Blockade of GRP78 Translocation to the Cell Surface by HDAC6 Inhibition Suppresses Proliferation of Cholangiocarcinoma Cells

KIM, CHORONG; Lee, Seonmin; Kim, Danbee; Lee, Da Sol; Lee, Eunjung; Yoo, Changhoon; Kim, Kyu-Pyo

doi:10.21873/anticanres.15505

Cited by 11 publications

(12 citation statements)

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“…Enhanced transcriptional activity of p53 by ACY-1215 is also found in triple-negative breast cancer ( Cao et al, 2022 ). In cholangiocarcinoma, ACY-1215 suppresses GRP78 translocation to the cell surface via PI3K/AKT pathway, which inhibits proliferation and promotes apoptosis ( Kim et al, 2022 ). Growth inhibition has also been observed in colon cancer cells, prostate cancer cells, glioma cells and gallbladder cancer cells ( Tan et al, 2019 ; Corno et al, 2020 ; Huang et al, 2020 ; Ruan et al, 2021 ).…”

Section: Acy-1215 In Cancermentioning

confidence: 99%

Role of Selective Histone Deacetylase 6 Inhibitor ACY-1215 in Cancer and Other Human Diseases

et al. 2022

Front. Pharmacol.

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The deacetylation process regulated by histone deacetylases (HDACs) plays an important role in human health and diseases. HDAC6 belongs to the Class IIb of HDACs family, which mainly modifies non-histone proteins located in the cytoplasm. HDAC6 plays a key role in tumors, neurological diseases, and inflammatory diseases. Therefore, targeting HDAC6 has become a promising treatment strategy in recent years. ACY-1215 is the first orally available highly selective HDAC6 inhibitor, and its efficacy and therapeutic effects are being continuously verified. This review summarizes the research progress of ACY-1215 in cancer and other human diseases, as well as the underlying mechanism, in order to guide the future clinical trials of ACY-1215 and more in-depth mechanism researches.

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Section: Acy-1215 In Cancermentioning

confidence: 99%

Role of Selective Histone Deacetylase 6 Inhibitor ACY-1215 in Cancer and Other Human Diseases

et al. 2022

Front. Pharmacol.

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“…Unlike other HDACs, the development of HDAC6-specific inhibitors has been relatively successful [ 6 , 7 , 47 ]. NN-390, the first HDAC6-selective inhibitor, has shown therapeutic potential for Group 3 medulloblastoma (MB), an aggressive pediatric brain tumor associated with leptomeningeal metastases and therapy resistance [ 48 ].…”

Section: Hdac6-selective Inhibitorsmentioning

confidence: 99%

“…NM-390 targets MB stem cells and demonstrates a 45-fold increased efficacy over HDAC6 inhibitor citarinostat (ACY-241) [ 48 ]. ACY-1215 was shown to inhibit the translocation of GRP78 to the plasma membrane by inhibiting the PI3K/AKT signaling [ 47 ]. It suppressed tumor growth by 50% in a xenograft model of cholangiocarcinoma cells [ 47 ].…”

Section: Hdac6-selective Inhibitorsmentioning

confidence: 99%

“…ACY-1215 was shown to inhibit the translocation of GRP78 to the plasma membrane by inhibiting the PI3K/AKT signaling [ 47 ]. It suppressed tumor growth by 50% in a xenograft model of cholangiocarcinoma cells [ 47 ]. ACY-1215 inhibited BCR-ABL signaling while increasing the expression of PTEN in chronic myeloid leukemia cells [ 49 ] and suppressed the proliferation of esophageal squamous cell carcinoma by inhibiting the PI3K/AKT/ERK pathway [ 50 ].…”

Section: Hdac6-selective Inhibitorsmentioning

confidence: 99%

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Targeting HDAC6 to Overcome Autophagy-Promoted Anti-Cancer Drug Resistance

Shim

Jeoung

2022

IJMS

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Histone deacetylases (HDACs) regulate gene expression through the epigenetic modification of chromatin structure. HDAC6, unlike many other HDACs, is present in the cytoplasm. Its deacetylates non-histone proteins and plays diverse roles in cancer cell initiation, proliferation, autophagy, and anti-cancer drug resistance. The development of HDAC6-specific inhibitors has been relatively successful. Mechanisms of HDAC6-promoted anti-cancer drug resistance, cancer cell proliferation, and autophagy are discussed. The relationship between autophagy and anti-cancer drug resistance is discussed. The effects of combination therapy, which includes HDAC6 inhibitors, on the sensitivity of cancer cells to chemotherapeutics and immune checkpoint blockade are presented. A summary of clinical trials involving HDAC6-specific inhibitors is also presented. This review presents HDAC6 as a valuable target for developing anti-cancer drugs.

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“…The PI3K/AKT signaling pathway is constitutively activated in UM which facilitates tumorigenesis processes such as cell survival, inhibition of apoptosis and angiogenesis [ 56 ]. In ACY-1215 treated cholangiocarcinoma cells, cell proliferation was blocked, and apoptosis was triggered via the PI3K/AKT pathway [ 57 ]. Kaliszczak et al (2016) demonstrated that cotreatment of HCT116 with HDAC6i and pan-AKT inhibitor/dual PI3K/mTOR inhibitor enhanced anti-tumor effects both in vitro and in vivo [ 58 ].…”

Section: Involvement Of Hdac6 In Tumor Growth Survival and Progressionmentioning

confidence: 99%

Evaluation of the Therapeutic Potential of Histone Deacetylase 6 Inhibitors for Primary and Metastatic Uveal Melanoma

Sundaramurthi

Giricz

Kennedy

2022

IJMS

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Patients diagnosed with metastatic uveal melanoma (MUM) have a poor survival prognosis. Unfortunately for this rare disease, there is no known cure and suitable therapeutic options are limited. HDAC6 inhibitors (HDAC6i) are currently in clinical trials for other cancers and show potential beneficial effects against tumor cell survival in vitro and in vivo. In MUM cells, HDAC6i show an anti-proliferative effect in vitro and in preclinical xenograft models. The use of HDAC6 inhibitors as a treatment option for MUM should be explored further. Therefore, this review discusses (1) what is known about HDAC6i in MUM and (2) whether HDAC6 inhibitors offer a potential therapeutic option for MUM.

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Blockade of GRP78 Translocation to the Cell Surface by HDAC6 Inhibition Suppresses Proliferation of Cholangiocarcinoma Cells

Cited by 11 publications

References 0 publications

Role of Selective Histone Deacetylase 6 Inhibitor ACY-1215 in Cancer and Other Human Diseases

Role of Selective Histone Deacetylase 6 Inhibitor ACY-1215 in Cancer and Other Human Diseases

Targeting HDAC6 to Overcome Autophagy-Promoted Anti-Cancer Drug Resistance

Evaluation of the Therapeutic Potential of Histone Deacetylase 6 Inhibitors for Primary and Metastatic Uveal Melanoma

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