Journal
ACS OMEGA
Volume 4, Issue 5, Pages 9228-9234Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsomega.9b00281
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Funding
- Hong Kong Baptist University [FRG2/17-18/003]
- Health and Medical Research Fund [HMRF/14150561]
- National Natural Science Foundation of China [21575121, 21775131]
- Hong Kong Baptist University Century Club Sponsorship Scheme 2018
- Interdisciplinary Research Matching Scheme [RC-IRMS/16-17/03]
- Interdisciplinary Research Clusters Matching Scheme [RC-IRCs/17-18/03]
- Collaborative Research Fund [C5026-16G]
- SKLEBA and HKBU Strategic Development Fund [SKLP_ 718_P04]
- Science and Technology Development Fund, Macao SAR [0072/2018/A2]
- University of Macau [MYRG2016-00151-ICMS-QRCM, MYRG2018-00187-ICMS]
- Natural Science Foundation of Jiangsu Province [BK20150283]
- National Natural Science Foundation of China (NSFC) [21505097]
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The peptidyl-prolyl isomerase Pin1 is correlated with the progression of cervical cancer via regulating numerous oncogenic and tumor suppressor pathways. p65 is a crucial regulator of tumorigenesis that is regulated by Pin1, and p65 signaling suppression can enhance the antitumor efficacy of doxorubicin (DOX). Here, we utilized a structural mimicry approach to synthesize a series of dibenzothiophene analogues and evaluated their ability to inhibit Pin1 activity. Compound 1a was identified as a potent Pin1 inhibitor that inhibited p65 signaling in vitro and in cervical cancer cells. Moreover, compound 1a enhanced the cytotoxicity of DOX in cervical cancer cells via reducing p65 nuclear accumulation and enhancing DOX uptake. These compounds are promising scaffolds for developing more potent Pin1 inhibitors against cervical cancer, either alone or in combination with anticancer drugs such as DOX.
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