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sun, h.

Publications and source records attributed to sun, h..

2 recordsLinked to original sources

AHR agonist ITE boosted PD1 antibodys effects by inhibiting myeloid-derived cells suppressive cells in an orthotopic mouse glioma model

Glioblastoma is a "cold" tumor lacking T cell infiltration and tryptophan metabolites such as kynurenine function as an immune suppressor by binding to aryl hydrocarbon receptor(AHR). Hence AHR antagonists have been developed and some shown to activate the immune response in IDO over-expressing cancer models. Paradoxically, AHR has been reported to block glioma cell invasion like a tumor suppressor, and how to target AHR in cancer remains an open question. We previously discovered that an AHR agonist ITE can effectively inhibit glioma invasion. Here we report that ITE combined with PD1 antibody significantly increased the infiltration of CD8+ T cells while reducing that of the myeloid-derived suppressive cells (MDSCs), extending mouse survival. To identify factors that possibly mediated ITEs effects, we analyzed RNA-seq data and discovered that ITE significantly down-regulated IL11, a known MDSC regulator. In contrast, kynurenine upregulated IL11, further supporting IL11 as an AHR target. Moreover, ITE inhibited IL11s induction of MDSC from mouse PBMC in vitro, supporting that IL11 might mediate ITEs MDSC regulation effects. The discovery of ITEs immune-activating effects highlighted the complexity of AHRs signaling in cancers. The unexpected increase in STAT3, downstream of IL11 provided clues for combination therapy development.

cancer biology↗

Celastrol directly inhibits PFKM to induce weight loss and leptin sensitization

Despite the prevalence of obesity and related health consequences around the globe, effective treatments for inducing healthy weight loss are still lacking. Celastrol is a pentacyclic triterpene that was recently identified as a potent anti-obesity agent. Celastrol increases sensitivity to leptin, but the molecular target of celastrol is unknown. Therefore, the mechanisms by which this agent exerts its anti-obesity effect remain elusive. Using tissue-specific ABPP (activity-based protein profiling), we found that PFKM, a rate-limiting enzyme for glycolysis in skeletal muscle, is a direct target of celastrol. Celastrol inhibited PFKM enzymatic activity, and Pfkm knockout mice were resistant to a high fat diet, were hypersensitive to exogenous leptin, and were unresponsive to celastrol. PFKM inhibition led to activation of AMPK and inactivation of ACC in cultured myotubes and mouse skeletal muscle. Specific loss of AMPK in muscle significantly attenuated the anti-obesity effects of celastrol. Further, PFKM inhibition and subsequent activation of the AMPK/ACC signaling pathway reduced levels of free fatty acids by switching energy expenditure and consequently decreasing levels of SOCS1 expression, which are both required for leptin sensitization in 293t/hLepRb cells and mice. Finally, using a high throughput compound screen we identified an alternative PFKM inhibitor, 3-79, which exhibits a strong anti-obesity effect and non-covalent binding capacity. This compound is a promising agent for treating obesity in the clinic.

physiology↗