Zobrazeno 1 - 10
of 16
pro vyhledávání: '"Paul D. Greenspan"'
Autor:
Alexandra E. Gould, Courtney Cullis, Lee Hong Myung, David Lok, Rachel E. Gershman, Scott R. Rowland, Miho Mizutani, Dave Janowick, Gipson Krista E, Vihren Kolev, Robert J. Griffin, Joe Conlon, Steve Stroud, Akito Hata, Jeffrey Ciavarri, Dylan Bradley England, Cardin David P, Sandeep Pusalkar, Paul D. Greenspan, Adnan O Abu-Yousif, Jenna Malley, Doanh Mai, Michael Shaw, Ji Zhang, Robert J. Skene, Hu Zhigen, Matthew A. Jones, Atsushi Matsuda, Shih-Chung Huang, Nina Molchanova, Xu Tianlin, Jian Huang, He Xu, Stepan Vyskocil, Nanda Gulavita, Francois Soucy, Gang Li, Yongbo Hu, Liting Ma, Steven P. Langston, Zhan Shi, Christelle C. Renou, Luhua Shen, Sean Harrison, Elise Nunes, Kenneth M. Gigstad, Yosuke Sato, Hirotake Mizutani
Publikováno v:
Journal of Medicinal Chemistry. 64:6902-6923
Stimulator of Interferon Genes (STING) plays an important role in innate immunity by inducing type I interferon production upon infection with intracellular pathogens. STING activation can promote increased T-cell activation and inflammation in the t
Autor:
Xingyue He, Mark G. Qian, Matthew O. Duffey, Larry Cohen, Michael D. Sintchak, Mi-Sook Kim, Jessica Riceberg, Vaishali Shindi, Kelly Connolly, Jianping Guo, Agatha Zawadzka, Rachel E. Gershman, Teresa A. Soucy, Neil Bence, Zhigen Hu, Xiaofeng Yang, Shumet A. Hailu, Nina Molchinova, Nanda Gulavita, Ji Zhang, Hirotake Mizutani, Keli Song, A D Patil, Scott Freeze, Jessica Grieves, Dylan Bradley England, Roushan Afroze, James J. Minissale, Anya Lublinsky, Mitsuhiro Ito, David Lok, Scott Weston Lane, William D. Mallender, Stephen Grossman, Kara Hoar, Nitya Durvasula, Bei-Ching Chuang, Yongbo Hu, Steven P. Langston, Sai M. Pulukuri, Miho Mizutani, Ryan Chau, Nancy Bump, Katherine M. Galvin, Christopher F. Claiborne, Paul D. Greenspan, He Xu, Gaulin Jeffrey L, Melissa Gallery, Douglas Bowman, Yana Wang, Koji Ono, Mcintyre Charles
Publikováno v:
Journal of medicinal chemistry. 64(5)
SUMOylation is a reversible post-translational modification that regulates protein function through covalent attachment of small ubiquitin-like modifier (SUMO) proteins. The process of SUMOylating proteins involves an enzymatic cascade, the first ste
Autor:
Mi-Sook Kim, Mansoureh Rezaei, Jouhara Chouitar, Katherine Brewer, Michael D. Smith, Alexandra E. Gould, Katherine Galvin, Shih-Chung Huang, Dong Mei Zhang, Sharmila Adhikari, Hirotake Mizutani, Steven P. Langston, Dylan England, Paul D. Greenspan, Emily F. Calderwood, Craig Fisher, Sean J. Harrison, Li-Ting Ma, Saurabh Menon, Roushan Afroze, Jeffery Gaulin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:1156-1160
Investigations of a biaryl ether scaffold identified tetrahydronaphthalene Raf inhibitors with good in vivo activity; however these compounds had affinity toward the hERG potassium channel. Herein we describe our work to eliminate this hERG activity
Autor:
John Newcomb, James M. Gavin, Nancy J. Bump, Stephen Tirrell, Lawrence R. Dick, Saurabh Menon, Jessica Huck, Petter Veiby, Benjamin S. Amidon, Yu Yang, Marc L. Hyer, Paul D. Greenspan, Fleming Paul E, Teresa A. Soucy, Jim Brownell, Michael Sintchak, Josh Powe, Steve Langston, Mark Manfredi, Judy Shi, Jeff Ciavarri, Darshan S. Sappal, Frank Bruzzese, Mike Kuranda, Katherine Galvin, Michael Milhollen, Ping Li, Neil F. Bence, Jing Tao Wu, Claudia Rabino, Chris Claiborne, Tary Traore, Jennifer Duffy, Jessica Riceberg, Robert J. Griffin, Kara Hoar, Anya Lublinsky, Bradley Stringer, Sai M Pulukuri
Publikováno v:
Nature medicine. 24(2)
The ubiquitin-proteasome system (UPS) comprises a network of enzymes that is responsible for maintaining cellular protein homeostasis. The therapeutic potential of this pathway has been validated by the clinical successes of a number of UPS modulator
Autor:
Emily F. Calderwood, Kathleen Aertgeerts, Michael D. Smith, Dylan Bradley England, Roushan Afroze, Ryan Chau, Stepan Vyskocil, Nancy E. Forsyth, Dong Mei Zhang, Ruth Adams, Stephen G. Stroud, O. P. Veiby, Christelle C. Renou, R. Scott Rowland, Erin Paske, Jane X. Liu, Ming Tregay, Michael D. Sintchak, Juliet A Williams, Shih-Chung Huang, Xu Tianlin, Bheemashankar Kulkarni, Sharmila Adhikari, Yuan Tian, Jason Yano, Christopher Blackburn, Paul D. Greenspan, Cheryl A. Farrer, Matthew O. Duffey, Liting Ma, Mi-Sook Kim, Qin Zhang, Sean Harrison, Hirotake Mizutani, Katherine M. Galvin, Alexandra E. Gould, Johnny J. Yang, Steven P. Langston, Dave Janowick, Natalia Iartchouk, Mansoureh Rezaei, Jeffery Gaulin, Khristofer Garcia, Hongbo Zeng, Ribo Guo, Tricia J. Vos, Jouhara Chouitar, Saurabh Menon
Publikováno v:
Journal of Medicinal Chemistry. 54:1836-1846
Inhibition of mutant B-Raf signaling, through either direct inhibition of the enzyme or inhibition of MEK, the direct substrate of Raf, has been demonstrated preclinically to inhibit tumor growth. Very recently, treatment of B-Raf mutant melanoma pat
Autor:
Michael H. Chin, Huanghai Zhou, Main Alan J, Susan Uziel-Fusi, Lester I. Barsky, Shripad S. Bhagwat, Kenneth E. Lipson, R. H. Jackson, Robert A. Doti, Alan R. Engle, Paul D. Greenspan, Lisa M. Frey
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 7:949-954
A series of N-aryl cinnamides has been prepared and assayed for antagonism of the leukotriene B4 receptor. Several compounds in this series were found to be highly potent antagonists of the human neutrophil receptor, based on a whole cell binding ass
Autor:
Kenneth E. Lipson, Huanghai Zhou, Lester I. Barsky, Robert A. Doti, Alan R. Engle, Paul D. Greenspan, Lisa M. Frey, R. H. Jackson, Michael H. Chin, Main Alan J, Shripad S. Bhagwat, Susan Uziel-Fusi
Publikováno v:
ChemInform. 28
A series of N-aryl cinnamides has been prepared and assayed for antagonism of the leukotriene B4 receptor. Several compounds in this series were found to be highly potent antagonists of the human neutrophil receptor, based on a whole cell binding ass
Autor:
Paul D. Greenspan, et al. et al.
Publikováno v:
ChemInform. 30
Autor:
Paul D. Greenspan, Susan Chen, Liting Ma, Jane X. Liu, Johnny J. Yang, Qin Zhang, Ruth Adams, Shih-Chung Huang, Bheemashankar Kulkarni, Ryan W. Chau, Masayuki Nagayoshi, Matthew O. Duffey, Shaoxia Yu, Christopher Blackburn, Khristofer Garcia, Katherine M. Galvin, Tricia J. Vos, Sean Harrison, R. Scott Rowland, Xu Tianlin, Steven P. Langston, Mi-Sook Kim, Saurabh Menon, Alexandra E. Gould
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(16)
The discovery of novel pyrazoline derivatives as B-Raf (V600E) inhibitors is described in this report. Chemical modification of the pyrazoline scaffold led to the development of SAR and identified potent and selective inhibitors of B-Raf (V600E). Det
Autor:
David Farley, J. R. Doughty, Scott Douglas Cowen, Elizabeth Quadros, Tommasi Ruben A, Leslie Wighton Mcquire, Andrew Wigg, Huanghai Zhou, Karen Toscano, David E. Coppa, Zheng Fang, Zengming Du, Siyuan Zhou, Paul D. Greenspan, Kirk Clark
Publikováno v:
Bioorganicmedicinal chemistry letters. 13(22)
To improve the pharmacokinetics of a previously reported series of dipeptidyl nitrile cathepsin B inhibitors, the P(2)-P(3) amide group was replaced with an arylamine. Further optimization of this template resulted in highly potent and selective inhi