General Information of This Peptide
Peptide ID
PEP00077
Peptide Name
KTVRTSADE
Structure
Sequence
KTVRTSADE
Peptide Type
Cyclic
Receptor Name
Fibronectin (FN1)
 Receptor Info 
PDC Transmembrane Types Cell targeting peptides (CTPs)
Formula
C40H70N14O15
Isosmiles
[H]N/C(N)=N/CCC[C@@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@]([H])([C@@H](C)O[H])NC(=O)[C@@H](N[H])CCCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CO[H])NC(=O)[C@]([H])([C@@H](C)O[H])NC1=O
InChI
InChI=1S/C40H70N14O15/c1-17(2)28-37(67)49-23(10-8-14-46-40(43)44)34(64)54-29(19(4)56)38(68)51-25(16-55)36(66)47-18(3)32(62)50-24(15-27(59)60)35(65)48-22(31(42)61)11-12-26(58)45-13-7-6-9-21(41)33(63)53-30(20(5)57)39(69)52-28/h17-25,28-30,55-57H,6-16,41H2,1-5H3,(H2,42,61)(H,45,58)(H,47,66)(H,48,65)(H,49,67)(H,50,62)(H,51,68)(H,52,69)(H,53,63)(H,54,64)(H,59,60)(H4,43,44,46)/t18-,19+,20+,21-,22-,23-,24-,25-,28-,29-,30-/m0/s1
InChIKey
JARIEEXGEICJNQ-MYDGDSNPSA-N
Pharmaceutical Properties
Molecule Weight
987.083
Polar area
493.4
Complexity
986.5145075
xlogp Value
-8.2842
Heavy Count
69
Rot Bonds
15
Hbond acc
16
Hbond Donor
17
Each Peptide-drug Conjugate Related to This Peptide
Full Information of The Activity Data of The PDC(s) Related to This Peptide
Dox-S-S-GFLG-C6-[KTVRTSADE] [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 15 Activity Data Related to This Level
Experiment 1 Reporting the Activity Data of This PDC [1]
Indication Prostate cancer
Efficacy Data Cell viability
22%
Administration Time 72 h
Administration Dosage 5 µM
Evaluation Method MTS assay
Description
Dox conjugate 13 was moderately toxic with a reduced cell proliferation to a range of 25-35% as compared to Dox which reduced cell proliferation in the range of 20-34% for all selected four cell lines. However, it was interesting to observe that Doce conjugate 14 was almost nontoxic (cell proliferation within the range of 89-96%) in all the cell lines as compared to Doce alone which reduced the cell proliferation in the range of 54-61% (Figure 9).

   Click to Show/Hide
In Vitro Model Prostate carcinoma LNCaP cell CVCL_0395
Experiment 2 Reporting the Activity Data of This PDC [1]
Indication Prostate cancer
Efficacy Data Cell viability
25%
Administration Time 72 h
Administration Dosage 5 µM
Evaluation Method MTS assay
Description
Dox conjugate 13 was moderately toxic with a reduced cell proliferation to a range of 25-35% as compared to Dox which reduced cell proliferation in the range of 20-34% for all selected four cell lines. However, it was interesting to observe that Doce conjugate 14 was almost nontoxic (cell proliferation within the range of 89-96%) in all the cell lines as compared to Doce alone which reduced the cell proliferation in the range of 54-61% (Figure 9).

   Click to Show/Hide
In Vitro Model Normal RWPE-1 cell CVCL_3791
Experiment 3 Reporting the Activity Data of This PDC [1]
Indication Prostate cancer
Efficacy Data Cell viability
28%
Administration Time 72 h
Administration Dosage 5 µM
Evaluation Method MTS assay
Description
Dox conjugate 13 was moderately toxic with a reduced cell proliferation to a range of 25-35% as compared to Dox which reduced cell proliferation in the range of 20-34% for all selected four cell lines. However, it was interesting to observe that Doce conjugate 14 was almost nontoxic (cell proliferation within the range of 89-96%) in all the cell lines as compared to Doce alone which reduced the cell proliferation in the range of 54-61% (Figure 9).

   Click to Show/Hide
In Vitro Model Prostate carcinoma DU145 cell CVCL_0105
Experiment 4 Reporting the Activity Data of This PDC [1]
Indication Prostate cancer
Efficacy Data Cell viability
38%
Administration Time 72 h
Administration Dosage 5 µM
Evaluation Method MTS assay
Description
Dox conjugate 13 was moderately toxic with a reduced cell proliferation to a range of 25-35% as compared to Dox which reduced cell proliferation in the range of 20-34% for all selected four cell lines. However, it was interesting to observe that Doce conjugate 14 was almost nontoxic (cell proliferation within the range of 89-96%) in all the cell lines as compared to Doce alone which reduced the cell proliferation in the range of 54-61% (Figure 9).

   Click to Show/Hide
In Vitro Model Prostate carcinoma PC-3 cell CVCL_0035
Experiment 5 Reporting the Activity Data of This PDC [1]
Indication Prostate cancer
Efficacy Data Cell viability
48%
Administration Time 72 h
Evaluation Method MTS assay
Description
An increase in the cytotoxicity of Dox and Dox/peptide 9 physical mixture as compared to the conjugate 13 over an incubation period of 24 h to 72 h. Conjugates 13 and 14 were found to be less cytotoxic as compared to drug alone in 24-72 h. These cells were not treated with TGF-, so very minimal or no overexpression of EDB-FN. Figure 10b showed the effect of overexpression of EDB-FN in the cell viability. There was no observed effect of TGF- treatment for the cytotoxicity of Dox and physical mixture of Dox/peptide 9 on the cell viability as compared to the TGF- untreated cell lines. However, conjugate 13 showed a decrease in cell viability by 17% after 72 h as compared to untreated cell lines. Similarly, Doce and Doce conjugate 14 showed decrease in cell viability by 16 and 10%, respectively, after 72 h. The physical mixtures of Doce/peptide 9 showed a decrease in cell viability by 16% as compared to untreated cells.

   Click to Show/Hide
In Vitro Model Prostate carcinoma LNCaP C4-2 cell CVCL_4782
Experiment 6 Reporting the Activity Data of This PDC [1]
Indication Prostate cancer
Efficacy Data Cell viability
70%
Administration Time 72 h
Evaluation Method MTS assay
Description
An increase in the cytotoxicity of Dox and Dox/peptide 9 physical mixture as compared to the conjugate 13 over an incubation period of 24 h to 72 h. Conjugates 13 and 14 were found to be less cytotoxic as compared to drug alone in 24-72 h. These cells were not treated with TGF-, so very minimal or no overexpression of EDB-FN. Figure 10b showed the effect of overexpression of EDB-FN in the cell viability. There was no observed effect of TGF- treatment for the cytotoxicity of Dox and physical mixture of Dox/peptide 9 on the cell viability as compared to the TGF- untreated cell lines. However, conjugate 13 showed a decrease in cell viability by 17% after 72 h as compared to untreated cell lines. Similarly, Doce and Doce conjugate 14 showed decrease in cell viability by 16 and 10%, respectively, after 72 h. The physical mixtures of Doce/peptide 9 showed a decrease in cell viability by 16% as compared to untreated cells.

   Click to Show/Hide
In Vitro Model Prostate carcinoma LNCaP C4-2 cell CVCL_4782
Experiment 7 Reporting the Activity Data of This PDC [1]
Indication Prostate cancer
Efficacy Data Cell viability
74%
Administration Time 2 h
Administration Dosage 100 nM
Description
The conjugate 13, peptide 9, and Dox showed no significant toxicity at or below 10 μM, possibly due to the shorter incubation time of 2 h.
In Vitro Model Prostate carcinoma PC-3 cell CVCL_0035
Experiment 8 Reporting the Activity Data of This PDC [1]
Indication Prostate cancer
Efficacy Data Cell viability
75%
Administration Time 2 h
Administration Dosage 1 µM
Description
The conjugate 13, peptide 9, and Dox showed no significant toxicity at or below 10 μM, possibly due to the shorter incubation time of 2 h.
In Vitro Model Prostate carcinoma PC-3 cell CVCL_0035
Experiment 9 Reporting the Activity Data of This PDC [1]
Indication Prostate cancer
Efficacy Data Cell viability
77%
Administration Time 48 h
Evaluation Method MTS assay
Description
An increase in the cytotoxicity of Dox and Dox/peptide 9 physical mixture as compared to the conjugate 13 over an incubation period of 24 h to 72 h. Conjugates 13 and 14 were found to be less cytotoxic as compared to drug alone in 24-72 h. These cells were not treated with TGF-, so very minimal or no overexpression of EDB-FN. Figure 10b showed the effect of overexpression of EDB-FN in the cell viability. There was no observed effect of TGF- treatment for the cytotoxicity of Dox and physical mixture of Dox/peptide 9 on the cell viability as compared to the TGF- untreated cell lines. However, conjugate 13 showed a decrease in cell viability by 17% after 72 h as compared to untreated cell lines. Similarly, Doce and Doce conjugate 14 showed decrease in cell viability by 16 and 10%, respectively, after 72 h. The physical mixtures of Doce/peptide 9 showed a decrease in cell viability by 16% as compared to untreated cells.

   Click to Show/Hide
In Vitro Model Prostate carcinoma LNCaP C4-2 cell CVCL_4782
Experiment 10 Reporting the Activity Data of This PDC [1]
Indication Prostate cancer
Efficacy Data Cell viability
78%
Administration Time 48 h
Evaluation Method MTS assay
Description
An increase in the cytotoxicity of Dox and Dox/peptide 9 physical mixture as compared to the conjugate 13 over an incubation period of 24 h to 72 h. Conjugates 13 and 14 were found to be less cytotoxic as compared to drug alone in 24-72 h. These cells were not treated with TGF-, so very minimal or no overexpression of EDB-FN. Figure 10b showed the effect of overexpression of EDB-FN in the cell viability. There was no observed effect of TGF- treatment for the cytotoxicity of Dox and physical mixture of Dox/peptide 9 on the cell viability as compared to the TGF- untreated cell lines. However, conjugate 13 showed a decrease in cell viability by 17% after 72 h as compared to untreated cell lines. Similarly, Doce and Doce conjugate 14 showed decrease in cell viability by 16 and 10%, respectively, after 72 h. The physical mixtures of Doce/peptide 9 showed a decrease in cell viability by 16% as compared to untreated cells.

   Click to Show/Hide
In Vitro Model Prostate carcinoma LNCaP C4-2 cell CVCL_4782
Experiment 11 Reporting the Activity Data of This PDC [1]
Indication Prostate cancer
Efficacy Data Cell viability
98%
Administration Time 2 h
Administration Dosage 100 µM
Description
The conjugate 13, peptide 9, and Dox showed no significant toxicity at or below 10 μM, possibly due to the shorter incubation time of 2 h.
In Vitro Model Prostate carcinoma PC-3 cell CVCL_0035
Experiment 12 Reporting the Activity Data of This PDC [1]
Indication Prostate cancer
Efficacy Data Cell viability
102%
Administration Time 2 h
Administration Dosage 10 nM
Description
The conjugate 13, peptide 9, and Dox showed no significant toxicity at or below 10 μM, possibly due to the shorter incubation time of 2 h.
In Vitro Model Prostate carcinoma PC-3 cell CVCL_0035
Experiment 13 Reporting the Activity Data of This PDC [1]
Indication Prostate cancer
Efficacy Data Cell viability
105%
Administration Time 2 h
Administration Dosage 10 µM
Description
The conjugate 13, peptide 9, and Dox showed no significant toxicity at or below 10 μM, possibly due to the shorter incubation time of 2 h.
In Vitro Model Prostate carcinoma PC-3 cell CVCL_0035
Experiment 14 Reporting the Activity Data of This PDC [1]
Indication Prostate cancer
Efficacy Data Cell viability
108%
Administration Time 24 h
Evaluation Method MTS assay
Description
An increase in the cytotoxicity of Dox and Dox/peptide 9 physical mixture as compared to the conjugate 13 over an incubation period of 24 h to 72 h. Conjugates 13 and 14 were found to be less cytotoxic as compared to drug alone in 24-72 h. These cells were not treated with TGF-, so very minimal or no overexpression of EDB-FN. Figure 10b showed the effect of overexpression of EDB-FN in the cell viability. There was no observed effect of TGF- treatment for the cytotoxicity of Dox and physical mixture of Dox/peptide 9 on the cell viability as compared to the TGF- untreated cell lines. However, conjugate 13 showed a decrease in cell viability by 17% after 72 h as compared to untreated cell lines. Similarly, Doce and Doce conjugate 14 showed decrease in cell viability by 16 and 10%, respectively, after 72 h. The physical mixtures of Doce/peptide 9 showed a decrease in cell viability by 16% as compared to untreated cells.

   Click to Show/Hide
In Vitro Model Prostate carcinoma LNCaP C4-2 cell CVCL_4782
Experiment 15 Reporting the Activity Data of This PDC [1]
Indication Prostate cancer
Efficacy Data Cell viability
110%
Administration Time 24 h
Evaluation Method MTS assay
Description
An increase in the cytotoxicity of Dox and Dox/peptide 9 physical mixture as compared to the conjugate 13 over an incubation period of 24 h to 72 h. Conjugates 13 and 14 were found to be less cytotoxic as compared to drug alone in 24-72 h. These cells were not treated with TGF-, so very minimal or no overexpression of EDB-FN. Figure 10b showed the effect of overexpression of EDB-FN in the cell viability. There was no observed effect of TGF- treatment for the cytotoxicity of Dox and physical mixture of Dox/peptide 9 on the cell viability as compared to the TGF- untreated cell lines. However, conjugate 13 showed a decrease in cell viability by 17% after 72 h as compared to untreated cell lines. Similarly, Doce and Doce conjugate 14 showed decrease in cell viability by 16 and 10%, respectively, after 72 h. The physical mixtures of Doce/peptide 9 showed a decrease in cell viability by 16% as compared to untreated cells.

   Click to Show/Hide
In Vitro Model Prostate carcinoma LNCaP C4-2 cell CVCL_4782
Doce-βA-thioether-CGFLG-C6-[KTVRTSADE] [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 10 Activity Data Related to This Level
Experiment 1 Reporting the Activity Data of This PDC [1]
Indication Prostate cancer
Efficacy Data Cell viability
45%
Administration Time 72 h
In Vitro Model Prostate carcinoma LNCaP C4-2 cell CVCL_4782
Experiment 2 Reporting the Activity Data of This PDC [1]
Indication Prostate cancer
Efficacy Data Cell viability
55%
Administration Time 72 h
Evaluation Method MTS assay
Description
An increase in the cytotoxicity of Dox and Dox/peptide 9 physical mixture as compared to the conjugate 13 over an incubation period of 24 h to 72 h. Conjugates 13 and 14 were found to be less cytotoxic as compared to drug alone in 24-72 h. These cells were not treated with TGF-, so very minimal or no overexpression of EDB-FN. Figure 10b showed the effect of overexpression of EDB-FN in the cell viability. There was no observed effect of TGF- treatment for the cytotoxicity of Dox and physical mixture of Dox/peptide 9 on the cell viability as compared to the TGF- untreated cell lines. However, conjugate 13 showed a decrease in cell viability by 17% after 72 h as compared to untreated cell lines. Similarly, Doce and Doce conjugate 14 showed decrease in cell viability by 16 and 10%, respectively, after 72 h. The physical mixtures of Doce/peptide 9 showed a decrease in cell viability by 16% as compared to untreated cells.

   Click to Show/Hide
In Vitro Model Prostate carcinoma LNCaP C4-2 cell CVCL_4782
Experiment 3 Reporting the Activity Data of This PDC [1]
Indication Prostate cancer
Efficacy Data Cell viability
78%
Administration Time 48 h
Evaluation Method MTS assay
Description
An increase in the cytotoxicity of Dox and Dox/peptide 9 physical mixture as compared to the conjugate 13 over an incubation period of 24 h to 72 h. Conjugates 13 and 14 were found to be less cytotoxic as compared to drug alone in 24-72 h. These cells were not treated with TGF-, so very minimal or no overexpression of EDB-FN. Figure 10b showed the effect of overexpression of EDB-FN in the cell viability. There was no observed effect of TGF- treatment for the cytotoxicity of Dox and physical mixture of Dox/peptide 9 on the cell viability as compared to the TGF- untreated cell lines. However, conjugate 13 showed a decrease in cell viability by 17% after 72 h as compared to untreated cell lines. Similarly, Doce and Doce conjugate 14 showed decrease in cell viability by 16 and 10%, respectively, after 72 h. The physical mixtures of Doce/peptide 9 showed a decrease in cell viability by 16% as compared to untreated cells.

   Click to Show/Hide
In Vitro Model Prostate carcinoma LNCaP C4-2 cell CVCL_4782
Experiment 4 Reporting the Activity Data of This PDC [1]
Indication Prostate cancer
Efficacy Data Cell viability
80%
Administration Time 48 h
Evaluation Method MTS assay
Description
An increase in the cytotoxicity of Dox and Dox/peptide 9 physical mixture as compared to the conjugate 13 over an incubation period of 24 h to 72 h. Conjugates 13 and 14 were found to be less cytotoxic as compared to drug alone in 24-72 h. These cells were not treated with TGF-, so very minimal or no overexpression of EDB-FN. Figure 10b showed the effect of overexpression of EDB-FN in the cell viability. There was no observed effect of TGF- treatment for the cytotoxicity of Dox and physical mixture of Dox/peptide 9 on the cell viability as compared to the TGF- untreated cell lines. However, conjugate 13 showed a decrease in cell viability by 17% after 72 h as compared to untreated cell lines. Similarly, Doce and Doce conjugate 14 showed decrease in cell viability by 16 and 10%, respectively, after 72 h. The physical mixtures of Doce/peptide 9 showed a decrease in cell viability by 16% as compared to untreated cells.

   Click to Show/Hide
In Vitro Model Prostate carcinoma LNCaP C4-2 cell CVCL_4782
Experiment 5 Reporting the Activity Data of This PDC [1]
Indication Prostate cancer
Efficacy Data Cell viability
95%
Administration Time 72 h
Administration Dosage 5 µM
Evaluation Method MTS assay
Description
Dox conjugate 13 was moderately toxic with a reduced cell proliferation to a range of 25-35% as compared to Dox which reduced cell proliferation in the range of 20-34% for all selected four cell lines. However, it was interesting to observe that Doce conjugate 14 was almost nontoxic (cell proliferation within the range of 89-96%) in all the cell lines as compared to Doce alone which reduced the cell proliferation in the range of 54-61% (Figure 9).

   Click to Show/Hide
In Vitro Model Normal RWPE-1 cell CVCL_3791
Experiment 6 Reporting the Activity Data of This PDC [1]
Indication Prostate cancer
Efficacy Data Cell viability
95%
Administration Time 24 h
Evaluation Method MTS assay
Description
An increase in the cytotoxicity of Dox and Dox/peptide 9 physical mixture as compared to the conjugate 13 over an incubation period of 24 h to 72 h. Conjugates 13 and 14 were found to be less cytotoxic as compared to drug alone in 24-72 h. These cells were not treated with TGF-, so very minimal or no overexpression of EDB-FN. Figure 10b showed the effect of overexpression of EDB-FN in the cell viability. There was no observed effect of TGF- treatment for the cytotoxicity of Dox and physical mixture of Dox/peptide 9 on the cell viability as compared to the TGF- untreated cell lines. However, conjugate 13 showed a decrease in cell viability by 17% after 72 h as compared to untreated cell lines. Similarly, Doce and Doce conjugate 14 showed decrease in cell viability by 16 and 10%, respectively, after 72 h. The physical mixtures of Doce/peptide 9 showed a decrease in cell viability by 16% as compared to untreated cells.

   Click to Show/Hide
In Vitro Model Prostate carcinoma LNCaP C4-2 cell CVCL_4782
Experiment 7 Reporting the Activity Data of This PDC [1]
Indication Prostate cancer
Efficacy Data Cell viability
96%
Administration Time 72 h
Administration Dosage 5 µM
Evaluation Method MTS assay
Description
Dox conjugate 13 was moderately toxic with a reduced cell proliferation to a range of 25-35% as compared to Dox which reduced cell proliferation in the range of 20-34% for all selected four cell lines. However, it was interesting to observe that Doce conjugate 14 was almost nontoxic (cell proliferation within the range of 89-96%) in all the cell lines as compared to Doce alone which reduced the cell proliferation in the range of 54-61% (Figure 9).

   Click to Show/Hide
In Vitro Model Prostate carcinoma LNCaP cell CVCL_0395
Experiment 8 Reporting the Activity Data of This PDC [1]
Indication Prostate cancer
Efficacy Data Cell viability
98%
Administration Time 72 h
Administration Dosage 5 µM
Evaluation Method MTS assay
Description
Dox conjugate 13 was moderately toxic with a reduced cell proliferation to a range of 25-35% as compared to Dox which reduced cell proliferation in the range of 20-34% for all selected four cell lines. However, it was interesting to observe that Doce conjugate 14 was almost nontoxic (cell proliferation within the range of 89-96%) in all the cell lines as compared to Doce alone which reduced the cell proliferation in the range of 54-61% (Figure 9).

   Click to Show/Hide
In Vitro Model Prostate carcinoma PC-3 cell CVCL_0035
Experiment 9 Reporting the Activity Data of This PDC [1]
Indication Prostate cancer
Efficacy Data Cell viability
99%
Administration Time 72 h
Administration Dosage 5 µM
Evaluation Method MTS assay
Description
Dox conjugate 13 was moderately toxic with a reduced cell proliferation to a range of 25-35% as compared to Dox which reduced cell proliferation in the range of 20-34% for all selected four cell lines. However, it was interesting to observe that Doce conjugate 14 was almost nontoxic (cell proliferation within the range of 89-96%) in all the cell lines as compared to Doce alone which reduced the cell proliferation in the range of 54-61% (Figure 9).

   Click to Show/Hide
In Vitro Model Prostate carcinoma DU145 cell CVCL_0105
Experiment 10 Reporting the Activity Data of This PDC [1]
Indication Prostate cancer
Efficacy Data Cell viability
100%
Administration Time 24 h
Evaluation Method MTS assay
Description
An increase in the cytotoxicity of Dox and Dox/peptide 9 physical mixture as compared to the conjugate 13 over an incubation period of 24 h to 72 h. Conjugates 13 and 14 were found to be less cytotoxic as compared to drug alone in 24-72 h. These cells were not treated with TGF-, so very minimal or no overexpression of EDB-FN. Figure 10b showed the effect of overexpression of EDB-FN in the cell viability. There was no observed effect of TGF- treatment for the cytotoxicity of Dox and physical mixture of Dox/peptide 9 on the cell viability as compared to the TGF- untreated cell lines. However, conjugate 13 showed a decrease in cell viability by 17% after 72 h as compared to untreated cell lines. Similarly, Doce and Doce conjugate 14 showed decrease in cell viability by 16 and 10%, respectively, after 72 h. The physical mixtures of Doce/peptide 9 showed a decrease in cell viability by 16% as compared to untreated cells.

   Click to Show/Hide
In Vitro Model Prostate carcinoma LNCaP C4-2 cell CVCL_4782
References
Ref 1 EDB-FN Targeted Peptide-Drug Conjugates for Use against Prostate Cancer. Int J Mol Sci. 2019 Jul 4;20(13):3291. doi: 10.3390/ijms20133291.