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Research citation

Rational design of a potent macrocyclic peptide inhibitor targeting the PD-1/PD-L1 protein-protein interaction.

Animal StudyModerate evidence

This record provides bibliographic details and links to the original research. An editorial study breakdown is not available.

What the researchers found

JMPDP-027 cyclic peptide blocked PD-1/PD-L1 with EC50 of 5.9 nM (comparable to pembrolizumab) and showed potent in vivo anticancer activity.

Why it matters

Antibody checkpoint inhibitors revolutionized cancer treatment but are expensive. Peptide alternatives could make immunotherapy more accessible.

The numbers in context

EC50 5.9 nM; comparable to pembrolizumab; serum stable; no toxicity; in vivo efficacy ≈ anti-PD-L1 mAb

How the study worked

Rational design and optimization of macrocyclic peptide. T cell restoration assay, serum stability, cytotoxicity, and CT26 colon carcinoma mouse model.

Who was studied

CT26 colon carcinoma mouse model

What this study cannot tell us

Single mouse tumor model. Manufacturing scalability not demonstrated. Long-term pharmacokinetics and safety unknown. Head-to-head with pembrolizumab not done in vivo.

Read the original research

Rational design of a potent macrocyclic peptide inhibitor targeting the PD-1/PD-L1 protein-protein interaction.

RSC advances, 11(38), 23270-23279

Citation

Miao, Qi; Zhang, Wanheng; Zhang, Kuojun; Li, He; Zhu, Jidong; Jiang, Sheng. (2021). Rational design of a potent macrocyclic peptide inhibitor targeting the PD-1/PD-L1 protein-protein interaction.. RSC advances, 11(38), 23270-23279. https://doi.org/10.1039/d1ra03118j