Ukrainskaya V M, Bobik T V, Argentova-Stevens A, Slutskaya E A, Kalinin R S, Gabibov A G, Stepanov A V
Laboratory of Biocatalysis, M. M. Shemyakin and Yu. A. Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, Moscow, Russia.
Bull Exp Biol Med. 2018 Jul;165(3):386-389. doi: 10.1007/s10517-018-4176-9. Epub 2018 Jul 12.
Death receptor 5 (DR5) is a promising target for antitumor therapy due to its high expression on different tumor cells. Resistance of various tumor cells against TRAIL, a natural ligand for the death receptors, reduces its therapeutic potential and prompts the search for novel agonists at these receptors. Previous screening across the combinatorial peptide library yielded a peptide sequence KVVLTHR that specifically binds DR5. Incorporation of this sequence into TNFα resulted in binding DR5 with mutant protein TNFα-mut and appearance of cytotoxicity against lymphoma cells.
死亡受体5（DR5）因其在不同肿瘤细胞上的高表达而成为抗肿瘤治疗的一个有前景的靶点。各种肿瘤细胞对死亡受体的天然配体TRAIL产生抗性，降低了其治疗潜力，并促使人们寻找这些受体的新型激动剂。先前对组合肽库的筛选产生了一个特异性结合DR5的肽序列KVVLTHR。将该序列整合到TNFα中导致其与突变蛋白TNFα-mut结合，并对淋巴瘤细胞产生细胞毒性。
