Zobrazeno 1 - 10
of 22
pro vyhledávání: '"Joan Guo"'
Autor:
David A. Claremon, Herbert Nar, Yi Zhao, Deepak S. Lala, Paula Krosky, Gerard McGeehan, Frank Himmelsbach, Joan Guo, Shi Meng, Rong Guo, Linghang Zhuang, Annette Schuler-Metz, Bradford S. Hamilton
Publikováno v:
European Journal of Pharmacology. 746:50-55
To combat the increased morbidity and mortality associated with the developing diabetes epidemic new therapeutic interventions are desirable. Inhibition of intracellular cortisol generation from cortisone by blocking 11β-hydroxysteroid dehydrogenase
Autor:
Bradford S. Hamilton, Frank Himmelsbach, Barbara A. Kruk, Joan Guo, Gerard McGeehan, Peter Lindblom, Rong Guo, Colin M. Tice, Brian M. McKeever, Linghang Zhuang, David A. Claremon, Judith A. Johnson, Katerina Leftheris, Lamont Howard, Salvacion Cacatian, Heike Schauerte, Annette Schuler-Metz, Richard Gregg, Reshma Panemangalore, Deepak S. Lala, Paula Krosky, Zhenrong Xu, Yuri Bukhtiyarov, Suresh B. Singh, Yuanjie Ye, Yi Zhao, Wei Zhao, Shi Meng
Publikováno v:
Bioorganicmedicinal chemistry. 25(14)
A potent, in vivo efficacious 11β hydroxysteroid dehydrogenase type 1 (11β HSD1) inhibitor (11j) has been identified. Compound 11j inhibited 11β HSD1 activity in human adipocytes with an IC50 of 4.3nM and in primary human adipose tissue with an IC
Autor:
Jing Zhou, Suresh B. Singh, Colin M. Tice, Rebecca Van Orden, Guozhou Chen, Geeta Kandpal, Shi Meng, Cheng-Guo Dong, Yuri Bukhtiyarov, Paul B. Noto, Stephen D. Lotesta, Wei Zhao, Lamont Howard, Katerina Leftheris, Andrew P. Marcus, Kristi Fan, Andrew W. Hardy, Deepak S. Lala, Paula Krosky, Linghang Zhuang, Brian M. McKeever, Gerard McGeehan, Kerri Lipinski, Ya-Jun Zheng, Joan Guo, Yi Zhao, Richard Gregg, David A. Claremon, Zhongren Wu
Publikováno v:
Bioorganicmedicinal chemistry letters. 26(20)
Liver X receptor (LXR) agonists have been reported to lower brain amyloid beta (Aβ) and thus to have potential for the treatment of Alzheimer's disease. Structure and property based design led to the discovery of a series of orally bioavailable, bra
Autor:
Deepak S. Lala, Paula Krosky, Kerri Lipinski, Colin M. Tice, Ya-Jun Zheng, Lamont Howard, Richard Gregg, Paul B. Noto, Yi Zhao, Kristi Fan, David A. Claremon, Zhongren Wu, Andrew W. Hardy, Rebecca Van Orden, Jing Zhou, Gerard McGeehan, Joan Guo, Cheng-Guo Dong, Stephen D. Lotesta, Geeta Kandpal, Jun Shimada, Zhijie Liu, Katerina Leftheris, Shi Meng, Suresh B. Singh, Guozhou Chen, Linghang Zhuang, Brian M. McKeever, Peter Lindblom, Yuri Bukhtiyarov, Wei Zhao
Publikováno v:
Journal of medicinal chemistry. 59(7)
This article describes the application of Contour to the design and discovery of a novel, potent, orally efficacious liver X receptor β (LXRβ) agonist (17). Contour technology is a structure-based drug design platform that generates molecules using
Autor:
David A. Claremon, Zhongren Wu, Ishchenko Alexey, Jing Yuan, Robert D. Simpson, Richard K. Harrison, Joan Guo, Suresh B. Singh, Salvacion Cacatian, Zhenrong Xu, Colin M. Tice, Judith A. Johnson, Lawrence W. Dillard, Lanqi Jia, Gerard McGeehan, Yuri Bukhtiyarov, Wei Zhao, Baldwin John J, Christopher P. Doe, Brian M. McKeever
Publikováno v:
ACS Medicinal Chemistry Letters. 2:747-751
Structure guided optimization of a series of nonpeptidic alkyl amine renin inhibitors allowed the rational incorporation of additional polar functionality. Replacement of the cyclohexylmethyl group occupying the S1 pocket with a (R)-(tetrahydropyran-
Autor:
Reshma Panemangalore, Judith A. Johnson, Colin M. Tice, Wei He, Brian M. McKeever, Yi Zhao, Zhenrong Xu, Peter Lindblom, Joseph G. Bruno, Yuri Bukhtiyarov, Joan Guo, Salvacion Cacatian, Wei Zhao, Jennifer Berbaum, Jennifer Togias, Boyd B. Scott, David A. Claremon, Rong Guo, Linghang Zhuang, Barbara A. Kruk, Yuanjie Ye, Suresh B. Singh, Paula Krosky, Richard K. Harrison, Gerard McGeehan, Patrick J. Carroll
Publikováno v:
Journal of Medicinal Chemistry. 54:6050-6062
Structure based design led directly to 1,3-oxazinan-2-one 9a with an IC(50) of 42 nM against 11β-HSD1 in vitro. Optimization of 9a for improved in vitro enzymatic and cellular potency afforded 25f with IC(50) values of 0.8 nM for the enzyme and 2.5
Autor:
Joan Guo, Boyd B. Scott, David A. Claremon, Reshma Panemangalore, Zhongren Wu, Ross Bentley, Lanqi Jia, Lawrence W. Dillard, Colin M. Tice, Patrick T. Flaherty, Ishchenko Alexey, Suresh B. Singh, Jennifer M. Mason, Jing Yuan, Gerard McGeehan, Yuri Bukhtiyarov, Christopher P. Doe, Richard K. Harrison, Wei Zhao, Robert D. Simpson, Zhenrong Xu, Salvacion Cacatian, Baldwin John J, Maria Grazia Cappiello, Brian M. McKeever, Jennifer Berbaum
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:694-699
Structure-guided drug design led to new alkylamine renin inhibitors with improved in vitro and in vivo potency. Lead compound 21a, has an IC50 of 0.83 nM for the inhibition of human renin in plasma (PRA). Oral administration of 21a at 10 mg/kg result
Autor:
Helen Kim Cho, Terrence Coleman, Steve Burgess, Joan Guo, Terri Harder, Oscar Maldonado, Dan Xu, James R. Merson, Cindy Wei Li, Kam Chan, Paul Cockle, Karin Jooss, Steve Kurzyniec
Publikováno v:
Journal of Clinical Oncology. 35:e23084-e23084
e23084 Background: Sunitinib is a receptor tyrosine kinase inhibitor (RTK) approved as a monotherapy for the treatment of advanced RCC, gastrointestinal stromal tumors and advanced pancreatic neuroendocrine tumors. At the approved doses, it inhibits
Autor:
Roland E. Dolle, Linda O’Brien, Marc Orlowski, John C. Reader, Cullen L. Cavallaro, Ying Jin, William J. Egan, Wenni Li, Mark Piznik, Joan Guo, Biji Jacob-Samuel, Carolyn DiIanni Carroll, Andrew Laird Roughton, Kevin J. Bowman, Qian Zhao
Publikováno v:
Journal of Combinatorial Chemistry. 2:716-731
A statistical sampling protocol is described to assess the fidelity of libraries encoded with molecular tags. The methodology, termed library QA, is based on the combined application of tag decode analysis and single bead LC/MS. The physical existenc
Publikováno v:
Molecular Diversity. 5:35-49
Libraries encoded with electrophoric tags present a uniquechallenge with respect to library quality control and characterization. Libraries are prepared on Tentagel resin in 200-fold redundancy wherein each resin particle containsone compound per one