Distance to the closest PDE4 residue and substrate/inhibitor effects for PDE4 with large changes in rolipram sensitivity (Atienza et al., 1999; Pillai et al., 1993)
| Km cAMP | Fold ΔIC50 for Rolipram | Distance | ||
|---|---|---|---|---|
| cAMP | Rolipram | |||
| μm | Å | |||
| PDE4BΔwt | 2 | |||
| D241A | 7 | 390 | 7.0 | 7.0 |
| D241N | 3 | 270 | ||
| I410T | 340 | 260 | 3.0 | 3.0 |
| I410N | 1200 | 910 | ||
| T407A | 18 | 330 | 4.0 | 2.8 |
| Y403C | 19 | 8 | 5.5 | 4.3 |
| F414S | 25 | 8 | 6.3 | 3.5 |
Substrate K m, change in IC50 (compared with wild-type), and closest distance between wild-type side chain and the docked drug, as obtained by the AutoDock program, are indicated.