PPIRE00670
Target Protein Information
| Protein_Name | Serine/threonine-protein kinase PAK 1 |
|---|---|
| Protein_Sequence | MSNNGLDIQDKPPAPPMRNTSTMIGAGSKDAGTLNHGSKPLPPNPEEKKKKDRFYRSILPGDKTNKKKEKERPEISLPSDFEHTIHVGFDAVTGEFTGMPEQWARLLQTSNITKSEQKKNPQAVLDVLEFYNSKKTSNSQKYMSFTDKSAEDYNSSNALNVKAVSETPAVPPVSEDEDDDDDDATPPPVIAPRPEHTKSVYTRSVIEPLPVTPTRDVATSPISPTENNTTPPDALTRNTEKQKKKPKMSDEEILEKLRSIVSVGDPKKKYTRFEKIGQGASGTVYTAMDVATGQEVAIKQMNLQQQPKKELIINEILVMRENKNPNIVNYLDSYLVGDELWVVMEYLAGGSLTDVVTETCMDEGQIAAVCRECLQALEFLHSNQVIHRDIKSDNILLGMDGSVKLTDFGFCAQITPEQSKRSTMVGTPYWMAPEVVTRKAYGPKVDIWSLGIMAIEMIEGEPPYLNENPLRALYLIATNGTPELQNPEKLSAIFRDFLNRCLEMDVEKRGSAKELLQHQFLKIAKPLSSLTPLIAAAKEATKNNH |
| Organism_Source | Homo sapiens |
| Functional_Classification | Kinase |
| Cellular_Localization | Cytoplasm |
| Gene_Names | PAK1 |
| UniProt_ID | Q13153 |
| Protein-Protein Interaction Networks | |
Peptide Basic Information
| Peptide_Name | RMR peptide |
|---|---|
| Peptide_Sequence | RMRVTPSTPSPR |
| Peptide_Length | 12 |
| Peptide_SMILES | CSCC[C@H](NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(C)C |
| Chemical_Modification | None |
| Cyclization_Method | None |
| Linear/Cyclic | Linear |
| N-terminal_Modification | Free |
| C-terminal_Modification | Free |
| Amino_Acid_Distribution | |
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Peptide Physicochemical
| Molecular_Weight | 1384.62 |
|---|---|
| Aliphatic_Index | 24.16667 |
| Aromaticity | 0.00000 |
| Average_Rotatable_Bonds | 3.33333 |
| Charge_at_pH_7 | 2.99797 |
| Isoelectric_Point | 12.80107 |
|---|---|
| Number_of_Hydrogen_Bond_Acceptors | 21 |
| Number_of_Hydrogen_Bond_Donors | 23 |
| Topological_Polar_Surface_Area | 623.67000 |
| X_logP_energy | -8.80519 |
Interaction Information
| Affinity | Ki=1.68 uM |
|---|---|
| Affinity_Assay | Intrinsic Fluorescence Quenching Assay |
| PDB_ID | None |
| Type | Inhibitor |
| Structure | |
Reference Information
| Document_Type | Research Articles |
|---|---|
| Title | Small peptide inhibitor from the sequence of RUNX3 disrupts PAK1-RUNX3 interaction and abrogates its phosphorylation-dependent oncogenic function. |
| Release_Year | 2021 |
| PMID | 34253860 |
| DOI | 10.1038/s41388-021-01927-x |