LPrA2

LPrA2 is a 26-amino acid peptide antagonist of the leptin receptor (Ob-R) corresponding to residues 70–95 of human leptin (Site II, arm b). Developed by researchers at the Morehouse School of Medicine, LPrA2 competitively binds to the leptin receptor, thereby blocking leptin-mediated signaling pathways such as JAK2/STAT3, MAPK/ERK, and PI3K/Akt. This inhibition suppresses the expression of pro-angiogenic and pro-proliferative downstream targets, including VEGF, VEGFR2, and cyclin D1. LPrA2 has been investigated as a potential therapeutic agent for obesity-related cancers, particularly breast cancer (including triple-negative breast cancer) and pancreatic cancer. To overcome its poor aqueous solubility and short half-life, LPrA2 is frequently evaluated in modified formulations, such as pegylated (PEG-LPrA2) or iron oxide nanoparticle-conjugated (IONP-LPrA2) forms.

Other names

leptin peptide receptor antagonist 2leptin receptor antagonist 2