General Information of This Peptide
Peptide ID
PEP00099
Peptide Name
p6
Structure
Sequence
NDLMNRA
Peptide Type
Linear
PDC Transmembrane Types Cell targeting peptides (CTPs)
Formula
C32H56N12O12S
Isosmiles
[H]NC(=O)C[C@H](N[H])C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)N[H])C(=O)N[C@@H](CCC/N=C(/N)N[H])C(=O)N[C@@H](C)C(=O)O
InChI
InChI=1S/C32H56N12O12S/c1-14(2)10-19(43-30(54)21(13-24(47)48)42-25(49)16(33)11-22(34)45)28(52)41-18(7-9-57-4)27(51)44-20(12-23(35)46)29(53)40-17(6-5-8-38-32(36)37)26(50)39-15(3)31(55)56/h14-21H,5-13,33H2,1-4H3,(H2,34,45)(H2,35,46)(H,39,50)(H,40,53)(H,41,52)(H,42,49)(H,43,54)(H,44,51)(H,47,48)(H,55,56)(H4,36,37,38)/t15-,16-,17-,18-,19-,20-,21-/m0/s1
InChIKey
LTQKWXOKPROJTI-BPSSIEEOSA-N
Pharmaceutical Properties
Molecule Weight
832.939
Polar area
425.8
Complexity
832.3861362
xlogp Value
-5.5947
Heavy Count
57
Rot Bonds
29
Hbond acc
13
Hbond Donor
13
The Activity Data of This Peptide
Peptide Activity Information 1 [1]
Binding rate 2.17%
Binding Affinity Assay
To assess the binding capacity of the candidate peptides, peptide-FITC conjugates were incubated at 0, 4 or 8 ?M with 106 PBMC cells at 37 C for 30 min.
Experimental Condition Mouse peripheral mononuclear cell PBMC
Peptide Activity Information 2 [1]
Binding rate 6.90%
Binding Affinity Assay
To assess the binding capacity of the candidate peptides, peptide-FITC conjugates were incubated at 0, 4 or 8 ?M with 106 HL-60 cells at 37 C for 30 min.
Experimental Condition Human leukemic cell HL-60
Each Peptide-drug Conjugate Related to This Peptide
Full Information of The Activity Data of The PDC(s) Related to This Peptide
P6-chlorambucil [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data A20 growth inhibition
22.00%
Administration Time 72 h
Administration Dosage 50 µM
Evaluation Method XTT assay
Description
Conjugation of the drugs to P4 affected their efficacy toward A20 cells. For chlorambucil and melphalan, conjugation reduced the cytotoxic effect and this was significant for chlorambucil at 25 μM (p = 0.0013). On the other hand, conjugation significantly improved the cytotoxic effect of bendamustine at 25 (p = 0.043) and 50 μM (p = 0.048). The efficacies of all P6-conjugates were significantly lower than those of P4-conjugates at concentrations above 10 μM.

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In Vitro Model Mouse reticulum cell sarcoma A20 cell CVCL_1940
P6-melphalan [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data A20 growth inhibition
25.00%
Administration Time 72 h
Administration Dosage 50 µM
Evaluation Method XTT assay
Description
Conjugation of the drugs to P4 affected their efficacy toward A20 cells. For chlorambucil and melphalan, conjugation reduced the cytotoxic effect and this was significant for chlorambucil at 25 μM (p = 0.0013). On the other hand, conjugation significantly improved the cytotoxic effect of bendamustine at 25 (p = 0.043) and 50 μM (p = 0.048). The efficacies of all P6-conjugates were significantly lower than those of P4-conjugates at concentrations above 10 μM.

   Click to Show/Hide
In Vitro Model Mouse reticulum cell sarcoma A20 cell CVCL_1940
P6-bendamustine [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data A20 growth inhibition
28.00%
Administration Time 72 h
Administration Dosage 50 µM
Evaluation Method XTT assay
Description
Conjugation of the drugs to P4 affected their efficacy toward A20 cells. For chlorambucil and melphalan, conjugation reduced the cytotoxic effect and this was significant for chlorambucil at 25 μM (p = 0.0013). On the other hand, conjugation significantly improved the cytotoxic effect of bendamustine at 25 (p = 0.043) and 50 μM (p = 0.048). The efficacies of all P6-conjugates were significantly lower than those of P4-conjugates at concentrations above 10 μM.

   Click to Show/Hide
In Vitro Model Mouse reticulum cell sarcoma A20 cell CVCL_1940
References
Ref 1 Gold nanoparticles stabilize peptide-drug-conjugates for sustained targeted drug delivery to cancer cells. J Nanobiotechnology. 2018 Mar 30;16(1):34. doi: 10.1186/s12951-018-0362-1.