Histone deacetylases (HDACs) exhibit increased expression in cancer and promote oncogenesis via the acetylation of or interactions with key transcriptional regulators. HDAC inhibitors (HDACis) decrease HDAC activity to selectively inhibit the occurrence and development of tumors. Our study screened and obtained a new HDACi structure. experiments have showed that among the leads, Z31216525 significantly inhibited the proliferation and induced the apoptosis of epithelial ovarian cancer (EOC) cells. experiments demonstrated that compared to the control, Z31216525 significantly inhibited tumor growth and showed very low toxicity. Further mechanistic studies revealed that Z31216525 may exert an antitumor effect by inhibiting the expression of the c-Myc gene. Collectively, our studies identified a novel HDACi that is expected to become a new potential therapeutic drug for EOC and has important value for the design of new HDACi structures.
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http://dx.doi.org/10.7150/ijbs.62339 | DOI Listing |
Ann Hematol
November 2024
Department of Hematology, The First Affiliated Hospital, Harbin Medical University, Harbin, China.
B-cell acute lymphocytic leukemia (B-ALL) is a malignant proliferative B-lymphocyte disease. Although the outcome of B-ALL has greatly improved with combined chemotherapy, immunotherapy, and hematopoietic stem cell transplantation, some patients still experience drug resistance, relapse and a low long-term survival rate, therefore, finding novel approaches to improve the outcome of adult B-ALL patients is critical. Our previous studies revealed that the selective histone deacetylase inhibitor (HDACi) chidamide can inhibit the Wnt/β-catenin signaling pathway by inhibiting MYCN and increasing the expression of DKK3 in B-ALL cells.
View Article and Find Full Text PDFJ Med Chem
December 2024
Institute of Pharmaceutical und Medicinal Chemistry, Heinrich Heine University Düsseldorf, 40225 Düsseldorf, Germany.
Histone deacetylase inhibitors (HDACi) are established anticancer drugs, especially in hematological cancers. This study aimed to design, synthesize, and evaluate a set of HDACi featuring a pentyloxyamide connecting unit linker region and substituted phenylthiazole cap groups. A structural optimization program yielded HDACi with nanomolar inhibitory activity against histone deacetylase class I/IIb enzymes.
View Article and Find Full Text PDFJ Colloid Interface Sci
February 2025
The Fifth Affiliated Hospital, The Affiliated Panyu Central Hospital, Guangzhou Municipal and Guangdong Provincial Key Laboratory of Molecular Target & Clinical Pharmacology, the NMPA and State Key Laboratory of Respiratory Disease, The School of Pharmaceutical Sciences, Guangzhou Medical University, Guangzhou, Guangdong 511436, China. Electronic address:
Lung cancer remains one of the most fatal cancers worldwide, with a high incidence of metastasis and a low 5-year survival rate. Histone deacetylase inhibitors (HDACis) have shown significant potential in lung cancer treatment, but their clinical use is often hindered by poor water solubility, rapid clearance, and systemic toxicity. In this study, we developed a novel therapeutic strategy by camouflaging black phosphorus (BP) with M1 macrophage membranes (MB) and loaded HDACi suberoylanilide hydroxamic acid (SAHA) onto the camouflaged black phosphorus (MB) for targeted lung cancer therapy.
View Article and Find Full Text PDFJ Transl Med
November 2024
Department of Oncology, Key Laboratory of Carcinogenesis and Cancer Invasion of Ministry of Education, National Clinical Research Center for Geriatric Disorders, Xiangya Hospital, Central South University, Xiangya Road 110, Changsha, 410078, China.
Histone deacetylase inhibitors (HDACis) have shown a significant antitumor effect in clinical studies, and PXD101 is a novel HDACi which can cross the blood-brain barrier. In this study, we showed that PXD101 could significantly inhibit the proliferation and invasion of glioblastoma (GBM) cells, while promoting their apoptosis and radiosensitivity. Furthermore, it was found that PXD101 exerted its antitumor function by upregulating the expression of the growth arrest and DNA damage inducible protein α (GADD45A).
View Article and Find Full Text PDFBiomark Res
November 2024
Department of Clinical Pharmacology, Hunan Key Laboratory of Pharmacogenetics and National Clinical Research Center for Geriatric Disorders, Xiangya Hospital, Central South University, Changsha, 410008, China.
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