Zobrazeno 1 - 10
of 39
pro vyhledávání: '"Brett A. Tounge"'
Autor:
Tara Mezzasalma Haarlander, Karen Carroll, Sharon L. Burke, Shariff Bayoumy, Ingrid Christa Deckman, Cuifen Huo, Richard Alexander, Monica Singer, Matthew J. Todd, Yue-Mei Zhang, Kristi A. Leonard, Cindy Milligan, Robyn Williams, Kenneth J. Rhodes, Robert H. Scannevin, Keli Dzordzorme, John Spurlino, Brett A. Tounge, Diane M. Maguire, Paul F. Jackson, Celine Schalk-Hihi, Lawrence C. Kuo, Eric Devine, Frank A. Lewandowski
Publikováno v:
The Journal of biological chemistry. 292(43)
Aberrant activation of matrix metalloproteinases (MMPs) is a common feature of pathological cascades observed in diverse disorders, such as cancer, fibrosis, immune dysregulation, and neurodegenerative diseases. MMP-9, in particular, is highly dynami
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ef7e2f60e01bada9e1e4fd469d2a6f02
https://pubmed.ncbi.nlm.nih.gov/29079642
https://pubmed.ncbi.nlm.nih.gov/29079642
Publikováno v:
Current Topics in Medicinal Chemistry. 9:1718-1724
Fragment-based drug discovery (FBDD) is an important new tool to understand the molecule basis of ligand-biological target interactions. By combining optimal fragments, it is often possible to construct larger molecular weight compounds that have gre
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d2f146de4fa2b7ad854682add0396035
https://doi.org/10.2174/156802609790102365
https://doi.org/10.2174/156802609790102365
Publikováno v:
Drug Discovery Today. 14:278-283
The use of fragment-based drug discovery (FBDD) has increased in recent years since it is more likely to produce a better optimized compound of lower molecular weight. Ligand efficiency (LE) has become important for assessing fragments, HTS hits, and
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::70bbeb2aa77265b49f321f1febe45e7b
https://doi.org/10.1016/j.drudis.2008.11.007
https://doi.org/10.1016/j.drudis.2008.11.007
Publikováno v:
Journal of Medicinal Chemistry. 51:2432-2438
Ligand efficiency (i.e., potency/size) has emerged as an important metric in drug discovery. In general, smaller, more efficient ligands are believed to have improved prospects for good drug properties (e.g., bioavailability). Our analysis of thousan
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9e843bcfbf6e4c04a06bfc41ab0457ee
https://doi.org/10.1021/jm701255b
https://doi.org/10.1021/jm701255b
Autor:
Lisa Minor, John C. Spurlino, Alexander N. Barnakov, Stephen C. Yabut, Michael J. Costanzo, Kimberley B. White, Yuanping Wang, Brett A. Tounge, Cynthia M. Milligan, Bruce E. Maryanoff, Han-Cheng Zhang, Frank A. Lewandowski
Publikováno v:
Letters in Drug Design & Discovery. 5:116-121
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::9214330d7fe57c6b8f9c06fd2f885ea1
https://doi.org/10.2174/157018008783928418
https://doi.org/10.2174/157018008783928418
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:4258-4261
Ligand efficiency is a simple metric for assessing whether a ligand derives its potency from optimal fit with the protein target or simply by virtue of making many contacts. Comparison of protein-ligand binding affinities for over 8000 ligands with 2
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::88addcaacd470e9833c39886f5b5825e
https://doi.org/10.1016/j.bmcl.2007.05.038
https://doi.org/10.1016/j.bmcl.2007.05.038
Autor:
Bruce P. Damiano, Dana L. Johnson, Shyamali Ghosh, Brunner Livia, Brett A. Tounge, Jef C. Proost, William J. Hoekstra, Judith Baker, Robert A. Galemmo, Rosemary J. Santulli, Bruce E. Maryanoff, Candace Burns, William A. Kinney, Corte Bart De, Liu Li, Robert W. Tuman
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:5227-5232
The synthesis and SAR of a new class of piperidine-based αvβ3/αvβ5 integrin antagonists is described. Replacement of an amide bond in a prototype isonipecotamide by a C–C isostere, and adjustment of the spacer length between the carboxylic acid
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::331e139a8252211e93d606ef30ad5fd8
https://doi.org/10.1016/j.bmcl.2004.06.061
https://doi.org/10.1016/j.bmcl.2004.06.061
Autor:
Charles H. Reynolds, Brett A. Tounge
Publikováno v:
Journal of Chemical Information and Computer Sciences. 44:1810-1815
We have developed a new method for assigning a drug-like score to reagents. This algorithm uses topological torsion (TT) 2D descriptors to compute the subsimilarity of any given reagent to a substructural element of any compound in the CMC. The utili
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0353d987b5dca414105385ee2af0fe6b
https://doi.org/10.1021/ci049854j
https://doi.org/10.1021/ci049854j
Publikováno v:
Organic Letters. 6:309-312
[structure: see text] We have prepared 7,9-diazabicyclo[4.2.2]dec-3-ene-8,10-dione (3) and 7,9-diazabicyclo[4.2.2]decane-8,10-dione (4), which differ by virtue of the degree of unsaturation in the bridging carbacyclic tether on a 2,5-diketopiperazine
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8172f56d0b8efd0e4ab895a0f199c843
https://doi.org/10.1021/ol036101u
https://doi.org/10.1021/ol036101u
Autor:
Jack A. Kauffman, Michael J. Costanzo, William A. Kinney, Rosemary J. Santulli, Stephen C. Yabut, Brett A. Tounge, Patricia Andrade-Gordon, Edward C. Lawson, Diane K. Luci, Hoekstra William J
Publikováno v:
Letters in Drug Design & Discovery. 1:14-18
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::4cebab9524db6475d2791ace4a2e054a
https://doi.org/10.2174/1570180043485644
https://doi.org/10.2174/1570180043485644