Summary of Retinoid Activity
| Retinoids . | Transcriptional Activity* . | Anti-AP–1 Activity‡ . | ED50 (nmol/L)1-153 . | Synergy With ATRA1-155 . | ||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| % at 10−7nmol/L . | EC50 (nmol/L)† . | |||||||||||
| RARα . | RARβ . | RARγ . | RXRα . | RARα . | RARβ . | RARγ . | RXRα . | HL-60 . | NB4 . | |||
| ATRA | 57 | 75 | 85 | 15 | 45 | 5 | 2 | 1,000 | (+) | 30 | 1 | |
| SR11302(A) | 0 | −8 | −3 | −1 | >1,000 | >1,000 | >1,000 | >1,000 | (+) | NR | NR | N |
| SR11363(B) | 6 | 34 | 37 | 15 | >10,000 | >10,000 | 170 | >10,000 | ND | NR | NR | N |
| SR11345(C) | 0 | −5 | −9 | 152 | >1,000 | >1,000 | >1,000 | 21 | ND | NR | NR | N |
| SR11278(D) | 10 | 154 | 26 | −5 | >1,000 | 55 | 80 | >1,000 | ND | 70 | 70 | Y (4.5) |
| SR11276(E) | 109 | 100 | 94 | 67 | 18 | 3 | 3 | 37 | ND | 7 | 6 | Y (7.5) |
| Retinoids . | Transcriptional Activity* . | Anti-AP–1 Activity‡ . | ED50 (nmol/L)1-153 . | Synergy With ATRA1-155 . | ||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| % at 10−7nmol/L . | EC50 (nmol/L)† . | |||||||||||
| RARα . | RARβ . | RARγ . | RXRα . | RARα . | RARβ . | RARγ . | RXRα . | HL-60 . | NB4 . | |||
| ATRA | 57 | 75 | 85 | 15 | 45 | 5 | 2 | 1,000 | (+) | 30 | 1 | |
| SR11302(A) | 0 | −8 | −3 | −1 | >1,000 | >1,000 | >1,000 | >1,000 | (+) | NR | NR | N |
| SR11363(B) | 6 | 34 | 37 | 15 | >10,000 | >10,000 | 170 | >10,000 | ND | NR | NR | N |
| SR11345(C) | 0 | −5 | −9 | 152 | >1,000 | >1,000 | >1,000 | 21 | ND | NR | NR | N |
| SR11278(D) | 10 | 154 | 26 | −5 | >1,000 | 55 | 80 | >1,000 | ND | 70 | 70 | Y (4.5) |
| SR11276(E) | 109 | 100 | 94 | 67 | 18 | 3 | 3 | 37 | ND | 7 | 6 | Y (7.5) |
Activation (%) at 10−7 mol/L retinoid compared with 10−6 mol/L ATRA for RARs and 10−6mol/L 9-cis-RA for RXRα.
EC50, concentration of retinoid giving 50% response of 10−6 mol/L ATRA for RARs and 10−6 mol/L 9-cis-RA for RXRα on the (TREpal)2-tk-CAT construct or response at 10−5 mol/L retinoid, which ever is greater, for retinoids whose maximal response is >30% of that of 10−6 mol/L ATRA for RARs and 10−6 mol/L 9-cis -RA for RXRα.
ND, not done.
ED50, concentration of retinoid giving 50% inhibition of clonal growth; NR, not reached; ND, not determined.
N, no; Y, yes; ( ), fold-induction of CD11b on HL-60 cells in the presence of 10−11 mol/L ATRA plus the novel retinoid (10−11 mol/L) compared with ATRA-treated control.