A high throughput screen identifies nefopam as targeting cell proliferation in β-catenin driven neoplastic and reactive fibroproliferative disorders

PLoS ONE

Volumn 7, Issue 5, 2012, Pages

  Poon, Raymond ^a   Hong, Helen ^a   Wei, Xin ^b   Pan, James ^c   Alman, Benjamin A ^a,c  

^a HOSPITAL FOR SICK CHILDREN   (Canada)

^b PRINCESS MARGARET HOSPITAL   (Canada)

^c UNIVERSITY OF TORONTO   (Canada)

Author keywords

[No Author keywords available]

Indexed keywords

BETA CATENIN; NEFOPAM; ANTINEOPLASTIC AGENT;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTIPROLIFERATIVE ACTIVITY; APOPTOSIS; ARTICLE; CELL VIABILITY; CONTROLLED STUDY; DESMOID TUMOR; DRUG SCREENING; FEMALE; FIBROBLAST; FIBROMATOSIS; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; HUMAN TISSUE; HYPERTROPHIC SCAR; IN VITRO STUDY; IN VIVO STUDY; MALE; MESENCHYME CELL; MOUSE; NONHUMAN; SKIN INJURY; TUMOR CELL; TUMOR REGRESSION; WOUND HEALING; ANIMAL; CELL PROLIFERATION; CELL SURVIVAL; CYTOLOGY; DRUG EFFECT; INJURY; MESODERM; METABOLISM; PATHOLOGY; PHENOTYPE; SKIN; TUMOR CELL LINE;

MUS;

ANIMALS; ANTINEOPLASTIC AGENTS; BETA CATENIN; CELL LINE, TUMOR; CELL PROLIFERATION; CELL SURVIVAL; CICATRIX, HYPERTROPHIC; DRUG EVALUATION, PRECLINICAL; FEMALE; FIBROBLASTS; FIBROMATOSIS, AGGRESSIVE; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; MALE; MESODERM; MICE; NEFOPAM; PHENOTYPE; SKIN; WOUND HEALING;

EID: 84861638965     PISSN: None     EISSN: 19326203     Source Type: Journal    
DOI: 10.1371/journal.pone.0037940     Document Type: Article

References (51)

1. Alman BA, Li C, Pajerski ME, Diaz-Cano S, Wolfe HJ, (1997) Increased beta-catenin protein and somatic APC mutations in sporadic aggressive fibromatoses (desmoid tumors). Am J Pathol 151: 329-334.
2. Cheon SS, Wei Q, Gurung A, Youn A, Bright T, et al. (2006) Beta-catenin regulates wound size and mediates the effect of TGF-beta in cutaneous healing. FASEB J 20: 692-701.
3. Chen Y, Whetstone HC, Lin AC, Nadesan P, Wei Q, et al. (2007) Beta-Catenin Signaling Plays a Disparate Role in Different Phases of Fracture Repair: Implications for Therapy to Improve Bone Healing. PLoS Medicine 4: e249.
4. Lam AP, Gottardi CJ, (2011) beta-catenin signaling: a novel mediator of fibrosis and potential therapeutic target. Curr Opin Rheumatol 23: 562-567.
5. Clark RA, (1993) Biology of dermal wound repair. Dermatol Clin 11: 647-666.
6. Singer AJ, Clark RA, (1999) Cutaneous wound healing. N Engl J Med 341: 738-746.
7. Chen Y, Whetstone HC, Youn A, Nadesan P, Chow EC, et al. (2007) Beta-catenin signaling pathway is crucial for bone morphogenetic protein 2 to induce new bone formation. J Biol Chem 282: 526-533.
8. Cheon S, Poon R, Yu C, Khoury M, Shenker R, et al. (2005) Prolonged beta-catenin stabilization and tcf-dependent transcriptional activation in hyperplastic cutaneous wounds. Lab Invest 85: 416-425.
9. Cheon SS, Cheah AY, Turley S, Nadesan P, Poon R, et al. (2002) beta-Catenin stabilization dysregulates mesenchymal cell proliferation, motility, and invasiveness and causes aggressive fibromatosis and hyperplastic cutaneous wounds. Proc Natl Acad Sci U S A 99: 6973-6978.
10. Cheon SS, Nadesan P, Poon R, Alman BA, (2004) Growth factors regulate beta-catenin-mediated TCF-dependent transcriptional activation in fibroblasts during the proliferative phase of wound healing. Exp Cell Res 293: 267-274.
11. Bock O, Schmid-Ott G, Malewski P, Mrowietz U, (2006) Quality of life of patients with keloid and hypertrophic scarring. Arch Dermatol Res 297: 433-438.
12. Clark RA, (1996) U.S. markets for wound management products. In: Clark RA, editors. The molecular and cellular biology of wound repair new york plenium press pp. 3-20.
13. Alman BA, Goldberg MJ, Naber SP, Galanopoulous T, Antoniades HN, et al. (1992) Aggressive fibromatosis. J Pediatr Orthop 12: 1-10.
14. Couture J, Mitri A, Lagace R, Smits R, Berk T, et al. (2000) A germline mutation at the extreme 3′ end of the APC gene results in a severe desmoid phenotype and is associated with overexpression of beta-catenin in the desmoid tumor. Clin Genet 57: 205-212.
15. Tejpar S, Nollet F, Li C, Wunder JS, Michils G, et al. (1999) Predominance of beta-catenin mutations and beta-catenin dysregulation in sporadic aggressive fibromatosis (desmoid tumor). Oncogene 18: 6615-6620.
16. Yang JC, Chang AE, Baker AR, Sindelar WF, Danforth DN, et al. (1998) Randomized prospective study of the benefit of adjuvant radiation therapy in the treatment of soft tissue sarcomas of the extremity. J Clin Oncol 16: 197-203.
17. Tejpar S, Li C, Yu C, Poon R, Denys H, et al. (2001) Tcf-3 expression and beta-catenin mediated transcriptional activation in aggressive fibromatosis (desmoid tumour). Br J Cancer 85: 98-101.
18. Bowley E, O'Gorman DB, Gan BS, (2007) Beta-catenin signaling in fibroproliferative disease. J Surg Res 138: 141-150.
19. Weisman JL, Liou AP, Shelat AA, Cohen FE, Guy RK, et al. (2006) Searching for new antimalarial therapeutics amongst known drugs. Chem Biol Drug Des 67: 409-416.
20. Peacock CD, Wang Q, Gesell GS, Corcoran-Schwartz IM, Jones E, et al. (2007) Hedgehog signaling maintains a tumor stem cell compartment in multiple myeloma. Proc Natl Acad Sci U S A 104: 4048-4053.
21. Heel RC, Brogden RN, Pakes GE, Speight TM, Avery GS, (1980) Nefopam: a review of its pharmacological properties and therapeutic efficacy. Drugs 19: 249-267.
22. Tischler AS, Lee YC, Costopoulos D, Nunnemacher G, DeLellis RA, et al. (1986) Establishment of a continuous somatostatin-producing line of medullary thyroid carcinoma cells from BALB/c mice. J Endocrinol 110: 309-313.
23. Vermes I, Haanen C, Steffens-Nakken H, Reutelingsperger C, (1995) A novel assay for apoptosis. Flow cytometric detection of phosphatidylserine expression on early apoptotic cells using fluorescein labelled Annexin V. J Immunol Methods 184: 39-51.
24. Tobin WE, Gold RH, (1972) Nefopam hydrochloride: a novel muscle relaxant. J Clin Pharmacol New Drugs 12: 230-238.
25. Smits R, van der Houven, van Oordt W, Luz A, Zurcher C, Jagmohan-Changur S, et al. (1998) Apc1638N: a mouse model for familial adenomatous polyposis-associated desmoid tumors and cutaneous cysts. Gastroenterology 114: 275-283.
26. Wang RI, Waite EM, (1979) The clinical analgesic efficacy of oral nefopam hydrochloride. J Clin Pharmacol 19: 395-402.
27. Pillans PI, Woods DJ, (1995) Adverse reactions associated with nefopam. N Z Med J 108: 382-384.
28. Esposito E, Romandini S, Merlo-Pich E, Mennini T, Samanin R, (1986) Evidence of the involvement of dopamine in the analgesic effect of nefopam. Eur J Pharmacol 128: 157-164.
29. Marazziti D, Rotondo A, Ambrogi F, Cassano GB, (1991) Analgesia by nefopam: does it act through serotonin? Drugs Exp Clin Res 17: 259-261.
30. Girard P, Pansart Y, Coppe MC, Verniers D, Gillardin JM, (2004) Role of the histamine system in nefopam-induced antinociception in mice. Eur J Pharmacol 503: 63-69.
31. Verleye M, Andre N, Heulard I, Gillardin JM, (2004) Nefopam blocks voltage-sensitive sodium channels and modulates glutamatergic transmission in rodents. Brain Res 1013: 249-255.
32. Gainetdinov RR, Premont RT, Bohn LM, Lefkowitz RJ, Caron MG, (2004) Desensitization of G protein-coupled receptors and neuronal functions. Annu Rev Neurosci 27: 107-144.
33. Beaulieu JM, Gainetdinov RR, Caron MG, (2007) The Akt-GSK-3 signaling cascade in the actions of dopamine. Trends Pharmacol Sci 28: 166-172.
34. Juarez-Rojop IE, Granados-Soto V, Diaz-Zagoya JC, Flores-Murrieta FJ, Torres-Lopez JE, (2006) Involvement of cholecystokinin in peripheral nociceptive sensitization during diabetes in rats as revealed by the formalin response. Pain 122: 118-125.
35. Vuga LJ, Ben-Yehudah A, Kovkarova-Naumovski E, Oriss T, Gibson KF, et al. (2009) WNT5A is a regulator of fibroblast proliferation and resistance to apoptosis. Am J Respir Cell Mol Biol 41: 583-589.
36. Wunder JS, Nielsen TO, Maki RG, O'Sullivan B, Alman BA, (2007) Opportunities for improving the therapeutic ratio for patients with sarcoma. Lancet Oncol 8: 513-524.
37. Yao H, Ashihara E, Maekawa T, (2011) Targeting the Wnt/beta-catenin signaling pathway in human cancers. Expert Opin Ther Targets 15: 873-887.
38. Sato M, (2006) Upregulation of the Wnt/beta-catenin pathway induced by transforming growth factor-beta in hypertrophic scars and keloids. Acta Derm Venereol 86: 300-307.
39. Hwang I, Seo EY, Ha H, (2009) Wnt/beta-catenin signaling: a novel target for therapeutic intervention of fibrotic kidney disease. Arch Pharm Res 32: 1653-1662.
40. Wei J, Melichian D, Komura K, Hinchcliff M, Lam AP, et al. (2011) Canonical Wnt signaling induces skin fibrosis and subcutaneous lipoatrophy: a novel mouse model for scleroderma? Arthritis Rheum 63: 1707-1717.
41. Varallo VM, Gan BS, Seney S, Ross DC, Roth JH, et al. (2003) Beta-catenin expression in Dupuytren's disease: potential role for cell-matrix interactions in modulating beta-catenin levels in vivo and in vitro. Oncogene 22: 3680-3684.
42. Kim TH, Kim SH, Seo JY, Chung H, Kwak HJ, et al. (2011) Blockade of the Wnt/beta-catenin pathway attenuates bleomycin-induced pulmonary fibrosis. Tohoku J Exp Med 223: 45-54.
43. Henderson WR Jr, Chi EY, Ye X, Nguyen C, Tien YT, et al. (2010) Inhibition of Wnt/beta-catenin/CREB binding protein (CBP) signaling reverses pulmonary fibrosis. Proc Natl Acad Sci U S A 107: 14309-14314.
44. Li C, Bapat B, Alman BA, (1998) Adenomatous polyposis coli gene mutation alters proliferation through its beta-catenin-regulatory function in aggressive fibromatosis (desmoid tumor). Am J Pathol 153: 709-714.
45. Henriksson E, Kjellen E, Wahlberg P, Wennerberg J, Kjellstrom JH, (2006) Differences in estimates of cisplatin-induced cell kill in vitro between colorimetric and cell count/colony assays. In Vitro Cell Dev Biol Anim 42: 320-323.
46. Yokoyama N, Yin D, Malbon CC, (2007) Abundance, complexation, and trafficking of Wnt/beta-catenin signaling elements in response to Wnt3a. J Mol Signal 2: 11.
47. Nakamura T, Sano M, Songyang Z, Schneider MD, (2003) A Wnt- and beta-catenin-dependent pathway for mammalian cardiac myogenesis. Proc Natl Acad Sci U S A 100: 5834-5839.
48. Silkstone D, Hong H, Alman BA, (2008) Beta-catenin in the race to fracture repair: in it to Wnt. Nat Clin Pract Rheumatol 4: 413-419.
49. Case MT, Smith JK, Nelson RA, (1975) Reproductive, acute and subacute toxicity studies with nefopam in laboratory animals. Toxicol Appl Pharmacol 33: 46-51.
50. Poon R, Smits R, Li C, Jagmohan-Changur S, Kong M, et al. (2001) Cyclooxygenase-two (COX-2) modulates proliferation in aggressive fibromatosis (desmoid tumor). Oncogene 20: 451-460.
51. Aymard G, Warot D, Demolis P, Laville I, Diquet B, (2002) Sensitive determination of nefopam and its metabolite desmethyl-nefopam in human biological fluids by HPLC. J Pharm Biomed Anal 30: 1013-1021.