Zobrazeno 1 - 10
of 81
pro vyhledávání: '"Christine C. Chung"'
Autor:
James I. Fells, Wensheng Yu, Younong Yu, Richard J. O. Barnard, Christine C. Chung, Bonnie J. Howell, Shouning Xu, Daniel J. Klein, Joseph A. Kozlowski, Joseph L. Duffy, Dane Clausen, Jian Liu, M. Katharine Holloway, Robert W. Myers, Guoxin Wu, Takao Suzuki, Lin Deng, Jin Wu, Ming Wang
Publikováno v:
Journal of Medicinal Chemistry. 64:4709-4729
We describe the discovery of histone deacetylase (HDACs) 1, 2, and 3 inhibitors with ethyl ketone as the zinc-binding group. These HDACs 1, 2, and 3 inhibitors have good enzymatic and cellular activity. Their serum shift in cellular potency has been
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a4c8b7b2d8a7b239d36c3d11df82ab88
https://doi.org/10.1021/acs.jmedchem.0c02150
https://doi.org/10.1021/acs.jmedchem.0c02150
Autor:
Dong-Ming Shen, Michael Wolff, Shirly Pinto, Deodial Guiadeen, Bindhu V. Karanam, James M. Balkovec, Arto D. Krikorian, Shuwen He, Maria Madeira, Donald M. Sperbeck, Andreas Verras, Judyann Wiltsie, Jian Liu, Jackie Shang, Tim Cernak, Beth Ann Murphy, Qingmei Hong, Christine C. Chung, Ravi P. Nargund, Kevin D. Dykstra, Judith N. Gorski, Robert J. DeVita, Sharon Tong, Tianying Jian, Lisa M. Sonatore, Jeffrey T. Kuethe, Jianying Xiao, Jinqi Liu, Zhong Lai, Zhicai Wu, Mikhail Reibarkh, Ginger X. Yang, Yang Yu
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 29:1182-1186
Previously disclosed benzimidazole-based DGAT1 inhibitors containing a cyclohexane carboxylic acid moiety suffer from isomerization at the alpha position of the carboxylic acid group, generating active metabolites which exhibit DGAT1 inhibition compa
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6d804bc7e0890d2b1abe6ee34b194779
https://doi.org/10.1016/j.bmcl.2019.03.025
https://doi.org/10.1016/j.bmcl.2019.03.025
Autor:
Joseph L. Duffy, James I. Fells, Younong Yu, Bonnie J. Howell, Hyunjin M. Kim, Wensheng Yu, Dane Clausen, M. Katharine Holloway, Christine C. Chung, Robert W. Myers, Jin Wu, Richard J. O. Barnard, Daniel J. Klein, Joseph A. Kozlowski, Steve S. Carroll, Guoxin Wu, Jian Liu, Joseph Kelly
Publikováno v:
ACS Med Chem Lett
[Image: see text] HIV persistence in latently infected, resting CD4(+) T cells is broadly considered a barrier to eradicate HIV. Activation of the provirus using latency-reversing agents (LRAs) followed by immune-mediated clearance to purge reservoir
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::525b4192080895b98514a52d14d59d11
https://europepmc.org/articles/PMC7357218/
https://europepmc.org/articles/PMC7357218/
Autor:
Robert J. De Vita, Zhi-Cai Shi, Bindhu V. Karanam, Beth Ann Murphy, Shuwen He, Tianying Jian, Christine C. Chung, Maria Madeira, Qingmei Hong, Tim Cernak, Ravi P. Nargund, James M. Balkovec, Donald M. Sperbeck, Min Liu, Andreas Verras, Judyann Wiltsie, Jian Liu, Lisa M. Sonatore, Sharon Tong, Shirly Pinto, Deodial Guiadeen, Michael Wolff, Zhicai Wu, Dong-Ming Shen, Arto D. Krikorian, Yang Yu, Judith N. Gorski, Petr Vachal, Jianying Xiao, Jinqi Liu, Zhong Lai
Publikováno v:
Bioorganicmedicinal chemistry letters. 29(11)
The parallel medicinal chemistry (PMC) was effectively applied to accelerate the optimization of diacylglycerol O-acyltransferase I (DGAT-1) inhibitors. Through a highly collaborative and iterative library design, synthesis and testing, a benzimidazo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5d0380ff27cfdf10ca6e079a9a149965
https://pubmed.ncbi.nlm.nih.gov/30952592
https://pubmed.ncbi.nlm.nih.gov/30952592
Autor:
Shirly Pinto, Deodial Guiadeen, David X. Yang, Tianying Jian, Ravi P. Nargund, Donald M. Sperbeck, Tim Cernak, Qingmei Hong, James M. Balkovec, Christine C. Chung, Dong-Ming Shen, Jeffrey T. Kuethe, Sharon Tong, Pauline C. Ting, Judyann Wiltsie, Jack Gibson, Lisa M. Sonatore, Zhicai Wu, Ginger X. Yang, Michael Wolff, Judith N. Gorski, Robert J. DeVita, Yang Yu, Jian Liu, JeanMarie Lisnock, Zhong Lai, Shuwen He, Jianying Xiao, Jinqi Liu, Bindhu V. Karanam, Arto D. Krikorian, Kevin D. Dykstra, Maria Madeira
Publikováno v:
ACS Medicinal Chemistry Letters. 5:1082-1087
We report the discovery of a novel series of DGAT1 inhibitors in the benzimidazole class with a piperdinyl-oxy-cyclohexanecarboxylic acid moiety. This novel series possesses significantly improved selectivity against the A2A receptor, no ACAT1 off-ta
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5736a4f35707b793d0b53f6a00a346de
https://doi.org/10.1021/ml5003426
https://doi.org/10.1021/ml5003426
Autor:
David Won-Shik Kim, Ravi P. Nargund, Zhicai Wu, Maria Madeira, Jian Liu, JeanMarie Lisnock, Tianying Jian, Jeffrey T. Kuethe, Bindhu V. Karanam, Qingmei Hong, Dong-Ming Shen, Michael Wolff, Sharon Tong, Jack Gibson, Zhong Lai, Shirly Pinto, Deodial Guiadeen, Yang Yu, Donald M. Sperbeck, Beth Ann Murphy, James M. Balkovec, Christine C. Chung, Dunlu Chen, Judyann Wiltsie, Jinqi Liu, Xiaoli Chen, Shuwen He, Arto D. Krikorian, Lisa M. Sonatore, Pauline C. Ting, Judith N. Gorski, Robert J. DeVita, Ginger X. Yang
Publikováno v:
ACS Medicinal Chemistry Letters. 4:773-778
We report the design and synthesis of a series of novel DGAT1 inhibitors in the benzimidazole class with a pyridyl-oxy-cyclohexanecarboxylic acid moiety. In particular, compound 11A is a potent DGAT1 inhibitor with excellent selectivity against ACAT1
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::38cc6718ba0c1555d5839bf034018f4f
https://doi.org/10.1021/ml400168h
https://doi.org/10.1021/ml400168h
Autor:
Jiaping Zhang, Andrew K.P. Taggart, Steven J. Stout, Shirly Pinto, Larissa Wilsie, Xun Chen, Xuelei S. Song, David G. McLaren, Jason E. Imbriglio, Margarita Garcia-Calvo, George H. Addona, Christine C. Chung, Lisa M. Sonatore, Oksana C. Palyha
Publikováno v:
Journal of biomolecular screening. 21(2)
Mass spectrometry offers significant advantages over other detection technologies in the areas of hit finding, hit validation, and medicinal chemistry compound optimization. The foremost obvious advantage is the ability to directly measure enzymatic
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c5a8c17dafb11e5453ff6e2222e4a4bf
https://pubmed.ncbi.nlm.nih.gov/26403520
https://pubmed.ncbi.nlm.nih.gov/26403520
Autor:
Michael J. Forrest, Matthew J. Wyvratt, Lex H.T. Van der Ploeg, Kajal Patel, Michael H. Fisher, Ann E. Weber, Jiafang He, Anthony Mastracchio, Emma R. Parmee, Michael R. Tota, Euan Macintyre, Scott D. Edmondson, Xinchun Tong, Naphtali A. O'Connor, Joseph M. Metzger, Jeff P. Varnerin, Christine C. Chung, Scott Hofsess
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:3983-3987
Aryldihydropyridazinones and aryldimethylpyrazolones with 2-benzyl vinylogous amide substituents have been identified as potent PDE3B subtype selective inhibitors. Dihydropyridazinone 8a (PDE3B IC 50 =0.19 nM, 3A IC 50 =1.3 nM) was selected for in vi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a716655952e30da51f523a1480673a13
https://doi.org/10.1016/j.bmcl.2003.08.056
https://doi.org/10.1016/j.bmcl.2003.08.056
Autor:
Margaret Wu, Cai Li, Robert W. Myers, Michael R. Tota, Michael E. Lassman, Christine C. Chung, Maryann Powles, Corey N. Miller, Jun Wang, Bindhu V. Karanam, Gino Salituro, Sheo B. Singh, Kenneth P. Ellsworth, Bei B. Zhang, Sang Ho Lee
Platensimycin (PTM) is a recently discovered broad-spectrum antibiotic produced by Streptomyces platensis . It acts by selectively inhibiting the elongation-condensing enzyme FabF of the fatty acid biosynthesis pathway in bacteria. We report here tha
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d06a8a194f9234738800a07d3d73077d
https://europepmc.org/articles/PMC3069196/
https://europepmc.org/articles/PMC3069196/
Autor:
Alexander Pasternak, Paul Mazur, Michael R. Tota, Stephen D. Goble, Lihu Yang, Donna L. Hreniuk, Andrew D. Howard, Reynalda deJesus, Sander G. Mills, Christine C. Chung, Scott D. Feighner
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(21)
This Letter describes optimization of ghrelin receptor antagonists and inverse agonists starting from a screening hit.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fdfcd1b4cde935121608bb1f09ea58b2
https://pubmed.ncbi.nlm.nih.gov/19767208
https://pubmed.ncbi.nlm.nih.gov/19767208