Zobrazeno 1 - 10
of 16
pro vyhledávání: '"Philip J. Merta"'
Publikováno v:
PLoS ONE, Vol 10, Iss 3, p e0114363 (2015)
Constitutive activation of the Janus kinase (JAK)/signal transducer and activator of transcription (STAT) axis is fundamental to the molecular pathogenesis of a host of hematological disorders, including acute leukemias and myeloproliferative neoplas
Externí odkaz:
https://doaj.org/article/0d6bfec9019c409fab628f1f0498b7b3
Autor:
Philip J. Merta, Amanda M. Olson, Fritz G. Buchanan, Nirupama B. Soni, Donald J. Osterling, Alan S. Florjancic, Debra Ferguson, David Maag, Eric F. Johnson, Yunsong Tong, Alexander R. Shoemaker, Maricel Torrent, Kenneth D. Bromberg, Thomas D. Penning, Loren M. Lasko
Publikováno v:
ACS Medicinal Chemistry Letters. 6:58-62
Aided by molecular modeling, compounds with a pyrimidine-based tricyclic scaffold were designed and confirmed to inhibit Wee1 kinase. Structure-activity studies identified key pharmacophores at the aminoaryl and halo-benzene regions responsible for b
Autor:
Kerren K. Swinger, Magdalena Przytulinska, Yunsong Tong, Alan S. Florjancic, Eric F. Johnson, Philip J. Merta, Kent D. Stewart, Thomas D. Penning, Nirupama B. Soni, Alexander R. Shoemaker, John E. Harlan, Haizhong Zhu
Publikováno v:
ACS Medicinal Chemistry Letters. 4:211-215
To investigate the role played by the unique pre-DFG residue Val 195 of Cdc7 kinase on the potency of azaindole-chloropyridines (1), a series of novel analogues with various chloro replacements were synthesized and evaluated for their inhibitory acti
Autor:
Zhi-Fu Tao, Nan-Horng Lin, Hing L. Sham, Saul H. Rosenberg, Yunsong Tong, Kent D. Stewart, Peter Kovar, Mai-Ha Bui, Zehan Chen, Haiying Zhang, Philip J. Merta, Chang Park, Akiyo Claiborne, Magdalena Przytulinska, Donald J. Osterling, Thomas J. Sowin, Gaoquan Li, Jennifer J. Bouska, Amanda Olson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:5665-5670
A series of 1,4-dihydroindeno[1,2-c]pyrazole compounds with a cyanopyridine moiety at the 3-position of the tricyclic pyrazole core was explored as potent CHK-1 inhibitors. The impact of substitutions at the 6 and/or 7-position of the core on pharmac
Autor:
Tianyuan Zhang, Richard A. G. Smith, Rohinton Edalji, Yu-Gui Gu, John L. Baranowski, William J. Sanders, Bruce A. Beutel, Liping Yu, Philip J. Hajduk, Annapur Gurulingappa Shivakumar, Stephan J. Kakavas, Frank L. Wagenaar, Darlene J. Balli, Steven F. Betz, Richard F. Clark, Kenneth M. Comess, Eric J. Hebert, J. Owen McCall, Jamey Mack, Linda E. Chovan, Randy E. Metzger, Thomas F. Holzman, Anne Y. Saiki, Sarah A. Dorwin, Niru B. Soni, Mai Bui, Angela M. Nilius, Susan J. Thornewell, Cooper Curt S, Mark E. Schurdak, Michael L. Coen, Rolf Wagner, Alan S. Florjancic, Philip J. Merta, Claude G. Lerner, Charlotte Woodall, Candace Black-Schaefer, John E. Harlan, Mengli Cai, Karl A. Walter, Xenia B. Searle, Stephen W. Fesik
Publikováno v:
Chemical Biology & Drug Design. 69:395-404
As part of a fully integrated and comprehensive strategy to discover novel antibacterial agents, NMR- and mass spectrometry-based affinity selection screens were performed to identify compounds that bind to protein targets uniquely found in bacteria
Autor:
Niru B. Soni, Rolf Wagner, Steve D. Pratt, Teresa A. Rosenberg, Linda E. Chovan, Darlene J. Balli, Candace Black-Schaefer, Angela M. Nilius, Philip J. Merta, Moshe Weitzberg, Mira M. Hinman, Bruce A. Beutel, Frank L. Wagenaar, Douglas Kalvin
Publikováno v:
Journal of Medicinal Chemistry. 49:4842-4856
We describe the synthesis and antibacterial activity of a series of tetracyclic naphthyridones. The members of this series act primarily via inhibition of bacterial translation and belong to the class of novel ribosome inhibitors (NRIs). In this pape
Autor:
Randy E. Metzger, Stephan J. Kakavas, Philip J. Merta, Xiaoan Ruan, Richard T. Chang, Claude G. Lerner, Christian Wagner, Bruce A. Beutel
Publikováno v:
Antimicrobial Agents and Chemotherapy. 49:2767-2777
Restriction enzyme modulation of transformation efficiencies (REMOTE) is a method that makes use of genome restriction maps and experimentally observed differences in transformation efficiencies of genomic DNA restriction digests to discover the loca
Autor:
Richard F. Clark, Xiaoan Ruan, Xiaoling Xuei, Rolf Wagner, Ping Zhong, Caroline A. David, Steve D. Pratt, Moshe Weitzberg, Candace Black-Schaefer, Linus L. Shen, Peter J. Dandliker, Yingna Cai, Erika E. Englund, Stephan J. Kakavas, Angela M. Nilius, Niru B. Soni, Mai Bui, Melissa M. Daly, Philip J. Merta, Danli L. Towne, Bruce A. Beutel, Linda E. Chovan, Zhensheng Cao, Robert K. Hickman, Anne Y. Saiki, Claude G. Lerner
Publikováno v:
Antimicrobial Agents and Chemotherapy. 47:3831-3839
We report the discovery and characterization of a novel ribosome inhibitor (NRI) class that exhibits selective and broad-spectrum antibacterial activity. Compounds in this class inhibit growth of many gram-positive and gram-negative bacteria, includi
Publikováno v:
Nature Chemical Biology. 7:200-202
Although it is increasingly being recognized that drug-target interaction networks can be powerful tools for the interrogation of systems biology and the rational design of multitargeted drugs, there is no generalized, statistically validated approac
Publikováno v:
PLoS ONE
PLoS ONE, Vol 10, Iss 3, p e0114363 (2015)
PLoS ONE, Vol 10, Iss 3, p e0114363 (2015)
Constitutive activation of the Janus kinase (JAK)/signal transducer and activator of transcription (STAT) axis is fundamental to the molecular pathogenesis of a host of hematological disorders, including acute leukemias and myeloproliferative neoplas