JAK inhibition as a therapeutic strategy for immune and inflammatory diseases

DM Schwartz, Y Kanno, A Villarino, M Ward… - Nature reviews Drug …, 2017 - nature.com
The discovery of cytokines as key drivers of immune-mediated diseases has spurred efforts
to target their associated signalling pathways. Janus kinases (JAKs) are essential signalling …

Discovery and development of Janus Kinase (JAK) inhibitors for inflammatory diseases: Miniperspective

JD Clark, ME Flanagan, JB Telliez - Journal of medicinal chemistry, 2014 - ACS Publications
The Janus kinases (JAKs) are a family of intracellular tyrosine kinases that play an essential
role in the signaling of numerous cytokines that have been implicated in the pathogenesis of …

[HTML][HTML] Inhibition of interleukin-1 receptor-associated kinase 1 (IRAK1) as a therapeutic strategy

JW Singer, A Fleischman, S Al-Fayoumi… - Oncotarget, 2018 - ncbi.nlm.nih.gov
Abstract Interleukin-1 receptor-associated kinases (IRAK1, IRAK2, IRAK3 [IRAK-M], and
IRAK4) are serine-threonine kinases involved in toll-like receptor and interleukin-1 signaling …

Selective JAK inhibitors in development for rheumatoid arthritis

P Norman - Expert opinion on investigational drugs, 2014 - Taylor & Francis
Introduction: The JAK kinases are a family of four tyrosine receptor kinases that play a
pivotal role in cytokine receptor signalling pathways via their interaction with signal …

Small-molecule kinase inhibitors for the treatment of nononcologic diseases

Z Xie, X Yang, Y Duan, J Han… - Journal of medicinal …, 2021 - ACS Publications
Great successes have been achieved in developing small-molecule kinase inhibitors as
anticancer therapeutic agents. However, kinase deregulation plays essential roles not only …

Synthetic opportunities and challenges for macrocyclic kinase inhibitors

JA Amrhein, S Knapp, T Hanke - Journal of Medicinal Chemistry, 2021 - ACS Publications
Macrocycles are typically cyclic variants of inhibitors derived from uncyclized canonical
molecules or from natural products. For medicinal chemistry, drug-like macrocycles have …

Dual-target Janus kinase (JAK) inhibitors: Comprehensive review on the JAK-based strategies for treating solid or hematological malignancies and immune-related …

P Shen, Y Wang, X Jia, P Xu, L Qin, X Feng, Z Li… - European journal of …, 2022 - Elsevier
Janus kinases (JAKs) are the non-receptor tyrosine kinases covering JAK1, JAK2, JAK3,
and TYK2 which regulate signal transductions of hematopoietic cytokines and growth factors …

A comprehensive review of new small molecule drugs approved by the FDA in 2022: Advance and prospect

YR Bai, X Yang, KT Chen, XD Cuan, YD Zhang… - European Journal of …, 2024 - Elsevier
In 2022, the US Food and Drug Administration approved a total of 16 marketing applications
for small molecule drugs, which not only provided dominant scaffolds but also introduced …

Recent advances of colony-stimulating factor-1 receptor (CSF-1R) kinase and its inhibitors

MI El-Gamal, SK Al-Ameen, DM Al-Koumi… - Journal of medicinal …, 2018 - ACS Publications
Colony stimulation factor-1 receptor (CSF-1R), which is also known as FMS kinase, plays an
important role in initiating inflammatory, cancer, and bone disorders when it is …

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 …