[HTML][HTML] A comprehensive overview of globally approved JAK inhibitors

AM Shawky, FA Almalki, AN Abdalla, AH Abdelazeem… - Pharmaceutics, 2022 - mdpi.com
Janus kinase (JAK) is a family of cytoplasmic non-receptor tyrosine kinases that includes
four members, namely JAK1, JAK2, JAK3, and TYK2. The JAKs transduce cytokine signaling …

The molecular details of cytokine signaling via the JAK/STAT pathway

R Morris, NJ Kershaw, JJ Babon - Protein Science, 2018 - Wiley Online Library
More than 50 cytokines signal via the JAK/STAT pathway to orchestrate hematopoiesis,
induce inflammation and control the immune response. Cytokines are secreted …

In vitro and in vivo characterization of the JAK1 selectivity of upadacitinib (ABT-494)

JM Parmentier, J Voss, C Graff, A Schwartz… - BMC rheumatology, 2018 - Springer
Background Anti-cytokine therapies such as adalimumab, tocilizumab, and the small
molecule JAK inhibitor tofacitinib have proven that cytokines and their subsequent …

The growth hormone receptor: mechanism of receptor activation, cell signaling, and physiological aspects

F Dehkhoda, CMM Lee, J Medina… - Frontiers in …, 2018 - frontiersin.org
The growth hormone receptor (GHR), although most well known for regulating growth, has
many other important biological functions including regulating metabolism and controlling …

The molecular regulation of Janus kinase (JAK) activation

JJ Babon, IS Lucet, JM Murphy, NA Nicola… - Biochemical …, 2014 - portlandpress.com
The JAK (Janus kinase) family members serve essential roles as the intracellular signalling
effectors of cytokine receptors. This family, comprising JAK1, JAK2, JAK3 and TYK2 (tyrosine …

Biology and significance of the JAK/STAT signalling pathways

H Kiu, SE Nicholson - Growth factors, 2012 - Taylor & Francis
Since its discovery two decades ago, the activation of the Janus kinase/signal transducers
and activators of transcription (JAK/STAT) pathway by numerous cytokines and growth …

Halogen atoms in the modern medicinal chemistry: hints for the drug design

MZ Hernandes, SMT Cavalcanti… - Current drug …, 2010 - ingentaconnect.com
A significant number of drugs and drug candidates in clinical development are halogenated
structures. For a long time, insertion of halogen atoms on hit or lead compounds was …

JAK2 Exon 12 Mutations in Polycythemia Vera and Idiopathic Erythrocytosis

LM Scott, W Tong, RL Levine, MA Scott… - … England Journal of …, 2007 - Mass Medical Soc
Background The V617F mutation, which causes the substitution of phenylalanine for valine
at position 617 of the Janus kinase (JAK) 2 gene (JAK2), is often present in patients with …

Mechanism of activation of protein kinase JAK2 by the growth hormone receptor

AJ Brooks, W Dai, ML O'Mara, D Abankwa, Y Chhabra… - Science, 2014 - science.org
Introduction Class I cytokines regulate key processes such as growth, lactation,
hematopoiesis, and immune function and contribute to oncogenesis. Although the …

JAK inhibitors and COVID-19

G Levy, P Guglielmelli, P Langmuir… - Journal for …, 2022 - pmc.ncbi.nlm.nih.gov
During SARS-CoV-2 infection, the innate immune response can be inhibited or delayed, and
the subsequent persistent viral replication can induce emergency signals that may culminate …