Zobrazeno 1 - 7
of 7
pro vyhledávání: '"Kristen L. Arienti"'
Autor:
Lars Karlsson, Neelakandha S. Mani, Todd K. Jones, Steven Nguyen, Pragnya J. Desai, Cheryl A. Grice, Kristen L. Arienti, Robin L. Thurmond, Frank U. Axe, James P. Edwards, Mike Randal, Siquan Sun, Danielle K. Wiener, Michael K. Ameriks, Jing Liu, Alice Lee-Dutra, Damara Gebauer
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:2370-2374
A series of pyrazole-based thioethers were prepared and found to be potent cathepsin S inhibitors. A crystal structure of 13 suggests that the thioether moiety may bind to the S3 pocket of the enzyme. Additional optimization led to the discovery of a
Checkpoint Kinase Inhibitors: SAR and Radioprotective Properties of a Series of 2-Arylbenzimidazoles
Autor:
Anders Brunmark, Danielle K. Neff, Shelby Crawford, Lars Karlsson, Kelly J. McClure, Alice Lee, J. Guy Breitenbucher, Chennagiri R. Pandit, Frank U. Axe, Kristen L. Arienti, Jon Blevitt, Liming Huang
Publikováno v:
Journal of Medicinal Chemistry. 48:1873-1885
The discovery of a series of novel, potent, and highly selective inhibitors of the DNA damage control kinase chk2 is disclosed. Here we report the first SAR study around inhibitors of this kinase. High-throughput screening of purified human chk2 led
Autor:
William Charles Ripka, Scott W. Nelson, Kevin M. Short, Michael J. Newman, Richard B. Honzatko, Karl Norvell, Frank U. Axe, Kristen L. Arienti, Deborah H. Slee, Tassie L. Collins, Todd K. Jones, Jun-young Choe, Herbert J. Fromm, Rachel Denise Anne Kimmich, Suzanne J. Romano
Publikováno v:
Journal of Biological Chemistry. 278:51176-51183
A highly constrained pseudo-tetrapeptide (OC252-324) further defines a new allosteric binding site located near the center of fructose-1,6-bisphosphatase. In a crystal structure, pairs of inhibitory molecules bind to opposite faces of the enzyme tetr
Autor:
James P. Edwards, James W. Kong, Kristen L. Arienti, Keith B. Marschke, Thomas R. Caferro, Robert I. Higuchi, Luc J. Farmer, Robert L. Davis, Todd K. Jones, Josef D. Ringgenberg, Lawrence G. Hamann
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 9:1335-1340
A series of human androgen receptor (hAR) agonists based on 4-alkyl-; 4,4-dialkyl-; and 3,4-dialkyl-1,2,3,4-tetrahydro-8-pyridono[5,6-g]quinoline was synthesized and evaluated in competitive receptor binding assays and an androgen receptor cotransfec
Autor:
Neelakhanda S. Mani, Dale E. Mais, Francisco J. López, Kristen L. Arienti, Lin Zhi, Yun Oliver Long, William T. Schrader, Todd K. Jones, James P. Edwards, and Andrés Negro-Vilar, Thomas R. Caferro, Keith B. Marschke, Robert I. Higuchi
Publikováno v:
Journal of medicinal chemistry. 50(10)
Recent interest in orally available androgens has fueled the search for new androgens for use in hormone replacement therapy and as anabolic agents. In pursuit of this, we have discovered a series of novel androgen receptor modulators derived from 7H
Autor:
Haripada Khatuya, Alice Lee-Dutra, Lars Karlsson, J. Guy Breitenbucher, Steven Nguyen, Kristen L. Arienti, Michael D. Hack, Daniel J. Buzard, Robin L. Thurmond, James P. Edwards, Pragnya J. Desai
Publikováno v:
Bioorganicmedicinal chemistry letters. 16(23)
A series of 2-arylbenzimidazoles was synthesized and found to bind with high affinity to the human histamine H4 receptor. Structure–activity relationships were investigated through library preparation and evaluation as well as traditional medicinal
Autor:
Robert I. Higuchi, Kristen L. Arienti, Francisco J. López, Neelakhanda S. Mani, Dale E. Mais, Thomas R. Caferro, Yun Oliver Long, Todd K. Jones, James P. Edwards, Lin Zhi, William T. Schrader, Andrés Negro-Vilar, Keith B. Marschke
Publikováno v:
Journal of Medicinal Chemistry; May2007, Vol. 50 Issue 10, p2486-2496, 11p