Zobrazeno 1 - 10
of 17
pro vyhledávání: '"Kimberly Suzanne Para"'
Autor:
Malcolm MacKenny, Alan Stobie, Christopher James Deur, Keri Lynn Greene, Cory Michael Stiff, Xinmin Gan, Paul V. Fish, Florian Wakenhut, Kimberly Suzanne Para, Keith A. Reeves, D.W.T. Hoople, Gavin A. Whitlock, Thomas Ryckmans
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:2562-2566
Single enantiomer (SS) and (RR) 2-[(phenoxy)(phenyl)methyl]morpholine derivatives 5, 8-23 are inhibitors of monoamine reuptake. Target compounds were prepared using an enantioselective synthesis employing a highly specific enzyme-catalysed resolution
Autor:
Keri Lynn Greene, Melean Visnick, Christine Nylund Kolz, James L. Mobley, Thomas B. Lanni, Kimberly Suzanne Para, Theodore J. Baginski, Marya Liimatta, David T. Dudley
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:756-760
The Type 1 PI3Kinases comprise a family of enzymes, which primarily phosphorylate PIP2 to give the second messenger PIP3, a key player in many intracellular signaling processes [Science, 2002, 296, 1655; Trends Pharmacol. Sci.2003, 24, 366]. Of the f
Autor:
Kimberly Suzanne Para, J. Ronald Rubin, Elizabeth A. Lunney, James H. Fergus, Christine Humblet, Tomi K. Sawyer, and James S. Marks
Publikováno v:
Journal of the American Chemical Society. 119:12471-12476
The SH2 domain of pp60c-src (Src), a nonreceptor tyrosine kinase, facilitates signal transduction in a number of cell types through binding to cognate phosphorylated protein sequences. Phosphotyrosine-containing peptides have been shown to bind to th
Autor:
Roman Herrera, Elizabeth A. Lunney, Kimberly Suzanne Para, Narayanan Surendran, James H. Fergus, Aurash Shahripour, Mark Stephen Plummer, Susan E. Hubbell, Christine Humblet, Barbra H. Stewart, Tomi K. Sawyer, Alan R. Saltiel, Charles J. Stankovic, James S. Marks
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 7:1909-1914
Incorporation of 4-phosphonodifluoromethyl-phenylalanine (F2Pmp) and 4-phosphono-phenylalanine into SH2 targeted peptides and peptidomimetic ligands was found to effect binding affinity and selectivity of these ligands toward the Src and Abl SH2 doma
Autor:
Tomi K. Sawyer, Kimberly Suzanne Para, Alan R. Saltiel, Debra R. Holland, James S. Marks, James H. Fergus, Elizabeth A. Lunney, J. R. Rubin, Christine Humblet, Aurash Shahripour, Mark Stephen Plummer
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 7:1107-1112
Based on the X-ray structures of the pp60Src (Src) SH2 domain complexed with two high affinity phosphopeptide ligands (Glu-Pro-Gln-pTyr-Glu-Glu-Ile-Pro-Ile-Tyr-Leu, and Ac-pTyr-Glu- D -Hcy-NH2; Hcy = homocyclohexylalanine), we report herein the desig
Autor:
Roman Herrera, Elizabeth A. Lunney, James H. Fergus, Charles J. Stankovic, Christine Humblet, Kimberly Suzanne Para, Susan E. Hubbell, Tomi K. Sawyer, James S. Marks, Aurash Shahripour, Alan R. Saltiel, Mark Stephen Plummer
Publikováno v:
Bioorganic & Medicinal Chemistry. 5:41-47
Potent ligands of the Src SH2 domain, discovered through structure-based drug design efforts, with the general structure Ac-pTyr-Glu-NRR′ are disclosed.
Autor:
Kimberly Suzanne Para, Christine Humblet, Charles J. Stankovic, Susan E. Hubbell, J. R. Rubin, Roman Herrera, Elizabeth A. Lunney, James S. Marks, Tomi K. Sawyer, Alan R. Saltiel, Aurash Shahripour, Mark Stephen Plummer, James H. Fergus
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 6:1209-1214
We have designed and synthesized a series of phosphorylated penta- and tri-peptides of general structures Rx-Glu-Glu-Ile-Glu and Rx-Glu- D -Trp-NH2, where Rx represents a phosphotyrosine mimetic. These peptides show binding affinity to pp60src SH2 do
Autor:
Kimberly Suzanne Para, Carolyn Nouhan, Edmund L. Ellsworth, J. V. N. Vara Prasad, Alexander Pavlovsky, Donna Ferguson, Peter J. Tummino
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 6:1133-1138
Systematic substitutions on 6-phenyl and 3-SCH 2 Ph rings of inhibitor 1 , were carried out to optimize the inhibitory activity against HIV PR. These studies lead to 3-Sbenzyl esters with enhanced potency. The X-ray crystal structure of 32 bound to H
Autor:
Peter J. Tummino, Donna Ferguson, B. A. Steinbaugh, Kimberly Suzanne Para, Harriet W. Hamilton, J. V. N. Vara Prasad, Elizabeth A. Lunney, C. John Blankley
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 6:1099-1104
In a study of 4-hydroxy-pyran-2-ones as possible inhibitors of HIV protease, a series of compounds were synthesized following the Topliss operational scheme for substitution on a phenyl group at the 6 position of the pyrone. In addition, a number of
Publikováno v:
Journal of Heterocyclic Chemistry. 31:1619-1624
A series of 3-(substituted sulfanyl)-4-hydroxy-6-substituted-pyran-2-ones were synthesized for Human immunodeficiency virus-1 protease inhibition. These compounds were synthesized in a simple and convergent fashion to allow us a rapid preparation of