Table 1. ZMC1-mediated toxicity and p53 refolding in H1299 cells expressing p53 mutants.
EC50 data and fits are shown in Figure 5 and antibody-monitored refolding data are shown in Figure 6A and Figure 7. aYes, PAB240 staining level was reduced significantly (Fig. after ZMC1 treatment; No, PAB240) staining level was not significantly changed after ZMC1 treatment. Sample size: 3; replicates: 2–3 independent experiments; outliers/exclusions: no.
| Mutant | EC50 (nM) | p53 refoldinga |
|---|---|---|
| Untransfected cells | >1000 | Not applicable |
| Empty vector | >1000 | Not applicable |
| Zinc-binding class | ||
| R175H | 5 | Yes |
| C176S | 2 | Yes |
| L194F | 5 | Yes |
| P152L | >1000 | No |
| R282Q | >1000 | No |
| Stability class | ||
| Y234A | 10 | Yes |
| Y234C | >1000 | No |
| V272M | 2 | Yes |
| E285K | >1000 | No |
| Mixed zinc-binding/stability class | ||
| M237I | >1000 | Yes |
| DNA-binding class | ||
| R273H | >1000 | Yes |
| R280K | >1000 | No |