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IQ motif containing GTPase activating protein 1
(IQGAP1); MAP kinase 1 (MAPK1; ERK-2); MAPK3 (ERK-1)

Cell culture and mouse studies identified a peptide-based inhibitor of IQGAP1 that could help treat cancer. A 32-amino-acid residue domain of IQGAP1 that interacts with ERK-1 and ERK-2 was isolated and subsequently modified with a Tat peptide sequence to improve cell permeability. In a mouse model for pancreatic cancer, intraperitoneal injection of the peptide increased survival compared with injection of a scrambled peptide. In cultured, drug-resistant BRAF mutant melanoma cell lines, the peptide decreased growth compared with a scrambled peptide. Next steps include further developing peptide and small molecule inhibitors of IQGAP1.

SciBX 6(18); doi:10.1038/scibx.2013.435
Published online May 9, 2013

Patent application filed; available for licensing

Jameson, K.L. et al. Nat. Med.; published online April 21, 2013;
Contact: Paul A. Khavari, Stanford University School of Medicine, Stanford, Calif.