Literature DB >> 18608772

A high density assay format for the detection of novel cytotoxic agents in large chemical libraries.

David Shum1, Constantin Radu, Earl Kim, Muriel Cajuste, Yufang Shao, Venkatraman E Seshan, Hakim Djaballah.   

Abstract

In response to the need for inexpensive high throughput assays for anti-cancer drug screening, a 1536-well microtiter plate based assay utilizing the Alamar Blue fluorescent dye as a measure of cellular growth was validated in 10 microL assay volume. Its robustness was assessed in a screen against a library of 2000 known bioactives; with an overall Z' value of 0.89 for assay robustness, several known cytotoxic agents were identified including and not limited to anthracyclines, cardiac glycosides, gamboges, and quinones. To further test the sensitivity of the assay, IC50 determinations were performed in both 384-well and 1536-well formats and the obtained results show a very good correlation between the two density formats. These findings demonstrate that this newly developed assay is simple to set up, robust, highly sensitive and inexpensive. It could potentially provide a rapid way to screen established and primary tumor cell lines against large chemical libraries.

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Year:  2008        PMID: 18608772      PMCID: PMC3710589          DOI: 10.1080/14756360701810082

Source DB:  PubMed          Journal:  J Enzyme Inhib Med Chem        ISSN: 1475-6366            Impact factor:   5.051


  23 in total

1.  A Simple Statistical Parameter for Use in Evaluation and Validation of High Throughput Screening Assays.

Authors: 
Journal:  J Biomol Screen       Date:  1999

2.  Indanocine, a microtubule-binding indanone and a selective inducer of apoptosis in multidrug-resistant cancer cells.

Authors:  L M Leoni; E Hamel; D Genini; H Shih; C J Carrera; H B Cottam; D A Carson
Journal:  J Natl Cancer Inst       Date:  2000-02-02       Impact factor: 13.506

3.  Quantification of mitogen induced human lymphocyte proliferation: comparison of alamarBlue assay to 3H-thymidine incorporation assay.

Authors:  R de Fries; M Mitsuhashi
Journal:  J Clin Lab Anal       Date:  1995       Impact factor: 2.352

4.  A new rapid and simple non-radioactive assay to monitor and determine the proliferation of lymphocytes: an alternative to [3H]thymidine incorporation assay.

Authors:  S A Ahmed; R M Gogal; J E Walsh
Journal:  J Immunol Methods       Date:  1994-04-15       Impact factor: 2.303

5.  Activation of the cAMP signaling pathway increases apoptosis in human B-precursor cells and is associated with downregulation of Mcl-1 expression.

Authors:  J H Myklebust; D Josefsen; H K Blomhoff; F O Levy; S Naderi; J C Reed; E B Smeland
Journal:  J Cell Physiol       Date:  1999-07       Impact factor: 6.384

6.  A new alkaloid AM-2282 OF Streptomyces origin. Taxonomy, fermentation, isolation and preliminary characterization.

Authors:  S Omura; Y Iwai; A Hirano; A Nakagawa; J Awaya; H Tsuchya; Y Takahashi; R Masuma
Journal:  J Antibiot (Tokyo)       Date:  1977-04       Impact factor: 2.649

7.  Comparison of alamar blue and MTT assays for high through-put screening.

Authors:  R Hamid; Y Rotshteyn; L Rabadi; R Parikh; P Bullock
Journal:  Toxicol In Vitro       Date:  2004-10       Impact factor: 3.500

8.  Microtiter plate assay for the measurement of glutathione and glutathione disulfide in large numbers of biological samples.

Authors:  M A Baker; G J Cerniglia; A Zaman
Journal:  Anal Biochem       Date:  1990-11-01       Impact factor: 3.365

9.  Comparison of the usefulness of the MTT, ATP, and calcein assays to predict the potency of cytotoxic agents in various human cancer cell lines.

Authors:  Henrik Mueller; Matthias U Kassack; Michael Wiese
Journal:  J Biomol Screen       Date:  2004-09

10.  A sensitive new bioassay for tumor necrosis factor.

Authors:  T A Shahan; P D Siegel; W G Sorenson; W G Kuschner; D M Lewis
Journal:  J Immunol Methods       Date:  1994-10-14       Impact factor: 2.303

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  24 in total

1.  A high content assay to assess cellular fitness.

Authors:  Christophe Antczak; Jeni P Mahida; Chanpreet Singh; Paul A Calder; Hakim Djaballah
Journal:  Comb Chem High Throughput Screen       Date:  2014-01       Impact factor: 1.339

2.  Identification of benzofuran-4,5-diones as novel and selective non-hydroxamic acid, non-peptidomimetic based inhibitors of human peptide deformylase.

Authors:  Christophe Antczak; David Shum; Bhramdeo Bassit; Mark G Frattini; Yueming Li; Elisa de Stanchina; David A Scheinberg; Hakim Djaballah
Journal:  Bioorg Med Chem Lett       Date:  2011-06-12       Impact factor: 2.823

3.  Identification and preliminary characterization of novel small molecules that inhibit growth of human lung adenocarcinoma cells.

Authors:  Romel Somwar; David Shum; Hakim Djaballah; Harold Varmus
Journal:  J Biomol Screen       Date:  2009-12

4.  Cell viability assessment: toward content-rich platforms.

Authors:  Christina Nicole Ramirez; Christophe Antczak; Hakim Djaballah
Journal:  Expert Opin Drug Discov       Date:  2010-01-29       Impact factor: 6.098

5.  Rationale for Using Irreversible Epidermal Growth Factor Receptor Inhibitors in Combination with Phosphatidylinositol 3-Kinase Inhibitors for Advanced Head and Neck Squamous Cell Carcinoma.

Authors:  Nicole L Michmerhuizen; Elizabeth Leonard; Chloe Matovina; Micah Harris; Gabrielle Herbst; Aditi Kulkarni; Jingyi Zhai; Hui Jiang; Thomas E Carey; J Chad Brenner
Journal:  Mol Pharmacol       Date:  2019-03-11       Impact factor: 4.436

Review 6.  Arrayed functional genetic screenings in pluripotency reprogramming and differentiation.

Authors:  Rodrigo Alexandre Panepucci; Ildercílio Mota de Souza Lima
Journal:  Stem Cell Res Ther       Date:  2019-01-11       Impact factor: 6.832

7.  A high-throughput screen for alpha particle radiation protectants.

Authors:  Jonathan H Seideman; David Shum; Hakim Djaballah; David A Scheinberg
Journal:  Assay Drug Dev Technol       Date:  2010-07-26       Impact factor: 1.738

8.  In vitro viability and cytotoxicity testing and same-well multi-parametric combinations for high throughput screening.

Authors:  Andrew L Niles; Richard A Moravec; Terry L Riss
Journal:  Curr Chem Genomics       Date:  2009-06-11

9.  Structure-activity relationships of 6-(2,6-dichlorophenyl)-8-methyl-2-(phenylamino)pyrido[2,3-d]pyrimidin-7-ones: toward selective Abl inhibitors.

Authors:  Christophe Antczak; Darren R Veach; Christina N Ramirez; Maria A Minchenko; David Shum; Paul A Calder; Mark G Frattini; Bayard Clarkson; Hakim Djaballah
Journal:  Bioorg Med Chem Lett       Date:  2009-10-23       Impact factor: 2.823

10.  Synthesis of antiproliferative Cephalotaxus esters and their evaluation against several human hematopoietic and solid tumor cell lines: uncovering differential susceptibilities to multidrug resistance.

Authors:  Joseph D Eckelbarger; Jeremy T Wilmot; Matthew T Epperson; Chandar S Thakur; David Shum; Christophe Antczak; Leonid Tarassishin; Hakim Djaballah; David Y Gin
Journal:  Chemistry       Date:  2008       Impact factor: 5.236

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