Publications by authors named "Ig Jun Cho"
Target class profiling (TCP) is a chemical biology approach to investigate understudied biological target classes. TCP is achieved by developing a generalizable assay platform and screening curated compound libraries to interrogate the chemical biological space of members of an enzyme family. In this work, we took a TCP approach to investigate inhibitory activity across a set of small-molecule methyltransferases (SMMTases), a subclass of methyltransferase enzymes, with the goal of creating a launchpad to explore this largely understudied target class.
View Article and Find Full Text PDFInhibitor of apoptosis proteins (IAPs) are overexpressed in the majority of cancers and prevent apoptosis by inhibiting caspases. IAPs have therefore attracted considerable attention as potential targets for anticancer therapy. Here, we demonstrated that HM90822 (abbreviated HM822; a new synthetic IAP antagonist) induced apoptotic cell death via proteasome-dependent degradation of BIR2/3 domain-containing IAPs in human pancreatic cancer cells.
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- The study examined how different forms (enantiomers) of zaltoprofen, particularly S(+)-zaltoprofen, affect inflammation and pain compared to the whole racemic zaltoprofen.
- S(+)-zaltoprofen was found to be effective in reducing inflammation in a specific paw edema model, while R(-)-zaltoprofen showed no effect, indicating that S(+)-zaltoprofen is the main anti-inflammatory agent.
- Although none of the forms provided significant pain relief at lower doses in a writhing model, they did show analgesic effects at higher doses, suggesting a complex relationship between the zaltoprofen forms and their pain-relieving properties.
Widdrol, a natural sesquiterpene present in Juniperus sp., has been shown to exert anticancer and antifungal effects. Emerging evidence has suggested that AMP-activated protein kinase (AMPK), which functions as a cellular energy sensor, is a potential therapeutic target for human cancers.
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- TNF-alpha is a key inflammatory cytokine linked to chronic diseases like rheumatoid arthritis and inflammatory bowel disease, making it a target for new treatments.* -
- The study introduces DBM1285, a novel compound that effectively reduces TNF-alpha production in various immune cells but does not affect its mRNA levels, indicating a post-transcriptional regulation mechanism.* -
- DBM1285 works by inhibiting the p38 MAPK enzyme, leading to decreased inflammation in mouse models, suggesting its potential as a therapeutic option for diseases related to excessive TNF-alpha.*
(R)-4-(3,4-Dihydro-8,8-dimethyl)-2H,8H-benzo[1,2-b:3,4-b']dipyran-3yl)-1,3-benzenediol (glabridin), a flavonoid present in licorice extract, is known to have antimicrobial, anti-inflammatory, and cardiovascular protective activities. In the present study, we report the inhibitory effect of glabridin on nitric oxide (NO) production and inducible nitric oxide (iNOS) gene expression in murine macrophages. Glabridin attenuated lipopolysaccharide (LPS)-induced NO production in isolated mouse peritoneal macrophages and RAW 264.
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