Zobrazeno 1 - 10
of 12
pro vyhledávání: '"Ingrid C, Choong"'
Autor:
Graham K. Farrington, Jessica E. Friedman, Joshua C. Yoburn, Alexey Lugovskoy, William Michael Flanagan, Stephan K. Miller, Brian C. Cunningham, Amy D. Fung, Adrian Whitty, Molly M. He, Jun Wang, Annemarie Stroustrup Smith, Mark T. Cancilla, John Eldredge, Leslie A. Cruz, Johan D. Oslob, Teresa G. Cachero, Andrew C. Braisted, Eric S. Day, Ingrid C. Choong
Publikováno v:
Science. 310:1022-1025
We have identified a small-molecule inhibitor of tumor necrosis factor α (TNF-α) that promotes subunit disassembly of this trimeric cytokine family member. The compound inhibits TNF-α activity in biochemical and cell-based assays with median inhib
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::2a6ce3328b91c59024e2eaf119ff3ef0
https://doi.org/10.1126/science.1116304
https://doi.org/10.1126/science.1116304
Autor:
Thomas O'Brien, Matthew T Burdett, Dennis Lee, Eric M Gordon, Warren L DeLano, Joni W. Lam, Phuongly Pham, Ingrid C. Choong, Willard Lew, Darin Allen, Bruce Fahr
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:3651-3655
The design and synthesis of a series of novel, reversible, small molecule inhibitors of caspase-3 are described.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::47ef57df2ac796814a3ca81e3e0220b1
https://doi.org/10.1016/j.bmcl.2003.08.024
https://doi.org/10.1016/j.bmcl.2003.08.024
Autor:
Bruce Fahr, Warren L DeLano, Dennis Lee, Phuongly Pham, Christian Wiesmann, Matthew T Burdett, Daniel A. Erlanson, Tinh N Luong, Eric M Gordon, Darin Allen, Willard Lew, Joni W. Lam, Thomas O'Brien, Robert S. McDowell, Ingrid C. Choong
Publikováno v:
Journal of Medicinal Chemistry. 45:5005-5022
The design, synthesis, and in vitro activities of a series of potent and selective small-molecule inhibitors of caspase-3 are described. From extended tethering, a salicylic acid fragment was identified as having binding affinity for the S(4) pocket
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ed26c9c092922d168df5cd60556898d7
https://doi.org/10.1021/jm020230j
https://doi.org/10.1021/jm020230j
Autor:
Bruce Fahr, Yafan Lu, Iana Serafimova, David E. Stockett, Phuongly Pham, Junfa Fan, Ingrid C. Choong, Duncan Walker, Ute Hoch, Sravanthi Cheeti, Erica Chan, Michelle R. Arkin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:5763-5765
The identification of a selective CDK2, 7, 9 inhibitor 4 with improved permeability is described. Compound 4 exhibits comparable CDK selectivity profile to SNS-032, but shows improved permeability and higher bioavailability in mice.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::303937ba3989812bb0cb962ae59184ed
https://doi.org/10.1016/j.bmcl.2008.09.073
https://doi.org/10.1016/j.bmcl.2008.09.073
Autor:
Jonathan A. Ellman, Ingrid C. Choong
Publikováno v:
ChemInform. 31
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::a579034f30ba37728049ab96d158112a
https://doi.org/10.1002/chin.200002070
https://doi.org/10.1002/chin.200002070
Autor:
Michael K. Ameriks, James P. Edwards, Jian Zhu, Lars Karlsson, Bart L. Staker, Hans E. Purkey, Damara Gebauer, Ingrid C. Choong, Siquan Sun, Robin L. Thurmond, Scott D. Bembenek, Matthew T Burdett, Yin Gu
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(14)
A pyridazin-4-one fragment 4 (hCatS IC50 = 170 μM) discovered through Tethering was modeled into cathepsin S and predicted to overlap in S2 with the tetrahydropyridinepyrazole core of a previously disclosed series of CatS inhibitors. This fragment s
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::db0724023e642a3d9c338e4a46b68cbe
https://pubmed.ncbi.nlm.nih.gov/20541404
https://pubmed.ncbi.nlm.nih.gov/20541404
Autor:
Bruce Fahr, Junfa Fan, Duncan Walker, Sravanthi Cheeti, Ute Hoch, Erica Chan, Phuongly Pham, Ingrid C. Choong, Yafan Lu, Iana Serafimova, David E. Stockett
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(23)
Modifications of the isonipecotic acid fragment of SNS-032 results in analogs which are more permeable and lower effluxed than SNS-032. The enantiomerically pure synthesis and the in vivo profile of analog 20 is described.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8da9bc8309e1c73e79a6b57e6f045ab0
https://pubmed.ncbi.nlm.nih.gov/18926699
https://pubmed.ncbi.nlm.nih.gov/18926699
Autor:
Michael J. Romanowski, Yafan Lu, Junfa Fan, Raymond V. Fucini, Hans E. Purkey, Willard Lew, Erica VanderPorten, Joshua C. Yoburn, Bruce T. Fahr, Minna Bui, Ingrid C. Choong, Hanan Emily, Jiang Zhu, Phuongly Pham, Yang Liu, Marc J. Evanchik, Robert A. Elling, Kenneth J. Barr, Wenjin Yang
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(20)
A series of 2-amino-pyrazolopyridines was designed and synthesized as Polo-like kinase (Plk) inhibitors based on a low micromolar hit. The SAR was developed to provide compounds exhibiting low nanomolar inhibitory activity of Plk1; the phenotype of t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3b95acafa1a6d4c413fbf0fb6fce7aae
https://pubmed.ncbi.nlm.nih.gov/18793847
https://pubmed.ncbi.nlm.nih.gov/18793847
Autor:
Molly M, He, Annemarie Stroustrup, Smith, Johan D, Oslob, William M, Flanagan, Andrew C, Braisted, Adrian, Whitty, Mark T, Cancilla, Jun, Wang, Alexey A, Lugovskoy, Josh C, Yoburn, Amy D, Fung, Graham, Farrington, John K, Eldredge, Eric S, Day, Leslie A, Cruz, Teresa G, Cachero, Stephan K, Miller, Jessica E, Friedman, Ingrid C, Choong, Brian C, Cunningham
Publikováno v:
Science (New York, N.Y.). 310(5750)
We have identified a small-molecule inhibitor of tumor necrosis factor alpha (TNF-alpha) that promotes subunit disassembly of this trimeric cytokine family member. The compound inhibits TNF-alpha activity in biochemical and cell-based assays with med
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::896527c8737cc4d728d7f4577b06518d
https://pubmed.ncbi.nlm.nih.gov/16284179
https://pubmed.ncbi.nlm.nih.gov/16284179
Autor:
Warren L DeLano, Dennis Lee, Eric M Gordon, Tinh N Luong, Joni W. Lam, Daniel A. Erlanson, Christian Wiesmann, W. Michael Flanagan, Matthew T Burdett, Thomas O'Brien, Robert Lowell Simmons, Ingrid C. Choong
Publikováno v:
Nature biotechnology. 21(3)
Cysteine aspartyl protease-3 (caspase-3) is a mediator of apoptosis and a therapeutic target for a wide range of diseases. Using a dynamic combinatorial technology, 'extended tethering', we identified unique nonpeptidic inhibitors for this enzyme. Ex
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::62829f42dec6ed5f887d68528a40e76e
https://pubmed.ncbi.nlm.nih.gov/12563278
https://pubmed.ncbi.nlm.nih.gov/12563278