Highly selective inhibition of tyrosine kinase 2 (TYK2) for the treatment of autoimmune diseases: discovery of the allosteric inhibitor BMS-986165
ST Wrobleski, R Moslin, S Lin, Y Zhang… - Journal of Medicinal …, 2019 - ACS Publications
Small molecule JAK inhibitors have emerged as a major therapeutic advancement in
treating autoimmune diseases. The discovery of isoform selective JAK inhibitors that …
treating autoimmune diseases. The discovery of isoform selective JAK inhibitors that …
Discovery of tyrosine kinase 2 (TYK2) inhibitor (PF-06826647) for the treatment of autoimmune diseases
BS Gerstenberger, C Ambler, EP Arnold… - Journal of Medicinal …, 2020 - ACS Publications
Tyrosine kinase 2 (TYK2) is a member of the JAK kinase family that regulates signal
transduction downstream of receptors for the IL-23/IL-12 pathways and type I interferon …
transduction downstream of receptors for the IL-23/IL-12 pathways and type I interferon …
Selective inhibitors of JAK1 targeting an isoform-restricted allosteric cysteine
ME Kavanagh, BD Horning, R Khattri, N Roy… - Nature chemical …, 2022 - nature.com
The Janus tyrosine kinase (JAK) family of non-receptor tyrosine kinases includes four
isoforms (JAK1, JAK2, JAK3, and TYK2) and is responsible for signal transduction …
isoforms (JAK1, JAK2, JAK3, and TYK2) and is responsible for signal transduction …
Identification of N-Methyl Nicotinamide and N-Methyl Pyridazine-3-Carboxamide Pseudokinase Domain Ligands as Highly Selective Allosteric Inhibitors of Tyrosine …
R Moslin, Y Zhang, ST Wrobleski, S Lin… - Journal of Medicinal …, 2019 - ACS Publications
As a member of the Janus (JAK) family of nonreceptor tyrosine kinases, TYK2 plays an
important role in mediating the signaling of pro-inflammatory cytokines including IL-12, IL …
important role in mediating the signaling of pro-inflammatory cytokines including IL-12, IL …
Allosteric TYK2 inhibition: Redefining autoimmune disease therapy beyond JAK1-3 inhibitors
LT Jensen, KE Attfield, M Feldmann, L Fugger - EBioMedicine, 2023 - thelancet.com
JAK inhibitors impact multiple cytokine pathways simultaneously, enabling high efficacy in
treating complex diseases such as cancers and immune-mediated disorders. However, their …
treating complex diseases such as cancers and immune-mediated disorders. However, their …
Advances in the discovery of selective JAK inhibitors
CJ Menet, L Van Rompaey, R Geney - Progress in medicinal chemistry, 2013 - Elsevier
In this review, we describe the current knowledge of the biology of the JAKs. The JAK family
comprises the four nonreceptor tyrosine kinases JAK1, JAK2, JAK3, and Tyk2, all key …
comprises the four nonreceptor tyrosine kinases JAK1, JAK2, JAK3, and Tyk2, all key …
Discovery of a potent and selective tyrosine kinase 2 inhibitor: TAK-279
S Leit, J Greenwood, S Carriero, S Mondal… - Journal of Medicinal …, 2023 - ACS Publications
TYK2 is a key mediator of IL12, IL23, and type I interferon signaling, and these cytokines
have been implicated in the pathogenesis of multiple inflammatory and autoimmune …
have been implicated in the pathogenesis of multiple inflammatory and autoimmune …
Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of ((S)-2,2-Difluorocyclopropyl)((1R,5S)-3-(2-((1-methyl-1H-pyrazol-4-yl) …
A Fensome, CM Ambler, E Arnold… - Journal of medicinal …, 2018 - ACS Publications
Cytokine signaling is an important characteristic of autoimmune diseases. Many pro-
inflammatory cytokines signal through the Janus kinase (JAK)/Signal transducer and …
inflammatory cytokines signal through the Janus kinase (JAK)/Signal transducer and …
Tricyclic covalent inhibitors selectively target Jak3 through an active site thiol
ER Goedken, MA Argiriadi, DL Banach… - Journal of Biological …, 2015 - ASBMB
The action of Janus kinases (JAKs) is required for multiple cytokine signaling pathways, and
as such, JAK inhibitors hold promise for treatment of autoimmune disorders, including …
as such, JAK inhibitors hold promise for treatment of autoimmune disorders, including …
Discovery of CP-690,550: a potent and selective Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases and organ transplant rejection
ME Flanagan, TA Blumenkopf… - Journal of medicinal …, 2010 - ACS Publications
There is a critical need for safer and more convenient treatments for organ transplant
rejection and autoimmune disorders such as rheumatoid arthritis. Janus tyrosine kinases …
rejection and autoimmune disorders such as rheumatoid arthritis. Janus tyrosine kinases …
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