Table 3.
Peptide inhibitors of JNK
| Protein from which inhibitor derived | Peptide name | Amino acid sequence (residue numbers) | Identification | IC50 (and/or Ki when reported) | PDB entry | References |
|---|---|---|---|---|---|---|
| c-Jun | TAT-cJun peptidea | Y-G-R-K-K-R-R-Q-R-R-R-G-I-L-K-Q-S-M-T-L-N-L-A-D-P-V-G-S-L-K-P-H-L-R-A-K-N(33–57) | δ-domain of c-Jun | Not determined, but used in cells at 100 μM concentration | – | [73] |
| JIP1 | TI-JIP | R-P-K-R-P-T-T-L-N-L-F(153–163) | JNK interaction domain of JIP1 | Ki0.39 +/− 0.08 μMin vitro | 1UKH/1UKI | [75], [79] |
| TAT-TIJIPa | G-R-K-K-R-R-Q-R-R-R-P-P-R-P-K-R-P-T-T-L-N-L-F (153–163) | JNK interaction domain of JIP1 | Not determined, but used in cells at 10 μM concentration | – | [78] | |
| JIP1 peptide | R-P-K-R-P-T-T-L-N-L-F-P-Q-V-P-R-S-Q-D(153–171) | JNK interaction domain of JIP1 | Not determined | – | [76] | |
| LJNKi (XG101)a | G-R-K-K-R-R-Q-R-R-R-P-P-R-P-K-R-P-T-T-L-N-L-F-P-Q-V-P-R-S-Q-D (153–171) | IC50 ∼ 1 μM in vitro | – | [76], [77] | ||
| DJNKi (XG102)a,b | t-d-q-s-r-p-v-q-p-f-l-n-l-t-t-p-r-k-p-r-p-p-r-r-r-q-r-r-k-k-r-g (171–153) | Not determined, but 15–20-fold less potent than L-JNKI | – | [76,77] |
a
Cell-permeable vector sequence is underlined.
b
Amino acids denoted without capitals are the D-amino acid forms.