RKL

RKL is a novel peptide-based degrader targeting N6-methyladenosine (m6A) methyltransferase-like 3 (METTL3). Developed by researchers at the Fourth Military Medical University and Hunan University, RKL is designed to address immune escape and resistance to immunotherapy in advanced urothelial carcinoma (aUC). METTL3 is often significantly upregulated in aUC, where it contributes to tumor progression and resistance to immune checkpoint inhibitors (ICIs) by promoting the expression of genes that regulate cancer-associated fibroblast proliferation. RKL functions as a targeted protein degrader, utilizing a peptide-based approach to induce the degradation of the METTL3 protein. In preclinical models, RKL has demonstrated high toxicity to urothelial carcinoma cell lines and significant synergistic antitumor activity when combined with ICIs, leading to high complete response rates in mouse models.

Other names

METTL3 peptide degrader RKLMETTL-3 peptide degrader RKLMETTL 3 peptide degrader RKL