Amine-Urea-Mediated Asymmetric Cycloadditions between Nitrile Oxides and o -Hydroxystyrenes by Dual Activation

2017 ◽  
Vol 129 (39) ◽  
pp. 12098-12101 ◽  
Author(s):  
Hiroyuki Suga ◽  
Yohei Hashimoto ◽  
Yasunori Toda ◽  
Kazuaki Fukushima ◽  
Hiroyoshi Esaki ◽  
...  
Keyword(s):  
Nitrile Oxides ◽  
Dual Activation ◽  
Asymmetric Cycloadditions

Amine-Urea-Mediated Asymmetric Cycloadditions between Nitrile Oxides and o -Hydroxystyrenes by Dual Activation

2017 ◽  
Vol 56 (39) ◽  
pp. 11936-11939 ◽  
Author(s):  
Hiroyuki Suga ◽  
Yohei Hashimoto ◽  
Yasunori Toda ◽  
Kazuaki Fukushima ◽  
Hiroyoshi Esaki ◽  
...  
Keyword(s):  
Nitrile Oxides ◽  
Dual Activation ◽  
Asymmetric Cycloadditions

Diacylfuroxans Are Masked Nitrile Oxides That Inhibit GPX4 Covalently

2019 ◽  
Author(s):  
John Eaton ◽  
Richard A. Ruberto ◽  
Anneke Kramm ◽  
Vasanthi S. Viswanathan ◽  
Stuart Schreiber
Keyword(s):  
Molecular Mechanism ◽  
Mechanism Of Action ◽  
Therapeutic Target ◽  
Biologically Active ◽  
Drug Resistant ◽  
Nitrile Oxides ◽  
Molecular Mechanism Of Action

<div><div><div><p>GPX4 represents a promising yet difficult-to-drug therapeutic target for the treatment of, among others, drug-resistant cancers. While most GPX4 inhibitors rely on a chloroacetamide moiety to modify covalently the protein’s catalytic selenocysteine residue, the discovery and mechanistic elucidation of structurally diverse GPX4-inhibiting molecules has uncovered novel electrophilic warheads that bind and inhibit GPX4. Here we report our discovery that diacylfuroxans can act as masked nitrile oxides that inhibit GPX4 covalently. These observations illuminate a novel molecular mechanism of action for biologically active furoxans and also suggest that nitrile oxides may be uniquely suited to targeting GPX4.</p></div></div></div>

Synergistic Immunostimulation through the Dual Activation of Toll-like Receptor 3/9 with Spherical Nucleic Acids

ACS Nano ◽  
2021 ◽  
Author(s):  
Ziyin N. Huang ◽  
Cassandra E. Callmann ◽  
Lisa E. Cole ◽  
Shuya Wang ◽  
Chad A. Mirkin
Keyword(s):  
Nucleic Acids ◽  
Toll Like Receptor ◽  
Dual Activation ◽  
Spherical Nucleic Acids
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