title: Minimal C-terminal modification boosts peptide self-assembling ability for necroptosis of cancer cells.
abstract: Here we reported the first case in which enhancing self-assembling ability boosts anti-cancer efficacy through a simple and minimal modification of the C-terminus of a d-tripeptide. By only a 2% change of the molecular weight, this facile approach increases the inhibitory activity by over an order of magnitude (IC50 from 431 to 23 μM) towards an osteosarcoma cell line.
authors.affiliation: Department of Chemistry, Brandeis University, 415 South Street, Waltham, Massachusetts 02454, USA. bxu@brandeis.edu.
authors.forename: Zhaoqianqi
authors.initials: Z
authors.lastname: Feng
authors.forename: Huaimin
authors.initials: H
authors.lastname: Wang
authors.forename: Xuewen
authors.initials: X
authors.lastname: Du
authors.forename: Junfeng
authors.initials: J
authors.lastname: Shi
authors.forename: Jie
authors.initials: J
authors.lastname: Li
authors.forename: Bing
authors.initials: B
authors.lastname: Xu
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D002460:Cell Line; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D015394:Molecular Structure; D008970:Molecular Weight; D009842:Oligopeptides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D012516:Osteosarcoma / Q000188:drug therapy* / Q000473:pathology*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D009842:Oligopeptides