Membrane Protein‐Instructed Peptide Self‐Assembly for Cancer Therapy

Abnormal membrane proteins often play a crucial role in the development and progression of cancer, making them ideal targets for cancer treatment. However, traditional membrane protein inhibitor‐based therapies only benefit a small part of patients and suffer from notorious drug resistance due to their occupation‐driven pharmacology. Recently, membrane protein‐instructed peptide self‐assembly has emerged as a powerful tool in precision cancer treatment. Due to its unique merits such as high tumor targeting specificity, long‐term membrane retention, and excellent functional scalability, this strategy is expected to effectively overcome key limitations of traditional membrane protein‐targeting anticancer strategies. This review summarizes research advances in membrane protein‐instructed peptide self‐assembly for cancer therapy over the past five years. First, we introduce the design principles and representative self‐assembly strategies. Subsequently, we highlight the applications and underlying mechanisms of this approach in various cancer treatment modalities, including chemotherapy, molecular targeted therapy, phototherapy, radiotherapy, immunotherapy, and image‐guided surgery. Finally, we briefly outline current challenges and future directions in this field.