AUNP-12

AUNP-12（CAS No. 1353563-85-5）is a competitive antagonist targeting the PD-1/PD-L1 pathway. The peptide sequence is Ser-Asn-Thr-Ser-Glu-Ser-Phe-Lys(Ser-Asn-Thr-Ser-Glu-Ser-Phe)-Phe-Arg-Val-Thr-Gln-Leu-Ala-Pro-Lys-Ala-Gln-Ile-Lys-Glu-NH2. By antagonizing the binding of PD-1 to PD-L1 and PD-L2, it blocks immunosuppressive signaling, participates in regulating the PD-1/PD-L1 immune checkpoint pathway, and thereby restores T-cell activity, promotes dendritic cell maturation, and remodels the tumor immune microenvironment.

In cell culture, it is mainly used for in vitro PD-L1-targeted binding validation, T-cell activation, and dendritic cell maturation assays; the commonly used competitive binding concentration is 6μg/mL.

Common animal study models include mouse 4T1 breast cancer, CT26 colorectal cancer, B16F10 melanoma, and MDA-MB-231/MCF-7 breast cancer tumor models.

In animal studies, the intravenous dose is 2mg/kg when used as a fluorescence imaging probe; the intraperitoneal / intravenous dose is 3mg/kg/ day (for 14 consecutive days) when used as a therapeutic peptide; when used as a component for nanomedicine modification, it can exert effects via tumor microenvironment-responsive release; it can also be used for preclinical tumor immunotherapy and near-infrared fluorescence molecular imaging research.

References:

[1] Cheng Y, Chen Q, Guo Z, Li M, Yang X, Wan G, Chen H, Zhang Q, Wang Y. An Intelligent Biomimetic Nanoplatform for Holistic Treatment of Metastatic Triple-Negative Breast Cancer via Photothermal Ablation and Immune Remodeling. ACS Nano. 2020 Nov 24;14(11):15161-15181. doi: 10.1021/acsnano.0c05392. Epub 2020 Nov 4. PMID: 33143424.

[2] Hu C, Song Y, Zhang Y, He S, Liu X, Yang X, Gong T, Huang Y, Gao H. Sequential delivery of PD-1/PD-L1 blockade peptide and IDO inhibitor for immunosuppressive microenvironment remodeling via an MMP-2 responsive dual-targeting liposome. Acta Pharm Sin B. 2023 May;13(5):2176-2187. doi: 10.1016/j.apsb.2023.02.009. Epub 2023 Feb 21. PMID: 37250156; PMCID: PMC10213972.

[3] Hao Y, Liu T, Zhou H, Peng J, Li K, Chen Y. The GSH responsive indocyanine green loaded PD-1 inhibitory polypeptide AUNP12 modified MOF nanoparticles for photothermal and immunotherapy of melanoma. Front Bioeng Biotechnol. 2023 Oct 19;11:1294074. doi: 10.3389/fbioe.2023.1294074. PMID: 37929188; PMCID: PMC10622763.

[4] Zhang X, Wang P, Shi G, Tang C, Xue H. AUNP-12 Near-Infrared Fluorescence Probes across NIR-I to NIR-II Enable In Vivo Detection of PD-1/PD-L1 Axis in the Tumor Microenvironment. Bioconjug Chem. 2024 Jul 17;35(7):1064-1074. doi: 10.1021/acs.bioconjchem.4c00266. Epub 2024 Jul 9. PMID: 38980173; PMCID: PMC11261610.