cyclic peptide PROTAC

The cyclic peptide PROTAC refers to a specific proteolysis-targeting chimera (PROTAC) described in research (PMID 37849747) that utilizes a cyclic peptide ligand to target the palmitoyltransferase DHHC3 (ZDHHC3) for degradation. By inducing the proteasomal degradation of DHHC3, the agent inhibits the palmitoylation of Programmed cell death 1 ligand 1 (PD-L1), a critical post-translational modification required for PD-L1 stability and cell-surface expression. This reduction in PD-L1 levels aims to overcome immune evasion in tumors, specifically studied in human cervical cancer models. The cyclic peptide design offers improved stability and degradation efficiency compared to earlier linear peptide versions, providing a more sustained anti-PD-L1 effect.

Other names

cyclic peptide-based PROTACDHHC3-degrading cyclic peptide PROTACDHHC-3-degrading cyclic peptide PROTACDHHC 3-degrading cyclic peptide PROTAC