尽管医疗保健部门发展迅猛，癌症仍是全球第二致命疾病。目前常规癌症治疗主要包括化疗和放疗，但这些疗法往往伴有少至严重的副作用，而放疗通常又十分昂贵。为了克服这些问题，针对性纳米载体已被用于输送化疗药物。然而，最近对几种具有抗癌活性的蛋白质的使用报告，并进一步将它们用作药物载体，引起了对癌症治疗研究的极大关注。生物分子，特别是蛋白质，由于生物相容性、生物降解性和结构灵活性等多种有利属性而成为癌症治疗的可行替代品。多项体外和体内研究表明，从动物、植物和细菌物种中提取的各种蛋白质，在其本身和不同的结构构像下，对恶性细胞表现出强烈的细胞毒性和抗增殖特性。此外，这些蛋白质的表面调控特性有助于结合各种抗癌药物和靶向配体，从而使它们成为癌症治疗中有效的输送剂。本文讨论了从通用外源源获得的各种蛋白质及其如何转化为有效的抗癌剂。我们还全面讨论了不同膳食蛋白质如牛α-乳清蛋白和鸡蛋白溶菌酶及其共轭物的肿瘤杀灭机制。我们还阐述了如何将蛋白质纳米结构用作输送癌症药物和疗效学的载体，以及为提高它们的体内输送和靶向而采用的各种策略。我们还讨论了FDA批准的基于蛋白质的抗癌制剂以及处于不同临床试验阶段的制剂。版权所有©2023 Elsevier B.V.。

Despite the remarkable advancement in the health care sector, cancer remains the second most fatal disease globally. The existing conventional cancer treatments primarily include chemotherapy, which has been associated with little to severe side effects, and radiotherapy, which is usually expensive. To overcome these problems, target-specific nanocarriers have been explored for delivering chemo drugs. However, recent reports on using a few proteins having anticancer activity and further use of them as drug carriers have generated tremendous attention for furthering the research towards cancer therapy. Biomolecules, especially proteins, have emerged as suitable alternatives in cancer treatment due to multiple favourable properties including biocompatibility, biodegradability, and structural flexibility for easy surface functionalization. Several in vitro and in vivo studies have reported that various proteins derived from animal, plant, and bacterial species, demonstrated strong cytotoxic and antiproliferative properties against malignant cells in native and their different structural conformations. Moreover, surface tunable properties of these proteins help to bind a range of anticancer drugs and target ligands, thus making them efficient delivery agents in cancer therapy. Here, we discuss various proteins obtained from common exogenous sources and how they transform into effective anticancer agents. We also comprehensively discuss the tumor-killing mechanisms of different dietary proteins such as bovine α-lactalbumin, hen egg-white lysozyme, and their conjugates. We also articulate how protein nanostructures can be used as carriers for delivering cancer drugs and theranostics, and strategies to be adopted for improving their in vivo delivery and targeting. We further discuss the FDA-approved protein-based anticancer formulations along with those in different phases of clinical trials.Copyright © 2023 Elsevier B.V. All rights reserved.