已对5-氨基乙酰基丙酸（5-ALA）的治疗性质进行了广泛的研究，用于癌症检测和光动力治疗（PDT）。当外源给予5-ALA时，癌细胞内会将其转化为原卟啉Ⅸ（PpIX），在受光照射后生成活性氧物质（ROS）。这个过程使得针对性的细胞死亡诱导和癌症检测成为可能。考虑到血红素生物合成在亿万年间高度保守的性质，我们猜测在5-ALA过载引起的PpIX或血红素的过度积累时可能存在一些自然机制来防止其发生。因此，我们预计在外源给予5-ALA后蛋白质表达谱会有所改变。为了理解细胞对5-ALA的反应，我们调查了蛋白质表达的变化，并确认在膀胱、前列腺、肺和宫颈癌细胞中，OR1B1是一个有潜力的靶标。OR1B1的表达只在5-ALA和氯化铁的情况下观察到，突出了血红素在这一发现中的核心作用。免疫荧光和电子显微镜证实了OR1B1的亚细胞定位。这些发现提示5-ALA在癌细胞中的转化和OR1B1的表达有可能增强癌症检测并发展替代治疗，包括免疫疗法。这种方法克服了PDT的局限性，为有效和有针对性的癌症干预开辟了新的途径。版权所有 © 2023 作者。Elsevier B.V. 发表。

The therapeutic properties of 5-aminolevulinic acid (5-ALA) have been extensively studied for cancer detection and treatment using photodynamic therapy (PDT). When administered externally, 5-ALA is converted to protoporphyrin IX (PpIX) in cancer cells, which generates reactive oxygen species (ROS) upon exposure to light. This process enables targeted cell death induction and cancer detection. Given the highly conserved nature of heme biosynthesis over billions of years, we hypothesized that natural mechanisms might exist to prevent excessive accumulation of PpIX or heme resulting from 5-ALA overload. Therefore, we anticipated alterations in protein expression profiles upon exogenous administration of 5-ALA. To understand cellular responses to 5-ALA, we investigated protein expression changes and identified OR1B1 as a promising target in bladder, prostate, lung, and cervical cancer cells. OR1B1 expression was observed only with 5-ALA and ferrous chloride, highlighting the central role of heme in this discovery. Immunofluorescence and electron microscopy confirmed OR1B1's sub-cellular localization. These findings suggest that 5-ALA transformation in cancer cells and OR1B1 expression have potential for enhancing cancer detection and developing alternative treatments, including immunotherapy. This approach overcomes the limitations of PDT and opens new avenues for effective and targeted cancer interventions.Copyright © 2023 The Authors. Published by Elsevier B.V. All rights reserved.