Zobrazeno 1 - 10
of 10
pro vyhledávání: '"Skalitzky Donald James"'
Autor:
Jie Gao, Skalitzky Donald James, Bing Yang, Junping Zhang, Charles A Lesch, Xiaolong Tian, Chenxi Qiao, Chad A. Van Huis, Clarke Taylor, Laura L. Carter, Tao Zheng, Weiping Zou, Rodney W. Morgan, Peter L. Toogood, Yahong Wang, Kellie Demock, Gary D. Glick, Xiao Hu, Jacques Moisan, Chrystal M. Paulos, JoAnn Scatina, Changxin Huo, Thomas Daniel Aicher, Alexander R. Hurd, Omar M Beleh, Ling-Yang Hao
Publikováno v:
Journal of medicinal chemistry. 64(18)
Retinoic acid receptor-related orphan receptor γ (RORc, RORγ, or NR1F3) is the nuclear receptor master transcription factor that drives the function and development of IL-17-producing T helper cells (Th17), cytotoxic T cells (Tc17), and subsets of
Autor:
Ron Sarver, Christopher Whitehead, Heidi Baum, James Hicks, Richard Gowan, Brian Sanchez, Xiao Kang Lu, Susan E. Bove, Joseph A. Cornicelli, Howard Miller, Sandra Lightle, Aurash B Shahripour, Katherine Welch, Craig Banotai, Jayvardhan Pandit, Mark S. Plummer, Timothy Braden, David Beidler, Adam Ogden, Skalitzky Donald James, Annise Paige Goodman, Howard Roark, Nalini Sadagopan, Charles J. Stankovic, Cindy Spessard, Xi Qiang Shen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:3438-3442
We identified potent, selective PDE2 inhibitors by optimizing residual PDE2 activity in a series of PDE4 inhibitors, while simultaneously minimizing PDE4 activity. These newly designed PDE2 inhibitors bind to the PDE2 enzyme in a cGMP-like mode in co
Autor:
Skalitzky Donald James, Craig Banotai, Jayvardhan Pandit, Adam Ogden, James Hicks, Annise Paige Goodman, Xiao Kang Lu, Howard Miller, Howard Roark, Susan E. Bove, Sandra Lightle, Aurash B Shahripour, Timothy Braden, Mark S. Plummer, Katherine Welch, Charles J. Stankovic, Ron Sarver, Joseph A. Cornicelli, Christopher Whitehead, Brian Sanchez, Nalini Sadagopan, Heidi Baum, Richard Gowan, David Beidler, Xi Qiang Shen, Cindy Spessard
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:3443-3447
Selective phosphodiesterase 2 (PDE2) inhibitors are shown to have efficacy in a rat model of osteoarthritis (OA) pain. We identified potent, selective PDE2 inhibitors by optimizing residual PDE2 activity in a series of phosphodiesterase 4 (PDE4) inhi
Autor:
Skalitzky Donald James, Karen A. Maegley, Stanley William Kupchinsky, Pei Pei Kung, Anne Ekker, Laura Anne Bloom, Leslie A. Kuhn, Peter W. Rose, Jerry J. Meng, Zehnder Luke Raymond, M. Catherine Johnson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:2829-2833
The structure-based design, chemical synthesis, and biological evaluation of novel MTAP substrates are described. These compounds incorporate various C5′-moieties and are shown to have different k cat / K m values compared with the natural MTAP sub
Autor:
Marakovits Joseph T, David R. Newell, Stephen E. Webber, Zdenek Hostomsky, Roger J. Griffin, Karen A. Maegley, Anne Ekker, Skalitzky Donald James, Bernard T. Golding, Robert Almassy, A. Hilary Calvert, Xiao-Hong Yu, Jianke Li, Eastman Brian Walter, Nicola J. Curtin
Publikováno v:
Journal of Medicinal Chemistry. 46:210-213
Novel tricyclic benzimidazole carboxamide poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors have been synthesized. Several compounds were found to be powerful chemopotentiators of temozolomide and topotecan in both A549 and LoVo cell lines. In vitro
Autor:
Suzanne Kyle, Michael A. Batey, Christopher R. Calabrese, Stacie S. Canan, Nicola J. Curtin, Stephen E. Webber, Zdenek Hostomsky, Karen A. Maegley, Huw D. Thomas, Lan-Zhen Wang, David R. Newell, Skalitzky Donald James
Publikováno v:
Molecular cancer therapeutics. 6(3)
Poly(ADP-ribose) polymerase (PARP)-1 (EC 2.4.2.30) is a nuclear enzyme that promotes the base excision repair of DNA breaks. Inhibition of PARP-1 enhances the efficacy of DNA alkylating agents, topoisomerase I poisons, and ionizing radiation. Our aim
Autor:
Mary Hess, Simon Bailey, Christie Lance Christopher, Jack H. Kellum, Brett H. Simmons, Guy A. McClellan, Paul S. Humphries, Kathleen M. Ogilvie, Jonathon V. Almaden, Skalitzky Donald James, Young Ha Kim, Shaoxian Sun, Thomas J. Carlson, David M. Wilhite, James D. Fraser, Zehnder Luke Raymond, Sandra J. Barnum, Quyen-Quyen T. Do
Publikováno v:
Bioorganicmedicinal chemistry letters. 16(23)
A series of novel pyridine-3-propanoic acids was synthesized. A structure–activity relationship study of these compounds led to the identification of potent dual PPARα/γ agonists with varied isoform selectivity. Based on the results of efficacy s
Autor:
Nicola J. Curtin, Canan-Koch Stacie S, Elena Notarianni, Jianke Li, Suzanne Kyle, Stephen E. Webber, Barbara W. Durkacz, Skalitzky Donald James, Michael A. Batey, Karen A. Maegley, David R. Newell, Ian J. Stratford, Robert Arnold Kumpf, Kaye J. Williams, Huw D. Thomas, A. Hilary Calvert, Robert Almassy, Zdenek Hostomsky, Lan-Zhen Wang, Stephanie Barton, Christopher R. Calabrese
Publikováno v:
Scopus-Elsevier
Background: Poly(ADP-ribose) polymerase-1 (PARP-1) facilitates the repair of DNA strand breaks. Inhibiting PARP-1 increases the cytotoxicity of DNA-damaging chemotherapy and radiation therapy in vitro. Because classical PARP-1 inhibitors have limited
Autor:
Karen A. Maegley, Zdenek Hostomsky, Stephen E. Webber, Skalitzky Donald James, Bernard T. Golding, Alex William White, Xiao-Hong Yu, Jianke Li, Suzanne Kyle, Roger J. Griffin, Eastman Brian Walter, Nicola J. Curtin
Publikováno v:
Bioorganicmedicinal chemistry letters. 14(10)
The synthesis and biological evaluation of a new series of amine-substituted 2-arylbenzimidazole-4-carboxamide inhibitors of the DNA-repair enzyme poly(ADP-ribose) polymerase-1 (PARP-1) is reported. The introduction of an amine substituent at the 2-a
Autor:
Hiep T. Luu, Rose Ann Ferre, Fausto Maldonado, Peter S. Dragovich, Amy K. Patick, Skalitzky Donald James, Shella A. Fuhrman, Ye Hua, David A. Matthews, Shao Song Chu, Fora Chan, Edward L. Brown, Leora S. Zalman, Theodore O. Johnson, Eastman Brian Walter, Siegfried Reich, Michelle Yang, Stephen T. Worland, James W. Meador, Thomas F. Hendrickson
Publikováno v:
Journal of medicinal chemistry. 45(10)
Utilizing the tools of parallel synthesis and structure-based design, a new class of Michael acceptor-containing, irreversible inhibitors of human rhinovirus 3C protease (HRV 3CP) was discovered. These inhibitors are shown to inhibit HRV-14 3CP with