Copyright 2015 OncoRx Pharmaceuticals, Inc.  All rights reserved.

Selected Bibliography

 ​“Roles of dopamine receptors and their antagonist thioridazine in hepatoma metastasis.”  

Lu M, Li J, Luo Z, Zhang S, Xue S, Wang K, Shi Y, Zhang C, Chen H, Li Z; Onco Targets Ther. 2015 22;8:1543-52.

“Identification of thioridazine, an antipsychotic drug, as an antiglioblastoma and anticancer stem cell agent using public gene expression data.” Cheng HW, Liang YH, Kuo YL, Chuu CP, Lin CY, Lee MH, Wu AT, Yeh CT, Chen E, Whang-Peng J, Su CL, Huang CY., Cell Death Dis. 2015 7;6

“Activation of protein phosphatase 2A tumor suppressor as potential treatment of pancreatic cancer.” Chien W, Sun QY, Lee KL, Ding LW, Wuensche P, Torres-Fernandez LA, Tan SZ, Tokatly I, Zaiden N, Poellinger L, Mori S, Yang H, Tyner JW, Koeffler HP. Mol Oncol. 2015 9(4):889-905.

“Thioridazine specifically sensitizes drug-resistant cancer cells through highly increase in apoptosis and P-gp inhibition.”
Choi AR, Kim JH, Yoon S., Tumour Biol. 2014 35(10):9831-8.

 “Thioridazine inhibits angiogenesis and tumor growth by targeting the VEGFR-2/PI3K/mTOR pathway in ovarian cancer xenografts.” 

Park MS, Dong SM, Kim BR, Seo SH, Kang S, Lee EJ, Lee SH, Rho SB. Oncotarget. 14 15;5(13):4929-34. 

 “Phenothiazines induce PP2A-mediated apoptosis in T cell acute lymphoblastic leukemia.” Gutierrez A, Pan L, Groen RW, Baleydier F, Kentsis A, Marineau J, Grebliunaite R, Kozakewich E, Reed C, Pflumio F, Poglio S, Uzan B, Clemons P, VerPlank L, An F, Burbank J, Norton S, Tolliday N, Steen H, Weng AP, Yuan H, Bradner JE, Mitsiades C, Look AT, Aster JC.; J Clin Invest. 2014 Feb;124(2):644-55.

 "The [phenothiazine] antipsychotic agent chlorpromazine induces autophagic cell death by inhibiting the Akt/mTOR pathway in human U-87MG glioma cells." Shin SY, Lee KS, Choi YK, Lim HJ, Lee HG, Lim Y, Lee YH.; Carcinogenesis. 2013 34(9):2080-9.

 “A drug repositioning approach identifies tricyclic antidepressants as inhibitors of small cell lung cancer and other neuroendocrine tumors.” Jahchan NS, Dudley JT, Mazur PK, Flores N, Yang D, Palmerton A, Zmoos AF, Vaka D, Tran KQ, Zhou M, Krasinska K, Riess JW, Neal JW, Khatri P, Park KS, Butte AJ, Sage J.; Cancer Discov. 2013 3(12):1364-77.  

“Anti-angiogenic effects of thioridazine involving the FAK-mTOR pathway.” 

Byun HJ, Lee JH, Kim BR, Kang S, Dong SM, Park MS, Lee SH, Park SH, Rho SB. Microvasc Res. 2012 84(3): 227-34.

“Identification of drugs including a dopamine receptor antagonist [thioridazine] that selectively target cancer stem cells.”
Sachlos E, Risueño RM, Laronde S, Shapovalova Z, Lee JH, Russell J, Malig M, McNicol JD, Fiebig-Comyn A, Graham M, Levadoux-Martin M, Lee JB, Giacomelli AO, Hassell JA, Fischer-Russell D, Trus MR, Foley R, Leber B, Xenocostas A, Brown ED, Collins TJ, Bhatia M. Cell. 2012 149(6):1284-97.

“Thioridazine induces apoptosis by targeting the PI3K/Akt/mTOR pathway in cervical and endometrial cancer cells.”
Kang S, Dong SM, Kim BR, Park MS, Trink B, Byun HJ, Rho SB. Apoptosis. 2012 17(9):989-97.

“Thioridazine induces apoptosis of multidrug-resistant mouse lymphoma cells transfected with the human ABCB1 and inhibits the expression of P-glycoprotein.”  Spengler G, Molnar J, Viveiros M, Amaral L.; Anticancer Res. 2011 31(12):4201-5.

“A gene signature-based approach identifies thioridazine as an inhibitor of phosphatidylinositol-3'-kinase (PI3K)/AKT pathway in ovarian cancer cells.” Rho SB, Kim BR, Kang S., Gynecol Oncol. 2011 120(1):121-7.

“Image-based chemical screening identifies drug efflux inhibitors in lung cancer cells.”

Xia X, Yang J, Li F, Li Y, Zhou X, Dai Y, Wong ST.; Cancer Res. 2010 1;70(19):7723-33.

 “Metabolic activation of the phenothiazine antipsychotics chlorpromazine and thioridazine to electrophilic iminoquinone species in human liver microsomes and recombinant P450s.” Wen B, Zhou M.; Chem Biol Interact. 2009 181(2):220-6. 

“In vitro differential sensitivity of melanomas to phenothiazines [thioridazine] is based on the presence of codon 600 BRAF mutation.”

Ikediobi ON, Reimers M, Durinck S, Blower PE, Futreal AP, Stratton MR, Weinstein JN., Mol Cancer Ther. 2008 7(6):1337-46.

 “Bioactivation of the tricyclic antidepressant amitriptyline and its metabolite nortriptyline to arene oxide intermediates in human liver microsomes and recombinant P450s.”  Wen B, Ma L, Zhu M.; Chem Biol Interact. 2008 173(1):59-67.

“The Development of Novel Small Molecule Inhibitors [thioridazine] of the Phosphoinositide- 3-Kinase Pathway through High-Throughput Cell-Based Screens”, 
William R. Sellers, M.D. Award Number: W81XWH-04-1-0169 TITLE: Dana-Farber Cancer Institute Boston, Massachusetts ; February 2006.