Peptides have many advantages over traditional therapeutics, including small molecules and other biologics, because of their low toxicity and immunogenicity, while still exhibiting efficacy. This review discusses the benefits and mechanism of action of apolipoprotein mimetic peptides in tumor biology and their potential utility in treating various cancers. Among lipoproteins in the circulation, high-density lipoprotein (HDL) and its constituents including apolipoprotein A-I (apoA-I; the predominant protein in HDL), apoJ, and apoE, harbor anti-tumorigenic activities. Peptides that mimic apoA-I function have been developed through molecular mimicry of the amphipathic α-helices of apoA-I. Oral apoA-I mimetic peptides remodel HDL, promote cholesterol efflux, sequester oxidized lipids, and activate anti-inflammatory processes. ApoA-I and apoJ mimetic peptides ameliorate various metrics of cancer progression and have demonstrated efficacy in preclinical models in the inhibition of ovarian, colon, breast, and metastatic lung cancers. Apolipoprotein mimetic peptides are poorly absorbed when administered orally and rapidly degraded when injected into the circulation. The small intestine is the major site of action for apoA-I mimetic peptides and recent studies suggest that modulation of immune cells in the lamina propria of the small intestine is, in part, a potential mechanism of action. Finally, several recent studies underscore the use of reconstituted HDL as target-specific nanoparticles carrying poorly soluble or unstable therapeutics to tumors even across the blood-brain barrier. Preclinical studies suggest that these versatile recombinant lipoprotein based nanoparticles and apolipoprotein mimetics can serve as safe, novel drug delivery, and therapeutic agents for the treatment of a number of cancers.

与传统疗法（包括小分子和其他生物制剂）相比，肽具有许多优势，因为它们具有低毒性和免疫原性，同时仍具有疗效。本综述讨论了载脂蛋白模拟肽在肿瘤生物学中的益处和作用机制及其在治疗各种癌症中的潜在用途。在循环中的脂蛋白中，高密度脂蛋白 (HDL) 及其成分包括载脂蛋白 AI（apoA-I；HDL 中的主要蛋白质）、apoJ 和 apoE，具有抗肿瘤活性。模拟 apoA-I 功能的肽是通过对 apoA-I 的两亲性 α-螺旋进行分子模拟而开发的。口服 apoA-I 模拟肽可重塑 HDL、促进胆固醇流出、隔离氧化脂质并激活抗炎过程。ApoA-I 和 apoJ 模拟肽改善了癌症进展的各种指标，并在临床前模型中证明了在抑制卵巢癌、结肠癌、乳腺癌和转移性肺癌方面的功效。载脂蛋白模拟肽口服给药时吸收差，注射入循环时迅速降解。小肠是 apoA-I 模拟肽的主要作用部位，最近的研究表明，小肠固有层中免疫细胞的调节部分是一种潜在的作用机制。最后，最近的几项研究强调了使用重组的 HDL 作为靶向特异性纳米颗粒，即使穿过血脑屏障，也可以携带难溶或不稳定的肿瘤治疗剂。