keyword
MENU ▼
Read by QxMD icon Read
search

IQ-1S

keyword
https://www.readbyqxmd.com/read/26923672/a-novel-dual-no-donating-oxime-and-c-jun-n-terminal-kinase-inhibitor-protects-against-cerebral-ischemia-reperfusion-injury-in-mice
#1
Dmitriy N Atochin, Igor A Schepetkin, Andrei I Khlebnikov, Victor I Seledtsov, Helen Swanson, Mark T Quinn, Paul L Huang
The c-Jun N-terminal kinase (JNK) has been shown to be an important regulator of neuronal cell death. Previously, we synthesized the sodium salt of 11H-indeno[1,2-b]quinoxalin-11-one (IQ-1S) and demonstrated that it was a high-affinity inhibitor of the JNK family. In the present work, we found that IQ-1S could release nitric oxide (NO) during its enzymatic metabolism by liver microsomes. Moreover, serum nitrite/nitrate concentration in mice increased after intraperitoneal injection of IQ-1S. Because of these dual actions as JNK inhibitor and NO-donor, the therapeutic potential of IQ-1S was evaluated in an animal stroke model...
April 8, 2016: Neuroscience Letters
https://www.readbyqxmd.com/read/25784649/anti-inflammatory-effects-and-joint-protection-in-collagen-induced-arthritis-after-treatment-with-iq-1s-a-selective-c-jun-n-terminal-kinase-inhibitor
#2
Igor A Schepetkin, Liliya N Kirpotina, Deepa Hammaker, Irina Kochetkova, Andrei I Khlebnikov, Sergey A Lyakhov, Gary S Firestein, Mark T Quinn
c-Jun N-terminal kinases (JNKs) participate in many physiologic and pathologic processes, including inflammatory diseases. We recently synthesized the sodium salt of IQ-1S (11H-indeno[1,2-b]quinoxalin-11-one oxime) and demonstrated that it is a high-affinity JNK inhibitor and inhibits murine delayed-type hypersensitivity. Here we show that IQ-1S is highly specific for JNK and that its neutral form is the most abundant species at physiologic pH. Molecular docking of the IQ-1S syn isomer into the JNK1 binding site gave the best pose, which corresponded to the position of cocrystallized JNK inhibitor SP600125 (1,9-pyrazoloanthrone)...
June 2015: Journal of Pharmacology and Experimental Therapeutics
1
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"