膜活性多肽纳米制剂及抗肿瘤治疗作用研究数据集

抗肿瘤药物的治疗模式由化学治疗，靶向治疗，到免疫治疗一路不断发展，各显所长。然而在临床上，肿瘤治疗始终面临着多药耐药、治疗面窄、应答率低等问题。“膜活性药物”作为一种基于新理念的治疗模式，受到自然进化中广泛存在的以破坏生物膜为手段的细胞杀伤方式的启发（例如针对微生物的宿主防御、真核细胞的炎性死亡、T细胞介导的打孔杀伤等），有望避免或极大改善药物耐药现象，且能实现对免疫系统的广谱性激活，从而可能成为一类强有力的新型广谱型抗肿瘤药物。本课题开展了利用阳离子疏水性多肽调控癌细胞ROS水平实现选择性杀伤、克服多药耐药、以及激活机体抗癌免疫效应的研究，并在此类药物的活体抑瘤研究中取得了国际领先的成果和进展。取得成果包括：赖氨酸疏水性多肽对癌细胞的选择性杀伤受多肽聚集度的精确调控，以及铱复合精氨酸多肽的穿膜杀伤及“一药二效”。分别发表在期刊：J. Med. Chem. 2020, 63, 1132-41，以及Chem. Sci. 2020, 11, 9126-9133。数据量约25 MB。

The therapeutic modalities of antitumor drugs have evolved from chemotherapy, targeted therapy to immunotherapy, each with its own unique strengths. However, in clinical practice, tumor therapy still faces challenges including multidrug resistance, narrow therapeutic spectrum, and low response rate. "Membrane-active drugs", a novel therapeutic paradigm based on innovative concepts, are inspired by the widely conserved cytolytic mechanisms targeting biological membranes that exist in natural evolution, such as host defense against microorganisms, pyroptosis of eukaryotic cells, and T cell-mediated pore-forming cytotoxicity. Such agents are expected to avoid or greatly alleviate drug resistance, enable broad-spectrum activation of the immune system, and thus potentially emerge as a powerful new class of broad-spectrum antitumor drugs. This study investigated the use of cationic hydrophobic peptides to regulate reactive oxygen species (ROS) levels in cancer cells for selective killing, overcoming multidrug resistance, and activating the body's anticancer immune responses, and achieved internationally leading outcomes and progress in in vivo tumor inhibition studies of these agents. The key findings include: the selective killing of cancer cells by lysine-based hydrophobic peptides is precisely regulated by the peptides' aggregation degree, as well as the membrane-penetrating cytotoxicity and "dual efficacy of one drug" exhibited by iridium-conjugated arginine peptides. These works were respectively published in *Journal of Medicinal Chemistry* (2020, 63, 1132–1141) and *Chemical Science* (2020, 11, 9126–9133). The dataset has a size of approximately 25 MB.

搜集汇总

背景与挑战

背景概述

该数据集聚焦于膜活性多肽纳米制剂在抗肿瘤治疗中的研究，旨在通过调控癌细胞活性氧水平实现选择性杀伤、克服多药耐药并激活抗癌免疫效应。研究成果包括赖氨酸疏水性多肽的选择性杀伤机制和铱复合精氨酸多肽的穿膜杀伤效应，相关成果已发表于国际期刊。