Dietary compounds as potent inhibitors of the signal transducers and activators of transcription (STAT) 3 regulatory network

Trécul, Anne; Morceau, Franck; Dicato, Mario; Diederich, Marc

doi:10.1007/s12263-012-0281-y

Table 1 Inhibitors of STAT3 synthesis, their targets, mode of inhibition and cellular effects, adapted from Yue and Turkson 2009)

From: Dietary compounds as potent inhibitors of the signal transducers and activators of transcription (STAT) 3 regulatory network

Inhibitor	Target site	Mode of inhibition of STAT3 function	Cellular effects	References
PY*LKTK	domain SH2	Dimerization	↓ Malignant cell growth and transformation	Turkson et al. (2001)
Y*LPQTV	domain SH2	Dimerization	ND	Ren et al. (2003)
SS610	domain SH2	Dimerization	↓ Malignant cell growth and transformation	Turkson et al. (2004)
SS610	domain SH2	Dimerization	↑ Apoptosis	Turkson et al. (2004)
S3I-M2001	domain SH2	Dimerization	↓ Malignant cell growth	Siddiquee et al. (2007)
S3I-M2001	domain SH2	Dimerization	↑ Apoptosis, ↓ Migration	Siddiquee et al. (2007)
STA-21	domain SH2	Dimerization	↑ Apoptosis	Song et al. (2005)
S3I-201	domain SH2	Dimerization	↓ Cell growth	Siddiquee et al. (2007)
S3I-201	domain SH2	Dimerization	↑ Apoptosis	Siddiquee et al. (2007)
Stattic	domain SH2	Phosphorylation	↑ Apoptosis	Schust et al. (2006)
Catechol-containing compounds	domain DBD	DNA-binding	ND	Hao et al. (2008)
IS3 295	domain DBD	DNA-binding	↓ Cell growth	Turkson et al. (2005)
IS3 295	domain DBD	DNA-binding	↑ Apoptosis	Turkson et al. (2005)
CPA-1, CPA-7	domain DBD	DNA-binding	↓ Cell growth	Turkson et al. (2004)
CPA-1, CPA-7	domain DBD	DNA-binding	↑ Apoptosis	Turkson et al. (2004)
Galiellalactone	domain DBD	DNA-binding	↓ Cell growth	Weidler et al. (2000)
Galiellalactone	domain DBD	DNA-binding	↑ Apoptosis	Weidler et al. (2000)
Peptide aptamers	domain DBD	DNA-binding	↓ Cell growth	Nagel-Wolfrum et al. (2004)
Peptide aptamers	domain DBD	DNA-binding	↑ Apoptosis	Nagel-Wolfrum et al. (2004)
Decoy ODN	domain DBD	Compete against endogenous DNA cis element	↓ Cell growth	Leong et al. (2003)
Decoy ODN	domain DBD	Compete against endogenous DNA cis element	↑ Apoptosis	Leong et al. (2003)
G-quartet ODN	domain SH2	Phosphorylation	↓ Cell growth	Jing et al. (2006)
G-quartet ODN	domain SH2	Phosphorylation	↑ Apoptosis	Jing et al. (2006)
Peptides	ND	Transcriptional activity	↓ Cell growth	Timofeeva et al. (2007)
Peptides	ND	Transcriptional activity	↑ Apoptosis	Timofeeva et al. (2007)
JSI-124 & derivatives	JAK?	Phosphorylation	↓ Cell growth	Blaskovich et al. (2003)
JSI-124 & derivatives	JAK?	Phosphorylation	↑ Apoptosis, ↓ invasiveness	Blaskovich et al. (2003)
Withacnistin	JAK?	Phosphorylation	↓ Proliferation, ↑ apoptosis	Sun et al. (2005)

↑ increase, ↓ decrease

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