CGFYWLRSC-GG-D(KLAKLAK)2

CGFYWLRSC-GG-D(KLAKLAK)2 is a targeted pro-apoptotic peptidomimetic designed for the treatment of hematological malignancies, including leukemia and lymphoma. It consists of a neuropilin-1 (NRP-1) binding motif (CGFYWLRSC) linked via a diglycine (GG) spacer to a pro-apoptotic peptide sequence, D(KLAKLAK)2. The targeting motif binds to NRP-1, a transmembrane glycoprotein overexpressed on malignant hematopoietic cells and solid tumors, facilitating receptor-mediated internalization. Once inside the cell, the D(KLAKLAK)2 moiety disrupts mitochondrial membranes, inducing apoptosis. Research conducted at MD Anderson Cancer Center has demonstrated potent anti-leukemic effects in human leukemia and lymphoma cell lines and patient-derived AML and ALL specimens, while sparing normal bone marrow cells.

Other names

NRP-1 binding pro-apoptotic peptideNRP1 binding pro-apoptotic peptideNRP 1 binding pro-apoptotic peptide