Lactaptin

Lactaptin is a naturally occurring peptide derived from human milk kappa-casein (residues 57–134); its recombinant analogue, RL2, induces apoptosis in a variety of tumor cells through the mitochondrial (intrinsic) pathway. RL2 enters cells, dissipates the mitochondrial membrane potential, activates initiator caspases (caspases 8, 9) and effector caspases (caspases 3, 7), downregulates anti-apoptotic Bcl-2 protein, and leads to p53-independent apoptotic cell death. Notably, RL2 also modulates autophagy and its cytotoxicity can be enhanced by autophagy inhibitors. RL2 and related peptides show potential as novel anticancer therapeutics, being effective against several tumor cell types while sparing non-malignant cells[1][2][8][9][10]. Key clarification: The submitted \"target\" is not a classical drug target (e.g. protein receptor or enzyme); lactaptin and its recombinant analogue RL2 act as effector peptides to induce cell death, not as therapeutic targets themselves. The core mechanistic focus is on their ability to trigger the mitochondrial pathway of apoptosis in cancer cells.

Other names

RL2recombinant analogue RL2human milk pro-apoptotic peptidekappa-casein (fragment)

Induction of mitochondria-mediated apoptosis via dissipation of mitochondrial membrane potential, activation of initiator caspases (caspase-8, caspase-9), activation of effector caspases (caspase-3, -7), downregulation of Bcl-2, p53-independent cell death; can also modulate autophagy