Da‐You Ma

Discovery of a novel napabucasin derivative B16 as a potent STAT3 inhibitor for the treatment of triple-negative breast cancer

Xu Deng, Yao Li, Ling Chen, Yuanzhu Xie et autres

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ASS1 inhibits liver cancer by promoting CAD ubiquitination and reversing the urea cycle and pyrimidine synthesis imbalance

Zhengnan Ming, Tiao Luo, Zizheng Zou, Wensong Luo et autres

BACKGROUND: The urea cycle and pyrimidine synthesis occur mainly in the liver and undergo opposite changes during hepatocarcinogenesis. Argininosuccinate synthase 1 (ASS1) and carbamoyl-phosphate synthetase 2, aspartate transcarbamylase, and dihydroorotase (CAD) are key enzymes in the urea cycle and pyrimidine synthesis, respectively, …

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Discovery of a Novel Silybin Derivative for the Treatment of Metabolic Dysfunction-Associated Steatohepatitis

Zhongtai Sui, Mo Li, Xueyi Wang, Cailin Luo et autres

MASH has become the leading cause of liver disease worldwide, and the prevalence of MASH is steadily increasing. The development of new drugs for the treatment of MASH is urgent. Silybin has been used for decades in liver protection, but its insufficient …

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LM2I leads to CAD ubiquitination and liver cancer suppression through activation of ASS1

Zhengnan Ming, Tiao Luo, Zizheng Zou, Wensong Luo et autres

The urea cycle occurs mainly in the liver and undergoes changes during hepatocarcinogenesis. Argininosuccinate synthase 1 (ASS1) is a key enzyme in the urea cycle and is expressed at low levels in certain cancers. LM2I, a specific activator of ASS1, exhibits significant …

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Spinosyn A derivatives as ASS1 activators and tumor inhibitors

Xinyu Huang, Xiaohe Liu, Na Xu, Ting Peng et autres

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Design, Synthesis, and Biological Activity of Novel Quinone Derivatives as Potent STAT3 Inhibitors for Psoriasis Treatment

Ling Chen, Liuliu Wang, Jinlei Gao, Yuanzhu Xie et autres

Psoriasis, which severely affects the sufferer’s life quality, is a chronic skin disease still lacking satisfactory medication. Recently, signal transducer and activator of transcription 3 (STAT3) was revealed playing an important role in the progression of psoriasis. In this paper, a total …

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Synthesis and biological evaluation of novel isoxazoloquinone derivatives as potent STAT3-targeting antipsoriasis agents

Ling Chen, Shuaiwen Zhu, Yuanzhu Xie, Liuliu Wang et autres

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Structure simplification of GNE-140 and discovery of a pyridone based analogue as a potential lead for hLDHA inhibitors

Wenhui Mo, Su-You Liu, Da‐You Ma

Abstract In this paper, taking GNE-140, a structurally complicated hLDHA inhibitor, as a lead compound, 19 simple analogues with a pyrimidone, pyranone or pyridone core were designed and conveniently synthesized. Subsequent biological evaluation indicated that although the pyrimidone core had a weak …

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Spinosyn A and Its Derivative Inhibit Colorectal Cancer Cell Growth via the EGFR Pathway

Kunjian Peng, Zizheng Zou, Jijia Li, Yuanzhu Xie et autres

Spinosyn A (SPA), derived from a soil microorganism, Saccharopolyspora spinosa, and its derivative, LM2I, has potential inhibitory effects on a variety of cancer cells. However, the effects of SPA and LM2I in inhibiting the growth of human colorectal cancer cells and the …

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An Isoxazoloquinone Derivative Inhibits Tumor Growth by Targeting STAT3 and Triggering Its Ubiquitin-Dependent Degradation

Yuanzhu Xie, Shuaiwen Zhu, Ling Chen, Hongdou Liu et autres

BACKGROUND: Triple-negative breast cancer (TNBC) is the most aggressive breast cancer subtype, with shorter five-year survival than other breast cancer subtypes, and lacks targeted and hormonal treatment strategies. The signal transducer and activator of transcription 3 (STAT3) signaling is up-regulated in various …

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Naturally-occurring spinosyn A and its derivatives function as argininosuccinate synthase activator and tumor inhibitor

Zizheng Zou, Xiyuan Hu, Tiao Luo, Zhengnan Ming et autres

Argininosuccinate synthase (ASS1) is a ubiquitous enzyme in mammals that catalyzes the formation of argininosuccinate from citrulline and aspartate. ASS1 genetic deficiency in patients leads to an autosomal recessive urea cycle disorder citrullinemia, while its somatic silence or down-regulation is very common …

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Synthesis and biological evaluation of novel isothiazoloquinoline quinone analogues

Ling Chen, Yuanzhu Xie, Lijun Liu, Zizheng Zou et autres

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