High-throughput screen for the chemical inhibitors of antiapoptotic Bcl-2 family proteins by multiplex flow cytometry

Assay and Drug Development Technologies

Volumn 9, Issue 5, 2011, Pages 465-474

  Curpan, Ramona F ^a   Simons, Peter C ^b   Zhai, Dayong ^c   Young, Susan M ^b   Carter, Mark B ^b   Bologa, Cristian G ^d   Oprea, Tudor I ^d   Satterthwait, Arnold C ^c   Reed, John C ^c   Edwards, Bruce S ^b   Sklar, Larry A ^b  

^a ACADEMY OF ROMANIAN SCIENTISTS   (Romania)

^b UNIVERSITY OF NEW MEXICO HEALTH SCIENCES CENTER   (United States)

^c BURNHAM INSTITUTE   (United States)

^d UNIVERSITY OF NEW MEXICO SCHOOL OF MEDICINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

BH3 PROTEIN; BIM PROTEIN; CID 1243212; CID 650929; CID 666339; FLUORESCEIN; GLUTATHIONE; GLUTATHIONE TRANSFERASE; GREEN FLUORESCENT PROTEIN; HYBRID PROTEIN; LIGAND; PROTEIN BCL 2; PROTEIN BCL 2 INHIBITOR; PROTEIN INHIBITOR; UNCLASSIFIED DRUG;

ARTICLE; CONCENTRATION RESPONSE; DRUG PROTEIN BINDING; FLOW CYTOMETRY; FLUORESCENCE POLARIZATION; HIGH THROUGHPUT SCREENING; ISOTHERMAL TITRATION CALORIMETRY; PROCESS OPTIMIZATION; PROTEIN PROTEIN INTERACTION; VALIDATION PROCESS;

ANIMALS; APOPTOSIS; APOPTOSIS REGULATORY PROTEINS; BINDING, COMPETITIVE; CALORIMETRY; CLINICAL TRIALS AS TOPIC; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DISCOVERY; DRUG EVALUATION, PRECLINICAL; FLOW CYTOMETRY; FLUORESCENCE POLARIZATION; GLUTATHIONE; GREEN FLUORESCENT PROTEINS; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; MEMBRANE PROTEINS; MODELS, CHEMICAL; MOLECULAR TARGETED THERAPY; PROTEIN BINDING; PROTO-ONCOGENE PROTEINS; PROTO-ONCOGENE PROTEINS C-BCL-2; REPRODUCIBILITY OF RESULTS; SMALL MOLECULE LIBRARIES;

EID: 80053351708     PISSN: 1540658X     EISSN: 15578127     Source Type: Journal    
DOI: 10.1089/adt.2010.0363     Document Type: Article

References (20)

1. Carson RT, Vignali DA: Simultaneous quantitation of 15 cytokines using a multiplexed flow cytometric assay. J Immunol Methods 1999;227:41-52.
2. Tessema M, Simons PC, Cimino DF, Sanchez L, Waller A, Posner RG, Wandinger- Ness A, Prossnitz ER, Sklar LA: Glutathione-S-transferase-green fluorescent protein fusion protein reveals slow dissociation from high site density beads and measures free GSH. Cytometry A 2006;69:326-334.
3. Zuck P, Lao Z, Skwish S, Glickman JF, Yang K, Burbaum J, Inglese J: Ligandreceptor binding measured by laser-scanning imaging. Proc Natl Acad Sci U S A 1999;96:11122-11127.
4. Adams JM, Cory S: The Bcl-2 apoptotic switch in cancer development and therapy. Oncogene 2007;26:1324-1337.
5. Oltersdorf T, Elmore SW, Shoemaker AR, Armstrong RC, Augeri DJ, Belli BA, Bruncko M, Deckwerth TL, Dinges J, Hajduk PJ, Joseph MK, Kitada S, Korsmeyer SJ, Kunzer AR, Letai A, Li C, Mitten MJ, Nettesheim DG, Ng S, Nimmer PM, O'Connor JM, Oleksijew A, Petros AM, Reed JC, Shen W, Tahir SK, Thompson CB, Tomaselli KJ, Wang B, Wendt MD, Zhang H, Fesik SW, Rosenberg SH: An inhibitor of Bcl-2 family proteins induces regression of solid tumours. Nature 2005;435:677-681.
6. Reed JC, Pellecchia M: Apoptosis-based therapies for hematologic malignancies. Blood 2005;106:408-418.
7. Chen L, Willis SN, Wei A, Smith BJ, Fletcher JI, Hinds MG, Colman PM, Day CL, Adams JM, Huang DC: Differential targeting of prosurvival Bcl-2 proteins by their BH3-only ligands allows complementary apoptotic function. Mol Cell 2005;17:393-403.
8. van Delft MF, Wei AH, Mason KD, Vandenberg CJ, Chen L, Czabotar PE, Willis SN, Scott CL, Day CL, Cory S, Adams JM, Roberts AW, Huang DC: The BH3 mimetic ABT-737 targets selective Bcl-2 proteins and efficiently induces apoptosis via Bak/Bax If Mcl-1 is neutralized. Cancer Cell 2006;10:389-399.
9. Luciano F, Krajewska M, Ortiz-Rubio P, Krajewski S, Zhai D, Faustin B, Bruey JM, Bailly-Maitre B, Lichtenstein A, Kolluri SK, Satterthwait AC, Zhang XK, Reed JC: Nur77 converts phenotype of Bcl-B, an antiapoptotic protein expressed in plasma cells and myeloma. Blood 2007;109:3849-3855.
10. Lipinski CA, Lombardo F, Dominy BW, Feeney PJ: Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. Adv Drug Deliv Rev 2001;46:3-26.
11. Zhai D, Jin C, Satterthwait AC, Reed JC: Comparison of chemical inhibitors of antiapoptotic Bcl-2-family proteins. Cell Death Differ 2006; 13:1419-1421.
12. Edwards BS, Young SM, Oprea TI, Bologa CG, Prossnitz ER, Sklar LA: Biomolecular screening of formylpeptide receptor ligands with a sensitive, quantitative, highthroughput flow cytometry platform. Nat Protoc 2006;1:59-66.
13. Black CB, Duensing TD, Trinkle LS, Dunlay RT: Cell-based screening using highthroughput flow cytometry. Assay Drug Dev Technol 2010;9:13-20.
14. Simons PC, Young SM, Carter MB, Waller A, Zhai D, Reed JC, Edwards BS, Sklar LA: Simultaneous in vitro molecular screening of protein-peptide interactions by flow cytometry using six Bcl-2 family proteins as examples. Nature Protocols, in press.
15. Labi V, Grespi F, Baumgartner F, Villunger A: Targeting the Bcl-2-regulated apoptosis pathway by BH3 mimetics: A breakthrough in anticancer therapy? Cell Death Differ 2008;15:977-987.
16. Zhang H, Nimmer P, Rosenberg SH, Ng SC, Joseph M: Development of a highthroughput fluorescence polarization assay for Bcl-x(L). Anal Biochem 2002;307:70-75.
17. Zhang JH, Chung TD, Oldenburg KR: A simple statistical parameter for use in evaluation and validation of high throughput screening assays. J Biomol Screen 1999;4:67-73.
18. Zhai D, Ke N, Zhang H, Ladror U, Joseph M, Eichinger A, Godzik A, Ng SC, Reed JC: Characterization of the anti-apoptotic mechanism of Bcl-B. Biochem J 2003;376:229-236.
19. Zhai D, Jin C, Huang Z, Satterthwait AC, Reed JC: Differential regulation of Bax and Bak by anti-apoptotic Bcl-2 family proteins Bcl-B and Mcl-1. J Biol Chem 2008;283:9580-9586.
20. Krajewska M, Kitada S, Winter JN, Variakojis D, Lichtenstein A, Zhai D, Cuddy M, Huang X, Luciano F, Baker CH, Kim H, Shin E, Kennedy S, Olson AH, Badzio A, Jassem J, Meinhold-Heerlein I, Duffy MJ, Schimmer AD, Tsao M, Brown E, Sawyers A, Andreeff M, Mercola D, Krajewski S, Reed JC: Bcl-B expression in human epithelial and nonepithelial malignancies. Clin Cancer Res 2008;14:3011-3021.