Calming the cytokine storm of COVID-19 through inhibition of JAK2/STAT3 signaling
BK Gajjela, MM Zhou - Drug discovery today, 2022 - Elsevier
The outbreak of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has
caused the unprecedented COVID-19 pandemic, which has infected over 178 million people …
caused the unprecedented COVID-19 pandemic, which has infected over 178 million people …
Points to consider for the treatment of immune-mediated inflammatory diseases with Janus kinase inhibitors: a consensus statement
Objectives Janus kinase inhibitors (JAKi) have been approved for use in various immune-
mediated inflammatory diseases. With five agents licensed, it was timely to summarise the …
mediated inflammatory diseases. With five agents licensed, it was timely to summarise the …
Janus kinases (JAKs): The efficient therapeutic targets for autoimmune diseases and myeloproliferative disorders
P Xu, P Shen, B Yu, X Xu, R Ge, X Cheng… - European Journal of …, 2020 - Elsevier
Abstract The Janus kinases or 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 …
essential role in the signaling of numerous cytokines that have been implicated in the …
KLIFS: a knowledge-based structural database to navigate kinase–ligand interaction space
OPJ Van Linden, AJ Kooistra, R Leurs… - Journal of medicinal …, 2014 - ACS Publications
Protein kinases regulate the majority of signal transduction pathways in cells and have
become important targets for the development of designer drugs. We present a systematic …
become important targets for the development of designer drugs. We present a systematic …
Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634
CJ Menet, SR Fletcher, G Van Lommen… - Journal of Medicinal …, 2014 - ACS Publications
Janus kinases (JAK1, JAK2, JAK3, and TYK2) are involved in the signaling of multiple
cytokines important in cellular function. Blockade of the JAK-STAT pathway with a small …
cytokines important in cellular function. Blockade of the JAK-STAT pathway with a small …
JAK/STAT signal transduction: promising attractive targets for immune, inflammatory and hematopoietic diseases
Q Gao, X Liang, AS Shaikh, J Zang, W Xu… - Current Drug …, 2018 - ingentaconnect.com
Background: JAK/STAT signal pathway, a requisite part in the signaling process of growth
factors and cytokines, has become attractive targets for numerous immune, inflammatory …
factors and cytokines, has become attractive targets for numerous immune, inflammatory …
Identification of potent and selective JAK1 lead compounds through ligand-based drug design approaches
S Babu, SK Nagarajan, S Sathish, VS Negi… - Frontiers in …, 2022 - frontiersin.org
JAK1 plays a significant role in the intracellular signaling by interacting with cytokine
receptors in different types of cells and is linked to the pathogenesis of various cancers and …
receptors in different types of cells and is linked to the pathogenesis of various cancers and …
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 …
Identification of C-2 Hydroxyethyl Imidazopyrrolopyridines as Potent JAK1 Inhibitors with Favorable Physicochemical Properties and High Selectivity over JAK2
M Zak, CA Hurley, SI Ward, P Bergeron… - Journal of medicinal …, 2013 - ACS Publications
Herein we report on the structure-based discovery of a C-2 hydroxyethyl moiety which
provided consistently high levels of selectivity for JAK1 over JAK2 to the …
provided consistently high levels of selectivity for JAK1 over JAK2 to the …
Discovery and Optimization of C-2 Methyl Imidazopyrrolopyridines as Potent and Orally Bioavailable JAK1 Inhibitors with Selectivity over JAK2
M Zak, R Mendonca, M Balazs, K Barrett… - Journal of Medicinal …, 2012 - ACS Publications
Herein we report the discovery of the C-2 methyl substituted imidazopyrrolopyridine series
and its optimization to provide potent and orally bioavailable JAK1 inhibitors with selectivity …
and its optimization to provide potent and orally bioavailable JAK1 inhibitors with selectivity …