HO-3867

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Background

HO-3867 is a novel curcumin analog and a selective inhibitor of STAT3. [1]STAT3 (signal transducer and activator of transcription 3) belongs to the STAT protein family. It mediates various gene expressions for numerous cellular functions, including cell growth, division and apoptosis. HO-3867 selectively blocked STAT3 phosphorylation, transcription, and DNA binding without inhibiting other STATs proteins. It activated apoptosis in ovarian cancer cells and showed minimal toxicity to healthy cells. [2] HO-3867 also significantly inhibited the proliferation of serum-stimulated SMCs and elevated the phosphorylated and total levels of PTENs in SMCs. [3] By inducing cell cycle arrest and apoptosis, HO-3867 reduced the high levels of pSTAT3 Ser727 in endometrial cancer cells. [4]In mice tumor xenograft, HO-3867 inhibited the tumor growth without toxic side effects, it also blocked PSTAT3/JAK1 and increased apoptotic marker cleaved Caspase 3/PARP. [2] [5] After rat carotid artery injury, HO-3867 inhibited neointima formation and upregulated PTEN expression. [3]

[1] Tierney BJ, McCann GA, Cohn DE, Eisenhauer E, Sudhakar M, Kuppusamy P, Hideg K, Selvendiran K. HO-3867, a STAT3 inhibitor induces apoptosis by inactivation of STAT3 activity in BRCA1-mutated ovarian cancer cells. Cancer Biol Ther. 2012 Jul;13(9):766-75.
[2] Rath KS, Naidu SK, Lata P, Bid HK, Rivera BK, McCann GA, Tierney BJ, Elnaggar AC, Bravo V, Leone G, Houghton P, Hideg K, Kuppusamy P, Cohn DE, Selvendiran K.HO-3867, a safe STAT3 inhibitor, is selectively cytotoxic to ovarian cancer. Cancer Res. 2014 Apr 15;74(8):2316-27.
[3] Selvendiran K, Kuppusamy ML, Bratasz A, Tong L, Rivera BK, Rink C, Sen CK, Kálai T, Hideg K, Kuppusamy P. Inhibition of vascular smooth-muscle cell proliferation and arterial restenosis by HO-3867, a novel synthetic curcuminoid, through up-regulation of PTEN expression. J Pharmacol Exp Ther. 2009 Jun;329(3):959-66.
[4] Tierney BJ, McCann GA, Naidu S, Rath KS, Saini U, Wanner R, Kuppusamy P,Suarez A, Goodfellow PJ, Cohn DE, Selvendiran K. Aberrantly activated pSTAT3-Ser727 in human endometrial cancer is suppressed by HO-3867, a novel STAT3 inhibitor. Gynecol Oncol. 2014 Oct;135(1):133-41.
[5] Selvendiran K, Tong L, Bratasz A, Kuppusamy ML, Ahmed S, Ravi Y, Trigg NJ, Rivera BK, Kálai T, Hideg K, Kuppusamy P. Anticancer efficacy of a difluorodiarylidenyl piperidone (HO-3867) in human ovarian cancer cells and tumor xenografts. Mol Cancer Ther. 2010 May;9(5):1169-79.