Article
Chemistry, Medicinal
Hualong Mo, Ruiqiang Zhang, Yajun Chen, ShuTing Li, Yao Wang, Wenbo Zou, Qiman Lin, Deng-Gao Zhao, Yarong Du, Kun Zhang, Yan-Yan Ma
Summary: Compound 21 is an effective anticancer agent that inhibits tumor growth by inhibiting autophagy and inducing cell apoptosis.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Food Science & Technology
Xiangsheng Zhang, Huan Kan, Yun Liu, Wu Ding
Summary: Plumbagin shows potential medicinal properties, including anticancer activities. It inhibits cell proliferation, blocks cell cycle, induces apoptosis and autophagy in endometrial cancer cells. The anticancer effects of PLB may be mediated by abrogating the PI3K/Akt pathway.
FOOD AND CHEMICAL TOXICOLOGY
(2021)
Review
Pharmacology & Pharmacy
Hae Jin Kee, Inkyeom Kim, Myung Ho Jeong
Summary: This article provides an overview of the pathogenesis of hypertension, current anti-hypertensive drugs, and the need for novel drugs. It focuses on the role and regulatory mechanisms of HDACs in hypertension and discusses the progress in developing HDAC inhibitors as potential therapeutic targets.
BIOCHEMICAL PHARMACOLOGY
(2022)
Review
Oncology
Amandine Badie, Christian Gaiddon, Georg Mellitzer
Summary: Our understanding of the identity of many cancers has greatly increased in recent years, leading to progress in early detection and treatment options. However, gastric cancer remains poorly treated with low survival rates. The lack of possibilities for early detection and the variations between tumors of gastric cancer patients are major challenges. Histone Deacetylases (HDACs) have been identified to be potentially related to gastric cancer. In this review, we summarize the current knowledge on the role of HDACs in gastric cancer development and their potential as early detection markers and targets for new treatment options.
Review
Oncology
Fengyi Guo, Hongjing Wang
Summary: This review summarizes the classification and mechanisms of action of histone deacetylase and the clinical application of their inhibitors in ovarian cancer. Histone deacetylase inhibitors show promising potential as anti-cancer drugs, and combination therapy with other anticancer drugs for synergistic effects can improve efficacy.
FRONTIERS IN ONCOLOGY
(2022)
Article
Pharmacology & Pharmacy
Chiara Zichittella, Marco Loria, Adriana Celesia, Diana Di Liberto, Chiara Corrado, Riccardo Alessandro, Sonia Emanuele, Alice Conigliaro
Summary: This study demonstrates that the expression of lncH19 contributes to ITF2357-induced apoptosis by stabilizing TP53. Overall, we suggest that lncH19 expression may be exploited to enhance HDACi-induced cell death and overcome 5-fluorouracil chemoresistance.
FRONTIERS IN PHARMACOLOGY
(2023)
Article
Engineering, Environmental
Jian-Li Chen, Xiao-Hui Jia, Xinyue Xia, Xuan Wu, Yan-Neng Xu, Gang Yuan, Ze-Yun Gu, Kathy Qian Luo, Ming-Heng Yuan, Ruibin Jiang, Jianfang Wang, Xiao-Ming Zhu
Summary: In this study, hollow ZrO2 nanoshells were synthesized to encapsulate both the autophagy inhibitor chloroquine (CQ) and the HDAC inhibitor vorinostat (Vor) for effective combinational cancer therapy. The ZrO2 nanoshells showed high loading capacities for both CQ and Vor and exhibited a controlled release profile. The codelivery system enhanced the autophagy inhibition and hyperacetylation level in the cells, resulting in a superior antitumor effect in 4T1 tumor-bearing mice.
CHEMICAL ENGINEERING JOURNAL
(2023)
Article
Chemistry, Medicinal
An-Min Zhou, Meng-Meng Wang, Yan Su, Zheng-Hong Yu, Hong-Ke Liu, Zhi Su
Summary: In this study, a new agent Ir-VPA was developed, which exhibited switching between apoptosis and autophagy in cervical cancer cells due to the inhibition of HDAC6 at different levels. Ir-VPA showed the best anticancer activity to HeLa cells, inducing severe DNA damages and cell cycle arrest at G2/M phase. The anticancer mechanism of Ir-VPA was dependent on the inhibitory performance of HDAC6, with caspase-dependent apoptosis at low concentration and autophagy with autophagy flux blockage at high concentration.
Article
Cell Biology
Yong Wang, Fen Liu, Chen Fang, Liyao Xu, Lin Chen, Zeyao Xu, Jiaquan Chen, Wei Peng, Biqi Fu, Yong Li
Summary: The combination treatment of RAPA and SAHA significantly enhances the inhibitory effect of radiotherapy on NSCLC, primarily by modulating the expression of DNA damage proteins and increasing radiotherapy sensitivity. This combined therapy also effectively inhibits tumor growth in the A549 xenograft model.
Article
Chemistry, Medicinal
Dimitrios Triantafyllos Gerokonstantis, Christiana Mantzourani, Dimitrios Gkikas, Kai-Chen Wu, Huy N. Hoang, Ierasia Triandafillidi, Ilianna Barbayianni, Paraskevi Kanellopoulou, Alexandros C. Kokotos, Panagiota Moutevelis-Minakakis, Vassilis Aidinis, Panagiotis K. Politis, David P. Fairlie, George Kokotos
Summary: Benzamides, as HDAC inhibitors, have shown promising anticancer activity and potential for treating fibrotic disorders.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Review
Oncology
Jason Lin, Shang-Chuen Wu
Summary: This review examines the role of protein serotonylation in transcriptional regulation, its potential impact on the epigenetic landscape, and its implications in lung and other types of cancer. The review discusses the mechanistic details of serotonylation and its connections to the epigenome, as well as the role of transglutaminase 2, in order to guide the development of optimized histone deacetylase inhibitor designs or combination therapies for cancer treatment.
Review
Cell Biology
Bingyi Zhou, Deliang Liu, Yuyong Tan
Summary: Cancer is the second leading cause of death worldwide, with digestive system cancers being a primary contributor. Acetylation and deacetylation play crucial roles in cancer development, with HDAC6 being a widely studied enzyme that is upregulated in various tumors and associated with clinicopathological characteristics. There is ongoing research on HDAC6 inhibitors and their potential in inhibiting tumor growth.
FRONTIERS IN CELL AND DEVELOPMENTAL BIOLOGY
(2021)
Review
Biochemistry & Molecular Biology
Svetlana Demyanenko, Valentina Dzreyan, Svetlana Sharifulina
Summary: Cerebral ischemia is the second leading cause of death worldwide, requiring multimodal stroke therapy. Histone deacetylase inhibitors have shown to be effective in protecting the brain from ischemic damage by inducing neurogenesis and angiogenesis in damaged brain areas, promoting functional recovery after stroke.
Article
Microbiology
Yueyue Duan, Liyan Cao, Cong Yuan, Xuepeng Suo, Xiangyu Kong, Yulong Gao, Xiangtong Li, Haixue Zheng, Xiaomei Wang, Qi Wang
Summary: p53 plays a critical role in inhibiting ALV replication by recruiting the HDAC1/2 complex to the ALV promoter. The acetylation status of ALV-bound histones H3 and H4 correlates with ALV viremia in infected chickens.
Article
Microbiology
Yueyue Duan, Liyan Cao, Cong Yuan, Xuepeng Suo, Xiangyu Kong, Yulong Gao, Xiangtong Li, Haixue Zheng, Xiaomei Wang, Qi Wang
Summary: The research demonstrates that p53 inhibits ALV replication by recruiting the HDAC1/2 complex to the ALV promoter, and the absence of p53 abolishes HDAC1/2 binding to the ALV promoter. Clinical samples from ALV-infected chickens show that the acetylation status of ALV-bound H3 and H4 histones correlates with ALV viremia.
Article
Biochemistry & Molecular Biology
Amit Kundu, Sreevarsha Gali, Swati Sharma, Jae Hyeon Park, So Young Kyung, Sam Kacew, In Su Kim, Kwang Youl Lee, Hyung Sik Kim
Summary: The study demonstrates that Tenovin-1 has a protective effect against renal fibrosis in HFD-induced ZDF rats, reducing inflammation, oxidative stress, apoptosis, and levels of urinary protein. Additionally, Tenovin-1 restores the abnormal architecture of the kidney and pancreas and decreases ECM protein levels.
Article
Biochemistry & Molecular Biology
Gi Min Park, Sun Ju Kong, Jae Hyeon Park, Ji Eun Kang, Sung Hwan An, Hyung Sik Kim, In Su Kim, Pulla Reddy Boggu, Young Hoon Jung
Summary: A concise synthesis of ent-conduramine C-1 and its derivatives has been achieved using commercially available D-ribose. The key steps in the synthesis involved regioselective and diastereoselective amination, chelation-controlled carbonyl addition, and intramolecular olefin metathesis. The synthesized compounds were evaluated for their inhibitory activity against alpha-glucosidase, with derivatives 18 and 19 showing stronger inhibition than acarbose.
CARBOHYDRATE RESEARCH
(2023)
Article
Biochemistry & Molecular Biology
Yeon Su Park, Joo Hee Han, Jae Hyeon Park, Ji Soo Choi, Seung Hyeon Kim, Hyung Sik Kim
Summary: Diabetic nephropathy is a common complication of diabetes, which often leads to end-stage renal disease with a high mortality rate. Current research focuses on identifying non-invasive biomarkers for early detection of diabetic nephropathy. This study found that the protein pyruvate kinase M2 (PKM2) can be detected in the urine of diabetic patients and may serve as a new biomarker for early diagnosis of diabetic nephropathy.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Chemistry, Organic
Nayoung Ko, Jeonghyun Min, Junghyea Moon, Nuraimi Farwizah Ismail, Kyeongwon Moon, Pargat Singh, Neeraj Kumar Mishra, Wonsik Lee, In Su Kim
Summary: The rhodium(III)-catalyzed conjugate addition of fi-trifluoromethylated enones with quinoline N-oxides for the site-selective incorporation of a trifluoromethyl group into biologically active molecules and pharmaceuticals has been demonstrated. The reaction shows excellent functional group tolerance and synthetic applicability, making it a valuable tool for gram-scale experiments and coupling product transformations.
JOURNAL OF ORGANIC CHEMISTRY
(2023)
Article
Oncology
Jong Seung Lim, So Young Kyung, Yukyoung Jeon, In Su Kim, Jong Hwan Kwak, Hyung Sik Kim
Summary: The study investigated the HDAC inhibitory and anticancer activities of ACT-3 in MCF-7 human breast cancer cells. ACT-3 and SAHA increased acetylated histone H3 levels and reduced HDAC1 and HDAC3 levels. ACT-3 inhibited cell proliferation, induced cell cycle arrest and apoptosis, and increased autophagic cell death in MCF-7 cells. ACT-3 also activated the ERK pathway to inhibit cell growth and promote apoptosis in MCF-7 cells.
Article
Oncology
Chunxue Jiang, Xiaodi Zhao, Taejoo Jeong, Ju Young Kang, Jae Hyeon Park, In Su Kim, Hyung Sik Kim
Summary: Prostate cancer is a serious threat to male health globally, and chemotherapy resistance is a pressing issue. The discovery of novel molecules and chemotherapy strategies is crucial. This study identified a specific PKM2 inhibitor, compound 3h, and evaluated its anticancer effects through molecular and cellular experiments. The results demonstrated that compound 3h inhibits proliferation of LNCaP cells by inducing apoptosis, autophagy, and inhibiting glycolysis and mitochondrial respiration. This research provides a new approach for the development of novel chemotherapy for prostate cancer.
Article
Environmental Sciences
Min Kook Kim, Ji Soo Kang, Amit Kundu, Hyung Sik Kim, Byung-Mu Lee
Summary: This study aimed to determine the optimal boiling time to reduce ptaquiloside (PTA) and assess the risk of consuming bracken fern (BF) containing PTA. High-performance liquid chromatography showed a 99% reduction in PTA concentration after boiling BF for 20 min. Risk assessment results indicated that boiling BF for 20 min resulted in safe levels of cancer and non-cancer exposure to PTA. However, exposure to PTA was considered unsafe under non-boiled BF and maximum daily exposure scenarios. Thus, boiling BF for at least 20 min is recommended to minimize PTA exposure.
Article
Biochemistry & Molecular Biology
Minjung Son, Ga Young Kim, Yejin Yang, Sugyeong Ha, Jeongwon Kim, Doyeon Kim, Hae Young Chung, Hyung Ryong Moon, Ki Wung Chung
Summary: The PPAR pan agonist MHY2013 effectively prevents renal fibrosis in both in vitro and in vivo models, suggesting its therapeutic potential against chronic kidney diseases. MHY2013 inhibits fibroblast activation and reduces inflammation through PPAR gamma and beta activation.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Review
Biochemistry & Molecular Biology
Sungpil Yoon, Hyung Sik Kim
Summary: Tumors contain drug-resistant cancer cells that lead to tumor recurrence, while drug-sensitive cancer cells can be reduced through apoptosis. Increasing apoptosis in drug-resistant cancer cells is important for first-line chemotherapy, and combining P-gp inhibitors can delay tumor recurrence. Low-dose bipolar drugs can inhibit P-gp and their combined therapy enhances sensitivity in drug-resistant cancer cells.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Pharmacology & Pharmacy
Min-Soo Kim, Yoo-Kyung Song, Ji-Soo Choi, Hye Young Ji, Eunsuk Yang, Joon Seok Park, Hyung Sik Kim, Min-Joo Kim, In-Kyung Cho, Suk-Jae Chung, Yoon-Jee Chae, Kyeong-Ryoon Lee
Summary: In this study, physiologically based pharmacokinetic (PBPK) models were developed and validated for enavogliflozin and its metabolite M1, which can effectively predict the pharmacokinetic characteristics under different physiological conditions.
Article
Biochemistry & Molecular Biology
Yuankuan Li, Sung Ho Lee, Meiyu Piao, Hyung Sik Kim, Kwang Youl Lee
Summary: This study found that Metallothionein 3 (MT3) plays an important role in the differentiation of 3T3-L1 cells into adipocytes. Overexpression of MT3 inhibited adipocyte differentiation and reduced the levels of adipogenic transcription factors C/EBPa and PPAR?. Further analysis revealed that MT3 suppressed the transcriptional activity of PPAR?, and this effect was not mediated by a direct interaction between MT3 and PPAR?. Additionally, MT3 overexpression decreased reactive oxygen species (ROS) levels during early adipocyte differentiation, while treatment with antimycin A, which induces ROS generation, restored the ROS levels.
Article
Infectious Diseases
Hyeon-Ji Hwang, Dan-dan Li, Jieun Lee, Min Kyung Kang, Hyung Ryong Moon, Joon-Hee Lee
Summary: Two synthetic compounds, MHY1383 and MHY1387, have been found to have antibiofilm effects on Pseudomonas aeruginosa at very low concentrations. This study investigated their anti-biofilm effects on various bacteria and found that both compounds effectively inhibited biofilm formation by Escherichia coli, Bacillus subtilis, and Staphylococcus aureus. However, they showed medium-dependent effects on Salmonella enterica at high concentrations. These compounds can be used at low concentrations against biofilms formed by different types of bacteria, but their combination with antibiotics may not always lower the MIC.
Review
Chemistry, Multidisciplinary
Neeraj Kumar Mishra, Amitava Rakshit, Kyeongwon Moon, Pargat Singh, In Su Kim
Summary: The synthesis and functionalization of privileged nitrogen heterocycles play a central role in drug discovery and material science. Tandem C-H functionalization and intramolecular annulation have gained significant attention for their ability to expedite the construction of heteroaromatic frameworks. While there has been progress in the [3 + 2] dipolar cycloaddition of azomethine imines with pi-unsaturated compounds, the combination of catalytic C-H functionalization and intramolecular cyclization using azomethine imines as both directing groups and dipolar units remains less explored.
BULLETIN OF THE KOREAN CHEMICAL SOCIETY
(2023)
Article
Biochemistry & Molecular Biology
Yong Jung Kang, Jung Yoon Jang, Young Hoon Kwon, Jun Ho Lee, Sanggwon Lee, Yujin Park, Young-Suk Jung, Eunok Im, Hyung Ryong Moon, Hae Young Chung, Nam Deuk Kim
Summary: MHY2245 induces cell cycle arrest through DNA damage-induced p53 activation and apoptosis via caspase activation, showing anticancer effects associated with DNA damage response.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)