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




DBAASP ID  DBAASPS_17185

DCTPep is developed by Dr.Zheng's team.