Zobrazeno 1 - 10
of 15
pro vyhledávání: '"Charles Willis Lugar"'
Autor:
Kristy Kikly, Howard Barff Broughton, William Chang, Selma Sapmaz, Richard Morphy, Holly A. Bina, Jim D. Durbin, Sherry Y Guo, Timothy Ivo Richardson, Jimmy P Steele, Ryan Edward Stites, Brian G. Getman, Vaught Grant Matthews, Veavi Ching-Yun Chang, Pamela K. Shetler, Greg L Durst, Denise D Edmondson, Rob Barr, Helene Rudyk, Charles Willis Lugar, Nita J. Patel, Christian Alexander Clarke, Kelly Wayne Furness, Nicole E New, David K. Clawson, Keith R. Stayrook, Mark Chambers, Brian Michael Mathes, Stephanie L. Stout, Wendy H. Gough
Publikováno v:
Journal of Medicinal Chemistry. 64:5470-5484
The Th17 pathway has been implicated in autoimmune diseases. The retinoic acid receptor-related orphan receptor C2 (RORγt) is a master regulator of Th17 cells and controls the expression of IL-17A. RORγt is expressed primarily in IL-17A-producing l
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::3a80dc241f7e50c8ddb367cc37ea913c
https://doi.org/10.1021/acs.jmedchem.0c01918
https://doi.org/10.1021/acs.jmedchem.0c01918
Autor:
Timothy Ivo Richardson, Chahrzad Montrose-Rafizadeh, Scott Alan Jones, Terry L. Moore, Thomas J. Bleisch, John J. Osborne, Charles Willis Lugar, Yu Kuo-Long, Jeffrey Alan Dodge, Pamela K. Shetler, Nita J. Patel, Christian Alexander Clarke, Andrew G. Geiser, Jose Eduardo Lopez, Rachelle J. Sells Galvin, Brian Stephen Muehl, Ying K. Yee, Norman Earle Hughes, Richard W. Zink
Publikováno v:
ACS Medicinal Chemistry Letters. 2:148-153
We report the synthesis and characterization of novel 3-aryl indoles as potent and efficacious progesterone receptor (PR) antagonists with potential for the treatment of uterine fibroids. These compounds demonstrated excellent selectivity over other
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::acdb4c9ff42035b27d8602e491bfe9d8
https://doi.org/10.1021/ml100220b
https://doi.org/10.1021/ml100220b
Publikováno v:
Combinatorial Chemistry & High Throughput Screening. 9:175-180
Growth hormone secretagogues (GHSs) are synthetic molecules that stimulate and amplify pulsatile pituitary growth hormone release, via a separate pathway distinct from GH releasing hormone/somatostatin. The activity of GHSs is not fully specific for
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ee09a3e579ec589fc8588e59ccef5224
https://doi.org/10.2174/138620706776055458
https://doi.org/10.2174/138620706776055458
Autor:
Mark L. Heiman, Andrea L. Woodson, Terry D. Lindstrom, David L. Smiley, Jeffrey Alan Dodge, Michael P. Clay, Charles Willis Lugar
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:5873-5876
2-(2-Amino-2-methyl-propionylamino)-5-phenyl-pentanoic acid [1-[1-(4-methoxy-phenyl)-1-methyl-2-oxo-2-pyrrolidin-1-yl-ethyl]-1H-imidazol-4-yl]-amide (LY444711, 6) is an orally active ghrelin agonist that binds with high affinity to and is a potent ac
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1115e1e96435f5d7beab6015823e2fe0
https://doi.org/10.1016/j.bmcl.2004.09.027
https://doi.org/10.1016/j.bmcl.2004.09.027
Autor:
Magee David Edward, Jeffrey Alan Dodge, Pamela K. Shetler, Mary D. Adrian, Henry Uhlman Bryant, Charles Willis Lugar
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:4281-4284
The pharmacology and SAR of representative equine estogens is described. 17alpha-Dihydroequilenin was found to prevent bone loss after 5 weeks of oral administration to ovariectomized rats. The stereochemical significance of the D-ring and the C/D ri
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c9ddfc7ea0e24394dbb1ae9326684cbe
https://doi.org/10.1016/j.bmcl.2003.09.060
https://doi.org/10.1016/j.bmcl.2003.09.060
Autor:
Joseph H. Kennedy, V. Scott Sharp, Timothy Alan Shepherd, Jeffrey Alan Dodge, John L Bowers, Charles Willis Lugar
Publikováno v:
Journal of Chromatography A. 872:75-84
Chromatographic separations of new growth hormone secretagogue compounds were developed to support structure–activity relationship (SAR) studies in conjunction with lead optimization. These new compounds differed from Merck’s MK-677 by having two
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e8d4c8133fa156706e7cda9be6f1a434
https://doi.org/10.1016/s0021-9673(99)01286-8
https://doi.org/10.1016/s0021-9673(99)01286-8
Autor:
Robert M. Amos, Yong Wang, Peter Stanley Borromeo, Robert J. Barr, Timothy Ivo Richardson, Gregory L. Durst, Jeffrey Alan Dodge, Harold E. Osborne, Bryan H. Norman, Scott Alan Jones, Chahrzad Montrose-Rafizadeh, and Amechand Boodhoo, Keyue Chen, Sherry Guo, Charles Willis Lugar, Venkatesh Krishnan
Publikováno v:
Journal of Medicinal Chemistry. 49:6155-6157
Benzopyran selective estrogen receptor beta agonist-1 (SERBA-1) shows potent, selective binding and agonist function in estrogen receptor beta (ERbeta) in vitro assays. X-ray crystal structures of SERBA-1 in ERalpha and beta help explain observed bet
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5f98e5d5151dc3683018dd3a7ed409f0
https://doi.org/10.1021/jm060491j
https://doi.org/10.1021/jm060491j
Autor:
John J. Osborne, Charles A. Frolik, Charles Willis Lugar, Andrew L. Glasebrook, Jeffrey Alan Dodge, David Lynn Phillips, Stephen Sung Yong Cho
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 7:993-996
Glucuronide conjugates 1 and 2, the major metabolites of raloxifene, have been prepared and their molecular interactions with the estrogen receptor determined.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::8d168db0cbda004518c96680971a0d5e
https://doi.org/10.1016/s0960-894x(97)00142-x
https://doi.org/10.1016/s0960-894x(97)00142-x
Autor:
Andrew L. Glasebrook, Larry A. Spangle, Lorri L. Short, Stephen Sung Yong Cho, David Lynn Phillips, Masahiko Sato, Jeffrey Alan Dodge, John J. Osborne, Charles A. Frolik, Henry Uhlman Bryant, Na N. Yang, Martin Michael John, Charles Willis Lugar
Publikováno v:
The Journal of Steroid Biochemistry and Molecular Biology. 61:97-106
Raloxifene (LY139481 HCl) is a selective estrogen receptor modulator (SERM) which blocks the effects of estrogen on some tissues, such as the breast and uterus, while mimicking estrogen in other tissues, such as bone. To study the origins of this uni
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f5ae701cbd776f8dd0570da840ae9d1c
https://doi.org/10.1016/s0960-0760(97)00008-3
https://doi.org/10.1016/s0960-0760(97)00008-3
Autor:
Macklin Brian Arnold, Paul L. Ornstein, D D Schoepp, J. D. Leander, Charles Willis Lugar, Peter Stanley Borromeo, David Lodge, N. K. Allen, Thomas J. Bleisch
Publikováno v:
Journal of Medicinal Chemistry. 39:2219-2231
A series of 6-substituted decahydroisoquinoline-3-carboxylic acids were prepared as excitatory amino acid (EAA) receptor antagonists. These compounds are antagonists at the N-methyl-D-aspartate (NMDA) and 2-amino-3-(5-methyl-3-hydroxyisoxazol-4-yl) p
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::94a405526c3761a60a97c8fb39e531c5
https://doi.org/10.1021/jm950912p
https://doi.org/10.1021/jm950912p