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Cell-based apoptosis assays in oncology drug discovery

, PhD & , PhD
Pages 583-596 | Published online: 21 May 2010

Bibliography

  • Schreiber SL. Chemical genetics resulting from a passion for synthetic organic chemistry. Bioorg Med Chem 1998;6:1127-52
  • Spring DR. Chemical genetics to chemical genomics: small molecules offer big insights. Chem Soc Rev 2005;34:472-82
  • Shim JS, Kwon HJ. Chemical genetics for therapeutic target mining. Expert Opin Ther Targets 2004;8:653-61
  • Nicholson DW, Thornberry NA. Apoptosis. Life and death decisions. Science 2003;299:214-15
  • An WF, Tolliday NJ. Introduction: cell-based assays for high throughput screening. Methods Mol Biol 2009;486:1-12
  • Schriemer DC, Kemmer D, Roberge M. Design of phenotypic screens for bioactive chemicals and identification of their targets by genetic and proteomic approaches. Comb Chem High Throughput Screen 2008;11:610-16
  • Landry Y, Gies JP. Drugs and their molecular targets: an updated overview. Fundam Clin Pharmacol 2008;22:1-18
  • Overington JP, Al-Lazikani B, Hopkins AL. How many drug targets are there? Nat Rev Drug Discov 2006;5:993-6
  • Berger SL, Kouzarides T, Shiekhattar R, Shilatifard A. An operational definition of epigenetics. Genes Dev 2009;23:781-3
  • Jana S, Paliwal J. Apoptosis: potential therapeutic targets for new drug discovery. Curr Med Chem 2007;14:2369-79
  • Reed JC. Drug insight: cancer therapy strategies based on restoration of endogenous cell death mechanisms. Nat Clin Pract Oncol 2006;3:388-98
  • Mehlen P, Puisieux A. Metastasis: a question of life or death. Nat Rev Cancer 2006;6:449-58
  • Reed JC. Apoptosis-based therapies. Nat Rev Drug Discov 2002;1:111-21
  • Reed JC, Tomaselli KJ. Drug discovery opportunities from apoptosis research. Curr Opin Biotechnol 2000;11:586-92
  • Kim R, Tanabe K, Uchida Y, Current status of the molecular mechanisms of anticancer drug-induced apoptosis. The contribution of molecular-level analysis to cancer chemotherapy. Cancer Chemother Pharmacol 2002;50:343-52
  • Kasibhatla S, Tseng B. Why target apoptosis in cancer treatment? Mol Cancer Ther 2003;2:573-80
  • Leung D, Abbenante G, Fairlie DP. Protease inhibitors: current status and future prospects. J Med Chem 2000;43:305-41
  • Thornberry NA. Caspases: key mediators of apoptosis. Chem Biol 1998;5:R97-R103
  • Hunter AM, LaCasse EC, Korneluk RG. The inhibitors of apoptosis (IAPs) as cancer targets. Apoptosis 2007;12:1543-68
  • Evan GI, Vousden KH. Proliferation, cell cycle and apoptosis in cancer. Nature 2001;411:342-8
  • Hanahan D, Weinberg RA. The hallmarks of cancer. Cell 2000;100:57-70
  • Reed JC. Dysregulation of apoptosis in cancer. J Clin Oncol 1999;17:2941-53
  • Cai SX, Drewe J, Kasibhatla S. A chemical genetics approach for the discovery of apoptosis inducers: from phenotypic cell based HTS assay and structure–activity relationship studies, to identification of potential anticancer agents and molecular targets. Curr Med Chem 2006;13:2627-44
  • Cai SX, Zhang HZ, Guastella J, Design and synthesis of rhodamine 110 derivative and caspase-3 substrate for enzyme and cell-based fluorescent assay. Bioorg Med Chem Lett 2001;11:39-42
  • Kolenko VM, Uzzo RG, Bukowski R, Finke JH. Caspase-dependent and -independent death pathways in cancer therapy. Apoptosis 2000;5:17-20
  • Hopkins AL, Groom CR. The druggable genome. Nat Rev Drug Discov 2002;1:727-30
  • Smukste I, Stockwell BR. Advances in chemical genetics. Annu Rev Genomics Hum Genet 2005;6:261-86
  • Sirisoma N, Pervin A, Zhang H, Discovery of N-(4-methoxyphenyl)-N, 2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration. J Med Chem 2009;52:2341-51
  • Cai SX, Drewe J, Kemnitzer W. Discovery of 4-aryl-4H-chromenes as potent apoptosis inducers using a cell- and caspase-based Anti-cancer Screening Apoptosis Program (ASAP): SAR studies and the identification of novel vascular disrupting agents. Anticancer Agents Med Chem 2009;9:437-56
  • Zhang H-Z, Kasibhatla S, Wang Y, Discovery, characterization and SAR of gambogic acid as a potent apoptosis inducer by a HTS assay. Bioorg Med Chem 2004;12:309-17
  • Kasibhatla S, Jessen K, Maliartchouk S, A role for transferrin receptor in triggering apoptosis when targeted with gambogic acid. Proc Natl Acad Sci USA 2005;102:12095-100
  • Zhang H-Z, Kasibhatla S, Kuemmerle J, Discovery and structure–activity relationship of 3-aryl-5-aryl-1,2,4-oxadiazoles as a new series of apoptosis inducers and potential anticancer agents. J Med Chem 2005;48:5215-23
  • Jessen K, English N, Wang J, The discovery and mechanism of action of novel tumor-selective and apoptosis-inducing 3,5-diaryl-1,2,4-oxadiazole series using a chemical genetics approach. Mol Cancer Ther 2005;4:761-71
  • Schreiber SL. Small molecules: the missing link in the central dogma. Nat Chem Biol 2005;1:64-6
  • Dobson CM. Chemical space and biology. Nature 2004;432:824-8
  • Vieth M, Erickson J, Wang J, Kinase inhibitor data modeling and de novo inhibitor design with fragment approaches. J Med Chem 2009;52:6456-66
  • Xie HZ, Li LL, Ren JX, Pharmacophore modeling study based on known spleen tyrosine kinase inhibitors together with virtual screening for identifying novel inhibitors. Bioorg Med Chem Lett 2009;19:1944-9
  • Ferrara P, Jacoby EJ. Evaluation of the utility of homology models in high throughput docking. Mol Model 2007;13:897-905
  • 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
  • Lien EJ, Wang PH. Lipophilicity, molecular weight, and drug action: reexamination of parabolic and bilinear models. J Pharm Sci 1980;69:648-50
  • Di L, Kerns EH. Profiling drug-like properties in discovery research. Curr Opin Chem Biol 2003;7:402-8
  • Leeson PD, Springthorpe B. The influence of drug-like concepts on decision-making in medicinal chemistry. Nat Rev Drug Discov 2007;6:881-90
  • Stockwell BR. Frontiers in chemical genetics. Trends Biotechnol 2000;18:449-55
  • Gassner NC, Tamble CM, Bock JE, Accelerating the discovery of biologically active small molecules using a high-throughput yeast halo assay. J Nat Prod 2007;70:383-90
  • Lazo JS, Brady LS, Dingledine R. Building a pharmacological lexicon: small molecule discovery in academia. Mol Pharmacol 2007;72:1-7
  • Brenk R, Schipani A, James D, Lessons learnt from assembling screening libraries for drug discovery for neglected diseases. ChemMedChem 2008;3:435-44
  • Algorithmic Procedures for Compound Selection for the MLSMR Collection – NIH Molecular Libraries Program. Available from: http://mli.nih.gov/mli/compound-repository/mlsmr-compounds
  • NIH Molecular Libraries Program. Available from: https://mli.nih.gov/mli/
  • Murray CW, Rees DC. The rise of fragment-based drug discovery. Nat Chem 2009;1:187-92
  • Bartoli S, Fincham CI, Fattori D. Fragment-based drug design: combining philosophy with technology. Curr Opin Drug Discov Devel 2007;10:422-9
  • Archer JR. History, evolution, and trends in compound management for high throughput screening. Assay Drug Dev Technol 2004;2:675-81
  • Yasgar A, Shinn P, Jadhav A, Compound management for quantitative high-throughput screening. JALA Charlottesv Va 2008;13:79-89
  • Thornberry NA, Rano TA, Peterson EP, A combinatorial approach defines specificities of members of the caspase family and granzyme B. Functional relationships established for key mediators of apoptosis. J Biol Chem 1997;272:17907-11
  • Stennicke HR, Salvesen GS. Biochemical characteristics of caspases-3, -6, -7, and -8. J Biol Chem 1997;272:25719-23
  • Leytus SP, Patterson WL, Mangel WF. New class of sensitive and selective fluorogenic substrates for serine proteinases. Amino acid and dipeptide derivatives of rhodamine. Biochem J 1983;215:253-60
  • Liu J, Bhalgat M, Zhang C, Fluorescent molecular probes V: a sensitive caspase-3 substrate for fluorometric assays. Bioorg Med Chem Lett 1999;9:3231-6
  • Zhang HZ, Kasibhatla S, Guastella J, N-Ac-DEVD-N'-(Polyfluorobenzoyl)-R110: novel cell-permeable fluorogenic caspase substrates for the detection of caspase activity and apoptosis. Bioconjug Chem 2003;14:458-63
  • McGovern SL, Caselli E, Grigorieff N, Shoichet BK. A common mechanism underlying promiscuous inhibitors from virtual and high-throughput screening. J Med Chem 2002;45:1712-22
  • Claassen G, Vaillancourt MT, Sirisoma N, Identification of CCT/TCP-1 as molecular target for small-molecule tumor inhibitor targeting Myc pathway. Abstract #5369 AACR Meeting Denver 2009
  • Claassen G, Brin E, Crogan-Grundy C, Selective activation of apoptosis by a novel set of 4-aryl-3-(3-aryl-1-oxo-2-propenyl)-2(1H)-quinolinones through a Myc-dependent pathway. Cancer Lett 2009;18:243-9
  • Kemnitzer W, Drewe J, Jiang S, Discovery of 4-aryl-4H-chromenes as new series of apoptosis inducers using a cell- and caspase-based highthroughput screening assay. 3. Structure–activity relationships of fused rings at the 7,8-positions. J Med Chem 2007;50:2858-64
  • Sirisoma N, Kasibhatla S, Nguyen B, Discovery of substituted 4-anilino-2-(2-pyridyl)pyrimidines as a new series of apoptosis inducers using a cell- and caspase-based high throughput screening assay. Part 1: structure–activity relationships of the 4-anilino group. Bioorg Med Chem 2006;14:7761-73
  • Kemnitzer W, Kuemmerle J, Jiang S, Discovery of 1-benzoyl-3-cyanopyrrolo[1,2-a]quinolines as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay. Part 1: structure–activity relationships of the 1- and 3-positions. Bioorg Med Chem Lett 2008;18:6259-64
  • Perez Fidalgo JA, Roda D, Rosello S, Aurora kinase inhibitors: a new class of drugs targeting the regulatory mitotic system. Clin Transl Oncol 2009;11:787-98
  • Chopra P, Sethi G, Dastidar SG, Ray A. Polo-like kinase inhibitors: an emerging opportunity for cancer therapeutics. Expert Opin Investig Drugs 2010;19:27-43
  • Burdine L, Kodadek T. Target identification in chemical genetics: the (often) missing link. Chem Biol 2004;11:593-7
  • Tochtrop GP, King RW. Target identification strategies in chemical genetics. Comb Chem High Throughput Screen 2004;7:677-88
  • Colca JR, Harrigan GG. Photo-affinity labeling strategies in identifying the protein ligands of bioactive small molecules: examples of targeted synthesis of drug analog photoprobes. Comb Chem High Throughput Screen 2004;7:699-704
  • Khersonsky SM, Jung DW, Kang TW, Facilitated forward chemical genetics using a tagged triazine library and zebrafish embryo screening. J Am Chem Soc 2003;125:11804-5
  • Diaz E, Pfeffer SR. TIP47: a cargo selection device for mannose 6-phosphate receptor trafficking. Cell 1998;93:433-43
  • Than GN, Turoczy T, Sumegi B, Overexpression of placental tissue protein 17b/TIP47 in cervical dysplasias and cervical carcinoma. Anticancer Res 2001;21:639-42
  • Duffner JL, Clemons PA, Koehler AN. A pipeline for ligand discovery using small-molecule microarrays. Curr Opin Chem Biol 2007;11:74-82
  • Bredel M, Jacoby E. Chemogenomics: an emerging strategy for rapid target and drug discovery. Nat Rev Genet 2004;5:262-75
  • Kim JK, Diehl JA. Nuclear cyclin D1: an oncogenic driver in human cancer. J Cell Physiol 2009;220:292-6
  • Liao DJ, Thakur A, Wu J, Perspectives on c-Myc, Cyclin D1, and their interaction in cancer formation, progression, and response to chemotherapy. Crit Rev Oncog 2007;13:93-158
  • Knight ZA, Shokat KM. Chemical genetics: where genetics and pharmacology meet. Cell 2007;128:425-30
  • Adrian FJ, Ding Q, Sim T, Allosteric inhibitors of Bcr-abl-dependent cell proliferation. Nat Chem Biol 2006;2:95-102
  • Ohren JF, Chen H, Pavlovsky A, Structures of human MAP kinase kinase 1 (MEK1) and MEK2 describe novel noncompetitive kinase inhibition. Nat Struct Mol Biol 2004;11:1192-7
  • Engel M, Hindie V, Lopez-Garcia LA, Allosteric activation of the protein kinase PDK1 with low molecular weight compounds. EMBO J 2006;25:5469-80
  • Hindie V, Stroba A, Zhang H, Structure and allosteric effects of low-molecular-weight activators on the protein kinase PDK1. Nat Chem Biol 2009;5:758-64
  • Barnett SF, Defeo-Jones D, Fu S, Identification and characterization of pleckstrin-homology-domain-dependent and isoenzyme-specific Akt inhibitors. Biochem J 2005;15:399-408
  • Agnew WS, Levinson SR, Brabson JS, Raftery MA. Purification of the tetrodotoxin-binding component associated with the voltage-sensitive sodium channel from Electrophorus electricus electroplax membranes. Proc Natl Acad Sci USA 1978;75:2606-10

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