Construction of drug screening cell model and application to new compounds inhibiting FITC-fibrinogen binding to CHO cells expressing human αIIbβ3

Yang, Jie; Yao, Jia; Chen, Jie; Wang, Xiaoning; Zhu, Tongyang; Chen, Lili; Chu, Ping

doi:10.1016/j.ejphar.2009.07.011

Cited by 7 publications

(14 citation statements)

References 20 publications

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“…Our results displayed that their anti-Abeta activities depended on the substitutes at position 2 of the tetrahydroisoquinoline nucleus. Phenylsulfonyl, benzyl or ortho-substituted benzoyl derivatives have higher anti-Abeta activities, such as compounds I-1, I-3, II-1, II-4, and II-6, which is supported by our previous research results that the phenylsulfonye group is necessary (Yang et al, 2009). Electron-withdrawing groups (EWG) at the position ortho of benzene are propitious to antiAbeta activities, such as chlorine (II-4) and nitryl groups (I-3).…”

Section: Construction Of Drug Screening Cell Model and Application Tosupporting

confidence: 67%

“…The anti-Abeta activities of unsubstituted phenylsulfonyl derivatives (I-1 and II-6) are evidently higher than that of I-2. We have reported that the nitrogen atom at 2 position of 1,2,3,4-tetrahydroisoquinoline interacted with the carboxyl group at the side chain of Asp179 of integrin alpha2b in the fashion of electrostatic interaction (Yang et al, 2009). Here the sulphonyl and carbonyl group at 2 position of 1,2,3,4-tetrahydroisoquinoline may interact with gamma-secrease in the same fashion to exhibit anti-Abeta activities.…”

Section: Construction Of Drug Screening Cell Model and Application Tomentioning

confidence: 96%

“…In a previous study, our group has constructed the drug screening cell model applied to some compounds inhibiting FITC-fibrinogen binding to human alphaIIbbeta3 expressed in CHO cells (Yang et al, 2009). We utilized the tetracycline-responsive system (Zhu, 1999) to express EGFP-tagged C99 fusion as a gamma-secretase substrate.…”

Section: Discussionmentioning

confidence: 99%

“…For stable expression, CHO cells were transfected and selected with G418 as described previously (Yang et al, 2009). Briefly, CHO cells were incubated in 24-well plates at a density of 5.5×105 cells per well for 24 h before transfection.…”

Section: Transfection and Selection Of Stably Transfected Cells Undermentioning

confidence: 99%

“…The cytotoxic effect of these compounds on normal CHO cells were tested by MTT assay and the IC 50 values were calculated from the dose-response curves (Basani et al, 2001;Yang et al, 2009). CHO were incubated into 96-well plates and cultured in DMEM supplemented with 10% FBS.…”

Section: Cytotoxicitymentioning

confidence: 99%

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Construction of Drug Screening Cell Model and Application to New Compounds Interfering Production and Accumulation of Beta-Amyloid by Inhibiting Gamma-Secretase

Wang¹,

Yang²,

Xu³

et al. 2011

Advanced Understanding of Neurodegenerative Diseases

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As a result, considerable attention is being focused on attempts to develop therapies for Alzheimer's disease that are directed towards metabolic pathways that involve Abeta. One way is to reduce production of Abeta through the upstream processing enzymes (betasecretase and gamma-secretase). gamma-secretase is a multi-subunit protease complex, minimally consists of four individual proteins: presenilin, nicastrin, APH-1, and PEN-2. Consequently, several gamma-secretase inhibitors have recently been described, including transition state analogs that mimic the gamma-secretase cleavage site on the immediate Abeta precursor (C99) and presumably compete with it for binding to the gamma-secretase enzymatic site (Netzer, et al., 2003). Here express gamma-secretase's substrate (such as EGFP-tagged C99 of APP) in the cultured cells (CHO) under control of tetracycline inducible system (Tet-off system) and then evaluate the efficiency of the inhibitors by ELISA (EnzymeLinked Immunosorbnent Assay) and Western blot. This paper focuses on construction of a drug screen model for AD's gamma-secretase inhibitors and further finds some active compounds possessing gamma-secretase inhibition activity.

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Section: Construction Of Drug Screening Cell Model and Application Tosupporting

confidence: 67%

Section: Construction Of Drug Screening Cell Model and Application Tomentioning

confidence: 96%

Section: Discussionmentioning

confidence: 99%

Section: Transfection and Selection Of Stably Transfected Cells Undermentioning

confidence: 99%

Section: Cytotoxicitymentioning

confidence: 99%

See 3 more Smart Citations

Construction of Drug Screening Cell Model and Application to New Compounds Interfering Production and Accumulation of Beta-Amyloid by Inhibiting Gamma-Secretase

Wang¹,

Yang²,

Xu³

et al. 2011

Advanced Understanding of Neurodegenerative Diseases

Self Cite

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Studies of tricyclic piperazine/piperidine furnished molecules as novel integrin αvβ3/αIIbβ3 dual antagonists using 3D-QSAR and molecular docking

Yan

Zhang

et al. 2011

Journal of Molecular Graphics and Modelling

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A new way to detect the interaction of DNA and anticancer drugs based on the decreased resonance light scattering signal and its potential application

Chen

Song

Peng

et al. 2011

Analyst

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A novel assay has been developed to detect the interaction of DNA and anticancer drugs based on the decreased resonance light scattering (RLS) technique. The proposed method can be used to study those drugs which do not produce a RLS-signal after binding to DNA. RLS was used to monitor the interaction of five anticancer drugs with DNA. The reaction between anticancer drugs and DNA took place in BR buffer solution. From the RLS assay, the sequence of five anticancer drugs activities was as follows: CTX < MTX < Pt < MMC < 5-Fu. Mammary cancer cell DNA (mcDNA) was involved to validate the RLS assay. The results showed that the sensitivities of the five anticancer drugs targeting both mcDNA and ctDNA increased in the same order. However the sensitivity of each drug to mcDNA was higher than that to ctDNA It is a significant innovation of the RLS method to detect the interaction of DNA and anticancer drugs and to obtain drug sensitivity, which provides new strategies to screen DNA targeted anticancer drugs.

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Construction of drug screening cell model and application to new compounds inhibiting FITC-fibrinogen binding to CHO cells expressing human αIIbβ3

Cited by 7 publications

References 20 publications

Construction of Drug Screening Cell Model and Application to New Compounds Interfering Production and Accumulation of Beta-Amyloid by Inhibiting Gamma-Secretase

Construction of Drug Screening Cell Model and Application to New Compounds Interfering Production and Accumulation of Beta-Amyloid by Inhibiting Gamma-Secretase

Studies of tricyclic piperazine/piperidine furnished molecules as novel integrin αvβ3/αIIbβ3 dual antagonists using 3D-QSAR and molecular docking

A new way to detect the interaction of DNA and anticancer drugs based on the decreased resonance light scattering signal and its potential application

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