Zobrazeno 1 - 10
of 20
pro vyhledávání: '"Guosen Ye"'
Autor:
Shailesh Bihari, Melissa H. Costell, Tara Bouchier, David J. Behm, Mark Burgert, Guosen Ye, Andrew D. Bersten, Stephanie Puukila, Elena Cavallaro, Dennis L. Sprecher, Dani-Louise Dixon
Publikováno v:
SSRN Electronic Journal.
Autor:
Eidam Hilary Schenck, Theresa J. Roethke, Linda S. Barton, Fox Ryan Michael, Steve Zhao, Kevin S. Thorneloe, David J. Behm, Guosen Ye, Patrick Stoy, Mui Cheung, Tram H. Hoang, Dennis A. Holt, Krista B. Goodman, Brian G. Lawhorn, Marlys Hammond, Mark A. Hilfiker, Carl Brooks, Jaclyn R. Patterson
Publikováno v:
ACS Med Chem Lett
[Image: see text] GSK2798745, a clinical candidate, was identified as an inhibitor of the transient receptor potential vanilloid 4 (TRPV4) ion channel for the treatment of pulmonary edema associated with congestive heart failure. We discuss the lead
Autor:
Guosen Ye, Arthur Shu, Dennis A. Holt, Patrick Stoy, Carla A. Donatelli, Larry J. Jolivette, Ralph A. Rivero, Mark Youngman, Lamont Roscoe Terrell, Jaclyn R. Patterson, Brian G. Lawhorn, Theresa J. Roethke
Publikováno v:
Journal of medicinal chemistry. 63(23)
Investigation of TRPV4 as a potential target for the treatment of pulmonary edema associated with heart failure generated a novel series of acyclic amine inhibitors displaying exceptional potency and PK properties. The series arose through a scaffold
Autor:
Theresa J. Roethke, Guosen Ye, Hong Zhang, Robert T. Gampe, Robert A. Reid, Brian G. Lawhorn, Tram H. Hoang, Dennis A. Holt, Bob Willette, Marlys Hammond, David G. Washburn, Sharada Manns, Mark A. Hilfiker, Steve Zhao, Fox Ryan Michael, Joanne Prendergast, Eidam Hilary Schenck, Amy M. Quinn, Lara S. Kallander, Sarah E. Dowdell, Alan R. Rendina, Elsie Diaz, Xuan Hong
Publikováno v:
ACS Medicinal Chemistry Letters. 9:736-740
[Image: see text] Bone Morphogenetic Protein 1 (BMP1) inhibition is a potential method for treating fibrosis because BMP1, a member of the zinc metalloprotease family, is required to convert pro-collagen to collagen. A novel class of reverse hydroxam
Autor:
Theresa J. Roethke, Weike Bao, Dennis A. Holt, David J. Behm, Eidam Hilary Schenck, Dennis Lee, Robert N. Willette, Kevin S. Thorneloe, Guosen Ye, Krista B. Goodman, Fox Ryan Michael, Mui Cheung, Carl Brooks, Sarah E. Dowdell, Xiaoping Xu, Michael Jonathan Bury
Publikováno v:
ACS Medicinal Chemistry Letters. 8:549-554
Transient Receptor Potential Vanilloid 4 (TRPV4) is a member of the Transient Receptor Potential (TRP) superfamily of cation channels. TRPV4 is expressed in the vascular endothelium in the lung and regulates the integrity of the alveolar septal barri
Autor:
Arthur Shu, Carla A. Donatelli, Sanchez Robert, Melissa H. Costell, Carl Brooks, Yanan He, Jeff J. McAtee, David J. Behm, Guosen Ye, Dennis A. Holt, Theresa J. Roethke, Brian G. Lawhorn, Grazyna Graczyk-Millbrandt, Lamont Roscoe Terrell, Edward J. Brnardic, Patrick Stoy, Linda S. Barton, Karl F. Erhard
Publikováno v:
Journal of medicinal chemistry. 61(21)
A novel series of pyrrolidine sulfonamide transient receptor potential vanilloid-4 (TRPV4) antagonists was developed by modification of a previously reported TRPV4 inhibitor (1). Several core-structure modifications were identified that improved TRPV
Autor:
Joshi M. Ramanjulu, G. Scott Pesiridis, Jingsong Yang, Nestor Concha, Robert Singhaus, Shu-Yun Zhang, Jean-Luc Tran, Patrick Moore, Stephanie Lehmann, H. Christian Eberl, Marcel Muelbaier, Jessica L. Schneck, Jim Clemens, Michael Adam, John Mehlmann, Joseph Romano, Angel Morales, James Kang, Lara Leister, Todd L. Graybill, Adam K. Charnley, Guosen Ye, Neysa Nevins, Kamelia Behnia, Amaya I. Wolf, Viera Kasparcova, Kelvin Nurse, Liping Wang, Ana C. Puhl, Yue Li, Michael Klein, Christopher B. Hopson, Jeffrey Guss, Marcus Bantscheff, Giovanna Bergamini, Michael A. Reilly, Yiqian Lian, Kevin J. Duffy, Jerry Adams, Kevin P. Foley, Peter J. Gough, Robert W. Marquis, James Smothers, Axel Hoos, John Bertin
Publikováno v:
Nature. 564(7736)
Stimulator of interferon genes (STING) is a receptor in the endoplasmic reticulum that propagates innate immune sensing of cytosolic pathogen-derived and self DNA1. The development of compounds that modulate STING has recently been the focus of inten
Autor:
Sven-Eric Jordt, Melanie Maya Kaelberer, Guosen Ye, Weifeng Song, Emma Leishman, Zhihong Yu, Eidam Hilary Schenck, Boyi Liu, Heather B. Bradshaw, Robert N. Willette, Kevin S. Thorneloe, Stephen F. Doran, Satyanarayana Achanta, Aiwei Sui, Shrilatha Balakrishna, Mui Cheung, Sadis Matalon
Publikováno v:
American Journal of Physiology-Lung Cellular and Molecular Physiology. 307:L158-L172
The treatment of acute lung injury caused by exposure to reactive chemicals remains challenging because of the lack of mechanism-based therapeutic approaches. Recent studies have shown that transient receptor potential vanilloid 4 (TRPV4), an ion cha
Autor:
Masahiro Suzuki, Akio Kobayashi, Mitsuru Takahashi, Steven M. Rubenstein, Takuya Matsui, Bei Shan, Kazuyuki Sugimoto, Marie-Louise Smith, Xiaolin Hao, Kexue Li, Yukihito Ishii, Masahiro Tanaka, Jian Ken Zhang, Frank Kayser, Mutsuyoshi Matsushita, Takashi Inaba, Rebekah Choi, Shoichi Sagawa, Nobuya Ogawa, Daisuke Tomimoto, Hidekazu Ozeki, Marc Labelle, Guosen Ye, Atsuhito Yoshida, Chihiro Okuma, Kiyosei Iio, Simon Jackson, Shichang Miao, Brian M. Fox, Noboru Furakawa, Dustin McMinn, Ji Ma
Publikováno v:
Journal of Medicinal Chemistry. 57:3464-3483
The discovery and optimization of a series of acyl CoA:diacylglycerol acyltransferase 1 (DGAT1) inhibitors based on a pyrimido[4,5-b][1,4]oxazine scaffold is described. The SAR of a moderately potent HTS hit was investigated resulting in the discover
Autor:
Joseph J. Romano, Jean-Luc Tran, Shu-Yun Zhang, Amaya I. Wolf, Liping Wang, H. Christian Eberl, Michael Klein, Marcus Bantscheff, Kelvin Nurse, Adam Kenneth Charnley, Ramanjulu Joshi M, Jessica L. Schneck, Stephanie Lehmann, Jim Clemens, Axel Hoos, Michael Adam, Christopher B. Hopson, Todd L. Graybill, Jeffrey Guss, Jerry L. Adams, John F. Mehlmann, Jingsong Yang, Robert Singhaus, Michael Reilly, Ana C. Puhl, Robert W. Marquis, Li Yue, John Bertin, Patrick Moore, Angel Morales, James F. Smothers, Kevin J. Duffy, Viera Kasparcova, Peter J. Gough, Giovanna Bergamini, Kevin Foley, Kamelia Behnia, Lara Kathryn Leister, Marcel Muelbaier, G. Scott Pesiridis, Neysa Nevins, James Kang, Yiqian Lian, Guosen Ye, Nestor O. Concha
Publikováno v:
Nature. 570:E53-E53
Change history: In this Letter, author Ana Puhl was inadvertently omitted; this error has been corrected online.An amendment to this paper has been published and can be accessed via a link at the top of the paper.