[PDF][PDF] Developing irreversible inhibitors of the protein kinase cysteinome

Q Liu, Y Sabnis, Z Zhao, T Zhang, SJ Buhrlage… - Chemistry & biology, 2013 - cell.com
Protein kinases are a large family of approximately 530 highly conserved enzymes that
transfer a γ-phosphate group from ATP to a variety of amino acid residues, such as tyrosine …

Inhibiting NF-κB activation by small molecules as a therapeutic strategy

SC Gupta, C Sundaram, S Reuter… - Biochimica et Biophysica …, 2010 - Elsevier
Because nuclear factor-κB (NF-κB) is a ubiquitously expressed proinflammatory transcription
factor that regulates the expression of over 500 genes involved in cellular transformation …

A small-molecule inhibitor of the NLRP3 inflammasome for the treatment of inflammatory diseases

RC Coll, AAB Robertson, JJ Chae, SC Higgins… - Nature medicine, 2015 - nature.com
The NOD-like receptor (NLR) family, pyrin domain–containing protein 3 (NLRP3)
inflammasome is a component of the inflammatory process, and its aberrant activation is …

Covalent modifiers: a chemical perspective on the reactivity of α, β-unsaturated carbonyls with thiols via hetero-Michael addition reactions

PA Jackson, JC Widen, DA Harki… - Journal of medicinal …, 2017 - ACS Publications
Although Michael acceptors display a potent and broad spectrum of bioactivity, they have
largely been ignored in drug discovery because of their presumed indiscriminate reactivity …

[HTML][HTML] Parthenolide promotes the repair of spinal cord injury by modulating M1/M2 polarization via the NF-κB and STAT 1/3 signaling pathway

T Gaojian, Q Dingfei, L Linwei, W Xiaowei… - Cell death …, 2020 - nature.com
Spinal cord injury (SCI) is a severe neurological disease; however, there is no effective
treatment for spinal cord injury. Neuroinflammation involves the activation of resident …

What made sesquiterpene lactones reach cancer clinical trials?

A Ghantous, H Gali-Muhtasib, H Vuorela, NA Saliba… - Drug discovery today, 2010 - Elsevier
Sesquiterpene lactones (SLs) are plant-derived compounds often used in traditional
medicine against inflammation and cancer. This review focuses on the chemical and …

[HTML][HTML] Activation of Nrf2 signaling by natural products-can it alleviate diabetes?

M Matzinger, K Fischhuber, EH Heiss - Biotechnology advances, 2018 - Elsevier
Type 2 diabetes mellitus (DM) has reached pandemic proportions and effective prevention
strategies are wanted. Its onset is accompanied by cellular distress, the nuclear factor …

[HTML][HTML] Anti-inflammatory compounds parthenolide and Bay 11-7082 are direct inhibitors of the inflammasome

C Juliana, T Fernandes-Alnemri, J Wu, P Datta… - Journal of Biological …, 2010 - ASBMB
Activation of the inflammasome generates the pro-inflammatory cytokines interleukin-1β and-
18, which are important mediators of inflammation. Abnormal activation of the inflammasome …

Advances in chemistry and bioactivity of parthenolide

RRA Freund, P Gobrecht, D Fischer… - Natural product reports, 2020 - pubs.rsc.org
Review covering up to 07/2019 (−)-Parthenolide is a germacrane sesquiterpene lactone,
available in ample amounts from the traditional medical plant feverfew (Tanacetum …

Recent developments in anti‐inflammatory natural products

R Gautam, SM Jachak - Medicinal research reviews, 2009 - Wiley Online Library
Many of the inflammatory diseases are becoming common in aging society throughout the
world. The clinically used anti‐inflammatory drugs suffer from the disadvantage of side …