Second Affiliated Hospital, Dalian Medical University, Dalian 116023, China.
College of Pharmacy, Dalian Medical University, Dalian 116044, China.
Molecules. 2023 Apr 14;28(8):3472. doi: 10.3390/molecules28083472.
Cytochrome P450 1A is one of the vital subfamilies of heme-containing cytochrome P450 enzymes belonging to an important exogenous metabolizing CYP in human. The abnormal of endoplasmic reticulum (ER) may directly affect the functional activity of ER-located CYP1A and be associated with the occurrence and development of various diseases. In the present study, we constructed a selective two-photon fluorescent probe for rapid and visual detection of endogenous CYP1A that was localized in the ER. could target the ER and detect the enzymatically active CYP1A in living cells and tissues. The monitoring ability of for the fluctuations in functionality level of CYP1A was confirmed using ER stressed A549 cell. Based on the ER-targeting two-photon probe for CYP1A, the close association of ER state and the functional activity of ER-locating CYP1A was confirmed, which would promote the deep understanding of the biofunction of CYP1A in various ER-related diseases.
细胞色素 P450 1A 是血红素细胞色素 P450 酶的重要亚家族之一,属于人类重要的外源性代谢 CYP。内质网(ER)的异常可能直接影响 ER 定位的 CYP1A 的功能活性,并与各种疾病的发生和发展有关。在本研究中,我们构建了一种用于快速和可视化检测内质网定位的内源性 CYP1A 的选择性双光子荧光探针。探针 可以靶向 ER,并在活细胞和组织中检测到酶活性的 CYP1A。使用内质网应激 A549 细胞证实了探针 对 CYP1A 功能水平波动的监测能力。基于内质网靶向 CYP1A 的双光子探针,证实了 ER 状态与 ER 定位 CYP1A 的功能活性密切相关,这将促进深入了解 CYP1A 在各种与 ER 相关疾病中的生物功能。