Table 1. Overview of RAS binding peptides.
Name (PDB ID) | RAS specificity | KD (nM) | Site on RAS | Properties | Ref. |
---|---|---|---|---|---|
Linear | |||||
RBDv1, RBDv12 | GTP-RAS | 3.35 2.52 | P4 | 14 aa, inhibits RAS signalling, reduces cancer cell growth | [69] |
SAH-SOS1 | GDP-/GTP-RAS | 106–175 | near P4 | 16 aa, blocks nucleotide exchange, reduces cancer cell growth | [70] |
225-11 (5WPL) | GTP-RAS | 3.3 | P4 | 32 aa, blocks effector interaction | [71] |
R11.1.6 (5UFQ) | RAS-G12D | 4 | switch II | 61 aa, blocks effector interaction, inhibits RAS signalling | [72] |
Cyclic | |||||
Cyclorasin 9A5 | GTP-RAS | 440 | near P4 | 11 aa, blocks effector interaction, inhibits RAS signalling | [73] |
Cyclorasin B4-27 | GTP-RAS | 21 | near P4 | 16 aa, blocks effector interaction (cellular BRET-assay) | [74] |
KRpep-2d (5XCO) | KRAS-G12D | 51 | P2 | 19 aa, inhibits RAS signalling, reduces cancer cell growth | [75–77] |
KS-58 | KRAS-G12D | 22 | P2 | 11 aa, inhibits RAS signalling, reduces cancer cell growth in vivo | [78,79] |
KD2 (6WGN) | GTP-KRAS-G12D | none | near P2 | 15 aa, blocks effector interaction | [80] |
Peptide and peptidomimetic RAS binders and their properties. The PDB ID is given if the complex with RAS was determined.