Zobrazeno 1 - 10
of 15
pro vyhledávání: '"Richard K Frisbie"'
Autor:
David Jonathan Wasilko, Brian S. Gerstenberger, Kathleen A. Farley, Wei Li, Jennifer Alley, Mark E. Schnute, Ray J. Unwalla, Jorge Victorino, Kimberly K. Crouse, Ru Ding, Parag V. Sahasrabudhe, Fabien Vincent, Richard K. Frisbie, Alpay Dermenci, Andrew Flick, Chulho Choi, Gary Chinigo, James J. Mousseau, John I. Trujillo, Philippe Nuhant, Prolay Mondal, Vincent Lombardo, Daniel Lamb, Barbara J. Hogan, Gurdeep Singh Minhas, Elena Segala, Christine Oswald, Ian W. Windsor, Seungil Han, Mathieu Rappas, Robert M. Cooke, Matthew F. Calabrese, Gabriel Berstein, Atli Thorarensen, Huixian Wu
Publikováno v:
Nature Communications, Vol 15, Iss 1, Pp 1-13 (2024)
Abstract The CC chemokine receptor 6 (CCR6) is a potential target for chronic inflammatory diseases. Previously, we reported an active CCR6 structure in complex with its cognate chemokine CCL20, revealing the molecular basis of CCR6 activation. Here,
Externí odkaz:
https://doaj.org/article/91af6bd491994266b492f68b0994ea6e
Autor:
Wei Li, Kimberly K Crouse, Jennifer Alley, Richard K Frisbie, Susan C Fish, Tatyana A Andreyeva, Lori A Reed, Mitchell Thorn, Giovanni DiMaggio, Carol B Donovan, Donald Bennett, Jeonifer Garren, Elias Oziolor, Jessie Qian, Leah Newman, Amanda P Vargas, Steven W Kumpf, Stefanus Johannes Steyn, Mark E Schnute, Atli Thorarensen, Martin Hegen, Erin Stevens, Mark Collinge, Thomas A Lanz, Fabien Vincent, Michael S Vincent, Gabriel Berstein
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. :JPET-AR
Autor:
Agustin Casimiro-Garcia, Christophe Allais, Agnes Brennan, Chulho Choi, Gabriela Dower, Kathleen A. Farley, Margaret Fleming, Andrew Flick, Richard K. Frisbie, Justin Hall, David Hepworth, Hannah Jones, John D. Knafels, Steve Kortum, Frank E. Lovering, John P. Mathias, Sashi Mohan, Paul M. Morgan, Chuenlei Parng, Kevin Parris, Nick Pullen, Franklin Schlerman, John Stansfield, Joseph W. Strohbach, Felix F. Vajdos, Fabien Vincent, Hong Wang, Xiaolun Wang, Robert Webster, Stephen W. Wright
Publikováno v:
Journal of medicinal chemistry. 65(1)
A diaryl ketone series was identified as vanin-1 inhibitors from a high-throughput screening campaign. While this novel scaffold provided valuable probe
Autor:
Jeanne Chang, Ravi G. Kurumbail, Margaret Fleming, Joanne Brodfuehrer, Katherine L. Lee, Frank Lovering, Shashi Mohan, Heather V. Dowty, Fabien Vincent, Jayasankar Jasti, Steve Kortum, Christoph W. Zapf, Jotham Wadsworth Coe, Christophe Allais, Strohbach Joseph Walter, Nikolaos Papaioannou, Ann Aulabaugh, Julia A. Guzova, Paul Morgan, Richard K. Frisbie, WeiDong Ding, David Hepworth
Publikováno v:
European Journal of Medicinal Chemistry. 145:606-621
Many diseases are believed to be driven by pathological levels of reactive oxygen species (ROS) and oxidative stress has long been recognized as a driver for inflammatory disorders. Apoptosis signal-regulating kinase 1 (ASK1) has been reported to be
Autor:
Lori Krim Gavrin, David Hepworth, Jennifer R. Thomason, Iain Kilty, Joel Adam Goldberg, Christoph W. Zapf, Vikram R. Rao, Brian P. Boscoe, Akshay Patny, Peter T. Symanowicz, Marina W.H. Shen, Kevin J. Curran, Elizabeth Murphy, Martin Hegen, Fabien Vincent, Richard Vargas, Satwik Kamtekar, Heidi M. Morgan, Heidi R. Hope, Richard K. Frisbie, Jeanne S. Chang, Ken Dower, Susan E. Drozda, Strohbach Joseph Walter, Mathias John Paul, David R. Anderson, Jacqueline E. Day, Stephen W. Wright, Ivan J. Samardjiev, Seungil Han, Julia H Shin, Frank Lovering, Andrea G Bree, Arthur Lee, Holly H. Soutter, Joanne Brodfuehrer, John David Trzupek, Brian Samas, Christoph Martin Dehnhardt, Michael Dennis Lowe, Catherine M. Ambler, Seung Won Chung, Eddine Saiah, Nikolaos Papaioannou, Pierce Betsy S, Jiangli Yan, Katherine L. Lee, Lih-Ling Lin, Chulho Choi
Publikováno v:
Journal of Medicinal Chemistry. 60:5521-5542
Through fragment-based drug design focused on engaging the active site of IRAK4 and leveraging three-dimensional topology in a ligand-efficient manner, a micromolar hit identified from a screen of a Pfizer fragment library was optimized to afford IRA
Autor:
Jane M. Withka, Daniel W. Kung, Russell A. Miller, Matthew S. Dowling, Aaron C. Smith, Angela Wolford, Heather Eng, Janice A. Brown, Jun Xiao, Kris A. Borzilleri, Ravi G. Kurumbail, David J. Edmonds, Jessica Ward, Amit S. Kalgutkar, Colin R. Rose, Tim F. Ryder, Meihua Tu, Dilinie P. Fernando, Emily Cokorinos, David Hepworth, James A. Landro, Kimberly O. Cameron, Matthew F. Calabrese, Christopher T. Salatto, Francis Rajamohan, Andre Shavnya, Markus Boehm, Yuxia Mao, Allan R. Reyes, Richard K. Frisbie, Nicole Caspers, Edward L. Conn, Samit Kumar Bhattacharya
Publikováno v:
Journal of Medicinal Chemistry. 59:8068-8081
Adenosine monophosphate-activated protein kinase (AMPK) is a protein kinase involved in maintaining energy homeostasis within cells. On the basis of human genetic association data, AMPK activators were pursued for the treatment of diabetic nephropath
Autor:
Seungil Han, Aaron C. Smith, Melissa S. Harris, Timothy A. Subashi, Shawn Cabral, Lise R. Hoth, Nicole Caspers, Francis Rajamohan, Philip A. Carpino, Parag Sahasrabudhe, Ravi G. Kurumbail, Hong Wang, Jessica Ward, Edward L. Conn, Kris A. Borzilleri, James A. Landro, Jane M. Withka, Janice A. Brown, Russell A. Miller, Kimberly O. Cameron, Allyn T. Londregan, Richard K. Frisbie, Xiayang Qiu, Matthew F. Calabrese, Allan R. Reyes, Rachelle Magyar, Kieran F. Geoghegan
Publikováno v:
Structure. 22:1161-1172
SummaryAMP-activated protein kinase (AMPK) is a principal metabolic regulator affecting growth and response to cellular stress. Comprised of catalytic and regulatory subunits, each present in multiple forms, AMPK is best described as a family of rela
Autor:
David W. Piotrowski, Bruce M. Bechle, Paul D. Bonin, David D. Boyer, Shawn D. Doran, Gayatri Balan, Richard K. Frisbie, Paul S. Humphries, Walter C. Soeller, James A. Southers, Robert M. Oliver, John William Benbow, Xiaojing Yang, Kenneth J. DiRico, Edward L. Conn
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:2400-2403
The development of a series of novel 1,2,3,4-tetrahydroisoquinolin-1-ones as antagonists of G protein-coupled receptor 40 (GPR40) is described. The synthesis, in vitro inhibitory values for GPR40, in vitro microsomal clearance and rat in vivo clearan
Characterization of 11 commercial pyrethroids on the functional attributes of rat brain synaptosomes
Publikováno v:
Pesticide Biochemistry and Physiology. 92:61-69
The action of 11 commercial pyrethroids on Ca 2+ influx and glutamate release was assessed using high-throughput functional assays with rat brain synaptosomes to better understand the mechanistic nature of pyrethroid-induced neurotoxicity and aid in
Publikováno v:
Pesticide Biochemistry and Physiology. 88:312-320
Effects of deltamethrin on voltage-sensitive calcium channels (VSCC) from rat brain (Cav2.2) expressed in Xenopus oocytes were assessed electrophysiologically. Deltamethrin reduced peak current of wild-type Cav2.2 in a stereospecific and concentratio