Current and future status of JAK inhibitors

DP McLornan, JE Pope, J Gotlib, CN Harrison - The lancet, 2021 - thelancet.com
An enhanced understanding of the importance of Janus kinase (JAK) and signal transducer
and activator of transcription (STAT) signalling in multiple disease states has led to an …

Mechanisms and consequences of Jak–STAT signaling in the immune system

AV Villarino, Y Kanno, JJ O'Shea - Nature immunology, 2017 - nature.com
Abstract Kinases of the Jak ('Janus kinase') family and transcription factors (TFs) of the STAT
('signal transducer and activator of transcription') family constitute a rapid membrane-to …

Structure of a Janus kinase cytokine receptor complex reveals the basis for dimeric activation

CR Glassman, N Tsutsumi, RA Saxton, PJ Lupardus… - Science, 2022 - science.org
Cytokines signal through cell surface receptor dimers to initiate activation of intracellular
Janus kinases (JAKs). We report the 3.6-angstrom–resolution cryo–electron microscopy …

Targeted protein degradation by PROTACs

TK Neklesa, JD Winkler, CM Crews - Pharmacology & therapeutics, 2017 - Elsevier
Targeted protein degradation using the PROTAC technology is emerging as a novel
therapeutic method to address diseases driven by the aberrant expression of a disease …

Adaptive chromatin remodeling drives glioblastoma stem cell plasticity and drug tolerance

BB Liau, C Sievers, LK Donohue, SM Gillespie… - Cell stem cell, 2017 - cell.com
Glioblastoma, the most common and aggressive malignant brain tumor, is propagated by
stem-like cancer cells refractory to existing therapies. Understanding the molecular …

[HTML][HTML] Dual targeting of oncogenic activation and inflammatory signaling increases therapeutic efficacy in myeloproliferative neoplasms

M Kleppe, R Koche, L Zou, P van Galen, CE Hill… - Cancer cell, 2018 - cell.com
Genetic and functional studies underscore the central role of JAK/STAT signaling in
myeloproliferative neoplasms (MPNs). However, the mechanisms that mediate …

JAK-STAT signaling in human disease: From genetic syndromes to clinical inhibition

Y Luo, M Alexander, M Gadina, JJ O'Shea… - Journal of Allergy and …, 2021 - Elsevier
Since its discovery, the Janus kinase-signal transduction and activation of transcription (JAK-
STAT) pathway has become recognized as a central mediator of widespread and varied …

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 …

AZD9150, a next-generation antisense oligonucleotide inhibitor of STAT3 with early evidence of clinical activity in lymphoma and lung cancer

D Hong, R Kurzrock, Y Kim, R Woessner… - Science translational …, 2015 - science.org
Next-generation sequencing technologies have greatly expanded our understanding of
cancer genetics. Antisense technology is an attractive platform with the potential to translate …

A dynamic N6-methyladenosine methylome regulates intrinsic and acquired resistance to tyrosine kinase inhibitors

F Yan, A Al-Kali, Z Zhang, J Liu, J Pang, N Zhao, C He… - Cell research, 2018 - nature.com
Abstract N 6-methyladenosine (m6A) on mRNAs is critical for various biological processes,
yet whether m6A regulates drug resistance remains unknown. Here we show that …