General Information of This Peptide-drug Conjugate (PDC)
PDC ID
PDC_00252
PDC Name
NLG-RGD
PDC Status
Investigative
Indication
In total 1 Indication(s)
Tumor
Structure
Peptide Name
c[DKP-RGD]
 Peptide Info 
Receptor Name
Indoleamine 2,3-dioxygenase 1 (IDO1)
 Receptor Info 
Drug Name
NLG919
 Drug Info 
Therapeutic Target
Indoleamine 2,3-dioxygenase 1 (IDO1)
 Target Info 
Linker Name
Succinic Acid
 Linker Info 
Peptide Modified Type
Modification by dosage
Modified Segment
Self-assemble
Formula
C48H63N15O12
#Ro5 Violations (Lipinski): 4 Molecular Weight 1042.125
Lipid-water partition coefficient (xlogp) -1.1686
Hydrogen Bond Donor Count (hbonddonor) 12
Hydrogen Bond Acceptor Count (hbondacc) 15
Rotatable Bond Count (rotbonds) 29
Full List of Activity Data of This Peptide-drug Conjugate
Obtained from the Model Organism Data
Click To Hide/Show 6 Activity Data Related to This Level
Experiment 1 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Percentage of CD4 T cells
32%
Administration Time 30 min
Administration Dosage 25 µM
Evaluation Method Quantification of tumor-infiltrating immune cells assay
MOA of PDC
Significantly, this nanoinhibitor boosts the antitumor immune response of PD-L1 blockade by increasing immune effector cells and reducing immunosuppressive cells.
Description
These findings support that aPD-L1 plus NLG-RGD NI efficiently elicits antitumor immunity by enhancing the activation and survival of immune effector cells and attenuating the accumulation immunosuppressive Treg cells.
In Vivo Model Pan02 tumor model.
In Vitro Model Normal CD4 T cell Homo sapiens
Experiment 2 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Percentage of CD8 T cells
34%
Administration Time 30 min
Administration Dosage 25 µM
Evaluation Method Quantification of tumor-infiltrating immune cells assay
MOA of PDC
Significantly, this nanoinhibitor boosts the antitumor immune response of PD-L1 blockade by increasing immune effector cells and reducing immunosuppressive cells.
Description
These findings support that aPD-L2 plus NLG-RGD NI efficiently elicits antitumor immunity by enhancing the activation and survival of immune effector cells and attenuating the accumulation immunosuppressive Treg cells.
In Vivo Model Pan02 tumor model.
In Vitro Model Normal CD8 T cell Homo sapiens
Experiment 3 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Percentage of IFN-γ-producing CD4 T cells
16%
Administration Time 30 min
Administration Dosage 25 µM
Evaluation Method Quantification of tumor-infiltrating immune cells assay
MOA of PDC
Significantly, this nanoinhibitor boosts the antitumor immune response of PD-L1 blockade by increasing immune effector cells and reducing immunosuppressive cells.
Description
These findings support that aPD-L3 plus NLG-RGD NI efficiently elicits antitumor immunity by enhancing the activation and survival of immune effector cells and attenuating the accumulation immunosuppressive Treg cells.
In Vivo Model Pan02 tumor model.
In Vitro Model Normal IFN-gamma-producing CD4 T cell Homo sapiens
Experiment 4 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Percentage of IFN-γ-producing CD8 T cells
40%
Administration Time 30 min
Administration Dosage 25 µM
Evaluation Method Quantification of tumor-infiltrating immune cells assay
MOA of PDC
Significantly, this nanoinhibitor boosts the antitumor immune response of PD-L1 blockade by increasing immune effector cells and reducing immunosuppressive cells.
Description
These findings support that aPD-L4 plus NLG-RGD NI efficiently elicits antitumor immunity by enhancing the activation and survival of immune effector cells and attenuating the accumulation immunosuppressive Treg cells.
In Vivo Model Pan02 tumor model.
In Vitro Model Normal IFN-gamma-producing CD4 T cell Homo sapiens
Experiment 5 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Percentage of NK cells
2%
Administration Time 30 min
Administration Dosage 25 µM
Evaluation Method Quantification of tumor-infiltrating immune cells assay
MOA of PDC
Significantly, this nanoinhibitor boosts the antitumor immune response of PD-L1 blockade by increasing immune effector cells and reducing immunosuppressive cells.
Description
These findings support that aPD-L6 plus NLG-RGD NI efficiently elicits antitumor immunity by enhancing the activation and survival of immune effector cells and attenuating the accumulation immunosuppressive Treg cells.
In Vivo Model Pan02 tumor model.
In Vitro Model Normal Natural killer cell Homo sapiens
Experiment 6 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Percentage of Treg cells
1%
Administration Time 30 min
Administration Dosage 25 µM
Evaluation Method Quantification of tumor-infiltrating immune cells assay
MOA of PDC
Significantly, this nanoinhibitor boosts the antitumor immune response of PD-L1 blockade by increasing immune effector cells and reducing immunosuppressive cells.
Description
These findings support that aPD-L5 plus NLG-RGD NI efficiently elicits antitumor immunity by enhancing the activation and survival of immune effector cells and attenuating the accumulation immunosuppressive Treg cells.
In Vivo Model Pan02 tumor model.
In Vitro Model Normal Regulatory CD4+ T cell Homo sapiens
References
Ref 1 Modularly Designed Peptide Nanoprodrug Augments Antitumor Immunity of PD-L1 Checkpoint Blockade by Targeting Indoleamine 2,3-Dioxygenase. J Am Chem Soc. 2020 Feb 5;142(5):2490-2496. doi: 10.1021/jacs.9b12232. Epub 2020 Jan 24.