. For example, isotopomer analysis is carried out using a combination of 2D 13C-1H edited experiments including HSQC, HCCHTOCSY and HSQC-TOCSY. We also make use of 77Se NMR for analyzing selenium metabolites involved in anticancer activity

Selected References:
T.W-M Fan (1996) Metabolite profiling by one- and two-dimensional NMR analysis of complex mixtures. Prog. NMR Spectrosc. 28, 161-219

Fan, T. W.-M., R. M. Higashi and A. N. Lane. (2000) “Chemical Characterization of a Chelator-Treated Soil Humate by Solution-State Multinuclear Two-Dimensional NMR with FTIR and Pyrolysis-GCMS”, Environmental Science and Technology 34, 1636-1646

Fan, T. W-M., Higashi, R.M.,. & Lane, A.N (2004) The Promise of Metabolomics in Cancer Molecular Therapeutics. Current Opin. Molec. Ther. In press Ramos, A., Lane, A.N., Hollingworth, D. & Fan, T.W-M.(2004) NMR determination of the secondary structure of the selenocysteine insertion element. Nucl. Acids Res. 32, 1746-1755

Robert Gray (Dept. Biochem. UofL)

Biochemistry of APRin. Our laboratory is using a variety of biochemical and biophysical methods to characterize the structure, stability and interactions of the alkaline proteinase inhibitor (APRin) from Pseudomonas aeruginosa. This proteinis an 11.5-kDa, high affinity, high specificity inhibitor of the serralysin class of zinc-dependent proteinases secreted by several Gram-negative bacteria (1-3).

We are using high resolution NMR to determine the solution conformation and dynamics of APRin. With 15N/13C labeled protein, most of the backbone and side chain assignments have been obtained (4). Analysis of the chemical shifts and NOEs reveals the secondary structure, and provides information about the dynamics on the N-terminal region essential for protease inhibition. The solution structure is currently being calculated. This will assist understanding the stability and binding mechanism of the inhibitor to its cognate metalloproteinase presently under investigation.

Selected References:
Feltzer, R. E., Gray, R. D., Dean, W. L., Pierce, W. M. Jr. (2000) Alkaline Proteinase Inhibitor of Pseudomonas aeruginosa. Interaction of Native and N-terminally Truncated Inhibitor Proteins with Pseudomonas Metalloproteinases. J. Biol. Chem. 275, 21002-21009

Feltzer, R. E., Trent, J. O., and Gray, R. D. (2003) Alkaline Proteinase Inhibitor of Pseudomonas aeruginosa: A Mutational and Molecular Dynamics Study of The Role of N-Terminal Residues in the Inhibition of Pseudomonas Alkaline Proteinase. J. Biol. Chem., 278, 25952-25957

Hege, T., Feltzer, R. E., Gray, R. D., and Baumann, U. (2001) Crystal Structure of a Complex Between Pseudomonas aeruginosa Alkaline Protease and its Cognate Inhibitor. J. Biol. Chem. 276, 35087-35092

Sengodagounder Arumugam, Robert D. Gray and Andrew N. Lane, 1H, 15N and 13C assignments of the alkaline proteinase inhibitor APRin from Pseudomonas aeruginosa. J. Biomolec NMR. Submitted

Andrew Lane (BCC)

My laboratory is concerned primarily with understanding the functional consequences of molecular interactions, especially protein-nucleic acid and protein-protein interactions, which often are the first step in starting a cascade of gene expression. We use high-resolution NMR methods to analyze the solution conformations and dynamics of macromolecules and more importantly the changes in these properties due to complex formation. In addition to our interests in detailed molecular structures and dynamics, we collaborate with a variety of cell and molecular biologists on the regulation of metabolic process that occur in cancer cells. This also uses NMR methods in concert with a variety of analytical techniques such as GC-MS, transcription and proteomics. We are therefore also involved in methods development to solve new problems as they arise.

Selected References:
Lane, A.N., Kelly, G., Ramos, A. & Frenkiel, T.A. (2001) Determining binding sites in protein-nucleic acid complexes by cross-saturation. J. Biomolec. NMR 21, 127-139 Nair, M., McIntosh, P.B., Frenkiel, T.A., Kelly, G., Taylor,I.A., Smerdon, S.J., & Lane A.N. (2003) NMR Structure of the DNA-binding Domain of the Cell Cycle protein, Mbp1 from Saccharomyces cerevisiae. Biochemistry, 42 1266 –1273

Gyi, J.I., Gao, D., Conn, G.L., Trent, J.O., Brown, T. & Lane, A.N. (2003) The solution structure of a DNA·RNA duplex containing 5-propynyl U and C; comparison with 5-Me modifications. Nucl. Acids Res 31, 2683-2693.

Ramos, A., Lane, A.N., Hollingworth, D. & Fan, T.W-M.(2004) NMR determination of the secondary structure of the selenocysteine insertion element. Nucl. Acids Res. 32, 1746-1755

Fan, T. W-M., Higashi, R.M.,. & Lane, A.N (2004) The Promise of Metabolomics in Cancer Molecular Therapeutics. Current Opin. Molec. Ther. 6:584-592

Booth, J., Brown, T., Vadhia, S.J., Lack, O., Cummins,W.J., Trent, J.O., & Lane A.N. .(2005) Determining the origin of the stabilization of DNA by 5- aminopropynylation of pyrimidines. Biochemistry. 44,4710-4719

Muriel Maurer (Dept. Chemistry UofL)

http://www.louisville.edu/a-s/chemistry/faculty/mcm/prf.htm
The Maurer group uses a combination of protein chemistry mass spectrometry and high resolution NMR to study molecular recognition and mecgan9osn in blood coagulation and related processes. Our focus is on the mechanism of thrombin activation of factor XIII.

A combination of kinetic studies, NMR, hydrogen/deuterium exchange coupled with MALDI-TOF mass spectrometry, and molecular modeling is being employed.

Selected References:
Turner, B.T., Sabo, T.M., Wilding, D., Maurer, M.C. (2004) “Mapping of Factor XIII Solvent Accessibility as a Function of Activation State Using Chemical Modification Methods”, Biochemistry 43, 9755-65.

Isetti, G., Maurer, M.C. (2004) “N-terminal Truncation of Factor XIII Activation Peptides (28-37) V34 and V34L does not Hinder Ability to Interact with Thrombin”, Biochemistry 43, 4150-4159.

Trumbo, T.A., Maurer, M.C. (2003) “V34I and V34A Substitutions Within the Factor XIII Activation Peptide Segment (28-41) Affect Interactions With the Thrombin Active Site”, Thrombosis and Haemostasis 89, 647-653.

Turner, B.T. Jr, Maurer, M.C. (2002) “Evaluating the Roles of Thrombin and Calcium in the Activation of Coagulation Factor XIII Using H/D Exchange and MALDI-TOF MS” Biochemistry 41, 7947-7954.

Anne-Frances Miller (Dept. Chemistry UK)

http://www.chem.uky.edu/research/miller/
The Miller research group uses a variety of spectroscopic techniques to address mechanisms of catalysis in the redox/metal dependent enzymes in the following three areas.

  1. Superoxide Dismutases. The Fe-SOD and Mn-SOD are being explored. EPR and NMR are used to explore the details of the mutant structures of these enzymes.
  2. Nitroreductase. Multidimensional NMR is applied to evaluate the mechanism of NR for the clean-up of the left-over of bombs.
  3. Peptide Deformylase. This is a novel drug target. The details of the catalytic mechanism and the interaction of the effective inhibitors with PDF are explored by spectroscopic pH titration using UV-visible spectrophotometer and NMR.

Selected References: Miller, Anne-Frances. Superoxide dismutases: active sites that save, but a protein that kills. Current Opinion in Chemical Biology (2004), 8(2), 162-168.

Jackson, Timothy A.; Yikilmaz, Emine; Miller, Anne-Frances; Brunold, Thomas C. Spectroscopic and computational study of a non-heme iron {Fe-NO}7 system: Exploring the geometric and electronic structures of the nitrosyl adduct of iron superoxide dismutase.J. Am. Chem. Soc. (2003), 125(27), 8348-8363.

Walsh, Joseph D.; Miller, Anne-Frances. NMR Shieldings and Electron Correlation Reveal Remarkable Behavior on the Part of the Flavin N5 Reactive Center. J. Phys. Chem. B (2003), 107(3), 854-863.

Koder, Ronald L.; Haynes, Chad A.; Rodgers, Michael E.; Rodgers, David W.; Miller, Anne-Frances. Flavin Thermodynamics Explain the Oxygen Insensitivity of Enteric Nitroreductases.Biochemistry (2002), 41(48), 14197-14205.

Peter Spielmann (Dept. Biochemistry, UK)

http://www.mc.uky.edu/biochemistry/Department/faculty/Spielmann/
We study and characterize the structural and dynamic features of damaged and undamaged DNA. These studies are used to elucidate the structural features for initial substrate recognition for the three main DNA repair pathways. Identification of these conformations may ultimately lead to the design of a new class of compounds to inhibit DNA repair and thereby enhance the effectiveness of DNA damaging antineoplastic therapeutics. Formation of carcinogen-DNA adducts alters the conformation and dynamics of the polymer in such a way that DNA conformations not accessible to undamaged DNA become available. These abnormal conformations may be the recognition motif for nucleotide excision repair (NER) and methyl directed mismatch repair (MMR). We have determined that covalent DNA damage alters both the structure and local high-frequency dynamics of the polymer for a preliminary set of molecules. These data suggest that there exist DNA conformations not easily accessible to undamaged DNA that become populated (or accessible) to damaged DNA. We use NMR techniques to obtain experimental data to describe the three-dimensional structure and internal dynamics of site-specifically damaged DNA and its undamaged counterpart. We have developed restrained molecular dynamics (rMD) computational procedures that provide good agreement between experimentally determined dynamic properties and dynamic features revealed by the rMD simulations.

Selected References:
Isaacs, R. J. and Spielmann, H. P. (2004) "A Model for Initial DNA Lesion Recognition by NER and MMR Based on Local Conformational Flexibility" DNA Repair 3, 455-64.

Isaacs, R. J. and Spielmann, H. P. (2004) "Insight into G-T Mismatch Recognition Using Molecular Dynamics with Time-Averaged Restraints Derived from NMR Spectroscopy" J. Am. Chem. Soc. 126, 583-90.

Isaacs, R. J., Rayens, W. T. and Spielmann, H. P. (2002) "Structural Differences in the NOE-Derived Structure of G-T Mismatched DNA Relative to Normal DNA Are Correlated With Differences in 13C Relaxation-Based Internal Dynamics" J. Mol. Biol 319 191-207.

Isaacs, R. J. and Spielmann, H. P. (2001) "NMR Evidence for Mechanical Coupling of Phosphate BI-BII Transitions With Deoxyribose Conformational Exchange in DNA" J. Mol. Biol. 311, 149-160.

Isaacs, R. J. and Spielmann, H. P. (2001) "Relationship of DNA Structure to Internal Dynamics: Correlation of Helical Parameters from NOE Based NMR Solution Structures of d(GCGTACGC)2 and d(CGCTAGCG)2 with 13C Order Parameters Implies Conformational Coupling in Dinucleotide Units" J. Mol. Biol. 307, 525-540.

Spielmann, H. P. (1998) "Dynamics of a Bis-intercalator DNA Complex by 1H Detected Natural Abundance 13C NMR Spectroscopy" Biochemistry 37, 16863-16876.

Spielmann, H. P. (1998) "Dynamics in Psoralen Damaged DNA by 1H Detected Natural Abundance 13C NMR Spectroscopy" Biochemistry 37, 5426 -5438.

John Trent (BCC): Nucleolin and G-quartet structures

www.browncancercenter.org/researchweb/trent/trent.html
We have expressed the RNA binding domains 1 and 2 of human nucleolin with the RGG tail in E. coli. The construct binds to a G-rich oligonucleotide aptamer DNA anticancer molecule, and is being further characterized by thermodynamic and NMR methods. The construct is being examined at high field by triple resonance methods using the 15N/13C labeled protein. The interaction surface with the DNA is being mapped using 15N labeled protein and a combination of HSQC-based chemical shift mapping and cross-saturation spectroscopy from the DNA imino protons. The combination of the protein structure, the residues involved in the protein-DNA interaction and the structure of the quartet will allow detailed modeling of the interaction, and provide the basis for understanding specific mutations on the functional properties. Isotopic labeling of the G-quartet by chemical synthesis is being used to verify features of the model.

Selected References:
Bates, PJ, Kahlon, JB, Thomas, SD, Trent, JO & Miller, DM (1999) J. Biol. Chem. 274, 26369-77

Dapic V, Abdomerovic V, Marrington R, Peberdy J, Rodger A, Trent JO, Bates PJ (2003) Biophysical and biological properties of quadruplex oligodeoxyribonucleotides Nucleic Acids Research 31, 2097-2107

Richard Wittebort (Dept. Chemistry UofL)

Our laboratory uses solid state NMR techniques to probe structure, dynamics and hydration in oligo and polypeptides. We have been measuring the chemical shielding tensors in single crystals of 13C and 15N labeled peptides. Recently we have been using ultrahigh field solid state NMR (at 18.8 T) to measure disorder and dynamics in unstructured proteins such as elastin. We are also expressing recombinant collagen peptides that are being studied by both solution and solid state NMR methods.

Selected References:
Chekmenev, E.Y., Xu, R.Z., Mashuta, M.S. and Wittebort, R.J., “Clycyl Ca Chemical Shielding in Tripeptides: Measurement by Solid-State NMR and Correlation with X-ray Structure and Theory”, J. Am. Chem. Soc., 124, 11894-11899 (2002)

Zhang, Q., E. Y. Chekmenev and R. J. Wittebort,"17O Quadrupole Coupling and Chemical Shielding Tensors in an H-bonded Carboxyl Group: Oxalic Acid", J. Am. Chem. Soc. 125, 9140-9146 (2003)

Cheruzel, L.E., Pometun, M.S., Cecil, M.R., Wittebort, R.J. and Buchanan, R.M., “Structures and Solid State Dynamics of One-Dimensional Water Chains Stabilized by Imidazole Channels”, Angewandte Chem, Int. Ed., 42, 5452-5455 (2003)

Chekmenev, E.Y., Zhang, Q., Waddell, K.W., Mashuta, M.S. and Wittebort, R.J. “15N Chemical Shielding in Glycyl Tripeptides: Measurement by Solid-State NMR and Correlation with X-ray Structure”, J. Am. Chem. Soc, 126, 379-384 (2004)

Pometun, M. S., Chekmenev, E.Y. and Wittebort, R.J. “Quantitative Observation of Backbone Disorder in Native Elastin”, J. Biol. Chem, 279, 7982-7987 (2004)

Other users:

J. Eaton (BCC): Oxygen-tolerant metabolism in HeLa cells

K. Ramos (Dept. Biochemistry): Metabolic profiling during nephrogenesis

R. Valdes (Dept. Pathology and Clinical Medicine): Structural identification of digoxin-like immunoreactive factors (DLIFs)

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