Small molecular inhibitors reverse cancer metastasis by blockading oncogenic PITPNM3

Liu, Zihao, Shi, Yu, Lv, Li, Chen, Jianing, Jiang, WenG. ORCID: https://orcid.org/0000-0002-3283-1111, Li, Jun, Lin, Qun, Fang, Xiaolin, Gao, Jingbo, Liu, Yujie, Liu, Qiang, Xu, Xiaoding, Song, Erwei and Gong, Chang 2022. Small molecular inhibitors reverse cancer metastasis by blockading oncogenic PITPNM3. Advanced Science 9 (35) , 2204649. 10.1002/advs.202204649

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Abstract

Most cancer‐related deaths are a result of metastasis. The development of small molecular inhibitors reversing cancer metastasis represents a promising therapeutic opportunity for cancer patients. This pan‐cancer analysis identifies oncogenic roles of membrane‐associated phosphatidylinositol transfer protein 3 (PITPNM3), which is crucial for cancer metastasis. Small molecules targeting PITPNM3 must be explored further. Here, PITPNM3‐selective small molecular inhibitors are reported. These compounds exhibit target‐specific inhibition of PITPNM3 signaling, thereby reducing metastasis of breast cancer cells. Besides, by using nanoparticle‐based delivery systems, these PITPNM3‐selective compounds loaded nanoparticles significantly repress metastasis of breast cancer in mouse xenograft models and organoid models. Notably, the results establish an important metastatic‐promoting role for PITPNM3 and offer PITPNM3 inhibition as a therapeutic strategy in metastatic breast cancer.

Item Type:	Article
Date Type:	Publication
Status:	Published
Schools:	Medicine
Additional Information:	License information from Publisher: LICENSE 1: URL: http://creativecommons.org/licenses/by/4.0/
Publisher:	Wiley Open Access
ISSN:	2198-3844
Date of First Compliant Deposit:	27 October 2022
Last Modified:	29 May 2023 05:12
URI:	https://orca.cardiff.ac.uk/id/eprint/153812

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