Article
Cell Biology
Dong Woo Kang, Won Chan Hwang, Yu Na Noh, Youra Kang, Younghoon Jang, Jung-Ae Kim, Do Sik Min
Summary: Phospholipase D1 (PLD1) is identified as a transcriptional target of histone deacetylase (HDAC) inhibitors and contributes to drug resistance in GBM. Inhibiting PLD1 can enhance the efficacy of HDAC inhibitors in treating GBM.
JOURNAL OF CELLULAR PHYSIOLOGY
(2021)
Article
Biophysics
Pengwei Hu, Miao Sun, Fengkun Lu, Sizhen Wang, Lei Hou, Yingjie Yu, Yunchang Zhang, Linhong Sun, Jianzhong Yao, Feng Yang, Chen Wang, Zhiqiang Ma
Summary: Combining PDT with HDACis enhances anti-tumor activity, but poor solubility and heterogeneous cellular uptake hinder the dual mode effect. Pyro@FPPS achieves controlled release of photosensitizers and HDACis, effectively inhibiting tumor proliferation and metastasis.
COLLOIDS AND SURFACES B-BIOINTERFACES
(2021)
Article
Neurosciences
Paulina Misztak, Magdalena Sowa-Kucma, Bernadeta Szewczyk, Gabriel Nowak
Summary: The study evaluated the impact of SAHA on the expression of several key proteins in the brain's signal transduction pathways, as well as the concentration of the oxidative stress product MDA. SAHA may prevent oxidative stress by decreasing MDA concentration and increasing p-AMPK expression, while also boosting neuroprotective and antidepressant protein levels.
NEUROTOXICITY RESEARCH
(2021)
Article
Oncology
Benigno C. Valdez, Bin Yuan, David Murray, Jeremy Leon Ramdial, Yago Nieto, Uday Popat, Xiaowen Tang, Borje S. Andersson
Summary: Combinations of nucleoside analog(s) and DNA alkylating agent(s) are used for cancer treatment. This study found that adding the HDAC inhibitor SAHA and the PARP inhibitor olaparib to the established drug combination can enhance the cytotoxicity of AML cells.
FRONTIERS IN ONCOLOGY
(2023)
Article
Oncology
Sarah Brown, Charlotte Pawlyn, Avie-Lee Tillotson, Debbie Sherratt, Louise Flanagan, Eric Low, Gareth J. Morgan, Cathy Williams, Martin Kaiser, Faith E. Davies, Matthew W. Jenner
Summary: The combination of vorinostat, bortezomib, and dexamethasone showed good response rates in relapsed myeloma, but was not well tolerated. Further optimization of histone deacetylase inhibitor-based combinations is needed to improve tolerability and enhance efficacy.
CLINICAL LYMPHOMA MYELOMA & LEUKEMIA
(2021)
Article
Chemistry, Medicinal
Negar Omidkhah, Razieh Ghodsi
Summary: NO-HDAC dual inhibitors have demonstrated satisfactory therapeutic effects in various diseases and possess high therapeutic potential.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Jie Wang, Zhuoxian Cao, Fang Wang, Pan Wang, Jianxiong An, Xiaozhong Fu, Ting Liu, Yan Li, Yongjun Li, Yonglong Zhao, Hening Lin, Bin He
Summary: The study discusses the rational design, synthesis, biological evaluation, molecular docking, and in vivo efficacy study of a class of HDAC inhibitors using N-acetyl lysine mimics derived from cysteine. These inhibitors demonstrated potent HDAC inhibition and broad cytotoxicity against several cancer cell lines, and compound 13d showed significant tumor growth inhibition in a A549 xenograft mice model.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Wenzhong Yan, Lijun Ling, Yiran Wu, Kexin Yang, Ruiquan Liu, Jinfeng Zhang, Simeng Zhao, Guisheng Zhong, Suwen Zhao, Hualiang Jiang, Chengying Xie, Jianjun Cheng
Summary: Adenosine serves as an immunosuppressive factor in the tumor microenvironment by activating the A(2A) adenosine receptor. Dual-acting compounds targeting A(2A)R and HDAC are potentially effective immunotherapeutic agents that show promising antitumor activity in vitro and in vivo.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Ping Sun, Jing Wang, Khadija S. Khan, Weiqin Yang, Billy Wai-Lung Ng, Nikita Ilment, Matthes Zessin, Emre F. Buelbuel, Dina Robaa, Frank Erdmann, Matthias Schmidt, Christophe Romier, Mike Schutkowski, Alfred Sze-Lok Cheng, Wolfgang Sippl
Summary: This study identifies a HDAC8 inhibitor with T cell modulatory properties and demonstrates its potential in reducing hepatocellular carcinoma tumorigenicity.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Review
Endocrinology & Metabolism
Jingru Yang, Cong Song, Xianquan Zhan
Summary: Protein acetylation is an important molecular event that is involved in various biological processes, including carcinogenesis. The modulation of protein acetylation levels can lead to the discovery of therapeutic drugs and lay the foundation for precision medicine in oncology.
FRONTIERS IN ENDOCRINOLOGY
(2022)
Article
Chemistry, Medicinal
Zhijie Wang, Donglin Wu, Xiaofei Zhao, Canlin Liu, Siming Jia, Qindi He, Fei Huang, Zitian Cheng, Tao Lu, Yadong Chen, Yun Chen, Pei Yang, Shuai Lu
Summary: AML patients need new therapies due to poor outcomes and relapse with single-target drugs. Inhibiting multiple oncogenic signals simultaneously is a promising strategy. This study developed novel dual FLT3/HDAC inhibitors through rational drug design and demonstrated their potential for AML treatment. The inhibitors blocked FLT3 and HDAC pathways, induced apoptosis, and arrested cell cycle.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Ying-Chao Duan, Lin-Feng Jin, Hong-Mei Ren, Shao-Jie Zhang, Yue-Jiao Liu, Yong-Tao Xu, Zi-Hao He, Yu Song, Hang Yuan, Shu-Hui Chen, Yuan-Yuan Guan
Summary: LSD1 and HDAC are closely related in various human cancers, and simultaneous pharmacological inhibition of them can have synergistic anti-cancer effects. Novel LSD1/HDAC bifunctional inhibitors were designed and synthesized, with compounds 5d and 5m showing potent anti-cancer activities and selectivity against other enzymes. Compound 5m, in particular, demonstrated superior in vitro anticancer potency against gastric cancer cell lines compared to existing drugs.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Pharmacology & Pharmacy
Jaione Auzmendi-Iriarte, Leire Moreno-Cugnon, Ander Saenz-Antonanzas, Daniela Grassi, Marian M. de Pancorbo, Maria-Angeles Arevalo, Ian C. Wood, Ander Matheu
Summary: The study found that levels of HDACs increase in microglial cells upon induction of senescence in vitro and in mouse and human hippocampal biopsies in vivo. Publicly available datasets showed changes in HDAC expression in different brain areas during physiological aging.
EXPERT OPINION ON THERAPEUTIC TARGETS
(2022)
Article
Gastroenterology & Hepatology
Ahmed M. Elfiky, Mohammed Ghiboub, Andrew Y. F. Li Yim, Ishtu L. Hageman, Jan Verhoeff, Manon de Krijger, Patricia H. P. van Hamersveld, Olaf Welting, Iris Admiraal, Shafaque Rahman, Juan J. Garcia-Vallejo, Manon E. Wildenberg, Laura Tomlinson, Richard Gregory, Inmaculada Rioja, Rab K. Prinjha, Rebecca C. Furze, Huw D. Lewis, Palwinder K. Mander, Sigrid E. M. Heinsbroek, Matthew J. Bell, Wouter J. de Jonge
Summary: This study investigates the utility of ESM-tagged HDACi in inflammatory bowel disease (IBD) and finds that it can specifically target monocytes and inflammatory macrophages, showing potential therapeutic benefits in IBD.
JOURNAL OF CROHNS & COLITIS
(2022)
Article
Biochemistry & Molecular Biology
Hairong Tang, Yuru Liang, Min Yu, Shaowen Cai, Kuiling Ding, Yang Wang
Summary: In this study, novel chiral 1,4-diarylazetidin-2-one-based hydroxamic acids were designed and synthesized as tubulin/HADC dual inhibitors, showing promising potential for cancer therapy. Compound 12a was found to effectively disrupt tubulin polymerization and inhibit HDAC1/8, as well as demonstrate strong antiproliferative activities against tumor cell lines. Moreover, 12a showed suitable physicochemical properties, high liver microsomal metabolic stability, and significant antitumor efficacy in vivo, making it a promising candidate for further development as a tubulin/HDAC dual inhibitor.
BIOORGANIC & MEDICINAL CHEMISTRY
(2023)
Article
Psychiatry
Yafit Levin, Rahel Bachem, Dorit Brafman, Menachem Ben-Ezra
Summary: Negative symptoms of schizophrenia have been overlooked, and this study found an association between negative symptoms and the risk of dissociative disorder, independently of depression and anxiety symptoms. It is important to consider both negative symptoms and dissociative symptoms in clinical practice to better understand their interaction.
JOURNAL OF PSYCHIATRIC RESEARCH
(2024)
Review
Psychiatry
Roland Mergl, Sarah M. Quaatz, Vanessa Lemke, Antje-Kathrin Allgaier
Summary: Women who have had miscarriages or stillbirths have an increased risk for depressive symptoms and disorders, with a wide range of prevalence rates. However, depressive symptoms tend to diminish over time.
JOURNAL OF PSYCHIATRIC RESEARCH
(2024)
Article
Psychiatry
Hai-Yang Wang, Lin Zhang, Bei-Yan Guan, Shi-Yao Wang, Cui-Hong Zhang, Ming-Fei Ni, Yan-Wei Miao, Bing-Wei Zhang
Summary: This study investigates the association between cognitive reappraisal and panic disorder (PD), and finds that PD patients have weakened functional connectivity between the prefrontal cortex (PFC) and the amygdala, which is associated with the severity of PD symptoms. Additionally, cognitive reappraisal is negatively correlated with PD severity, and the PFC-amygdala functional connectivity plays a mediating role in this association.
JOURNAL OF PSYCHIATRIC RESEARCH
(2024)
Article
Psychiatry
Yanqiang Tao, Xinyuan Zou, Qihui Tang, Wenxin Hou, Shujian Wang, Zijuan Ma, Gang Liu, Xiangping Liu
Summary: Depression and anxiety are prevalent mental disorders among adolescents. The study utilized network analysis to examine the symptom dimension of depression and anxiety in different age groups of adolescents. The results indicated that different age groups have different key symptoms and bridging symptoms, highlighting the importance of targeting specific symptoms at different stages of adolescence in treatment to alleviate the comorbidity of anxiety and depression.
JOURNAL OF PSYCHIATRIC RESEARCH
(2024)
Article
Psychiatry
Philip J. Batterham, Aliza Werner-Seidler, Bridianne O'Dea, Alison L. Calear, Kate Maston, Andrew Mackinnon, Helen Christensen
Summary: Screening for psychological distress in adolescents is important, and the Distress Questionnaire-5 (DQ5) is a reliable measure for this purpose. The study found that DQ5 had good fit to a unidimensional construct, strong criterion and predictive validity, and sensitivity to change. The brevity and ease of interpretation of DQ5 make it suitable for screening in schools.
JOURNAL OF PSYCHIATRIC RESEARCH
(2024)
Article
Psychiatry
Xiaoli Liu, Qianqian Chen, Fang Cheng, Wenhao Zhuang, Wenwu Zhang, Yiping Tang, Dongsheng Zhou
Summary: This study found working memory defects in adolescents with major depressive disorder compared to healthy controls based on mean oxy-hemoglobin changes, which can be useful for distinguishing adolescents with MDD from healthy controls.
JOURNAL OF PSYCHIATRIC RESEARCH
(2024)
Article
Psychiatry
Anders Nordahl-Hansen, Hugo Cogo-Moreira, Sareh Panjeh, Daniel S. Quintana
Summary: This article aims to determine empirically-derived effect size thresholds associated with psychotherapy for depressive disorders by calculating the effect size distribution. The findings indicate that the observed effect size thresholds are larger than the suggested guidelines, which has implications for interpreting study effects and planning future research.
JOURNAL OF PSYCHIATRIC RESEARCH
(2024)
Article
Psychiatry
Guangli Zhao, Liyong Yu, Peixin Chen, Keli Zhu, Lu Yang, Wenting Lin, Yucai Luo, Zeyang Dou, Hao Xu, Pan Zhang, Tianmin Zhu, Siyi Yu
Summary: This study investigated the neural mechanisms underlying emotional attention bias in patients with CID using ERP and rs-FC approaches. The results revealed abnormalities in attention processing and connectivity in the emotion-cognition networks of CID patients. This study provides a neural basis for understanding attention bias in CID.
JOURNAL OF PSYCHIATRIC RESEARCH
(2024)
Article
Psychiatry
Seungyeon Lee, Sora Mun, Jiyeong Lee, Hee-Gyoo Kang
Summary: Major depressive disorder is a prevalent condition worldwide, but the proportion of patients receiving treatment has not increased. Biomarkers related to drug-treatment responses can be used to monitor the effectiveness of medication. Serum protein levels were compared among patients with depression who received medication, those who did not, and a control group. Eight biomarkers were identified, which can be used to monitor the effectiveness of drug treatment.
JOURNAL OF PSYCHIATRIC RESEARCH
(2024)
Article
Psychiatry
Alfredo L. Sklar, Fang -Cheng Yeh, Mark Curtis, Dylan Seebold, Brian A. Coffman, Dean F. Salisbury
Summary: This study investigated semantic verbal fluency (SVF) impairments in first-episode psychosis patients within the schizophrenia spectrum. The findings revealed disruptions in both functional and structural connectivity in these patients, as well as an association between enhanced connectivity in the right hemisphere and worse SVF performance and longer disease duration.
JOURNAL OF PSYCHIATRIC RESEARCH
(2024)
Article
Psychiatry
Maksymilian Rejek, Blazej Misiak
Summary: This study investigates the association of the exposome score (ES) with psychosis risk in a non-clinical population. The results show that the ES is associated with the extended psychosis phenotype, suggesting its potential to identify individuals who may benefit from further psychosis risk assessment.
JOURNAL OF PSYCHIATRIC RESEARCH
(2024)