A β-lactamase reporter assay for monitoring the activation of the smoothened pathway

Assay and Drug Development Technologies

Volumn 5, Issue 6, 2007, Pages 785-792

  Osak, Bella ^a   Fitzgerald, Laura R ^a  

^a PFIZER INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

BETA LACTAMASE; SMOOTHENED PROTEIN; SONIC HEDGEHOG PROTEIN;

ANIMAL CELL; ARTICLE; ASSAY; CELL DIFFERENTIATION; CELL GROWTH; CONTROLLED STUDY; EMBRYO; EMBRYO DEVELOPMENT; FLUORESCENCE ACTIVATED CELL SORTING; HIGH THROUGHPUT SCREENING; MOUSE; NONHUMAN;

ANIMALS; BETA-LACTAMASES; CELL COUNT; CELL LINE; CLONING, MOLECULAR; DATA INTERPRETATION, STATISTICAL; DIMETHYL SULFOXIDE; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG EVALUATION, PRECLINICAL; ENZYME ACTIVATION; FLOW CYTOMETRY; GENES, REPORTER; INDICATORS AND REAGENTS; MICE; PLASMIDS; RECEPTORS, G-PROTEIN-COUPLED; SIGNAL TRANSDUCTION; TRANSFECTION;

EID: 38049055891     PISSN: 1540658X     EISSN: None     Source Type: Journal    
DOI: 10.1089/adt.2007.088     Document Type: Article

References (30)

1. Ingham PW, McMahon AP: Hedgehog signaling in animal development: paradigms and principles. Genes Dev 2001;14:3059-3087.
2. Xie J, Murone M, Luoh S-M, Ryan A, Gu Q, Zhang C, et al.: Activating Smoothened mutations in sporadic basal-cell carcinoma. Nature 1998;391:90-92
3. Beachy PA, Karhadkar SS, Berman DM: Tissue repair and stem cell renewal in carcinogenesis. Nature 2004;432:324-331.
4. Murone M, Rosenthal A, de Sauvage FJ: Sonic Hedgehog signaling by the Patched-Smoothened receptor complex. Curr Biol 1999;9:76-84.
5. Chen W, Ren XR, Nelson CD, Barak LS, Chen JK, Beachy PA, et al.: Activity-dependent internalization of Smoothened mediated by β-arrestin 2 and GRK2. Science 2004;306:2257-2260.
6. Keeler RF, Binns W: Teratogenic compounds of Veratrum californicum (Durand). V. Comparison of cyclopean effects of steroidal alkaloids from the plant and structurally related compounds from other sources. Teratology 1968;11:5-10.
7. Chen JK, Taipale J, Cooper MK, Beachy PA: Inhibition of Hh signaling by direct binding of cyclopamine to Smoothened. Genes Dev 2002;16:2743-2748.
8. Frank-Kamenetsky M, Zhang XM, Bottega S, Guicherit O, Wichterle H, Dudek H, et al.: Small molecule modulators of Hedghog signaling: identification and characterization of Smo agonists and antagonists. J Biol 2002;1:10.1-10.19.
9. Pepinsky RB, Shapiro RI, Want S, Chakraborty A, Gill A, Lepage DJ, et al.: Long-acting forms of Sonic Hedgehog with improved pharmacokinetic and pharmacodynamic properties are efficacious in a nerve injury model. J Pharm Sci 2002;91:371-387.
10. Tsuboi K, Shults CW: Intrastriatal injection of sonic Hedgehog reduces behavioural impairment in a rat model of Parkinson's disease. Exp Neurol 2002;173:95-104.
11. Taipale J, Chen JK, Kooper MK, Wang B, Mann K, Millenkivic L, et al.: Effects of oncogenic mutations in Smoothened and Patched can be reversed by cyclopamine. Nature 2000;406:1005-1009.
12. Williams JA, Guicherit OM, Zaharian BI, Xu Y, Hai L, Wichterle H, et al.: Identification of small molecule inhibitor of the Hedgehog signaling pathway. Effect on basal cell carcinoma-like lesions. Proc Natl Acad Sci U S A 2003;100:4616-4621.
13. Inglese J, Shamu CE, Guy RK: Reporting data from high-throughput screening of small-molecule libraries. Nat Chem Biol 2007;3:438-441.
14. Kiselyov AS: Targeting the hedgehog signaling pathway with small molecules. Anticancer Agents Med Chem 2006;6:445-449.
15. Klug A, Schwabe JW: Protein motifs 5. Zinc fingers. FASEB J 1995;9:597-604.
16. Vortkamp A, Gessler M, Grzeschik KH: Identification of optimized target sequences for the GLI3 zinc finger protein. DNA Cell Biol 1995;14:629-634.
17. Yoon JW, Liu CZ, Yang JT, Swart R, Iannaccone P, Walterhouse D: GLI activates transcription through a herpes simplex viral protein 16-like activation domain. J Biol Chem 1998;273:3496-3501.
18. Mizugishi K, Aruga J, Nakata K, Mikoshiba K: Molecular properties of zinc proteins as transcriptional regulators and their relationship to GLI proteins. J Biol Chem 2001;276:2180-2188.
19. Zlokarnik G, Negulescu PA, Knapp TE, Mere L, Burres N, Feng L, et al.: Quantitation of transcription and clonal selection of single living cells with β-lactamase as reporter. Science1998;279:84-88.
20. Chen JK, Taipale J, Young KE, Maiti T, Beachy PA: Small molecule modulation of Smo activity. Proc Natl Acad Sci U S A 2002;99:14071-14076.
21. Zhang JH, Chung TDY, Oldenberg KR: A simple statistical parameter for use in evaluation and validation of high throughput screening assays. J Biomol Screen 1999;4:67-73.
22. Bailey EC, Milenkovic L, Scott MP, Collawn JF, Johnson RL: Several PATCHED1 missense mutations display activity in patched1-deficient fibroblasts. J Biol Chem 2002;277:33632-33640.
23. Taipale J, Copper MK, Maiti T, Beachy PA: Patched acts catalytically to suppress the activity of Smoothened. Nature 2002;418:892-897.
24. Whitney M, Stack JH, Darke PL, Zheng W, Terzo J, Ingelese J, et al.: A collaborative screening program for the discovery of inhibitors of HCV NS2/3 cis-cleaving protease activity. J Biomol Screen 2002;7:149-154.
25. Kunapuli P, Ransom R, Murphy KL, Pettibone D, Kerby J, Grimwood S, et al.: Development of an intact cell reporter gene β-lactamase assay for G protein-coupled receptors for high-throughput screening. Anal Biochem 2003;314:16-29.
26. Zuck P, Murray EM, Stec E, Brobler JA, Simon AJ, Strulovici B, et al.: A cell-based β-lactamase reporter gene assay for the identification of inhibitors of hepatitis C virus replication. Anal Biochem 2004;334:344-355.
27. Hobson JP, Shihui L, Rønø B, Leppla SH, Bugge TH: Imaging specific cell-surface proteolytic activity in single living cells. Nat Methods 2006;3:259-261.
28. Peekhaus NT, Ferrer M, Chang T, Kornienko O, Schneeweis JE, Smith TS, et al.: A β-lactamase-dependent Gal4-estrogen receptor β transactivation assay for the ultra-high throughput screening of estrogen receptor β agonists in 3456 well format. Assay Drug Dev Technol 2003;1:789-800.
29. Chin J, Adams AD, Bouffard A, Green A, Lacson RG, Smith T, et al.: Miniaturization of cell-based β-lactamase-dependent FRET assays to ultra-high throughput formats to identify agonists of human liver X receptors. Assay Drug Dev Technol 2003;1:777-787.
30. Oosterom J, van Doornmalen EJP, Lobregt S, Blomehröhr M, Zaman GJR: High-throughput screening using β-lactamase reporter-gene technology for identification of low-molecular-weight antagonists of the human gonadotropin releasing hormone receptor. Assay Drug Dev Technol 2005;3:143-154.