Zobrazeno 1 - 10
of 74
pro vyhledávání: '"Harold B, Wood"'
Autor:
David A. Candito, Vladimir Simov, Anmol Gulati, Solomon Kattar, Ryan W. Chau, Blair T. Lapointe, Joey L. Methot, Duane E. DeMong, Thomas H. Graham, Ravi Kurukulasuriya, Mitchell H. Keylor, Ling Tong, Gregori J. Morriello, John J. Acton, Barbara Pio, Weiguo Liu, Jack D. Scott, Michael J. Ardolino, Theodore A. Martinot, Matthew L. Maddess, Xin Yan, Hakan Gunaydin, Rachel L. Palte, Spencer E. McMinn, Lisa Nogle, Hongshi Yu, Ellen C. Minnihan, Charles A. Lesburg, Ping Liu, Jing Su, Laxminarayan G. Hegde, Lily Y. Moy, Janice D. Woodhouse, Robert Faltus, Tina Xiong, Paul Ciaccio, Jennifer A. Piesvaux, Karin M. Otte, Matthew E. Kennedy, David Jonathan Bennett, Erin F. DiMauro, Matthew J. Fell, Santhosh Neelamkavil, Harold B. Wood, Peter H. Fuller, J. Michael Ellis
Publikováno v:
Journal of Medicinal Chemistry. 65:16801-16817
Autor:
Douglas G. Johns, Louis-Charles Campeau, Puja Banka, An Bautmans, Tjerk Bueters, Elisabetta Bianchi, Danila Branca, Paul G. Bulger, Inne Crevecoeur, Fa-Xiang Ding, Robert M. Garbaccio, Erik D. Guetschow, Yan Guo, Sookhee N. Ha, Jennifer M. Johnston, Hubert Josien, Eunkyung A. Kauh, Kenneth A. Koeplinger, Jeffrey T. Kuethe, Eseng Lai, Christine L. Lanning, Anita Y.H. Lee, Li Li, Anilkumar G. Nair, Edward A. O’Neill, S. Aubrey Stoch, David A. Thaisrivongs, Thomas J. Tucker, Petr Vachal, Kristien van Dyck, Frederic P. Vanhoutte, Bram Volckaert, Dennis G. Wolford, Andy Xu, Tian Zhao, Dan Zhou, Susan Zhou, Xiaohong Zhu, Hratch J. Zokian, Abbas Walji, Harold B. Wood
Publikováno v:
Circulation.
Background: Inhibition of PCSK9 (proprotein convertase subtilisin/kexin type 9)-low density lipoprotein receptor interaction with injectable monoclonal antibodies or small interfering RNA lowers plasma low density lipoprotein-cholesterol, but despite
Autor:
Thomas J. Tucker, Nianyu Li, Scott P. Salowe, Harold B. Wood, Danila Branca, Alan S. Bass, Rupesh P. Amin, BethAnn Murphy, Aurash Shahripour, Angela Kerekes, Abbas Walji, Nicole Buist, Jeffrey T. Kuethe, Huaibing He, Rodger Tracy, Kenneth A. Koeplinger, Weixun Wang, Bhavana Bhatt, Candice Alleyne, Sookhee Ha, Douglas G. Johns, Elisabetta Bianchi, Chengwei Wu, Peter Orth, Tjerk Bueters, Yusheng Xiong, Hratch J. Zokian, Michael J. Hafey, Mark W. Embrey, John Higgins
Publikováno v:
Journal of Medicinal Chemistry. 64:16770-16800
Proprotein convertase subtilisin-like/kexin type 9 (PCSK9) is a key regulator of plasma LDL-cholesterol (LDL-C) and a clinically validated target for the treatment of hypercholesterolemia and coronary artery disease. Starting from second-generation l
Autor:
Andrew M. Haidle, Antonella Converso, Harold B. Wood, Daniel J. Klein, John M. Sanders, Charles A. Lesburg, Ying-Duo Gao, Yi Zang, Matthew Tudor, Xin Cindy Yan
Publikováno v:
Journal of Chemical Information and Modeling. 60:4144-4152
Two orthogonal approaches for hit identification in drug discovery are large-scale in vitro and in silico screening. In recent years, due to the emergence of new targets and a rapid increase in the...
Autor:
Mitchell H. Keylor, Anmol Gulati, Solomon D. Kattar, Rebecca E. Johnson, Ryan W. Chau, Kaila A. Margrey, Michael J. Ardolino, Cayetana Zarate, Kelsey E. Poremba, Vladimir Simov, Gregori J. Morriello, John J. Acton, Barbara Pio, Xin Yan, Rachel L. Palte, Spencer E. McMinn, Lisa Nogle, Charles A. Lesburg, Donovon Adpressa, Shishi Lin, Santhosh Neelamkavil, Ping Liu, Jing Su, Laxminarayan G. Hegde, Janice D. Woodhouse, Robert Faltus, Tina Xiong, Paul J. Ciaccio, Jennifer Piesvaux, Karin M. Otte, Harold B. Wood, Matthew E. Kennedy, David Jonathan Bennett, Erin F. DiMauro, Matthew J. Fell, Peter H. Fuller
Publikováno v:
Journal of medicinal chemistry. 65(1)
The leucine-rich repeat kinase 2 (LRRK2) protein has been genetically and functionally linked to Parkinson's disease (PD), a disabling and progressive neurodegenerative disorder whose current therapies are limited in scope and efficacy. In this repor
Optimization of brain-penetrant picolinamide derived leucine-rich repeat kinase 2 (LRRK2) inhibitors
Autor:
Blair T. Lapointe, Jack D. Scott, Xin Cindy Yan, Haiqun Tang, Janice D Woodhouse, Kaleen Konrad Childers, Robert Faltus, Erin F. DiMauro, Solomon Kattar, Charles S. Yeung, Ravi Kurukulasuriya, Vladimir Simov, Hakan Gunaydin, Anmol Gulati, Joey L. Methot, Rachel L. Palte, Ellen C. Minnihan, Greg Morriello, J. Michael Ellis, Harold B. Wood, Santhosh Neelamkavil, Karin M. Otte, Michael J. Ardolino, Barbara Pio, Ping Liu, Laxminarayan G Hegde, Matthew J. Fell, Vanessa L. Rada, Peter Fuller, Paul J Ciaccio
Publikováno v:
RSC Med Chem
The discovery of potent, kinome selective, brain penetrant LRRK2 inhibitors is the focus of extensive research seeking new, disease-modifying treatments for Parkinson's disease (PD). Herein, we describe the discovery and evolution of a picolinamide-d
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6c8d45ea7dd7adda70471298a4476afa
https://europepmc.org/articles/PMC8292993/
https://europepmc.org/articles/PMC8292993/
Autor:
Harold B. Wood, Maria Madeira, Wayne M. Geissler, Conrad E. Raab, Randy R. Miller, Iain Martin
Publikováno v:
Journal of medicinal chemistry. 63(21)
Lipophilicity has a dominant effect on many parameters that determine unbound drug exposure as well as drug potency. Despite this, analysis of a large body of drug data indicates lipophilicity has no consistent directional impact on dose. This can be
Autor:
Weiguo Liu, Ramzi F. Sweis, Feroze Ujjainwalla, Remond Moningka, F. Anthony Romero, Yi Zang, Paul E. Finke, Zahid Hussain, Karen H. Dingley, Michael A. Plotkin, Andrew D. Howard, Jin Shang, Beth Ann Murphy, Jianming Bao, Gino Salituro, Harold B. Wood, Joseph L. Duffy
Publikováno v:
ACS Medicinal Chemistry Letters. 9:1088-1093
[Image: see text] A series of structurally diverse azaspirodecanone and spirooxazolidinone analogues were designed and synthesized as potent and selective somatostatin receptor subtype 5 (SSTR5) antagonists. Four optimized compounds each representing
Autor:
Margaret Wu, Aleksandr Petrov, Liangsu Wang, Yuyan Ding, Nina Xiaoyan Li, David E. Kelley, Ge Dai, Tamara Dlugos, Robert S. Sherwin, Harold B. Wood, Mark D. Erion, Liming Yang, Timothy J. Kowalski, Stacey N. Brown
Publikováno v:
Diabetes. 67:1401-1413
Insulin-induced hypoglycemia in diabetes is associated with impaired glucagon secretion. In this study, we tested whether stimulation of GPR119, a G-protein–coupled receptor expressed in pancreatic islet as well as enteroendocrine cells and previou
Autor:
Yi Zang, Weiguo Liu, Zhuyan Guo, Yasuko Kiyoi, Eleanor Pow, Lindsay Brown, Charles A. Lesburg, Brian Hawes, Terri M. Kelly, Emma Carswell, Santhosh Neelamkavil, Scott D. Edmondson, Andrew J. Cooke, KehDih Lai, Wayne M. Geissler, Harold B. Wood, Zahid Hussain
Publikováno v:
Bioorganicmedicinal chemistry letters. 30(16)
A series of 4, 4-disubstituted proline analogs were designed, synthesized, and tested for selective inhibition of blood coagulation factor XIa in search of new non-vitamin K antagonists based oral anticoagulants for potential prevention and treatment