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cHLH-p53R
General Information
DCTPep ID DCTPep02843
Peptide Name cHLH-p53R
Sequence GARELRRLERELRRLEGGGGGGGKLAALKFKLLWLKLAC
Sequence Length 39
UniProt ID Not available
PubChem CID Not available
Origin Synthetic
Type Synthetic peptide
Classification
ACP Tumor active peptide Membrane lysis Cell-penetrating peptides
Activity Information
| Cell Line | Disease | Activity | Assay | Testing Time | Literature |
|---|---|---|---|---|---|
| MDA-MB-231 | Breast adenocarcinoma | CC50=15.9 ± 2.3 μM | Resazurin assay | 26 h | 1 |
| MCF-7 | Invasive breast carcinoma of no special type | CC50=16.0 ± 0.5 μM | Resazurin assay | 26 h | 1 |
| MM96L | Melanoma | CC50=5.4 ± 0.3 μM | Resazurin assay | 26 h | 1 |
| MDA-MB-435S | Amelanotic melanoma | CC50=5.7 ± 0.4 μM | Resazurin assay | 26 h | 1 |
| K562 | Blast phase chronic myelogenous leukemia, BCR-ABL1 positive; Chronic myeloid leukemia | CC50=8.2 ± 0.4 μM | Resazurin assay | 26 h | 1 |
Hemolytic Activity Human erythrocytes: 50% Hemolysis>64 µM
Normal (non-cancerous) Cytotoxicity HFF-1: CC50=11.9 ± 1.0 µM; MCF-10A: CC50=8.0 ± 0.8 µM; Human PBMC: CC50=48.9 ± 5.3 µM
Target Not available
Affinity Not available
Mechanism (1) The positively charged peptide targets the negative surface of cancer cells via electrostatic attractions; (2) The peptide inserts into cell membranes and enters inside cells very efficaciously; (3) Once inside cells, the peptide induces toxicity through fusion and/or disruption of intracellular organelles; (4) The cell membrane is disrupted and the cells die.
Structure Information
PDB ID Not available
Predicted Structure DCTPep02843
(Please note that there is the predicted structure, predicted by AlphaFold)
Helicity Not available
Linear/Cyclic Cyclic
Disulfide/Other Bond TIE: N-terminal Chloroacetic acid<--->Cys39
N-terminal Modification CAA, Chloroacetic acid
C-terminal Modification Free
Other Modification None
Chiral L
Physicochemical Information
Formula C191H328N62O48S1
Absent amino acids DHIMNPQSTVY
Theoretical pI 10.91
Acidic residues 4
Basic residues 10
Polar residues 9
Molecular weight (Average) 4293.15
Molecular weight (Monoisotopic) 4290.49
Common amino acids L
Net charge 6
Instability index (II) 69.39
Aliphatic index 110.26
Grand average of hydropathicity (GRAVY) -0.262
Half Life
30 hours (mammalian reticulocytes, in vitro).
>20 hours (yeast, in vivo).
>10 hours (Escherichia coli, in vivo).
Extinction coefficients
Ext. coefficient 5500
Abs 0.1% (=1 g/l) 1.281, assuming all pairs of Cys residues form cystines
Ext. coefficient 5500
Abs 0.1% (=1 g/l) 1.281, assuming all Cys residues are reduced
Amino acid distribution
Literature Information
Literature 1
Pubmed ID 31390185
Title Cell Membrane Composition Drives Selectivity and Toxicity of Designed Cyclic Helix-Loop-Helix Peptides with Cell Penetrating and Tumor Suppressor Properties
Doi 10.1021/acschembio.9b00593
Year 2019
Patent
Patent ID Not available
Patent Title Not available
Other Iinformation Not available
Other Published ID Not available
External Code
DBAASP ID DBAASPS_17185
This work is licensed under a Creative Commons Attribution 4.0 International License.