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ABT-510 Peptide

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11/22/2013

ABT-510 Peptide

ABT-510 is a synthetic peptide that mimics the anti-angiogenic activity of the endogenous protein thrombospondin-1 (TSP-1). This peptide mimics thrombospondin-1 (TSP-1), block angiogenesis in vitro and in vivo and slow tumor growth. It was developed by Abbott Laboratories for the treatment of Solid Tumors, Lymphoma and Melanoma. The systematic name for the ABT-510 peptide is N-Acetyl-N-methylglycylglycyl-L-valyl-D-isoleucyl-L-threonyl-L-norvalyl-L-isoleucyl-N5-(diaminomethylene)-L-ornithyl-N-ethyl-L-prolinamide with the  molecular formula C46H83N13O11, an average mass of 994.231689 Da, a monoisotopic mass of 993.633484 Da and the  ChemSpider ID 5293759. ABT-510 is an antiangionic TSP-1 modified nonapeptide that was designed using the 7-mer active sequence GVITRIR of the second type I repeat as the target sequence. ABT-510 inhibits the formation of new blood vessels. Furthermore, ABT-510 inhibits the actions of several pro-angiogenic growth factors important to tumor neovascularization. In addition, the modified TSR peptide ABT-510 inhibits malignant glioma growth in vivo and induces apoptosis of brain microvessel endothelial cells (MvEC) propagated in vitro. ABT-510 also increases active TGF-1 levels in tumors. The term “neovascularization” describes the proliferation of blood vessels in tissue not normally containing them or the proliferation of blood vessels of a different kind than usual present in tissue. These pro-angiogenic growth factors include vascular endothelial growth factor (VEGF), basic fibroblast growth factor (bFGF), hepatocyte growth factor (HGF), and interleukin 8 (IL-8). Thrombospondin 1 (TSP-1) is a large multifunctional glycoprotein involved in multiple biological processes including angiogenesis, apoptosis, and activation of TGF-1. ABT-510 is a TSP-1 synthetic analog that mimic its antiangiogenic action. Tumors that over express TSP-1 grow slower, have fewer metastases, and decreased angiogenesis. Therefore, TSP-1 provides a novel target for the treatment of cancer.

ABT510 peptide

ABT510 peptide: Ac-Sar-Gly-Val-DIle-Thr-Nva-Ile-Arg-Pro-NHCH2CH3

Reference

Joshua C. Anderson, J. Robert Grammer, Wenquan Wang, L. Burton Nabors, Jack Henkin, Jerry E. Stewart Jr., Candece L. Gladson;  ABT-510, a Modified Type 1 Repeat Peptide of Thrombospondin, Inhibits Malignant Glioma Growth In Vivo by Inhibiting Angiogenesis.  Cancer Biology & Therapy 6:3, 454-462; March 2007]; ©2007 Landes Bioscience