2-Aminothiazole as a Novel Kinase Inhibitor Template. Structure−Activity Relationship Studies toward the Discovery of N-(2-Chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1 …

…, HF de Fex, KW McIntyre, DJ Shuster… - Journal of medicinal …, 2006 - ACS Publications
2-Aminothiazole (1) was discovered as a novel Src family kinase inhibitor template through
screening of our internal compound collection. Optimization through successive structure−…

Characterization of E-selectin-deficient mice: demonstration of overlapping function of the endothelial selectins

…, KM Lombard-Gillooly, DJ Shuster, J Hubbard… - Immunity, 1994 - cell.com
The Initial rolling Interaction of leukocytes with the blood vessel wall during leukocyte trafficking
has been postulated to rely on members of the selectin family of adhesion molecules. …

A highly selective inhibitor of IκB kinase, BMS‐345541, blocks both joint inflammation and destruction in collagen‐induced arthritis in mice

KW McIntyre, DJ Shuster, KM Gillooly… - … : Official Journal of …, 2003 - Wiley Online Library
Objective The transcription of several cytokines, cell adhesion molecules, and enzymes involved
in the inflammatory and destructive mechanisms of rheumatoid arthritis is dependent on …

IL-1 receptor accessory protein is an essential component of the IL-1 receptor

EB Cullinan, L Kwee, P Nunes, DJ Shuster… - The Journal of …, 1998 - journals.aai.org
The recently described IL-1R accessory protein (IL-1R AcP) interacts with IL-1β and the IL-1
type-IR (IL-1RI), but an essential requirement for IL-1R AcP in IL-1 signaling in vitro has not …

Reduced incidence and severity of collagen‐induced arthritis in interleukin‐12‐deficient mice

KW McIntyre, DJ Shuster, KM Gillooly… - European journal of …, 1996 - Wiley Online Library
Collagen‐induced arthritis (CIA) is an animal model for rheumatoid arthritis. The disease is
elicited by immunization of genetically susceptible DBA/1 mice with type II collagen, resulting …

Selective Itk inhibitors block T-cell activation and murine lung inflammation

…, DJ Shuster, XX Yang, R Townsend, J Postelnek… - Biochemistry, 2004 - ACS Publications
Nonreceptor protein tyrosine kinases including Lck, ZAP-70, and Itk play essential roles in T-cell
receptor (TCR) signaling. Gene knockout studies have revealed that mice lacking these …

Design, Synthesis, and Anti-inflammatory Properties of Orally Active 4-(Phenylamino)-pyrrolo[2,1-f][1,2,4]triazine p38α Mitogen-Activated Protein Kinase Inhibitors

…, KW McIntyre, S Pitt, DR Shen, DJ Shuster… - Journal of medicinal …, 2008 - ACS Publications
A novel structural class of p38 mitogen-activated protein (MAP) kinase inhibitors consisting
of substituted 4-(phenylamino)-pyrrolo[2,1-f][1,2,4]triazines has been discovered. An initial …

Rationally designed, conformationally constrained inverse agonists of RORγt—identification of a potent, selective series with biologic-like in vivo efficacy

…, M Yarde, ME Cvijic, S Li, DJ Shuster… - Journal of Medicinal …, 2019 - ACS Publications
RORγt is an important nuclear receptor that regulates the production of several pro-inflammatory
cytokines such as IL-17 and IL-22. As a result, RORγt has been identified as a potential …

Structure-based discovery of phenyl (3-phenylpyrrolidin-3-yl) sulfones as selective, orally active RORγt inverse agonists

…, DR Wu, M Yarde, DR Shen, DJ Shuster… - ACS Medicinal …, 2019 - ACS Publications
A new phenyl (3-phenylpyrrolidin-3-yl)sulfone series of RORγt inverse agonists was discovered
utilizing the binding conformation of previously reported bicyclic sulfonamide 1. Through …

Discovery of 4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a Clinical p38α MAP …

…, KW McIntyre, L Salter-Cid, DJ Shuster… - Journal of medicinal …, 2010 - ACS Publications
The discovery and characterization of 7k (BMS-582949), a highly selective p38α MAP kinase
inhibitor that is currently in phase II clinical trials for the treatment of rheumatoid arthritis, is …