236-237 - Diastereomer Lytic Peptides for Treatment of Solid Tumors and Metastasis
Description: 15-mer (Leu-Lys-Dleu- Leu-Lys-Dlys-Leu-Dleu-Dlys-Lys-Leu-Leu-Dlys-Leu-Leu) and 15-mer Histidin (H-Leu-Lys-D-Leu- Leu-His-D-Lys-Leu-D-Leu-D-Lys-His-Leu-Leu-D-Lys-Leu-Leu-NH2) are membrane-active peptides composed of both D- and L amino acids (diastereomers). These peptides have demonstrated potent anti-cancer and anti metastatic activities in several animal models including models for prostate and lung cancer. They were shown to successfully inhibit tumor growth when injected intratumorally or intraveneously. The 15-mer Histidine form shows reduced systemic toxicity.
References: Papo N, Braunstein A, Eshhar Z, Shai Y. 2004. Suppression of human prostate tumor growth in mice by a cytolytic D-, L-amino Acid Peptide: membrane lysis, increased necrosis, and inhibition of prostate-specific antigen secretion. Cancer Res. 64(16):5779-86.
Makovitzki A1, Fink A, Shai Y. 2009. Suppression of human solid tumor growth in mice by intratumor and systemic inoculation of histidine-rich and pH-dependent host defense-like lytic peptides. Cancer Res. 69(8):3458-63.