An in vivo large-scale chemical screening platform using Drosophila for anti-cancer drug discovery.

PubWeight™: 1.01‹?› | Rank: Top 15%

🔗 View Article (PMC 3597034)

Published in Dis Model Mech on September 20, 2012

Authors

Lee F Willoughby1, Tanja Schlosser, Samuel A Manning, John P Parisot, Ian P Street, Helena E Richardson, Patrick O Humbert, Anthony M Brumby

Author Affiliations

1: Cell Cycle and Development Laboratory, Peter MacCallum Cancer Centre, 7 St Andrews Place, East Melbourne 3002, Victoria, Australia.

Associated clinical trials:

Personalized Cancer Therapy for Patients With Metastatic Medullary Thyroid Cancer | NCT02363647

Articles citing this

Drosophila melanogaster: a model and a tool to investigate malignancy and identify new therapeutics. Nat Rev Cancer (2013) 1.30

EAG2 potassium channel with evolutionarily conserved function as a brain tumor target. Nat Neurosci (2015) 0.95

Src42A modulates tumor invasion and cell death via Ben/dUev1a-mediated JNK activation in Drosophila. Cell Death Dis (2013) 0.88

RNAi screening in Drosophila cells and in vivo. Methods (2014) 0.87

Anti-cancer drug discovery: update and comparisons in yeast, Drosophila, and zebrafish. Curr Mol Pharmacol (2014) 0.82

Dihydroisoxazole inhibitors of Anopheles gambiae seminal transglutaminase AgTG3. Malar J (2014) 0.78

Drosophila as a Potential Model for Ocular Tumors. Ocul Oncol Pathol (2015) 0.77

Hippo signaling promotes JNK-dependent cell migration. Proc Natl Acad Sci U S A (2017) 0.76

Metabolic regulation via enzyme filamentation. Crit Rev Biochem Mol Biol (2016) 0.75

The interplay between obesity and cancer: a fly view. Dis Model Mech (2016) 0.75

Mechanism of Axonal Contractility in Embryonic Drosophila Motor Neurons In Vivo. Biophys J (2016) 0.75

Cooperation of the BTB-Zinc finger protein, Abrupt, with cytoskeletal regulators in Drosophila epithelial tumorigenesis. Biol Open (2015) 0.75

The translational relevance of Drosophila in drug discovery. EMBO Rep (2016) 0.75

An inverse small molecule screen to design a chemically defined medium supporting long-term growth of Drosophila cell lines. Mol Biosyst (2014) 0.75

Insulin and TOR signal in parallel through FOXO and S6K to promote epithelial wound healing. Nat Commun (2016) 0.75

The Lantibiotic NAI-107 Efficiently Rescues Drosophila melanogaster from Infection with Methicillin-Resistant Staphylococcus aureus USA300. Antimicrob Agents Chemother (2016) 0.75

Myc suppresses tumor invasion and cell migration by inhibiting JNK signaling. Oncogene (2017) 0.75

Natural variation in a single amino acid substitution underlies physiological responses to topoisomerase II poisons. PLoS Genet (2017) 0.75

Articles cited by this

A Simple Statistical Parameter for Use in Evaluation and Validation of High Throughput Screening Assays. J Biomol Screen (1999) 32.67

Glutamine addiction: a new therapeutic target in cancer. Trends Biochem Sci (2010) 6.30

Q's next: the diverse functions of glutamine in metabolism, cell biology and cancer. Oncogene (2009) 5.81

Pharmacological rescue of synaptic plasticity, courtship behavior, and mushroom body defects in a Drosophila model of fragile X syndrome. Neuron (2005) 4.11

A genetic screen in Drosophila for metastatic behavior. Science (2003) 4.09

scribble mutants cooperate with oncogenic Ras or Notch to cause neoplastic overgrowth in Drosophila. EMBO J (2003) 3.60

The pathways of glutamate and glutamine oxidation by tumor cell mitochondria. Role of mitochondrial NAD(P)+-dependent malic enzyme. J Biol Chem (1984) 2.82

Life extension in Drosophila by feeding a drug. Proc Natl Acad Sci U S A (2002) 2.57

Oncogenic Ras diverts a host TNF tumor suppressor activity into tumor promoter. Dev Cell (2010) 2.46

Chemical genetic discovery of targets and anti-targets for cancer polypharmacology. Nature (2012) 2.33

The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901. Bioorg Med Chem Lett (2008) 2.28

Human disease models in Drosophila melanogaster and the role of the fly in therapeutic drug discovery. Pharmacol Rev (2011) 2.25

Identification of small molecules rescuing fragile X syndrome phenotypes in Drosophila. Nat Chem Biol (2008) 2.04

Secreted peptide Dilp8 coordinates Drosophila tissue growth with developmental timing. Science (2012) 2.03

Using Drosophila melanogaster to map human cancer pathways. Nat Rev Cancer (2005) 2.03

Imaginal discs secrete insulin-like peptide 8 to mediate plasticity of growth and maturation. Science (2012) 1.87

An innate immune response of blood cells to tumors and tissue damage in Drosophila. Dis Model Mech (2008) 1.84

Metabolism and action of amino acid analog anti-cancer agents. Pharmacol Ther (1990) 1.79

ZD6474 suppresses oncogenic RET isoforms in a Drosophila model for type 2 multiple endocrine neoplasia syndromes and papillary thyroid carcinoma. Cancer Res (2005) 1.60

Loss of PI3K blocks cell-cycle progression in a Drosophila tumor model. Oncogene (2011) 1.56

Identification of combinatorial drug regimens for treatment of Huntington's disease using Drosophila. Proc Natl Acad Sci U S A (2005) 1.45

Development of a Drosophila seizure model for in vivo high-throughput drug screening. Eur J Neurosci (2006) 1.29

Glutamine analogs promote cytoophidium assembly in human and Drosophila cells. J Genet Genomics (2011) 1.22

Cytidine 5'-triphosphate synthetase as a target for inhibition by the antitumor agent 3-deazauridine. Cancer Res (1974) 1.01

Acivicin in 1985. Adv Enzyme Regul (1985) 0.99

Increased CTP synthetase activity in cancer cells. Nature (1978) 0.98

Increased cytidine 5'-triphosphate synthetase activity in rat and human tumors. Cancer Res (1980) 0.97

Combinatorial effect of maytansinol and radiation in Drosophila and human cancer cells. Dis Model Mech (2011) 0.88

Chemical genetics and drug screening in Drosophila cancer models. J Genet Genomics (2011) 0.86

L-[alphaS, 5S]-alpha-amino-3-chloro-4,5-dihydro-5-isoxazoleacetic acid (NSC-163501): a new amino acid antibiotic with the properties of an antagonist of L-glutamine. Cancer Chemother Rep (1976) 0.83

Cytidine triphosphate synthetase activity in lymphoproliferative disorders. Cancer Res (1983) 0.81

Drosophila-based in vivo assay for the validation of inhibitors of the epidermal growth factor receptor/Ras pathway. J Biosci (2008) 0.81

Rapid in vivo inactivation by acivicin of CTP synthetase, carbamoyl-phosphate synthetase II, and amidophosphoribosyltransferase in hepatoma. Life Sci (1982) 0.80

Insecticide detoxification indicator strains as tools for enhancing chemical discovery screens. Pest Manag Sci (2011) 0.80

Oral idarubicin--an anthracycline derivative with unique properties. Ann Hematol (1993) 0.78

Articles by these authors

scribble mutants cooperate with oncogenic Ras or Notch to cause neoplastic overgrowth in Drosophila. EMBO J (2003) 3.60

Lgl, aPKC, and Crumbs regulate the Salvador/Warts/Hippo pathway through two distinct mechanisms. Curr Biol (2010) 2.97

A network of PDZ-containing proteins regulates T cell polarity and morphology during migration and immunological synapse formation. Immunity (2005) 2.97

SCRIB expression is deregulated in human prostate cancer, and its deficiency in mice promotes prostate neoplasia. J Clin Invest (2011) 2.60

Upstream regulation of the hippo size control pathway. Curr Biol (2010) 2.09

Using Drosophila melanogaster to map human cancer pathways. Nat Rev Cancer (2005) 2.03

Structure-guided design of a selective BCL-X(L) inhibitor. Nat Chem Biol (2013) 1.68

Multiscale modeling of form and function. Science (2009) 1.60

Sequence artefacts in a prospective series of formalin-fixed tumours tested for mutations in hotspot regions by massively parallel sequencing. BMC Med Genomics (2014) 1.53

The Salvador/Warts/Hippo pathway controls regenerative tissue growth in Drosophila melanogaster. Dev Biol (2010) 1.50

Asymmetric cell division of T cells upon antigen presentation uses multiple conserved mechanisms. J Immunol (2010) 1.46

Cell-intrinsic requirement for pRb in erythropoiesis. Blood (2004) 1.43

Polarity regulators and the control of epithelial architecture, cell migration, and tumorigenesis. Int Rev Cytol (2007) 1.40

APC/CFzr/Cdh1 promotes cell cycle progression during the Drosophila endocycle. Development (2008) 1.35

Abnormalities in cell proliferation and apico-basal cell polarity are separable in Drosophila lgl mutant clones in the developing eye. Dev Biol (2007) 1.33

Transcriptional output of the Salvador/warts/hippo pathway is controlled in distinct fashions in Drosophila melanogaster and mammalian cell lines. Cancer Res (2009) 1.25

Epidermal wound repair is regulated by the planar cell polarity signaling pathway. Dev Cell (2010) 1.25

Cell polarity in motion: redefining mammary tissue organization through EMT and cell polarity transitions. J Mammary Gland Biol Neoplasia (2010) 1.17

The lethal giant larvae tumour suppressor mutation requires dMyc oncoprotein to promote clonal malignancy. BMC Biol (2010) 1.17

Loss of the Drosophila cell polarity regulator Scribbled promotes epithelial tissue overgrowth and cooperation with oncogenic Ras-Raf through impaired Hippo pathway signaling. BMC Dev Biol (2011) 1.15

hScrib is a functional homologue of the Drosophila tumour suppressor Scribble. Oncogene (2003) 1.15

EKLF/KLF1 controls cell cycle entry via direct regulation of E2f2. J Biol Chem (2009) 1.13

Scribble mutants promote aPKC and JNK-dependent epithelial neoplasia independently of Crumbs. BMC Biol (2009) 1.09

The Scribble-Dlg-Lgl polarity module in development and cancer: from flies to man. Essays Biochem (2012) 1.09

Tumor suppressor scribble regulates assembly of tight junctions in the intestinal epithelium. Am J Pathol (2009) 1.07

Identification of novel Ras-cooperating oncogenes in Drosophila melanogaster: a RhoGEF/Rho-family/JNK pathway is a central driver of tumorigenesis. Genetics (2011) 1.06

Vimentin regulates scribble activity by protecting it from proteasomal degradation. Mol Biol Cell (2009) 1.04

Growth inhibition of Candida species and Aspergillus fumigatus by statins. FEMS Microbiol Lett (2006) 1.03

Scribble interacts with beta-catenin to localize synaptic vesicles to synapses. Mol Biol Cell (2009) 1.03

Scribble regulates an EMT polarity pathway through modulation of MAPK-ERK signaling to mediate junction formation. J Cell Sci (2013) 1.02

Homeodomain-interacting protein kinase regulates Hippo pathway-dependent tissue growth. Curr Biol (2012) 1.00

Discovery of 2-iminobenzimidazoles as a new class of trypanothione reductase inhibitor by high-throughput screening. Bioorg Med Chem Lett (2006) 0.97

Regulation of asymmetric cell division and polarity by Scribble is not required for humoral immunity. Nat Commun (2013) 0.95

Hfp inhibits Drosophila myc transcription and cell growth in a TFIIH/Hay-dependent manner. Development (2010) 0.95

Quinazoline sulfonamides as dual binders of the proteins B-cell lymphoma 2 and B-cell lymphoma extra long with potent proapoptotic cell-based activity. J Med Chem (2011) 0.95

Trypanothione reductase high-throughput screening campaign identifies novel classes of inhibitors with antiparasitic activity. Antimicrob Agents Chemother (2009) 0.93

Lgl, the SWH pathway and tumorigenesis: It's a matter of context & competition! Cell Cycle (2010) 0.92

Lgl/aPKC and Crb regulate the Salvador/Warts/Hippo pathway. Fly (Austin) (2010) 0.92

The Brm-HDAC3-Erm repressor complex suppresses dedifferentiation in Drosophila type II neuroblast lineages. Elife (2014) 0.90

Increasing intracellular bioavailable copper selectively targets prostate cancer cells. ACS Chem Biol (2013) 0.90

RNAi-mediated knock-down of arylamine N-acetyltransferase-1 expression induces E-cadherin up-regulation and cell-cell contact growth inhibition. PLoS One (2011) 0.90

Characterization of in vivo Dlg1 deletion on T cell development and function. PLoS One (2012) 0.88

Discovery of potent and selective benzothiazole hydrazone inhibitors of Bcl-XL. J Med Chem (2013) 0.86

Dihydroquinazolines as a novel class of Trypanosoma brucei trypanothione reductase inhibitors: discovery, synthesis, and characterization of their binding mode by protein crystallography. J Med Chem (2011) 0.85

Inhibitors of Leishmania GDP-mannose pyrophosphorylase identified by high-throughput screening of small-molecule chemical library. Antimicrob Agents Chemother (2010) 0.85

In Drosophila, RhoGEF2 cooperates with activated Ras in tumorigenesis through a pathway involving Rho1-Rok-Myosin-II and JNK signalling. Dis Model Mech (2013) 0.85

Identification of 5,6-substituted 4-aminothieno[2,3-d]pyrimidines as LIMK1 inhibitors. Bioorg Med Chem Lett (2011) 0.84

An efficient high-throughput screening method for MYST family acetyltransferases, a new class of epigenetic drug targets. J Biomol Screen (2011) 0.84

When cell cycle meets development. Development (2011) 0.83

The BTB-zinc finger transcription factor abrupt acts as an epithelial oncogene in Drosophila melanogaster through maintaining a progenitor-like cell state. PLoS Genet (2013) 0.83

All known in vivo functions of the Oct-2 transcription factor require the C-terminal protein domain. J Immunol (2004) 0.82

New tricks for old dogs: unexpected roles for cell cycle regulators revealed using animal models. Curr Opin Cell Biol (2004) 0.81

Geminin and Brahma act antagonistically to regulate EGFR-Ras-MAPK signaling in Drosophila. Dev Biol (2010) 0.81

Death takes a holiday--non-apoptotic role for caspases in cell migration and invasion. EMBO Rep (2013) 0.79

Localization, not important in all tumor-suppressing properties: a lesson learnt from scribble. Cells Tissues Organs (2013) 0.79

De-novo designed library of benzoylureas as inhibitors of BCL-XL: synthesis, structural and biochemical characterization. J Med Chem (2014) 0.78

Characterization of the novel broad-spectrum kinase inhibitor CTx-0294885 as an affinity reagent for mass spectrometry-based kinome profiling. J Proteome Res (2013) 0.78

Wingless signaling directly regulates cyclin E expression in proliferating embryonic PNS precursor cells. Mech Dev (2008) 0.77

Loss of APKC expression independently predicts tumor recurrence in superficial bladder cancers. Urol Oncol (2011) 0.76

Synthesis of conformationally constrained benzoylureas as BH3-mimetics. Org Biomol Chem (2012) 0.76

Regulation of Notch signaling and endocytosis by the Lgl neoplastic tumor suppressor. Cell Cycle (2015) 0.75

Making brundlefly, one gene at a time. Cell Res (2009) 0.75