Zobrazeno 1 - 10
of 30
pro vyhledávání: '"Donald J Osterling"'
Autor:
William N Pappano, Jun Guo, Yupeng He, Debra Ferguson, Sujatha Jagadeeswaran, Donald J Osterling, Wenqing Gao, Julie K Spence, Marina Pliushchev, Ramzi F Sweis, Fritz G Buchanan, Michael R Michaelides, Alexander R Shoemaker, Chris Tse, Gary G Chiang
Publikováno v:
PLoS ONE, Vol 10, Iss 7, p e0131716 (2015)
Histone methyltransferases are epigenetic regulators that modify key lysine and arginine residues on histones and are believed to play an important role in cancer development and maintenance. These epigenetic modifications are potentially reversible
Externí odkaz:
https://doaj.org/article/22fb11e246334a9a820a7722967d47ee
Autor:
David Maag, Eric F. Johnson, Donald J. Osterling, DeAnne F. Stolarik, Amanda M. Olson, Wenqing Gao, Julie L. Wilsbacher, Sanjay C. Panchal, Enrico L. DiGiammarino, Cherrie K. Donawho, Larry R. Solomon, Luis E. Rodriguez, Yan Shi, Todd A. Hopkins
Supplementary figures S1-S6, tables 1 and 2. Table S1. Body weight loss and health observations in HeyA8 xenograft tumor-bearing mice treated with PARP inhibitors or TMZ alone or in combination. Table S2. Summary of PK parameters in HeyA8 xenograft t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5bcfa08a35c000c13a490792d1596a75
https://doi.org/10.1158/1541-7786.22514481.v1
https://doi.org/10.1158/1541-7786.22514481.v1
Autor:
Andrew J. Souers, Wei Qiu, Thomas D. Penning, Darren C. Phillips, Xiaoqin Liu, Rick F. Clark, Joel D. Leverson, Amanda M. Olson, Chunqiu Lai, Daniel H. Albert, Gui-Dong Zhu, Yunsong Tong, Peter Kovar, Kenton L. Longenecker, Anthony Mastracchio, Morey L. Smith, Bailin Shaw, Alan S. Florjancic, Stephen K. Tahir, Donald J. Osterling
Publikováno v:
ACS Med Chem Lett
[Image: see text] Cyclin-dependent kinase 9 (CDK9) is a serine/threonine kinase involved in the regulation of transcription elongation. An inhibition of CDK9 downregulates a number of short-lived proteins responsible for tumor maintenance and surviva
Autor:
Niraj S. Trasi, Hitesh S. Purohit, Geoff G. Z. Zhang, Lynne S. Taylor, Wenqing Gao, DeAnne Stolarik, Gary J. Jenkins, Donald J. Osterling
Publikováno v:
Molecular Pharmaceutics. 16:3617-3625
Crystallization of drug from an amorphous formulation is expected to negatively impact its bioperformance following oral delivery. In evaluating this in vivo, neat crystalline drug is typically mixed with the amorphous formulation. However, this appr
Autor:
Gary J. Jenkins, Donald J. Osterling, Lynne S. Taylor, Xiaochun Lou, Geoff G. Z. Zhang, DeAnne Stolarik, Wenqing Gao, Venecia R Wilson
Publikováno v:
Journal of Controlled Release. 292:172-182
Enzalutamide is a fast crystallizing, hydrophobic compound that has solubility limited absorption in vivo. Given the low aqueous solubility of this compound, it was of interest to evaluate amorphous formulations in vitro and in vivo. Amorphous solid
Autor:
Geoff G. Z. Zhang, Kevin J. Edgar, Venecia R Wilson, Brittany L.B. Nichols, Xiaochun Lou, Gary J. Jenkins, Yifan Dong, Lynne S. Taylor, DeAnne Stolarik, Donald J. Osterling
Publikováno v:
Scientific Reports, Vol 10, Iss 1, Pp 1-12 (2020)
Scientific Reports
Scientific Reports
Amorphous solid dispersion (ASD) is a widely employed formulation technique for drugs with poor aqueous solubility. Polymers are integral components of ASDs, but mechanisms by which polymers lead to the generation and maintenance of supersaturated so
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:
Kenneth M. Comess, Steven Kennedy, Donald J. Osterling, Michael L. Curtin, Masoud Vedadi, Ramzi F. Sweis, Guillermo Senisterra, Mikkel Algire, Evelyne Lima-Fernandes, Dalia Barsyte-Lovejoy, Justin D. Dietrich, William N. Pappano, Bailin Shaw, David Maag, Dong Cheng, Cheryl H. Arrowsmith, Fengling Li, Marina A. Pliushchev, Kelly L Klinge, Jun Guo, Chaohong Sun, Andrew M. Petros, Gary G. Chiang, Magdalena M. Szewczyk, Huan-Qiu Li, Maricel Torrent, Scott Galasinski, Sujatha Selvaraju, Yupeng He, David Lindley, Clarissa G. Jakob, Sanjay C. Panchal, Wenqing Gao, Lance J Bigelow, Haizhong Zhu, Fritz G. Buchanan, Qin Wu
Publikováno v:
Nature chemical biology. 13(4)
Polycomb repressive complex 2 (PRC2) is a regulator of epigenetic states required for development and homeostasis. PRC2 trimethylates histone H3 at lysine 27 (H3K27me3), which leads to gene silencing, and is dysregulated in many cancers. The embryoni
Autor:
Patrick A. Marcotte, Jun Guo, Michael R. Michaelides, Steven K. Davidsen, David R. Reuter, Junling Li, Yanping Luo, Lori J. Pease, Chris Tse, Terrance J. Magoc, Ru-Qi Wei, Paul Tapang, Eric F. Johnson, Cherrie K. Donawho, Zehan Chen, Amanda M. Olson, Donald J. Osterling, Daniel H. Albert, Michael L. Curtin, Keith B. Glaser, Jennifer J. Bouska, Mai H. Bui, Robin R. Frey
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 343:617-627
ABT-348 [1-(4-(4-amino-7-(1-(2-hydroxyethyl)-1H-pyrazol-4-yl)thieno[3,2-c]pyridin-3-yl)phenyl)-3-(3-fluorophenyl)urea] is a novel ATP-competitive multitargeted kinase inhibitor with nanomolar potency (IC(50)) for inhibiting binding and cellular autop
Autor:
Cherrie K. Donawho, Jennifer J. Bouska, Chang Park, Yan Luo, Yan Shi, Xuesong Liu, Eric F. Johnson, Donald J. Osterling, Thomas D. Penning, Paul Ellis, Vincent L. Giranda, Jianchun Gong, Alexander R. Shoemaker, Viraj B. Gandhi, Gui-Dong Zhu, Amanda M. Olson
Publikováno v:
Bioorganic & Medicinal Chemistry. 20:4635-4645
PARP-1, the most abundant member of the PARP superfamily of nuclear enzymes, has emerged as a promising molecular target in the past decade particularly for the treatment of cancer. A number of PARP-1 inhibitors, including veliparab discovered at Abb