Targeting Carcinoma-Associated Fibroblasts Within the Tumor Stroma With a Fibroblast Activation Protein-Activated Prodrug | Zendy

W. Nathaniel Brennen | Zendy; David Rosen | Zendy; H. Wang | Zendy; John T. Isaacs | Zendy; Samuel R. Denmeade | Zendy

Open Access

Targeting Carcinoma-Associated Fibroblasts Within the Tumor Stroma With a Fibroblast Activation Protein-Activated Prodrug

Author(s) -

W. Nathaniel Brennen,

David Rosen,

H. Wang,

John T. Isaacs,

Samuel R. Denmeade

Publication year - 2012

Publication title -

jnci journal of the national cancer institute

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 5.797

H-Index - 356

eISSN - 1460-2105

pISSN - 0027-8874

DOI - 10.1093/jnci/djs336

Subject(s) - fibroblast activation protein, alpha , fibroblast , prodrug , cancer research , chemistry , cytotoxic t cell , tumor microenvironment , thapsigargin , neoplastic transformation , microbiology and biotechnology , biology , intracellular , cancer , biochemistry , carcinogenesis , in vitro , tumor cells , genetics , gene

Fibroblasts undergo a morphological transformation to a reactive phenotype in the tumor microenvironment characterized by the expression of proteins such as fibroblast activation protein (FAP), a post-prolyl endopeptidase with expression largely restricted to carcinoma-associated fibroblasts. Thapsigargin (TG) is a highly toxic natural plant product that triggers a rise in intracellular calcium levels and apoptosis. FAP is therefore a provocative target for the activation of prodrugs consisting of a FAP-specific peptide coupled to a potent cytotoxic analog of TG.

The content you want is available to Zendy users.

Already have an account? Click here to sign in.

Having issues? You can contact us here

Accelerating Research