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Highly-tumor-targeted PAD4 inhibitors with PBA modification inhibit tumors in vivo by specifically inhibiting the PAD4-H3cit-NETs pathway in neutrophils by Di Zhu; Yu Lu; Bo Hu; Yuheng Pang; Bingru Liu; Miao Zhang; Wenjing Wang; Yuji Wang is a Chemistry article available to read on EtoBox.
What is Highly-tumor-targeted PAD4 inhibitors with PBA modification inhibit tumors in vivo by specifically inhibiting the PAD4-H3cit-NETs pathway in neutrophils about?
As a new target for tumor therapy, PAD4 protein, shows excellent antitumor activity, and phenylboronic acid (PBA) could combine with sialic acid on the tumor surface to achieve dual targeting in situ and for metastatic tumors. The purpose of this study was therefore to modify PAD4 protein inhibitors with different phenylboronic acid groups in order to obtain highly-targeted PAD4 inhibitors. The activity and mechanism of these PBA-PAD4 inhibitors were studied in vitro by MTT assay, laser confocal analysis, and flow cytometry. The effects of the compounds on primary tumor and lung metastasis in mice were evaluated in vivo using a S180 sarcoma model and a 4T1 breast cancer model. In addition, cytometry mass (CyTOF) was used to analyze the immune microenvironment, and the results show that the PAD4 inhibitor 5i modified by m-PBA at the carboxyl terminal of ornithine skeleton had the best antitumor activity. In vitro evaluation of this activity revealed that 5i could not directly kill tumor cells but had a significant inhibitory effect on tumor cell metastasis. Further mechanism studies showed that 5i could be taken up by 4T1 cells in a time-dependent manner and distributed around the c
Who reads Highly-tumor-targeted PAD4 inhibitors with PBA modification inhibit tumors in vivo by specifically inhibiting the PAD4-H3cit-NETs pathway in neutrophils?
It is typically read by researchers, students, and practitioners in Chemistry.
- Author
- Di Zhu; Yu Lu; Bo Hu; Yuheng Pang; Bingru Liu; Miao Zhang; Wenjing Wang; Yuji Wang
- Publisher
- Elsevier BV
- Published
- 2023
- Language
- EN
- Field
- Chemistry (Physical Sciences)