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

MLN44

TRE DNA major groove

100% inhibition in EMSA assay at 25 μM

[129,130,131,132,133]

SR11302

TRE DNA

Treatment prior to TPA induction of tumours produced a 67.9% reduction in papillomas per mouse

[134,135,136]

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: K_d = 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: K_d = 39 nM (by ITC)

[145, 146]

FosW_CANDI

cJun LZ

For FosW_CANDI -cJun LZ: T_m = 52 degrees C(by CD)

Reduced affinity with no increase in selectivity compared to FosW

[154]

CPW

cJun LZ

For CPW-cJun LZ: K_d = 750 nM (by ITC)

[147]

FosU_isCan

cJun LZ

For FosU_isCAN-cJun LZ T_m of 57 °C (by CD)

[125]

A-Fos

cJun bZIP

For A-Fos-cJun bZIP: K_d = 30 pM (by CD thermal shift from T_m of 72.1 °C)

[148]