Zobrazeno 1 - 10
of 43
pro vyhledávání: '"Noel A. Powell"'
Autor:
Surabhi Nair, Mohammed Q. Qutaish, Noel Aaron Powell, Dima Chaar, Ali Ghayoor, Jack Heimann, Jesse J. Winters, Jenna M. Sullivan, Larry W. Hardy, Jon Oscherwitz, Israel Liberzon, Lauren E. Chaby, Ildiko Polyak, Elizabeth Rodriguez
Publikováno v:
Behavioural Brain Research. 396:112902
To interrogate whether altered function of the hippocampal-mPFC circuit underlies the deficit in fear extinction recall in rats subjected to single-prolonged stress (SPS), changes in brain region-specific metabolic rate were measured in male rats (co
Autor:
Justin A. Caravella, Daliya Banerjee, Noel A. Powell, Jason D. Fontenot, Andres McKenzie, Istvan J. Enyedy, Victor Sukbong Hong, Douglas Marcotte, Laura Silvian, Jianhua Chao, Kurt Van Vloten
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:2459-2463
RORγ plays a critical role in controlling a pro-inflammatory gene expression program in several lymphocyte lineages including T cells, γδ T cells, and innate lymphoid cells. RORγ-mediated inflammation has been linked to susceptibility to Crohn's
Autor:
Q. Kevin Fang, John Emmerson Campbell, Una Campbell, Philip Jones, Noel Aaron Powell, Vadim Alexandrov, Emily Sabath, Liming Shao, Kerry L. Spear, Irene Morganstern, Thomas H. Large, Taleen Hanania, Hua M. Zhong
Publikováno v:
MedChemComm. 7:1093-1101
Phenotypic drug discovery (PDD) is increasingly being recognized as a viable compliment to target-based drug discovery (TDD). By measuring functional changes, typically at a systems level, PDD can facilitate the identification of compounds having a d
Autor:
Cornel Catana, Lisa A. Perrin, Jeff Ohren, Jeremy J. Edmunds, John Quin, Derek James Sheehan, Sangita M. Baxi, Jennifer K. Hoffman, Jeffrey T. Kohrt, Amy M. Delaney, Fred L. Ciske, Michael Kaufman, Noel A. Powell, Patrick I. McConnell
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:1046-1050
We report the SAR around a series of 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase. 2-Aminophenethyl analogs demonstrate excellent potency but moderate kinase selectivity, while 2-aminobenzyl analogs that fill the Ala571 subpocket exhi
Autor:
Jo Ann Davis, Christopher F. Bigge, Mehran Jalaie, Seungil Han, Jeffrey F. Ohren, Jing Chen, Noel A. Powell, Fred A. Ciske, Agustin Casimiro-Garcia, Teresa Ellis, Ronald J. Heemstra, Declan Flynn, Nadia Esmaeil
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:767-772
Identification of a series of imidazo[4,5-c]pyridin-4-one derivatives that act as dual angiotensin II type 1 (AT1) receptor antagonists and peroxisome proliferator-activated receptor-γ (PPARγ) partial agonists is described. Starting from a known AT
Autor:
Yuli Wang, Derek James Sheehan, Cornel Catana, Doh-Yeel Lee, Amy M. Delaney, Lisa A. Perrin, Fang Sun, Jeff Ohren, Frank Schwende, Kevin J. Filipski, Patrick I. McConnell, Jeffrey T. Kohrt, Noel A. Powell, Michael Kaufman, Francis Bourbonais, Huifen Chen, Jeremy E. Edmunds
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:190-193
We report the discovery of a novel series of spiroindoline-based inhibitors of Sky kinase that bind in the ATP-binding site and exhibit high levels of kinome selectivity through filling the Ala571-subpocket. These inhibitors exhibit moderate oral bio
Autor:
Noel A. Powell, Joseph E. Duran, Timothy J. Hagen, Robert M. Kennedy, Fred L. Ciske, Daniel D. Holsworth, Cuiman Cai, Jeremy J. Edmunds, Daniele M. Leonard
Publikováno v:
Tetrahedron Letters. 51:4441-4444
We have optimized the Pd-catalyzed intramolecular α-arylation of 2-(2-halo-benzyl)-cyclohexanones and found that the use of 2-(dicyclohexylphosphino)-2′,4′,6′-tri-i-propyl-1,1′-biphenyl (X-Phos) as an added ligand led to a reproducible, effi
Publikováno v:
International Journal of Peptide and Protein Research. 44:427-434
RGD peptides are known as important ligands for integrin receptors in the cell adhesion process. The selectivity of RGD peptides for a certain integrin receptor is partly dependent on the RGD conformation and the residues surrounding the RGD sequence
Autor:
Chad A. Van Huis, Wendy Collard, Cuiman Cai, Michelle Mastronardi, Roxane Collins, Michael J. Ryan, Jeremy J. Edmunds, Erli Zhang, Mehran Jalaie, Chungang Gu, Ken Mennen, John W. Bryant, Patrick I. McConnell, Fred L. Ciske, Suzie Ferreira, Jacqueline E. Day, Daniel D. Holsworth, Noel A. Powell, Igor Mochalkin
Publikováno v:
Bioorganic & Medicinal Chemistry. 15:5912-5949
We report the design and synthesis of a series of 6-(2,4-diaminopyrimidinyl)-1,4-benzoxazin-3-ones as orally bioavailable small molecule inhibitors of renin. Compounds with a 2-methyl-2-aryl substitution pattern exhibit potent renin inhibition and go
Autor:
Joanne L. Viney, Victor Hong, Arthur G. Taveras, Chi-Chi Peng, Daliya Banerjee, Kevin Guertin, Laura Silvian, Richard H. Hutchings, Howard Jones, Douglas Marcotte, Liaomin Peng, Noel A. Powell, Kevin Little, Jianhua Chao, Tonika Bohnert, Kurt Van Vloten, Istvan J. Enyedy, Jason D. Fontenot
Publikováno v:
Bioorganicmedicinal chemistry letters. 25(15)
RORγt is a pivotal regulator of a pro-inflammatory gene expression program implicated in the pathology of several major human immune-mediated diseases. Evidence from mouse models demonstrates that genetic or pharmacological inhibition of RORγ activ