High-Throughput Drug Screening Facility: Publications



Veach DR, Namavari M, Beresten T, Balatoni J, Minchenko M, Djaballah H, Finn RD, Clarkson B, Gelovani JG, Bornmann WG, Larson SM “Synthesis and in vitro examination of [124I]-, [125I]- and [131I]-2-(4-iodophenylamino) pyrido[2,3-d]pyrimidin-7-one radiolabeled Abl kinase inhibitors” Nucl Med Biol 2005; 32:313-321.

Antczak C, Shum D, Escobar S, Bassit B, Kim E, Seshan VE, Wu N, Yang G, Ouerfelli O, Li YM, Scheinberg DA, Djaballah H “High-throughput identification of inhibitors of the cancer target human mitochondrial peptide deformylase” J Biomol Screen 2007; 12:521-535.

Deng L, Dai P, Ciro A, Smee DF, Djaballah H, Shuman S “Identification of novel antipoxviral agents: Mitoxanthrone inhibits Vaccinia virus replication by blocking virion assembly” J Virol 2007; 81:13392-402.

Veach DR, Namavari M, Pillarsetty N, Santos EB, Beresten-Kochetkov T, Lambek C, Punzalan BJ, Antczak C, Smith-Jones PM, Djaballah H, Clarkson B, Larson SM “Preparation of a fluorine-18 derivative of dasatinib” J Med Chem 2007; 50:5853-5857.

Ramajayam R, Giridhar R, Yadav MR, Djaballah H, Shum D, Radu C “Synthesis and antiproliferative activity of some diaryldiazepines and diarylpyrimidines” J Enzyme Inhib Med Chem 2007; 22:716-721.

Ramajayam R, Giridhar R, Yadav MR, Balaraman R, Djaballah H, Shum D, Radu C “Synthesis, antileukemic and antiplatelet activities of 2,3-diaryl-6,7-dihydro-5H-1,4-diazepines” Eur J Med Chem 2008; 43:2004-10.

Antczak C, Radu C, Djaballah H “A profiling platform for the identification of selective metalloprotease inhibitors” J Biomol Screen 2008; 13:285-294.

Eckelbarger JD, Wilmot JT, Epperson MT, Thakur CS, Shum D, Antczak C, Tarassishin L, Djaballah H, Gin DY “Synthesis of antiproliferative cephalotaxus esters and their evaluation against several human hematopoietic and solid tumor cell lines: Uncovering differential susceptibilities to multi-drug resistance” Chemistry 2008; 14:4293-306.

Desbordes SC, Placantonakis DG, Ciro A, Socci ND, Lee G, Djaballah H, Studer L “High-throughput screening assay for the identification of compounds regulating human embryonic stem cells self-renewal and differentiation” Cell Stem Cell 2008; 2:602-12.

Shum D, Radu C, Kim E, Cajuste M, Shao Y, Seshan VE, Djaballah H “A generic assay utilizing the Alamar Blue (resazurin) fluorescent dye for the detection of cytotoxic agents in chemical libraries screened in 1536-well plate” J Enzyme Inhib Med Chem 2008; 23:931-45.

Antczak C, Kloepping C, Radu C, Genski T, Müller-Kuhrt L, Siems K, de Stanchina E, Abramson DH, Djaballah H “Revisiting old drugs as novel agents for retinoblastoma: In vitro and In vivo antitumor activity of cardenolides” Invest Ophthalm Visual Science 2009; 50:3065-3073.

Antczak C, Shum D, Radu C, Seshan VE, Djaballah H “Development and validation of a high-density fluorescence polarization-based assay for the trypanosoma RNA triphosphatase TbCet1” Comb Chem High Thr Screen 2009; 12:258-68.

Shelton CC, Tian Y, Shum D, Radu C, Djaballah H, Li YM “A Miniaturized 1536-well format γ-Secretase Assay” Assay Drug Dev Technol 2009; 7:461-70.

Antczak C, Takagi T, Ramirez CN, Radu C, Djaballah H “Live cell imaging of caspase activation for high content screening” J Biomol Screen 2009; 14:956-969.

Somwar R, Shum D, Djaballah H, Varmus H “Identification and preliminary characterization of novel small molecules that inhibit growth of human lung adenocarcinoma cells” J Biomol Screen 2009; 14:1176-84.

Antczak C, Veach DR, Ramirez CN, Minchenko MA, Shum D, Calder PA, Frattini MG, Clarkson B, Djaballah H “Structure-activity relationships of 6-(2,6-dichlorophenyl)-8-methyl-2-(phenylamino) pyrido[2,3-d]pyrimidin-7-ones: Toward selective Abl inhibitors” Bioorg Med Chem Lett 2009; 19:6872-6.

Shelton CC, Zhu L, Chau D, Yang L, Wang R, Djaballah H, Zheng H, Li YM “Modulation of γ-secretase specificity using small molecule allosteric inhibitors” PNAS (USA) 2009; 106:20228-33.

Seideman JH, Shum D, Djaballah H, Scheinberg DA “A high-throughput screen for alpha particle radiation protectants” Assay Drug Dev Technol 2010; 8:602-14.

Steele I, Ramirez CN, Djaballah H “Human embryonic stem cells in drug discovery: Are we there yet?” Inter Drug Disc 2010; April/May issue, 38-41.

Djaballah H “An interview with Hakim Djaballah, Ph.D. Interview by Vicki Glaser” Assay Drug Dev Technol 2010; 8:519-525.

Shum D, Smith JL, Hirsch AJ, Bhinder B, Radu C, Stein DA, Nelson JA, Früh K, Djaballah H “High-content assay to identify inhibitors of dengue virus infection” Assay Drug Dev Technol 2010; 8:553-70.

Ramirez CN, Antczak C, Djaballah H “Cell viability assessment: Toward content-rich platforms” Exp Opin Drug Disc 2010; 5:223-233.

Ramirez CN, Ozawa T, Takagi T, Antczak C, Shum D, Graves R, Holland EC, Djaballah H “Validation of a high-content screening assay using whole-well imaging of transformed phenotypes” Assay Drug Dev Technol 2011; 9:247-261. Epub 2010 Dec 23.

Patel M, Paulus YM, Gobin YP, Djaballah H, Marr B, Dunkel IJ, Brodie S, Antczak C, Folberg R, Abramson DH “Intraarterial and oral digoxin therapy for retinoblastoma” Ophthalmic Genetics 2011; 32:147-50.

Takagi T, Shum D, Parisi M, Santos RE, Radu C, Calder P, Rizvi Z, Frattini MG, Djaballah H “Comparison of luminescence ADP production assay and radiometric scintillation proximity assay for Cdc7 kinase” Comb Chem High Through Screen 2011; 14:669-687.

Antczak C, Shum D, Bassit B, Frattini MG, Li YM, de Stanchina E, Scheinberg DA, Djaballah H “Identification of benzofuran-4,5-diones as novel and selective non-hydroxamic acid, non-peptidomimetic based inhibitors of human peptide deformylase” Bioorg Med Chem Lett 2011; 21:4528-4532.

Somwar R, Erdjument-Broomage H, Larsson E, Shum D, Lockwood WW, Sander C, Ouerfelli O, Tempst P, Djaballah H, Varmus H “Superoxide dismutase 1 is a probable target for a small molecule identified in a screen for inhibitors of the growth of lung adenocarcinoma cell lines” PNAS (USA) 2011; 108:16375-16380.

Antczak C, Bermingham A, Calder P, Malkov D, Song K, Fetter J, Djaballah H “Domain-Based Biosensor Assay to Screen for EGFR Modulators in Live Cells” Assay Drug Dev Technol 2012; 10:24-36.

Ibáñez G, Shum D, Blum G, Bhinder B, Radu C, Antczak C, Luo M, Djaballah H “A high throughput scintillation proximity imaging assay for protein methyltransferases” Comb Chem High Through Screen 2012; 15:359-371.

Tseng HM, Shum D, Bhinder B, Escobar S, Veomett NJ, Gin, DY, Tomkinson AE, Djaballah H, Scheinberg DA “A high throughput scintillation proximity based assay for human DNA ligase IV” Assay Drug Dev Technol 2012; 10:235-249.

Shum D, Bhinder B, Radu C, Calder P, Ramirez CN, Djaballah H “An image-based biosensor assay strategy to screen for modulators of the microRNA 21 biogenesis pathway” Comb Chem High Through Screen 2012; 15:529-541.

Antczak C, Mahida, J, Bhinder, B, Calder, PA, Djaballah H “A high-content biosensor based screen identifies cell permeable activators and inhibitors of EGFR function: Implications in drug discovery” J Biomol Screen 2012; 17:885-899.

Ramirez CN, Dure D, Djaballah H “Stem cells, cell based assays, and the world of small molecules” Drug Discovery World Summer 2012 issue, 54-62.

Feldman T, Kabaleeswaran V, Jang SB, Antczak C, Djaballah H, Wu H, Jiang X “A class of allosteric caspase inhibitors identified by high-throughput screening” Mol Cell 2012; 47:585-95.

Radu C, Adrar HS, Alamir A, Hatherley I, Trinh T, Djaballah H “Designs and concept-reliance of a fully automated high content screening platform” J Lab Autom 2012; 17:359-369.

Djaballah H “Random RNAi screening data analysis: A call for standardization” Comb Chem High Through Screen 2012; 15:685.

Bhinder B, Djaballah H “A simple method for analyzing actives in random RNAi screens: introducing the “H Score” for hit nomination and gene prioritization” Comb Chem High Through Screen 2012; 15:686-704.

Lee G, Ramirez CN, Kim H, Zeltner N, Liu B, Radu C, Bhinder B, Kim YJ, Choi IY, Mukherjee-Clavin B, Djaballah H, Studer L “IKBKAP expression rescue in neural crest of familial dysautonomia-iPSC cells by novel RT-PCR based high throughput screening” Nature Biotech 2012; 30:1244-1248.

Shum D, Bhinder B, Ramirez, CN, Radu C, Calder PA, Beauchamp L, Magdaleno S, Djaballah H “An arrayed RNAi genome-wide screen identifies candidate genes involved in the miRNA 21 biogenesis pathway” Assay Drug Dev Technol  2012 Sep 20. [Epub ahead of print]

Bhinder B, Antczak C, Ramirez CN, Shum D, Radu C, Liu-Sullivan N, Frattini MG, Djaballah H “An arrayed genome scale lentiviral enabled shRNA screen identifies lethal and rescuer gene candidates” Assay Drug Dev Technol 2012 Nov 30. [Epub ahead of print]

Kobos R, Nagai M, Tsuda M, Merl MY, Saito T, Laé M, Mo Q, Olshen A, Lianoglou S, Leslie C, Ostrovnaya I, Antczak C, Djaballah H, Ladanyi M “Combining integrated genomics and functional genomics to dissect the biology of a cancer-associated, aberrant transcription factor, the ASPSCR1-TFE3 fusion oncoprotein” J Pathol 2013 Jan 3. doi: 10.1002/path.4158. [Epub ahead of print]

Mahida JP, Antczak C, De Carlo D, Champ KG, Francis JH, Marr B, Polans AS, Albert DM, David H. Abramson DH, Djaballah H “A synergetic screening approach with companion effector for combination therapy: Application to retinoblastoma” PLOS One (Under review).

Bhinder  B, Djaballah H  “A comparative analysis of RNAi lethality screens identifies a core signature of 79 genes and reveals a striking hit enrichment in pooled shRNA formats: does gene(s) depletion per cell warrant essentiality?” Assay Drug Dev Technol (Submitted).

Shum D, Bhinder B, Ramirez, CN, Radu C, Calder PA, Beauchamp L, Magdaleno S, & Djaballah H “An arrayed RNAi genome-wide screen identifies candidate genes involved in the miRNA 21 biogenesis pathway” Assay Drug Dev Technol  2013; 11(3):191-205.

Bhinder B, Antczak C, Ramirez CN, Shum D, Radu C, Liu-Sullivan N, Frattini MG, Djaballah H “An Arrayed Genome Scale Lentiviral Enabled shRNA Screen Identifies Lethal & Rescuer Gene Candidates” Assay Drug Dev Technol 2013; 11(3):173-190.

Chau DM, Shum D, Radu C, Bhinder B, Gin D, Gilchrist ML, Djaballah H, Li YM “A Novel High-Throughput 1536-well Notch1 γ-Secretase AlphaLISA Assay” Comb Chem High Through Screen 2013; 16:415-424.

Fischer MA, Smith JL, Shum D, Stein DA, Parkins C, Bhinder B, Radu C, Hirsch AJ, Djaballah H, Nelson JA, Früh K “Flaviviruses are sensitive to inhibition of thymidine synthesis pathways” J Virol 2013; 87:9411-9419.

Bhinder B, Antczak C, Shum D, Radu C, Mahida JP, Liu-Sullivan N, Ibáñez G, Somalinga B, Calder PA, Djaballah H “Chemical & RNAi screening at MSKCC: a collaborative platform to discover & repurpose drugs to fight disease” Comb Chem High Through Screen 2014; 17:298-318.

Antczak C, Boyoung W, Radu C, Bhinder B, Holland EC, Djaballah H “A High Content Assay Strategy for the Identification and Profiling of ABCG2 Modulators in Live Cells” Assay Drug Dev Technol 2014; 12:28-42.

Smith JL, Stein DA, Shum D, Fischer MA, Radu C, Bhinder B, Djaballah H, Nelson JA, Früh K, Hirsch AJ “Inhibition of dengue virus replication by a class of small-molecule compounds that antagonize dopamine receptor d4 and downstream mitogen-activated protein kinase signaling” J Virol 2014; 10:5533-5542.

Blum G, Ibáñez G, Rao X, Shum D, Radu C, Djaballah H, Rice JC, Luo M “Small-Molecule Inhibitors of SETD8 with Cellular Activity” ACS Chem Biol. 2014 Sep 3. – In Process

Minuesa G, Antczak C, Shum D, Radu C, Bhinder B, Li Y, Djaballah H, Kharas MG “A 1536-well fluorescence polarization assay to screen for modulators of the MUSASHI family of RNA-binding proteins” Comb Chem High Throughput Screen. 2014;17(7):596-609.