Table 2.

Summary of known antagonists of the cJun-TRE DNA interaction. Included are known mode of binding as well as quantitative measures of activity for each antagonist identified

Antagonist	Target binding surface	Affinity/Antagonist Activity	Notes	References
MLN44	TRE DNA major groove	100% inhibition in EMSA assay at 25 μM		[129–133]
SR11302	TRE DNA	Treatment prior to TPA induction of tumours produced a 67.9% reduction in papillomas per mouse		[134–136]
Veratramine	TRE DNA	90% reduction in transactivation at 20 μM in luciferase reporter assay	ITC data collected but no binding affinity reported	[137]
KCR motif peptide-1-[N-[2-succinamidylethyl]amino] anthraquinones	TRE DNA	Approaching 100% inhibition in EMSA assay at 1 μM		[138]
T-5224	DBD of AP-1 proteins	IC50~10 μM		[51, 139, 140]
NY2267	cJun LZ	74% reduction in transactivation at 20 μM in luciferase reporter assay	Designed as c-Myc antagonist so not selective	[141]
cFos LZ	cJun LZ	For cFos LZ-cJun LZ: Kd = 26.6 μM (by ITC)		[142, 143]
JunB bZIP	cJun LZ	Eightfold excess of JunB reduced transactivation tenfold in a luciferase reporter assay		[88]
anti-Jun and anti-Fos SZ	cJun LZ	50% of Jun LZ or Fos LZ bound to the antagonist when the three are mixed in equimolar amounts		[144]
FosW	cJun LZ	For FosW-cJun LZ: Kd = 39 nM (by ITC)		[145, 146]
FosWCANDI	cJun LZ	For FosWCANDI -cJun LZ: Tm = 52 degrees C(by CD)	Reduced affinity with no increase in selectivity compared to FosW	[154]
CPW	cJun LZ	For CPW-cJun LZ: Kd = 750 nM (by ITC)		[147]
FosUisCan	cJun LZ	For FosUisCAN-cJun LZ Tm of 57 °C (by CD)		[125]
A-Fos	cJun bZIP	For A-Fos-cJun bZIP: Kd = 30 pM (by CD thermal shift from Tm of 72.1 °C)		[148]