QR-KLU

QR-KLU is a **peptide-drug conjugate (PDC)** designed for cancer therapy, specifically developed for combination with transarterial embolization (TAE) or transarterial chemoembolization (TACE) in hepatocellular carcinoma (HCC). The conjugate consists of two functional components: a VEGFR-targeting peptide **VEGF125-136** (sequence: QKRKRKKSRYKS, abbreviated as QR) linked to a **lytic peptide** (sequence: KLUKLUKKLUKLUK, abbreviated as KLU)[1]. The mechanism combines **dual functionality**: the QR component targets and binds to vascular endothelial growth factor receptor (VEGFR) on tumor endothelial cells and cancer cells, while the KLU component disrupts cell membranes through non-specific lytic activity[1]. This design enables both anti-angiogenic effects through VEGFR inhibition and direct cytotoxic effects through membrane disruption. In preclinical studies using VX2 rabbit tumor models, QR-KLU demonstrated superior anti-tumor activity compared to conventional chemotherapeutics like doxorubicin, achieving approximately 93% tumor necrosis rates[1]. The peptide showed enhanced cytotoxicity against both hepatocellular carcinoma cells (Huh7, IC50 7.3 ± 0.74 µM) and endothelial cells (HUVEC, IC50 10.7 ± 0.292 µM) compared to the lytic peptide alone[1]. QR-KLU also demonstrated favorable safety profiles with no significant liver or renal toxicity in animal models[1].

Other names

QKRKRKKSRYKS-KLUKLUKKLUKLUK