Zobrazeno 1 - 10
of 28
pro vyhledávání: '"Patrick, Brassil"'
Autor:
David T. Beattie, M. Teresa Pulido-Rios, Fei Shen, Melissa Ho, Eva Situ, Pam R. Tsuruda, Patrick Brassil, Melanie Kleinschek, Sharath Hegde
Publikováno v:
Journal of Inflammation, Vol 14, Iss 1, Pp 1-11 (2017)
Abstract Background An unmet need remains for safe and effective treatments to induce and maintain remission in inflammatory bowel disease (IBD) patients. The Janus kinase (JAK) inhibitor, tofacitinib, has demonstrated robust efficacy in ulcerative c
Externí odkaz:
https://doaj.org/article/d1b63811139649dbba728e06e5dfa193
Autor:
Rhiannon N Hardwick, Patrick Brassil, Ilaria Badagnani, Kimberly Perkins, Glenmar P Obedencio, Andrea S Kim, Michael W Conner, David L Bourdet, Eric B Harstad
Publikováno v:
Toxicological Sciences. 186:323-337
Izencitinib (TD-1473), an oral, gut-selective pan-Janus kinase (JAK) inhibitor under investigation for treatment of inflammatory bowel diseases, was designed for optimal efficacy in the gastrointestinal tract while minimizing systemic exposures and J
Autor:
Raj Bhandari, M. Teresa Pulido-Rios, David T Beattie, Reuben Sana, Brihad Abhyankar, Jonathan A. Leighton, Jacky Woo, Richard Graham, Eva Situ, Ravi Ganeshappa, Erik Sandvik, Melanie A. Kleinschek, Whitney Krey, David L. Boyle, Deanna D Nguyen, Julián Panés, William J. Sandborn, Patrick Brassil
Publikováno v:
Journal of Crohn's & Colitis
Journal of Crohn's & colitis, vol 14, iss 9
Journal of Crohn's & colitis, vol 14, iss 9
Background and Aims Oral systemic pan-Janus kinase [JAK] inhibition is effective for ulcerative colitis [UC] but is limited by toxicities. We describe preclinical to clinical translation of TD-1473—an oral gut-selective pan-JAK inhibitor—from in
Autor:
Jonathan M. Maher, Rui Zhang, Gopinath Palanisamy, Kimberly Perkins, Lynda Liu, Patrick Brassil, Alexander McNamara, Arthur Lo, Adam D. Hughes, Jitendra Kanodia, Svitlana Kulyk, Kristen J. Nikula, Hart S. Dengler, Amy Scandurra, Ingrid Lua, Eric Harstad
Publikováno v:
Toxicology and Applied Pharmacology. 438:115905
Systemic therapies targeting transforming growth factor beta (TGFβ) or TGFβR1 kinase (ALK5) have been plagued by toxicities including cardiac valvulopathy and bone physeal dysplasia in animals, posing a significant challenge for clinical developmen
Autor:
Jon Read, James W. Janetka, David Whitston, Haixia Wang, Jason Breed, Paul Lyne, Patrick Brassil, Nancy DeGrace, Michael Grondine, Qibin Su, Dorin Toader, Alexander Hird, Bin Yang, Chun Deng, Melissa Vasbinder, Stephanos Ioannidis, Yan Yu
Publikováno v:
Journal of Medicinal Chemistry. 61:1061-1073
Checkpoint kinase 1 (CHK1) inhibitors are potential cancer therapeutics that can be utilized for enhancing the efficacy of DNA damaging agents. Multiple small molecule CHK1 inhibitors from different chemical scaffolds have been developed and evaluate
Autor:
Melissa Ho, Patrick Brassil, Sharath S. Hegde, M. Teresa Pulido-Rios, Fei Shen, David Beattie, Pam R. Tsuruda, Melanie A. Kleinschek, Eva Situ
Publikováno v:
Journal of Inflammation, Vol 14, Iss 1, Pp 1-11 (2017)
Journal of Inflammation (London, England)
Journal of Inflammation (London, England)
Background An unmet need remains for safe and effective treatments to induce and maintain remission in inflammatory bowel disease (IBD) patients. The Janus kinase (JAK) inhibitor, tofacitinib, has demonstrated robust efficacy in ulcerative colitis pa
Autor:
Bin Yang, Sean Redmond, Robert Godin, James W. Janetka, Daniel John Russell, Kevin Daly, Michael S. Bodnarchuk, Qibin Su, Xiaolan Zheng, Les A. Dakin, Alexander Hird, Patrick Brassil, Maureen Hattersley
Publikováno v:
Bioorganicmedicinal chemistry. 28(2)
Aberrant hedgehog (Hh) pathway signaling is implicated in multiple cancer types and targeting the Smoothened (SMO) receptor, a key protein of the Hh pathway, has proven effective in treating metastasized basal cell carcinoma. Our lead optimization ef
Autor:
Howard B Haimes, Amy Kutschke, Gregory S. Basarab, Peter Doig, Vincent Galullo, John McNulty, Madhusudhan Reddy Gowravaram, Gregory G. Stone, Gunther Kern, Patrick Brassil, Virna J A Schuck
Publikováno v:
Journal of Medicinal Chemistry. 57:9078-9095
The compounds described herein with a spirocyclic architecture fused to a benzisoxazole ring represent a new class of antibacterial agents that operate by inhibition of DNA gyrase as corroborated in an enzyme assay and by the inhibition of precursor
Autor:
Phil Walker, Folkert Reck, John Breen, Joseph V. Newman, Charles J. Eyermann, David E. Ehmann, Janelle Comita-Prevoir, Stewart L. Fisher, Patrick Brassil, Mark Cronin, Richard A. Alm, Vincent Galullo, Marshall Morningstar, Barry R. Hayter, Tyler Grebe, Hajnalka E. Davis, Boudewijn Dejonge, Gloria Anne Breault, Bolin Geng
Publikováno v:
Journal of Medicinal Chemistry. 54:7834-7847
Novel non-fluoroquinolone inhibitors of bacterial type II topoisomerases (DNA gyrase and topoisomerase IV) are of interest for the development of new antibacterial agents that are not impacted by target-mediated cross-resistance with fluoroquinolones
Autor:
Ellen Freed, Lucienne Ronco, Timothy Pontz, Patrick Brassil, Haiqing Hu, Xiaolan Zheng, Muthusamy Jayaraman, Davies Audrey, Lillian Castriotta, Dennis Huszar, Maria-Elena Theoclitou, Murali V P Nadella, Daniel John Russell, Brian Aquila, Michael Collins, Vibha Oza, David Whitston, Tracy L. Deegan, Michael Howard Block, Deborah Lawson, Sandra Filla, Maniyan Padmanilayam, Erin Code, Paula Lewis, Jayachandran Ezhuthachan
Publikováno v:
Journal of Medicinal Chemistry. 54:6734-6750
Structure-activity relationship analysis identified (+)-N-(3-aminopropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-[1,2]thiazolo[5,4-d]pyrimidin-6-yl)-2-methylpropyl]-4-methylbenzamide (AZD4877), from a series of novel kinesin spindle protein (KSP) inhibitors,