Chen Chen
China Pharmaceutical University
AdductGene silencingCancerCircular dichroismCytotoxic T cellEndoplasmic reticulumChemistryApoptosisIn vitroIn vivoSTAT3MetastasisCysteineTriple-negative breast cancerReactive oxygen speciesCancer researchBreast cancerStereochemistryCell cultureCell biology
25Publications
6H-index
138Citations
Publications 30
Newest
#1Chen Chen (CPU: China Pharmaceutical University)H-Index: 6
#2Li-Jie Gong (CPU: China Pharmaceutical University)
Last. Jian-Guang Luo (CPU: China Pharmaceutical University)H-Index: 28
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Abstract null null Peroxiredoxin 6 (PRDX6), as a bifunctional enzyme with glutathione peroxidase activity (GPx) and Ca2+-independent phospholipase A2 (iPLA2) activity, has a higher expression in various cancer cells, which leads to the increase of antioxidant properties and promotes tumorigenesis. However, only a few inhibitors of PRDX6 have been discovered to date, especially the covalent inhibitors of PRDX6. Here, we firstly identified Withangulatin A (WA), a natural small molecule, as a novel...
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#1Chen Chen (CPU: China Pharmaceutical University)H-Index: 6
#2Tianyu Zhu (CPU: China Pharmaceutical University)H-Index: 5
Last. Ling-Yi Kong (CPU: China Pharmaceutical University)H-Index: 58
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Abstract null null The first rate-limiting enzyme of the serine synthesis pathway (SSP), phosphoglycerate dehydrogenase (PHGDH), is hyperactive in multiple tumors, which leads to the activation of SSP and promotes tumorigenesis. However, only a few inhibitors of PHGDH have been discovered to date, especially the covalent inhibitors of PHGDH. Here, we identified withangulatin A (WA), a natural small molecule, as a novel covalent inhibitor of PHGDH. Affinity-based protein profiling identified that...
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#1Dong-Rong Zhu (CPU: China Pharmaceutical University)H-Index: 5
#2Chen Chen (CPU: China Pharmaceutical University)H-Index: 6
Last. Jian-Guang Luo (CPU: China Pharmaceutical University)H-Index: 28
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Abstract null null Introduction null Previously, we have reported a withanolide-type steroid, named tubocapsenolide A (TA), which shows potent anti-proliferative activity in several cancer cell lines. However, its inhibitory effect on the Janus kinase/signal transducer and activator of transcription 3 (JAK/STAT3) pathway and therapeutic potential on osteosarcoma have not been reported. null null null Objectives null In the present study, we aimed to investigate the effect and molecular mechanism...
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#1Chen Chen (CPU: China Pharmaceutical University)H-Index: 6
#2Xiao-Qin Liu (CPU: China Pharmaceutical University)H-Index: 2
Last. Jian-Guang Luo (CPU: China Pharmaceutical University)H-Index: 28
view all 7 authors...
Abstract null null Increasing evidence have reported that NLRP3 inflammasome has a crucial role in various kinds of immunological diseases including colitis. However, there have only a few drug candidates directly targeting inflammasomes for the therapy of colitis. Here, we first reported that Tubocapsanolide A (TA), a natural small molecule, as a novel inhibitor of NLRP3 inflammasome for the treatment of colitis. TA inhibited the activation of NLRP3 inflammasome and suppressed the secretion of ...
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#1Wen-Li Wang (CPU: China Pharmaceutical University)H-Index: 6
#2Xiao-Qin Liu (CPU: China Pharmaceutical University)H-Index: 2
Last. Ling-Yi Kong (CPU: China Pharmaceutical University)H-Index: 58
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Abstract Taxodinoid A (1), an unprecedented bis-diterpenic anhydride featuring a 6/6/7/6/6/6 heptacyclic core skeletons, and three novel pyrane-fused abietane-type diterpene dimers (2-4), were obtained from the seeds of Taxodium distichum. Their structures were elucidated by spectroscopic data, X-ray crystallograph and electronic circular dichroism calculation. A biosynthetic pathway and suppressing migration activity against U2 OS cells were also discussed.
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#1Xiu-Tao WuH-Index: 1
Last. Jian-Guang LuoH-Index: 28
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Harringtonolide (HO), a natural product isolated from Cephalotaxus harringtonia, exhibits potent antiproliferative activity. However, little information has been reported on the systematic structure−activity relationship (SAR) of HO derivatives. Modifications on tropone, lactone, and allyl positions of HO (1) were carried out to provide 17 derivatives (2–13, 11a–11f). The in vitro antiproliferative activity against four cancer cell lines (HCT-116, A375, A549, and Huh-7) and one normal cell line ...
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#1Dong-Rong Zhu (CPU: China Pharmaceutical University)H-Index: 5
#2Shang Li (CPU: China Pharmaceutical University)H-Index: 1
Last. Jian-Guang Luo (CPU: China Pharmaceutical University)H-Index: 28
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Abstract Heat shock protein 90 (HSP90) is a chaperone protein that has been shown to regulate cancer progression. As a result, HSP90 has emerged as an attractive target for cancer therapy. Tubocapsenolide A (TA) is an anti-tumor component isolated from Tubocapsicum anomalum. Although the anti-tumor activity of TA was considered to be related to HSP90, the binding site and deep anti-tumor mechanisms still need to be elucidated. In this study, we found that TA is a covalent inhibitor of HSP90, whi...
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#1Dan Yan (CPU: China Pharmaceutical University)H-Index: 1
#2Xiao Xu (CPU: China Pharmaceutical University)H-Index: 5
Last. Ling-Yi Kong (CPU: China Pharmaceutical University)H-Index: 58
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Abstract On-demand therapy following effective tumor detection would considerably reduce the side effects of traditional chemotherapy. DT-diaphorase (DTD), whose level is strongly elevated in various tumors, is a cytosolic flavoenzyme that promotes intracellular reactive oxygen species (ROS) generation via the redox cycling of hydroquinones. Incorporation of the DTD-responsive substrate to the structures of the probe and prodrug may facilitate the tumor detection and therapy. Herein, we establis...
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#1Wu-Xi Zhou (CPU: China Pharmaceutical University)H-Index: 1
#2Chen Chen (CPU: China Pharmaceutical University)H-Index: 6
Last. Jian-Guang Luo (CPU: China Pharmaceutical University)H-Index: 28
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Abstract Novel withangulatin A (WA) derivatives were synthesized and evaluated for antiproliferative activity against four human cancer cell lines (U2OS, MDA-MB-231, HepG2, and A549). Among these derivatives, 10 exhibited the most potent antiproliferative activity, with an IC50 value of 74.0 nM against the human breast cancer cell line MDA-MB-231 and potency that was 70-fold that of WA (IC50 = 5.22 µM). Moreover, 10 caused G2-phase cell cycle arrest in a concentration-dependent manner and induce...
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#1Wu-Xi Zhou (CPU: China Pharmaceutical University)H-Index: 1
#2Chen Chen (CPU: China Pharmaceutical University)H-Index: 6
Last. Jian-Guang Luo (CPU: China Pharmaceutical University)H-Index: 28
view all 8 authors...
Abstract To develop novel GLS1 inhibitors as effective therapeutic agents for triple-negative breast cancer (TNBC), 25 derivatives were synthesized from the natural inhibitor withangulatin A (IC50 = 18.2 μM). Bioassay optimization identified a novel and selective GLS1 inhibitor 7 (IC50 = 1.08 μM). In MDA-MB-231 cells, 7 diminished cellular glutamate levels by blocking glutaminolysis pathway, further triggering the generation of reactive oxygen species to induce caspase-dependent apoptosis. Molec...
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