L
Lisa M. Shewchuk
Researcher at Research Triangle Park
Publications - 41
Citations - 3323
Lisa M. Shewchuk is an academic researcher from Research Triangle Park. The author has contributed to research in topics: Cathepsin K & Cyclin-dependent kinase 2. The author has an hindex of 24, co-authored 40 publications receiving 3146 citations. Previous affiliations of Lisa M. Shewchuk include Howard Hughes Medical Institute.
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Journal ArticleDOI
A Unique Structure for Epidermal Growth Factor Receptor Bound to GW572016 (Lapatinib): Relationships among Protein Conformation, Inhibitor Off-Rate, and Receptor Activity in Tumor Cells
Edgar R. Wood,Anne T. Truesdale,Octerloney B. McDonald,Derek Yuan,Anne M. Hassell,Scott Howard Dickerson,Byron Ellis,Christopher Pennisi,Earnest Horne,Karen Lackey,Krystal J. Alligood,David W. Rusnak,Tona M. Gilmer,Lisa M. Shewchuk +13 more
TL;DR: The slow off-rate ofGW572016 correlates with a prolonged down-regulation of receptor tyrosine phosphorylation in tumor cells and the differences in the off-rates of these drugs and the ability of GW572016 to inhibit ErbB-2 can be explained by the enzyme-inhibitor structures.
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Escherichia coli biotin holoenzyme synthetase/bio repressor crystal structure delineates the biotin- and DNA-binding domains.
TL;DR: The three-dimensional structure of BirA, the repressor of the Escherichia coli biotin biosynthetic operon, has been determined by x-ray crystallography and refined to a crystallographic residual of 19.0% at 2-A resolution.
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Oxindole-based inhibitors of cyclin-dependent kinase 2 (CDK2): design, synthesis, enzymatic activities, and X-ray crystallographic analysis.
H. N. Bramson,J. Corona,Stephen T. Davis,Scott Howard Dickerson,Mark P. Edelstein,Stephen V. Frye,Robert T. Gampe,Philip A. Harris,A.M. Hassell,William D. Holmes,Robert N. Hunter,Karen Lackey,B. Lovejoy,Michael Joseph Luzzio,Valerie G. Montana,Warren J. Rocque,David W. Rusnak,Lisa M. Shewchuk,James Marvin Veal,Duncan Herrick Walker,Lee F. Kuyper +20 more
TL;DR: Two closely related classes of oxindole-based compounds were shown to potently inhibit cyclin-dependent kinase 2 (CDK2) and showed potential utility in the prevention of chemotherapy-induced alopecia.
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Binding mode of the 4-anilinoquinazoline class of protein kinase inhibitor: X-ray crystallographic studies of 4-anilinoquinazolines bound to cyclin-dependent kinase 2 and p38 kinase.
Lisa M. Shewchuk,Anne M. Hassell,Bruce Wisely,Warren J. Rocque,William D. Holmes,James Marvin Veal,Lee F. Kuyper +6 more
TL;DR: In both inhibitor/kinase structures, the 4-anilinoquinazoline was bound in the ATP site with the quinazoline ring system oriented along the peptide strand that links the two domains of the protein and with the anilino substituent projecting into a hydrophobic pocket within the protein interior.
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Prevention of chemotherapy-induced alopecia in rats by CDK inhibitors.
Stephen T. Davis,Bill G. Benson,H. Neal Bramson,Dennis E. Chapman,Scott Howard Dickerson,Karen M. Dold,Derek J. Eberwein,Mark Edelstein,Stephen V. Frye,Robert T. Gampe,Robert J. Griffin,Philip A. Harris,Anne M. Hassell,William D. Holmes,Robert N. Hunter,Victoria B. Knick,Karen Lackey,Brett Lovejoy,Michael Joseph Luzzio,Doris M. Murray,Patricia G. Parker,Warren J. Rocque,Lisa M. Shewchuk,James Marvin Veal,Duncan Herrick Walker,Lee F. Kuyper +25 more
TL;DR: Inhibition of cyclin-dependent kinase 2 (CDK2) represents a potentially useful approach for the prevention of CIA in cancer patients by arresting the cell cycle and reducing the sensitivity of the epithelium to many cell cycle-active antitumor agents.