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Akademický článek

Remodeling tumor‐associated macrophage for anti‐cancer effects by rational design of irreversible inhibition of mitogen‐activated protein kinase‐activated protein kinase 2

Autor: Danyi Wang, Deqiao Sun, Xiaoyan Wang, Xia Peng, Yinchun Ji, Lu Tang, Qichang He, Danqi Chen, Ye Yang, Xuan Zhou, Bing Xiong, Jing Ai

Publikováno v: MedComm, Vol 5, Iss 7, Pp n/a-n/a (2024)

Abstract Mitogen‐activated protein kinase‐activated protein kinase 2 (MK2) emerges as a pivotal target in developing anti‐cancer therapies. The limitations of ATP‐competitive inhibitors, due to insufficient potency and selectivity, underscore

Externí odkaz: https://doaj.org/article/625b4ce35fc9407796898ac8892c510c

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Akademický článek

Structure-based drug discovery of novel fused-pyrazolone carboxamide derivatives as potent and selective AXL inhibitors

Autor: Feifei Fang, Yang Dai, Hao Wang, Yinchun Ji, Xuewu Liang, Xia Peng, Jiyuan Li, Yangrong Zhao, Chunpu Li, Danyi Wang, Yazhou Li, Dong Zhang, Dan Zhang, Meiyu Geng, Hong Liu, Jing Ai, Yu Zhou

Publikováno v: Acta Pharmaceutica Sinica B, Vol 13, Iss 12, Pp 4918-4933 (2023)

As a novel and promising antitumor target, AXL plays an important role in tumor growth, metastasis, immunosuppression and drug resistance of various malignancies, which has attracted extensive research interest in recent years. In this study, by empl

Externí odkaz: https://doaj.org/article/d516c2f765514631b7bf774badc1f3ce

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Akademický článek

Design, synthesis and biological evaluation of 4-aminoquinoline derivatives as receptor-interacting protein kinase 2 (RIPK2) inhibitors

Autor: Tiantian Fan, Yinchun Ji, Danqi Chen, Xia Peng, Jing Ai, Bing Xiong

Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 38, Iss 1, Pp 282-293 (2023)

Receptor-interacting protein kinase 2 (RIPK2) is an essential protein kinase mediating signal transduction by NOD1 and NOD2, which play an important role in regulating immune signalling. In this study, we designed and synthesised a novel series of 4-

Externí odkaz: https://doaj.org/article/42fea3ef7a9a45f7b493f714afa4c861

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Akademický článek

Discovery of 4-cyclopropyl-3-(2-((1-cyclopropyl-1H-pyrazol-4-yl) amino) quinazolin-6-yl)-N-(3-(trifluoromethyl) phenyl) benzamides as potent discoidin domain receptor inhibitors for the treatment of idiopathic pulmonary fibrosis

Autor: Qi Wang, Bixi Tang, Dandan Sun, Ying Dong, Yinchun Ji, Huanyu Shi, Liwei Zhou, Yueyue Yang, Menglan Luo, Qian Tan, Lin Chen, Yue Dong, Cong Li, Rongrong Xie, Yi Zang, Jingkang Shen, Bing Xiong, Jia Li, Danqi Chen

Publikováno v: Acta Pharmaceutica Sinica B, Vol 12, Iss 4, Pp 1943-1962 (2022)

Idiopathic pulmonary fibrosis (IPF) is a chronic fatal lung disease with a median survival time of 3–5 years. Inaccurate diagnosis, limited clinical therapy and high mortality together indicate that the development of effective therapeutics for IPF

Externí odkaz: https://doaj.org/article/9ad1dde89ea3450e890d43fa5a6ba6c3

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Akademický článek

Preclinical evaluation of 3D185, a novel potent inhibitor of FGFR1/2/3 and CSF-1R, in FGFR-dependent and macrophage-dominant cancer models

Autor: Xia Peng, Pengcong Hou, Yi Chen, Yang Dai, Yinchun Ji, Yanyan Shen, Yi Su, Bo Liu, Yueliang Wang, Deqiao Sun, Yuchen Jiang, Chuantao Zha, Zuoquan Xie, Jian Ding, Meiyu Geng, Jing Ai

Publikováno v: Journal of Experimental & Clinical Cancer Research, Vol 38, Iss 1, Pp 1-16 (2019)

Abstract Background The interaction between tumor cells and their immunosuppressive microenvironment promotes tumor progression and drug resistance. Thus, simultaneously targeting tumor cells and stromal cells is expected to have synergistic antitumo

Externí odkaz: https://doaj.org/article/4d6fda581db942d897ce0702a1011ea4

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Data from The Novel RET Inhibitor SYHA1815 Inhibits RET-Driven Cancers and Overcomes Gatekeeper Mutations by Inducing G1 Cell-Cycle Arrest through c-Myc Downregulation

Autor: Jing Ai, Yi Chen, Youhong Hu, Wenming Ren, Bing Xiong, Yanfen Fang, Yang Dai, Yinchun Ji, Xia Peng, Yuchen Jiang

Rearranged during transfection (RET), an oncogenic driver, has been found in multiple tumor types and is thus a promising anticancer therapeutic target. Novel selective RET inhibitors (RETi) that can overcome V804 gatekeeper mutations, endowing resis

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3c66a316eadbaf662fffff3b8a38c065
https://doi.org/10.1158/1535-7163.c.6542826.v1

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Data from Preclinical Evaluation of SCC244 (Glumetinib), a Novel, Potent, and Highly Selective Inhibitor of c-Met in MET-dependent Cancer Models

Autor: Meiyu Geng, Jian Ding, Jingkang Shen, Bing Xiong, Yuchi Ma, Yinglei Gao, Yiming Sun, Yi Su, Xinying Yang, Yanyan Shen, Yong Xi, Yinchun Ji, Xia Peng, Yi Chen, Jing Ai

Because the receptor tyrosine kinase c-Met plays a critical role in tumor growth, metastasis, tumor angiogenesis, and drug resistance, the c-Met axis represents an attractive therapeutic target. Herein, we report the first preclinical characterizatio

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::a3c1f8f80a5b5dd25ca12a3e745b6a72
https://doi.org/10.1158/1535-7163.c.6538083.v1

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