Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition

Jean‐Baptiste Telliez, Martin E. Dowty, Lu Wang, +33

ACS Chemical Biology

Jak1 InhibitionImmunologyImmune RegulationInnate ImmunityInflammatory Arthritis +28

Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of (( <i>S</i> )-2,2-Difluorocyclopropyl)((1 <i>R</i> ,5 <i>S</i> )-3-(2-((1-methyl-1 <i>H</i> -pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841)

Andrew Fensome, Catherine M. Ambler, Eric P. Arnold, +30

Journal of Medicinal Chemistry

Identification of <i>N</i>-{<i>cis</i>-3-[Methyl(7<i>H</i>-pyrrolo[2,3-<i>d</i>]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases

Michael L. Vazquez, Neelu Kaila, Joseph W. Strohbach, +32

Journal of Medicinal Chemistry

ImmunodeficienciesJanus KinasesImmunologyPharmacotherapyImmunotherapy +20

Discovery of Clinical Candidate 1-{[(2 <i>S</i> ,3 <i>S</i> ,4 <i>S</i> )-3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl]methoxy}-7-methoxyisoquinoline-6-carboxamide (PF-06650833), a Potent, Selective Inhibitor of Interleukin-1 Receptor Associated Kinase 4 (IRAK4), by Fragment-Based Drug Design

Katherine L. Lee, Catherine M. Ambler, David R. Anderson, +46

Journal of Medicinal Chemistry

JAK inhibition with tofacitinib suppresses arthritic joint structural damage through decreased RANKL production

Timothy P. LaBranche, Michael I. Jesson, Chad Storer, +17

Arthritis & Rheumatism

The Interleukin‐1 Receptor–Associated Kinase 4 Inhibitor PF‐06650833 Blocks Inflammation in Preclinical Models of Rheumatic Disease and in Humans Enrolled in a Randomized Clinical Trial

Aaron Winkler, Weiyong Sun, Saurav De, +24

Arthritis & Rheumatology

Selective functional inhibition of JAK‐3 is sufficient for efficacy in collagen‐induced arthritis in mice

Tsung H. Lin, Martin Hegen, Elizabeth Quadros, +26

Arthritis & Rheumatism

Jak‐3 SelectivityImmunologyCell ProliferationWhole BloodMusculoskeletal Research +20

Immediate sensory nerve-mediated respiratory responses to irritants in healthy and allergic airway-diseased mice

John B. Morris, Peter T. Symanowicz, Joshua E. Olsen, +3

Journal of Applied Physiology

AsthmaAllergic Airway-diseased MiceInflammatory Lung DiseaseLung InflammationAcetic Acid Vapors +16

Network pharmacology of JAK inhibitors

Devapregasan Moodley, Hideyuki Yoshida, Sara Mostafavi, +8

Proceedings of the National Academy of Sciences

Lack of role for the vanilloid receptor in response to several inspired irritant air pollutants in the C57Bl/6J mouse

Peter T. Symanowicz, Gerald Gianutsos, John B. Morris

Neuroscience Letters

Molecular PharmacologyMolecular PhysiologyVanilloid ReceptorMedicinePhysiology +4