Zobrazeno 1 - 10
of 12
pro vyhledávání: '"John Spurlino"'
Autor:
Hua-Rong Lu, Ioanna Petrounia, Zhijie Liu, Daniel Jason Krosky, Devine Zheng Huang, Guozhang Xu, John Spurlino, Michael David Gaul, Weixue Wang, An Hermans, June Zhi Xu, Cynthia M. Milligan, Jenson Qi, Renee L. DesJarlais
Publikováno v:
Bioorganicmedicinal chemistry letters. 30(23)
G-protein coupled receptor kinase 2 (GRK2), which is upregulated in the failing heart, appears to play a critical role in heart failure (HF) progression in part because enhanced GRK2 activity promotes dysfunction of β-adrenergic signaling and myocyt
Autor:
Anne M. Fourie, Steven D. Goldberg, Maxwell D. Cummings, Christoph Steeneck, Thomas Hoffmann, Xiaohua Xue, Michael Albers, Christian Gege, John Spurlino, Kristi A. Leonard, Marina I. Nelen, Cindy Milligan, James P. Edwards, Gerald Kleymann, Olaf Kinzel, Thomas Schlüter
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:1446-1455
The nuclear receptor retinoic acid receptor-related orphan receptor gamma t (RORγt) is a transcription factor that drives Th17 cell differentiation and IL-17 production in both innate and adaptive immune cells. The IL-23/IL-17 pathway is implicated
Autor:
Anne M. Fourie, Glenda Castro, John Spurlino, Rachel Nishimura, Xiaohua Xue, Maxwell D. Cummings, Maud Urbanski, Kevin D. Kreutter, Umar Maharoof, Aihua Wang, David A. Kummer, J. Kent Barbay, James P. Edwards, Kristi A. Leonard, Ronald L. Wolin, Hariharan Venkatesan, Marta Cristina Abad, Celine Schalk-Hihi, Craig R. Woods, Cynthia M. Milligan, Joan Pierce, Virginia M. Tanis
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 27:5277-5283
We identified 6-substituted quinolines as modulators of the retinoic acid receptor-related orphan receptor gamma t (RORγt). The synthesis of this class of RORγt modulators is reported, and optimization of the substituents at the quinoline 6-positio
Autor:
Maxwell D. Cummings, Thomas Schlueter, David A. Kummer, J. Kent Barbay, Krystal Herman, Craig R. Woods, John Spurlino, Kristi A. Leonard, Cynthia M. Milligan, Hariharan Venkatesan, Rachel Nishimura, Michael Albers, Ronald L. Wolin, James P. Edwards, Marina I. Nelen, Xiaohua Xue, Anne M. Fourie, Virginia M. Tanis, Brian Scott
Publikováno v:
Bioorganicmedicinal chemistry letters. 29(12)
We have previously reported the syntheses of a series of 3,6-disubstituted quinolines as modulators of the retinoic acid receptor-related orphan receptor gamma t (RORγt). These molecules are potent binders but are high molecular weight and they exhi
Autor:
Olaf Kinzel, Michael Albers, Brian Scott, John Spurlino, Gerald Kleymann, James P. Edwards, Thomas Schlüter, Dan Pippel, Xiaohua Xue, Christian Gege, Thomas J. Hoffmann, Kristi A. Leonard, Christoph Steeneck, Anne M. Fourie, Maxwell D. Cummings, Cynthia M. Milligan, Steven D. Goldberg, Kevin J. Coe
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 30:127205
The nuclear receptor retinoic acid receptor-related orphan receptor gamma t (RORγt) is a transcription factor that drives Th17 cell differentiation and IL-17 production in both innate and adaptive immune cells. The IL-23/IL-17 pathway is implicated
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
Autor:
Joseph Kent Barbay, Marta Cristina Abad, Ronald L. Wolin, Craig R. Woods, Cynthia M. Milligan, Kristi A. Leonard, Glenda Castro, John Spurlino, Celine Schalk-Hihi, Aihua Wang, Anne M. Fourie, Maxwell D. Cummings, Maud Urbanski, James P. Edwards, Kevin D. Kreutter, Umar Maharoof, Hariharan Venkatesan, David A. Kummer, Xiaohua Xue, Rachel Nishimura, Joan Pierce
Publikováno v:
Bioorganicmedicinal chemistry letters. 27(9)
A high-throughput screen of the ligand binding domain of the nuclear receptor retinoic acid-related orphan receptor gamma t (RORγt) employing a thermal shift assay yielded a quinoline tertiary alcohol hit. Optimization of the 2-, 3- and 4-positions
Autor:
Oliver S. Smart, Paul Emsley, Cary B. Bauer, David A. Case, John L. Markley, Joseph Marcotrigiano, Jasmine Young, Atsushi Nakagawa, Seth F. Harris, Haruki Nakamura, Wolfram Tempel, Radka Svobodová, T. Krojer, Pamela A. Williams, Robert T. Nolte, Catherine E. Peishoff, Jorg Hendle, Chenghua Shao, Jeff Blaney, Dale E. Tronrud, Paul D. Adams, Randy J. Read, Marc C. Nicklaus, Kirk Clark, Helen M. Berman, Jeffrey A. Bell, Evan E Bolton, Suzanna C. Ward, Stephen K. Burley, Alan E. Mark, Garib N. Murshudov, Victoria A. Feher, Matthew T. Miller, John Spurlino, Sameer Velankar, Steven Sheriff, Tom Darden, Wladek Minor, Talapady N. Bhat, John D. Westbrook, Gerard J. Kleywegt, Terry R. Stouch, Huanwang Yang, Gérard Bricogne, Thomas C. Terwilliger, Anil K. Padyana, Zukang Feng, Colin R. Groom, Andrzej Joachimiak, David G. Brown, Anthony Nicholls, Gaetano T. Montelione, Thomas Holder, Kathleen Aertgeerts, Stephen M. Soisson, Gregory L. Warren, Susan Pieniazek
Publikováno v:
Structure (London, England : 1993), vol 24, iss 4
Adams, PD; Aertgeerts, K; Bauer, C; Bell, JA; Berman, HM; Bhat, TN; et al.(2016). Outcome of the First wwPDB/CCDC/D3R Ligand Validation Workshop. Structure, 24(4), 502-508. doi: 10.1016/j.str.2016.02.017. Lawrence Berkeley National Laboratory: Lawrence Berkeley National Laboratory. Retrieved from: http://www.escholarship.org/uc/item/42h5d920
Adams, PD; Aertgeerts, K; Bauer, C; Bell, JA; Berman, HM; Bhat, TN; et al.(2016). Outcome of the First wwPDB/CCDC/D3R Ligand Validation Workshop. Structure, 24(4), 502-508. doi: 10.1016/j.str.2016.02.017. Lawrence Berkeley National Laboratory: Lawrence Berkeley National Laboratory. Retrieved from: http://www.escholarship.org/uc/item/42h5d920
Crystallographic studies of ligands bound to biological macromolecules (proteins and nucleic acids) represent\ud an important source of information concerning drug-target interactions, providing atomic level insights\ud into the physical chemistry of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e2fa7fc51624930579bc888e19578253
https://www.repository.cam.ac.uk/handle/1810/254110
https://www.repository.cam.ac.uk/handle/1810/254110
Autor:
Harrie J.M. Gijsen, Richard Alexander, Frederik J. R. Rombouts, Juan Antonio Vega, Oscar Delgado, Gregor James Macdonald, John Spurlino, Andrés A. Trabanco, Michiel Van Gool, Gary Tresadern, Dieder Moechars, Francisca Delgado
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:7255-7260
Aminopiperazinone inhibitors of BACE were identified by rational design. Structure based design guided idea prioritization and initial racemic hit 18a showed good activity. Modification in decoration and chiral separation resulted in the 40 nM inhibi
Autor:
Richard Alexander, John Spurlino
Publikováno v:
Frontiers in Drug Design & Discovery. 1:287-296