| ID | 1106 | |
| PMID | 21119619 | |
| Year | 2010 | |
| Sequence | ACSSSPSKHCGGRRR RRRRR | |
| Name | TD1-R8 | |
| Length | 20 | |
| N-Terminal Modification | Free | |
| C-Terminal Modification | Free | |
| Linear/ Cyclic | Linear | |
| Chirality | L | |
| Chemical Modification | None | |
| Origin of Peptide | Synthetic (by conjugating TD1 (ACSSSPSKHCG) and (oligoarginine) R8 ) | |
| Nature of Peptide/Cargo | MITF-siRNA inhibition of melanin synthesis and melanoma cell apoptosis. | |
| Mechanism | MITF-siRNA-silenced MITF gene expression effectively induced a significant reduction in tyrosinase (TYR), tyrosinase-related protein 1, and melanocortin 1 receptor (MC1R) levels. | |
| Cargo Sequence/Structure | MITF-siR: sense 5′-GCAGUACCUUUCUACCACUTT-3′ | |
| Name of cargo | Microphthalmia-associated transcription factor–siRNA (MITF-siR) | |
| Assay | Real-time PCR | |
| Enhancer | Hair clipped mice skin | |
| Properties of enhancer | Not applicable | |
| Concentration | 100 µg of cream containing 0.005% MITF-siR and arginine-rich peptide (TD1-R8). | |
| Incubation time | Cream applied once per day for 3 days and reading taken on 4th day | |
| Tissue permeability (value with units) | The cream penetrated the mouse skin and mouse skin exhibited a 52% and 34% decrease in MITF and TYR mRNA levels, respectively (versus naive control). | |
| Tissue Sample | Hair shaved back of BALB/c mice | |
| Ex vivo/In vivo/In vitro | in vivo | |
| STRUCTURE |
| |
| SMILES | N[C@@H](C)C(=O)N[C@@H](CS)C(=O)N[C@@H] (CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O) N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H] (CCCC[NH3])C(=O)N[C@@H](Cc1nc[nH]c1)C(=O)N [C@@H](CS)C(=O)NCC(=O)NCC(=O)N[C@@H](CCCNC(=[NH2]) N)C(=O)N[C@@H](CCCNC(=[NH2])N)C(=O)N[C@@H] (CCCNC(=[NH2])N)C(=O)N[C@@H](CCCNC(=[NH2]) N)C(=O)N[C@@H](CCCNC(=[NH2])N)C(=O)N[C@@H] (CCCNC(=[NH2])N)C(=O)N[C@@H](CCCNC (=[NH2])N)C(=O)N[C@@H](CCCNC(=[NH2])N)C=O | |