iRGD peptide TFA salt

Description: iRGD peptide (sequence: CRGDKGPDC) is a 9-amino acid cyclic peptide, and a molecular mimicry agent that was originally identified in an in vivo screening of phage display libraries in tumor-bearing mice. It triggers tissue penetration of drugs by first binding to av integrins, then proteolytically cleaved in the tumor to produce CRGDK/R to interact with neuropilin-1, and has tumor-targeting and tumor-penetrating properties. The peptide was able to home to tumor tissues, but in contrast to standard RGD (Arginylglycylaspartic acid)peptides, also spread much more extensively into extravascular tumortissue. It was later identified that this extravasation and transportthrough extravascular tumor tissue was due to the bifunctional action ofthe molecule: after the initial RGD-mediated tumor homing, anotherpharmacological motif is able to manipulate tumor microenvironment, making it temporarily accessible to circulating drugs. This second stepis mediated through specific secondary binding to neuropilin-1 receptor, and subsequent activation of a trans-tissue pathway, dubbed the C-end Rule (CendR) pathway.

References:

1. Puig-SausC, et al. iRGD tumor-penetrating peptide-modified oncolytic adenovirusshows enhanced tumor transduction, intratumoral dissemination andantitumor efficacy. Gene Ther. 2014 Aug; 21(8):767-74.

2. ZhangL, et al. Combination of NRP1-mediated iRGD with 5-fluorouracilsuppresses proliferation, migration and invasion of gastric cancercells. Biomed Pharmacother. 2017 Sep; 93:1136-1143.