Yong Chen

First Affiliated Hospital of Bengbu Medical College

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Lijuan Chen

State Key Laboratory of Biotherapy

Minghai Tang

Sichuan University

Haoyu Ye

Sichuan University

Heying Pei

Sichuan University

Ting Niu

West China Hospital of Sichuan University

Yuyao Yi

Sichuan University

Shoujun Zheng

Beijing Institute of Technology

Zejiang Zhu

Sichuan University

Dongni Yi

Mayo Clinic

Liping Gou

Sichuan Agricultural University

Cooperative Institutions

Sichuan University

181

West China Hospital of Sichuan University

119

State Key Laboratory of Biotherapy

Chinese Academy of Sciences

Chinese Academy of Medical Sciences & Peking Union Medical College

Capital Medical University

Sun Yat-sen University

Huazhong University of Science and Technology

Chengdu University

Central South University

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Discovery and Evaluation of 3-Quinoxalin Urea Derivatives as Potent, Selective, and Orally Available ATM Inhibitors Combined with Chemotherapy for the Treatment of Cancer via Goal-Oriented Molecule Generation and Virtual Screening

Journal of Medicinal Chemistry (2023)

Dexin Deng Yingxue Yang Yurong Zou Kongjun Liu Chufeng Zhang

ATM plays an important role in DNA damage response and is considered a potential target in cancer therapies. In this study, a goal-directed molecular generation approach based on ligand similarity and target specificity was applied to sample active molecules, and they were screened virtually to identify the theoretical lead compound 7a, which was later shown to inhibit ATM adequately. However, there is a main concern about its poor metabolic stability in vitro. Subsequent optimization was performed to improve the potency and selectivity toward ATM and attenuate the hepatic clearance in vitro, culminating in the identification of 10r with nanomolar ATM inhibition, excellent cellular sensitivity to radiation and chemotherapy drugs, and impressive pharmacokinetic profiles. Furthermore, 10r combined with irinotecan demonstrated a synergistic antitumor efficacy in SW620 xenograft models, suggesting that it could be a promising candidate drug combined with chemotherapy for the treatment of cancer.

10.1021/acs.jmedchem.3c00082

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Data from Purinostat Mesylate Is a Uniquely Potent and Selective Inhibitor of HDACs for the Treatment of BCR-ABL–Induced B-Cell Acute Lymphoblastic Leukemia

Linyu Yang Qiang Qiu Minghai Tang Fang Wang Yuyao Yi

<div>AbstractPurpose:This study was to perform preclinical evaluation of a novel class I and IIb HDAC-selective inhibitor, purinostat mesylate, for the treatment of Ph+ B-cell acute lymphoblastic leukemia (B-ALL).Experimental Design:Biochemical assays were used to test enzymatic activity inhibition of purinostat mesylate. Ph+ leukemic cell lines and patient cells were used to evaluate purinostat mesylate activity in vitro. BL-2 secondary transplantation Ph+ B-ALL mouse model was used to validate its efficacy, mechanism, and pharmacokinetics properties in vivo. BCR-ABL(T315I)–induced primary B-ALL mouse model and PDX mouse model derived from relapsed Ph+ B-ALL patient post TKI treatment were used to determine the antitumor effect of purinostat mesylate for refractory or relapsed Ph+ B-ALL. Long-term toxicity and hERG blockade assays were used to safety evaluation of purinostat mesylate.Results:Purinostat mesylate, a class I and IIb HDAC highly selective inhibitor, exhibited robust antitumor activity in hematologic cancers. Purinostat mesylate at low nanomolar concentration induced apoptosis, and downregulated BCR-ABL and c-MYC expression in Ph+ leukemia cell lines and primary Ph+ B-ALL cells from relapsed patients. Purinostat mesylate efficiently attenuated Ph+ B-ALL progression and significantly prolonged the survival both in BL-2 secondary transplantation model with clinical patient symptoms of Ph+ B-ALL, BCR-ABL(T315I)–induced primary B-ALL mouse model, and PDX model derived from patients with relapsed Ph+ B-ALL post TKI treatment. In addition, purinostat mesylate possesses favorable pharmacokinetics and low toxicity properties.Conclusions:Purinostat mesylate provides a new therapeutic strategy for patients with Ph+ B-ALL, including those who relapse after TKI treatment.</div>

Imatinib Mesylate

Mesylate

10.1158/1078-0432.c.6528252

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Figure S3 from Purinostat Mesylate Is a Uniquely Potent and Selective Inhibitor of HDACs for the Treatment of BCR-ABL–Induced B-Cell Acute Lymphoblastic Leukemia

Linyu Yang Qiang Qiu Minghai Tang Fang Wang Yuyao Yi

Toxicity studies of PM.

breakpoint cluster region

10.1158/1078-0432.22472535

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[alpha1-adrenoceptor antagonists and ejaculation dysfunction].

Yong Chen Hong Li Qiang Dong

alpha1-adrenoceptor antagonists are first-line agents for the treatment of lower urinary tract symptoms suggestive of benign prostatic hyperplasia, while their adverse effects on sexual function are reported frequently in recent years, especially the induction of ejaculatory dysfunction. This review presents the distribution of alpha 1-adrenoceptors in the male genital system and the relationship of alpha1-adrenoceptors with ejaculatory function. It also highlights the interesting phenomenon of ejaculatory dysfunction related to these drugs and its possible mechanism, with the intention to provide some essential clues for further research on this problem as well as some references to safer use of these drugs in clinical settings.

Ejaculation

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Rational design and appraisal of selective Cdc2-Like kinase 1 (Clk1) inhibitors as novel autophagy inducers for the treatment of acute liver injury (ALI)

European Journal of Medicinal Chemistry (2023)

Tao Yang Yingxue Yang Yong Chen Minghai Tang Mingsong Shi

DYRK1A

Inducer

10.1016/j.ejmech.2023.115168

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Discovery, Optimization, and Evaluation of Quinazolinone Derivatives with Novel Linkers as Orally Efficacious Phosphoinositide-3-Kinase Delta Inhibitors for Treatment of Inflammatory Diseases

Journal of Medicinal Chemistry (2021)

Kongjun Liu Dan Li Wei Zheng Mingsong Shi Yong Chen

Guided by molecular docking, a commonly used open-chain linker was cyclized into a five-membered pyrrolidine to lock the overall conformation of the propeller-shaped molecule. Different substituents were introduced into the pyrrolidine moiety to block oxidative metabolism. Surprisingly, it was found that a small methyl substituent could be used to alleviate the oxidative metabolism of pyrrolidine while maintaining or enhancing potency, which could be described as a "magic methyl". Further optimization around the "3rd blade" of the propeller led to identification of a series of potent and selective PI3Kδ inhibitors. Among them, compound 50 afforded an optimum balance of PK profiles and potency. Oral administration of 50 attenuated the arthritis severity in a dose-dependent manner in a collagen-induced arthritis model without obvious toxicity. Furthermore, 50 demonstrated excellent pharmacokinetic properties with high bioavailability, suggesting that 50 might be an acceptable candidate for treatment of inflammatory diseases.

Pyrrolidine

Chalcone

Pyrazole

10.1021/acs.jmedchem.1c00004

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An Approach of a Nonlinear Dynamic Model for Micellar Effects on Bimolecular Reactions

Journal of Colloid and Interface Science (1999)

Xiao-Nan Chen Xiao Cheng Zeng Yong Chen Siqing Chen

10.1006/jcis.1999.6146

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Citations (18)

Quantum recurrent encoder–decoder neural network for performance trend prediction of rotating machinery

Knowledge-Based Systems (2020)

Yong Chen Feng Li Jiaxu Wang Baoping Tang Xueming Zhou

Traverse

10.1016/j.knosys.2020.105863

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Consequences of post-disaster policies and relocation approaches: two communities from rural China

Disaster Prevention and Management An International Journal (2020)

Yong Chen Lulu He Dan Zhou

Purpose Post-disaster population resettlement is a complicated process, during which the restoration of livelihood and lifestyle plays a critical role in achieving a successful resettlement outcome. This paper attempts to examine how recovery policies and relocation approaches influence people's livelihood recovery and perception of wellbeing. It specifically investigates the role of farmland in producing a livelihood and maintaining a rural lifestyle among displaced people. Design/methodology/approach Through face-to-face questionnaire surveys and in-depth interviews with rural residents displaced from their villages after the Wenchuan earthquake in Sichuan, China, this study presents both quantitative and qualitative evidence to investigate how post-disaster policies and particularly the availability of farmland influence people's recovery and their satisfaction with the post-resettlement life. Findings Data suggest that availability of farmland, in spite of the size, makes big differences in post-disaster recovery because farmland provides resettled people with not only a livelihood to secure basic living but also a guarantee to maintain a rural lifestyle. Research limitations/implications More samples are needed for analyzing factors that significantly influence disaster-displaced farmers' recovery and wellbeing post resettlement. Practical implications This study can be used as an important reference for making plans for post-disaster recovery and population resettlement programs in other disaster-prone countries across the world. Originality/value Land-based relocation is proposed as a desirable approach to addressing challenges of livelihood restoration amongst the resettled population in rural areas of developing countries.

Relocation

Disaster Recovery

10.1108/dpm-11-2019-0347

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The Driving Force and Prediction of the Evolution of Land Use and Ecosystem Services Value——A case Study of Jiangsu Province

Shuitu baochi yanjiu (2010)

Yong Chen

By using the statistical data of land and related socio-economic indicators of Jiangsu province from 1999to 2007,this paper conducted a quantitative study on the evolution of land use and ecosystem services value,and then analyzed the driving factors.On this basis,aprediction is made by using the GM(1,1)model.The land of orchard,residential and industrial,traffic increased while ecosystem services value and the land of cultivated,forest,water decreased from 1999to 2007.From 2010to 2020,the various types of land and the ecosystem services value continued the same changing trend of 1999to 2007,but showing an expanding in trend.In 1999and 2020,the major factors that made the impact on the value of ecosystem services of Jiangsu province were gradually changing from the population,the level of agricultural modernization to the quality of the population,investment of fixed assets and the level of urbanization which indicated that the quality of the population,investment of fixed assets and the level of urbanization were increasingly becoming the main factors to impact the eco-environment in Jiangsu province.

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Orchard

Agricultural land

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