Zobrazeno 1 - 10
of 38
pro vyhledávání: '"Alan B. Northrup"'
Autor:
Wonsuk Chang, Michael D. Altman, Charles A. Lesburg, Samanthi A. Perera, Jennifer A. Piesvaux, Gottfried K. Schroeder, Daniel F. Wyss, Saso Cemerski, Yiping Chen, Edward DiNunzio, Andrew M. Haidle, Thu Ho, Ilona Kariv, Ian Knemeyer, Johnny E. Kopinja, Brian M. Lacey, Jason Laskey, Jongwon Lim, Brian J. Long, Yanhong Ma, Matthew L. Maddess, Bo-Sheng Pan, Jeremy P. Presland, Edward Spooner, Dietrich Steinhuebel, Quang Truong, Zhibo Zhang, Jianmin Fu, George H. Addona, Alan B. Northrup, Emma Parmee, James R. Tata, David Jonathan Bennett, Jared N. Cumming, Tony Siu, B. Wesley Trotter
Publikováno v:
Journal of medicinal chemistry. 65(7)
Stereochemically and structurally complex cyclic dinucleotide-based stimulator of interferon genes (STING) agonists were designed and synthesized to access a previously unexplored chemical space. The assessment of biochemical affinity and cellular po
Autor:
Richard Tschirret-Guth, Caroline McGregor, Mark Cartwright, Michael D. Altman, Suman Mukherjee, Iain Martin, Alan B. Northrup, Pierre Daublain, Kung-I Feng, Rebecca Nofsinger
Publikováno v:
Molecular Pharmaceutics. 14:1634-1645
The purpose of this research was to assess variability in pharmacokinetic profiles (PK variability) in preclinical species and identify the risk factors associated with the properties of a drug molecule that contribute to the variability. Exposure da
Autor:
Matthew G. Stanton, Sanjeev Munshi, Ian W. Davies, Kaleen Konrad Childers, Michael Hutton, Lee Warren, Mansuo Hayashi, Anna A. Zabierek, Alan B. Northrup, Alexander A. Szewczak, Hugh Nuthall, Andrew M. Haidle, Ben Munoz, Dapeng Chen, Hua-Poo Su, Yongquan Hou, Jason D. Katz, Andreas Harsch, Michael D. Altman, James P. Jewell
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 27:114-120
The initial structure activity relationships around an isoindoline uHTS hit will be described. Information gleaned from ligand co-crystal structures allowed for rapid refinements in both MARK potency and kinase selectivity. These efforts allowed for
Autor:
Andrew M. Haidle, Alan B. Northrup, Alexander A. Szewczak, Lee Warren, Jason D. Katz, James P. Jewell, Mansuo Hayashi, Hugh Nuthall, Andreas Harsch, Michael D. Altman, Ian W. Davies, Dapeng Chen, Kaleen Konrad Childers, Michael Hutton, Anna A. Zabierek, Matthew G. Stanton, Yongquan Hou, Ben Munoz
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 27:109-113
Attempts to optimize pharmacokinetic properties in a promising series of pyrrolopyrimidinone MARK inhibitors for the treatment of Alzheimer's disease are described. A focus on physical properties and ligand efficiency while prosecuting this series af
Autor:
Stephen E. Alves, Michael A. Crackower, Philip R Cooper, Alan B. Northrup, Dennis M. Zaller, Erich E Sirkowski, Gretchen A. Baltus, Cynthia J. Koziol-White, Steven L. Smock, Blanca E. Himes, Reynold A. Panettieri, Yanlin Jia
Publikováno v:
British Journal of Pharmacology. 173:3080-3087
Background and purpose Asthma manifests as a heterogeneous syndrome characterized by airway obstruction, inflammation and hyper-reactivity (AHR). Spleen tyrosine kinase (Syk) mediates allergen-induced mast cell degranulation, a central component of a
Autor:
Jie Zhang-Hoover, Chaomin Li, Erin F. Mulrooney, Christian Fischer, Alan B. Northrup, Melanie A. Kleinschek, Jeremy Presland, Brian M. Andresen, Anthony Donofrio, Jason D. Brubaker, Matthew Lloyd Childers, Thierry O. Fischmann, Jongwon Lim, Alexander Hicks, Sue Jin, James Baker, Lilly Y. Moy, Hongmin Chen, Antoaneta S. Necheva, Luis E. Torres, Ruojing Yang, Michael D. Altman, Craig R. Gibeau, Duan Liu, Heidi Ferguson, Charles A. Lesburg, John Maclean, Erica Leccese, Faruk Mansoor, Graham Smith, Sam Kattar, Yiping Chen, Larissa Rakhilina
Publikováno v:
Bioorganicmedicinal chemistry letters. 27(12)
Interleukin-1 receptor associated kinase 4 (IRAK4) has been implicated in IL-1R and TLR based signaling. Therefore selective inhibition of the kinase activity of this protein represents an attractive target for the treatment of inflammatory diseases.
Autor:
Lin Xu, Grace Chan, Melaney Bouthillette, Craig Rosenstein, Sathyajith E. Kumarasinghe, C. Gary Marshall, Tony Siu, Anjili Mathur, Alan B. Northrup, Michael D. Altman, Christopher J. Dinsmore, Matthew H. Katcher, Catherine White, Eric Bachman, Jonathan R. Young
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:1466-1471
This communication discusses the discovery of novel reverse tricyclic pyridones as inhibitors of Janus kinase 2 (JAK2). By using a kinase cross screening approach coupled with molecular modeling, a unique inhibitor–water interaction was discovered
Autor:
Emily Hickey, Stella H. Vincent, Hongshi Yu, John H. Shin, Michael A. Crackower, Hyun-Hee Lee, Malgorzata A Gil, Michael Caniga, Jessica P. Alexander, Lily Y. Moy, Alan B. Northrup, Gissela Lieber, Richard L. Miller, Richard W. Chapman, Erich E Sirkowski, Thomas A. Miller, Yanlin Jia, Hani Houshyar, Nancy Kelly, J. Michael Ellis, Xiomara Fernandez, Alan Wilhelm, Hongmin Chen, William M. Abraham
Publikováno v:
American Journal of Respiratory Cell and Molecular Biology. 49:1085-1092
Spleen tyrosine kinase (SYK) is a key activator of signaling pathways downstream of multiple surface receptors implicated in asthma. SYK function has been extensively studied in mast cells downstream of the high-affinity IgE receptor, FcεR1. Preclin
Autor:
Michael D. Altman, Christopher J. Dinsmore, John F. Reilly, Jonathan R. Young, Chaomin Li, Sangita B. Patel, Deborah Walker, Craig Rosenstein, David Joseph Guerin, Timothy Allison, Harold Hatch, Stephen M. Soisson, Sujal V. Deshmukh, Bart Lutterbach, Bo Sheng Pan, Danielle Falcone, Michael H. Reutershan, Keith W. Rickert, Matthew H. Katcher, Wei Lu, Melissa Chenard, Kevin J. Wilson, Alan B. Northrup, Alexander A. Szewczak, Matthew H. Daniels
Publikováno v:
Journal of Medicinal Chemistry. 56:2294-2310
This report documents the first example of a specific inhibitor of protein kinases with preferential binding to the activated kinase conformation: 5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one 11r (MK-8033), a dual c-Met/Ron inhibitor under investigati
Autor:
Cynthia J, Koziol-White, Yanlin, Jia, Gretchen A, Baltus, Philip R, Cooper, Dennis M, Zaller, Michael A, Crackower, Erich E, Sirkowski, Steven, Smock, Alan B, Northrup, Blanca E, Himes, Stephen E, Alves, Reynold A, Panettieri
Publikováno v:
British journal of pharmacology. 173(21)
Asthma presents as a heterogeneous syndrome characterized by airway obstruction, inflammation and hyper-reactivity (AHR). Spleen tyrosine kinase (Syk) mediates allergen-induced mast cell degranulation, a central component of allergen-induced inflamma