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

JW Singer, A Fleischman, S Al-Fayoumi… - …, 2018‏ - pmc.ncbi.nlm.nih.gov
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 pathways …

The recent advance of Interleukin-1 receptor associated kinase 4 inhibitors for the treatment of inflammation and related diseases

YR Bai, WG Yang, XH Hou, DD Shen, SN Zhang… - European Journal of …, 2023‏ - Elsevier
The interleukin-1 receptor associated kinase 4 (IRAK-4) is a member of serine-threonine
kinase family, which plays an important role in the regulation of interleukin-1 receptors (IL …

IRAK signalling in cancer

GW Rhyasen, DT Starczynowski - British journal of cancer, 2015‏ - nature.com
Innate immune signalling has an essential role in inflammation, and the dysregulation of
signalling components of this pathway is increasingly being recognised as an important …

IRAK-4 inhibitors for inflammation

Z Wang, H Wesche, T Stevens… - Current topics in …, 2009‏ - benthamdirect.com
Interleukin-1 receptor-associated kinases (IRAKs) are key components in the signal
transduction pathways utilized by interleukin-1 receptor (IL-1R), interleukin-18 receptor (IL …

Recent advances in the discovery of small molecule inhibitors of interleukin-1 receptor-associated kinase 4 (IRAK4) as a therapeutic target for inflammation and …

D Chaudhary, S Robinson… - Journal of medicinal …, 2015‏ - ACS Publications
IRAK4, a serine/threonine kinase, plays a key role in both inflammation and oncology
diseases. Herein, we summarize the compelling biology surrounding the IRAK4 signaling …

Discovery of CA-4948, an orally bioavailable IRAK4 inhibitor for treatment of hematologic malignancies

VR Gummadi, A Boruah, BR Ainan… - ACS Medicinal …, 2020‏ - ACS Publications
Small molecule potent IRAK4 inhibitors from a novel bicyclic heterocycle class were
designed and synthesized based on hits identified from Aurigene's compound library. The …

Endogenous ligands of TLR4 promote unresolving tissue fibrosis: Implications for systemic sclerosis and its targeted therapy

S Bhattacharyya, J Varga - Immunology letters, 2018‏ - Elsevier
Fibrosis, the hallmark of scleroderma or systemic sclerosis (SSc), is a complex, dynamic and
generally irreversible pathophysiological process that leads to tissue disruption, and lacks …

Recent advances in IRAK1: pharmacological and therapeutic aspects

KM Kim, NH Hwang, JS Hyun, D Shin - Molecules, 2024‏ - mdpi.com
Interleukin receptor-associated kinase (IRAK) proteins are pivotal in interleukin-1 and Toll-
like receptor-mediated signaling pathways. They play essential roles in innate immunity and …

Crystal structure of human IRAK1

L Wang, Q Qiao, R Ferrao, C Shen, JM Hatcher… - Proceedings of the …, 2017‏ - pnas.org
Interleukin 1 (IL-1) receptor-associated kinases (IRAKs) are serine/threonine kinases that
play critical roles in initiating innate immune responses against foreign pathogens and other …

Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88L265P Diffuse …

JS Scott, SL Degorce, R Anjum, J Culshaw… - Journal of medicinal …, 2017‏ - ACS Publications
Herein we report the optimization of a series of pyrrolopyrimidine inhibitors of interleukin-1
receptor associated kinase 4 (IRAK4) using X-ray crystal structures and structure based …