General Information of This Peptide
Peptide ID
PEP00014
Peptide Name
CGVVQQ
Structure
Sequence
CGVVQQ
Peptide Type
Linear
Receptor Name
Integrin alpha-V (ITGAV)
 Receptor Info 
PDC Transmembrane Types Cell targeting peptides (CTPs)
Formula
C25H44N8O9S
Isosmiles
[H]NC(=O)CC[C@H](NC(=O)[C@H](CCC(=O)N[H])NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CS[H])N[H])C(C)C)C(C)C)C(=O)O
InChI
InChI=1S/C25H44N8O9S/c1-11(2)19(32-18(36)9-29-21(37)13(26)10-43)24(40)33-20(12(3)4)23(39)30-14(5-7-16(27)34)22(38)31-15(25(41)42)6-8-17(28)35/h11-15,19-20,43H,5-10,26H2,1-4H3,(H2,27,34)(H2,28,35)(H,29,37)(H,30,39)(H,31,38)(H,32,36)(H,33,40)(H,41,42)/t13-,14-,15-,19-,20-/m0/s1
InChIKey
OPSDYZLPBCNMJG-QEFISFJRSA-N
Pharmaceutical Properties
Molecule Weight
632.741
Polar area
295
Complexity
632.295196
xlogp Value
-3.7735
Heavy Count
43
Rot Bonds
22
Hbond acc
10
Hbond Donor
10
Each Peptide-drug Conjugate Related to This Peptide
Full Information of The Activity Data of The PDC(s) Related to This Peptide
SN38-HKD [Investigative]
Identified from the Human Clinical Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Data of This PDC [1]
Indication Triple-negative breast cancer
Efficacy Data Tumor Growth Inhibition value (TGI)
43% (Day 14)
Administration Time 4-injection regimen (on day 0, 2, 4, and 6)
Administration Dosage 10 mg/kg
Evaluation Method Tumor volume detection assay
MOA of PDC
N38-HKD increases infiltration, activity, and viability of CD8+T cells, and thus inhibits the growth of primary tumors and pulmonary metastasis. This study highlights the synergistic modulation of cancerous cells and TECs with integrin-targeting PDC filaments as a promising strategy for TNBC chemoimmunotherapy.
Description
SN38-HKD/RGDR slowed the 4T1 tumor growth by 74%, while irinotecan and SN38-HKD only showed 28% and 43% tumor growth inhibition, respectively, which was further confirmed by its capability in reducing tumor burden.
In Vivo Model 4T1 tumor-bearing mice.
In Vitro Model Mammary carcinoma 4T1 cell CVCL_0125
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Data of This PDC [1]
Indication Triple-negative breast cancer
Efficacy Data Tumor Growth Inhibition value (TGI)
40% (Day 18)
Administration Time 4-injection regimen (on day 0, 2, 4, and 6)
Administration Dosage 10 mg/kg
Evaluation Method Tumor volume detection assay
MOA of PDC
N38-HKD increases infiltration, activity, and viability of CD8+T cells, and thus inhibits the growth of primary tumors and pulmonary metastasis. This study highlights the synergistic modulation of cancerous cells and TECs with integrin-targeting PDC filaments as a promising strategy for TNBC chemoimmunotherapy.
Description
SN38-HKD/RGDR slowed the 4T1 tumor growth by 74%, while irinotecan and SN38-HKD only showed 28% and 43% tumor growth inhibition, respectively, which was further confirmed by its capability in reducing tumor burden.
In Vivo Model EMT6 tumor-bearing mice.
In Vitro Model Mammary gland malignant neoplasms EMT6 cell CVCL_1923
SN38-HKD/RGDR [Investigative]
Identified from the Human Clinical Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Data of This PDC [1]
Indication Triple-negative breast cancer
Efficacy Data Tumor Growth Inhibition value (TGI)
74% (Day 14)
Administration Time 4-injection regimen (on day 0, 2, 4, and 6)
Administration Dosage 10 mg/kg
Evaluation Method Tumor volume detection assay
MOA of PDC
N38-HKD/RGDR increases infiltration, activity, and viability of CD8+ T cells, and thus inhibits the growth of primary tumors and pulmonary metastasis. This study highlights the synergistic modulation of cancerous cells and TECs with integrin-targeting PDC filaments as a promising strategy for TNBC chemoimmunotherapy.
Description
SN38-HKD/RGDR slowed the 4T1 tumor growth by 74%, while irinotecan and SN38-HKD only showed 28% and 43% tumor growth inhibition, respectively, which was further confirmed by its capability in reducing tumor burden.
In Vivo Model 4T1 tumor-bearing mice.
In Vitro Model Mammary carcinoma 4T1 cell CVCL_0125
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Data of This PDC [1]
Indication Triple-negative breast cancer
Efficacy Data Tumor Growth Inhibition value (TGI)
75% (Day 18)
Administration Time 4-injection regimen (on day 0, 2, 4, and 6)
Administration Dosage 10 mg/kg
Evaluation Method Tumor volume detection assay
MOA of PDC
N38-HKD/RGDR increases infiltration, activity, and viability of CD8+T cells, and thus inhibits the growth of primary tumors and pulmonary metastasis. This study highlights the synergistic modulation of cancerous cells and TECs with integrin-targeting PDC filaments as a promising strategy for TNBC chemoimmunotherapy.
Description
SN38-HKD/RGDR slowed the 4T1 tumor growth by 74%, while irinotecan and SN38-HKD only showed 28% and 43% tumor growth inhibition, respectively, which was further confirmed by its capability in reducing tumor burden.
In Vivo Model EMT6 tumor-bearing mice.
In Vitro Model Mammary gland malignant neoplasms EMT6 cell CVCL_1923
References
Ref 1 Inhibiting Endothelial Cell-Mediated T Lymphocyte Apoptosis with Integrin-Targeting Peptide-Drug Conjugate Filaments for Chemoimmunotherapy of Triple-Negative Breast Cancer. Adv Mater. 2024 Jan;36(3):e2306676. doi: 10.1002/adma.202306676. Epub 2023 Nov 30.