Research progress on the role of fibroblast activation protein in diagnosis and treatment of cancer

Abstract

Fibroblast activation protein (FAP) is a type II transmembrane protein, which is over-expressed in cancer-associated fibroblasts (CAFs). CAFs are tumor stromal cells that constitute a major component of cancer volume and are reportedly related to tumorigenesis, angiogenesis, metastasis, promotion of drug resistance and induction of tumor immunity. FAP is widely acknowledged as the signature protein of CAFs. At present, FAP inhibitors (FAPI) have achieved ideal results in tumor PET/computed tomography (CT) imaging. Theoretically, FAP-targeted drugs can inhibit tumor progression. Nonetheless, no satisfactory therapeutic effect has been observed so far, which has impeded their implementation in clinical practice. In this review, we describe the characteristics of FAP and its role in the occurrence and development of cancer. We also highlight the potential value of targeting FAP to improve current diagnostic and therapeutic approaches.

Synthesis and Preclinical Evaluation of Novel 99mTc-Labeled FAPI-46 Derivatives with Significant Tumor Uptake and Improved Tumor-to-Nontarget Ratios

“…In addition, stroma accounts for a high proportion (50–90%) of tumor components . Fibroblast activation protein (FAP) is a type II transmembrane serine protease (170 kDa) that is overexpressed in CAFs and is recognized as the signature protein of CAFs . Moreover, more than 90% of epithelial tumors are FAP positive, , and FAP-positive cells are less susceptible to antigen loss and treatment resistance than are tumor cells, making them important targets for diagnosis and therapy in recent years.…”

Preclinical evaluation and first-in-human study of Al18F-FAP-NUR for PET imaging cancer-associated fibroblasts

“…Fibroblast activation protein (FAP) is speci cally upregulated on the cell surface of cancer-associated broblasts (CAFs) but has little or no expression in quiescent broblasts within normal adult tissues [1][2][3][4][5]. The differential expression pattern highlights the important role of FAP as a potential target for cancer imaging and therapy [6][7][8][9][10].…”