Article
Chemistry, Medicinal
Bartosz Bieszczad, Damian Garbicz, Marta Switalska, Marta K. Dudek, Dawid Warszycki, Joanna Wietrzyk, Elzbieta Grzesiuk, Adam Mieczkowski
Summary: In this study, a library of 19 analogues of Vorinostat was developed and tested for their HDAC inhibition and cytotoxic effects on cancer and normal cell lines. Three compounds based on dibenzo[b,f]azocin-6(5H)-one, 11,12-dihydrodibenzo[b,f]azocin-6(5H)-one, and benzo[b]naphtho[2,3-f][1,5]diazocine-6,14(5H,13H)-dione scaffolds showed better HDAC inhibition and lower IC50 values in leukemic and lymphoma cell lines compared to Vorinostat. These compounds exhibited higher activity and selectivity against specific cancer cell lines and a correlation between HDAC inhibition and cytotoxic effects was observed.
Review
Pharmacology & Pharmacy
Abhishek Wahi, Priti Jain, Apurba Sinhari, Hemant R. Jadhav
Summary: The study of epigenetic translational modifications, particularly the disruption in the expression and activity of histone deacetylases (HDACs), has gained significant interest in the field of cancer research. HDACs play a vital role in various processes that contribute to cancer development and progression. HDAC inhibitors (HDACis), which have been developed as a therapeutic approach, show promising potential in treating cancer with reduced side effects compared to conventional synthetic inhibitors.
NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY
(2023)
Article
Immunology
Mahdieh Mehrpouri, Atieh Pourbagheri-Sigaroodi, Davood Bashash
Summary: This article outlines the role of epigenetic modulations, particularly histone deacetylases, in hematologic malignancies and their therapeutic potential. Research suggests that HDACs play a significant role in hematopoiesis and the development of blood cancers.
INTERNATIONAL IMMUNOPHARMACOLOGY
(2021)
Review
Biochemistry & Molecular Biology
Marta Halasa, Kamila Adamczuk, Grzegorz Adamczuk, Syeda Afshan, Andrzej Stepulak, Marek Cybulski, Anna Wawruszak
Summary: N-ε-lysine acetylation/deacetylation is a common post-translational modification regulated by histone acetyltransferases and histone deacetylases, influencing the properties and functions of histones and non-histone proteins, including transcription factors that alter cell signaling pathways and impact cancer progression. HDACs play a significant role in deacetylating targets, leading to the regulation of proteins involved in cell cycle and apoptosis, ultimately affecting tumor growth, invasion, and drug resistance. This review highlights the clinical importance of epigenetic modifications as a potential therapeutic target in cancer treatment.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Review
Pharmacology & Pharmacy
Eleftherios Spartalis, Konstantinos Kotrotsios, Dimosthenis Chrysikos, Michael Spartalis, Stavroula A. Paschou, Dimitrios Schizas, Konstantinos Tsamakis, Dimitrios Dimitroulis, Theodore Troupis, Nikolaos Nikiteas
Summary: The study evaluates the role of HDACIs in PTC treatment and outlines the current trends in research. While HDACIs show promising anti-cancer effects on PTC cell lines, they have not shown significant responses in clinical trials. Further research is needed to explore their potential as an additional treatment modality.
CURRENT PHARMACEUTICAL DESIGN
(2021)
Editorial Material
Microbiology
Tom Boissavy, Dante Rotili, Thomas Mouveaux, Emmanuel Roger, El Moukthar Aliouat, Christine Pierrot, Sergio Valente, Antonello Mai, Mathieu Gissot
Summary: Toxoplasmosis is a significant health issue for immune-deficient individuals and newborns of infected mothers. New compounds with potent anti-parasitic activity have been discovered, which can serve as therapeutic targets for the treatment of toxoplasmosis.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2023)
Review
Chemistry, Multidisciplinary
Siddhartha Das Pramanik, Amit Kumar Halder, Ushmita Mukherjee, Dharmendra Kumar, Yadu Nandan Dey, R. Mogana
Summary: This review examines the role of HDACs in cancer treatment. While clinical trials with HDACi as monotherapy have had mixed results, combination therapy with other anticancer drugs has shown synergistic effects, increasing efficacy and decreasing toxicity.
FRONTIERS IN CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Marcel K. W. Mackwitz, Eva Hesping, Korina Eribez, Andrea Schoeler, Yevgeniya Antonova-Koch, Jana Held, Elizabeth A. Winzeler, Katherine T. Andrews, Finn K. Hansen
Summary: This study reports on a new peptoid-based HDAC inhibitor with dual-stage antiplasmodial activity, showing potential activity against malaria parasites and selectivity for human cells. These data provide a foundation for future improvements to these dual-stage inhibitors as potential drug leads for malaria.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Health Care Sciences & Services
Nikolaos Garmpis, Christos Damaskos, Dimitrios Dimitroulis, Gregory Kouraklis, Anna Garmpi, Panagiotis Sarantis, Evangelos Koustas, Alexandros Patsouras, Iason Psilopatis, Efstathios A. Antoniou, Michail Karamouzis, Konstantinos Kontzoglou, Afroditi Nonni
Summary: This study found a relationship between HDAC-2 expression and clinical features and survival of breast cancer. Higher expression of HDAC-2 was correlated with the aggressiveness and poor prognosis of breast cancer.
JOURNAL OF PERSONALIZED MEDICINE
(2022)
Article
Biochemistry & Molecular Biology
Justine S. Habibian, Matthew J. Bolino, Bradley S. Ferguson
Summary: Skeletal muscle differentiation requires the activation of satellite cells to proliferate, differentiate, and fuse. This process is regulated by myogenic transcription factors, which are tightly controlled by intracellular signaling pathways, including the protein kinase D (PKD) family. In this study, the researchers found that inhibiting class I histone deacetylases (HDACs), specifically HDAC8, attenuated PKD phosphorylation in skeletal muscle cells, suggesting that HDAC8 may function as a feedback regulator of PKD phosphorylation during muscle differentiation.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2023)
Review
Biochemistry & Molecular Biology
Nikolaos Garmpis, Christos Damaskos, Anna Garmpi, Afroditi Nonni, Vasiliki E. Georgakopoulou, Efstathios Antoniou, Dimitrios Schizas, Panagiotis Sarantis, Alexandros Patsouras, Athanasios Syllaios, Christos Vallilas, Evangelos Koustas, Konstantinos Kontzoglou, Nikolaos Trakas, Dimitrios Dimitroulis
Summary: Colorectal cancer is a heterogeneous group of gastrointestinal tract tumors, and its pathogenesis involves multiple factors. Histone deacetylases have been found to be over-expressed in CRC and play an important role in its molecular pathophysiology.
CURRENT MEDICINAL CHEMISTRY
(2022)
Review
Chemistry, Medicinal
Gargi Nikhil Vaidya, Pooja Rana, Ashwini Venkatesh, Deep Rohan Chatterjee, Darshan Contractor, Dinesh Parshuram Satpute, Mithilesh Nagpure, Alok Jain, Dinesh Kumar
Summary: Epigenetic regulation of genes through post-translational modulation of proteins, particularly with HDAC inhibitors, shows promising potential in various disease therapies. The flexibility in structural design of HDAC inhibitors allows for easy customization to create multi-targeted hybrids to overcome limitations of conventional drugs. These inhibitors have entered different combination therapies and offer a novel approach to improve drug efficacy in treating diseases.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Review
Biochemistry & Molecular Biology
Anton Fruhauf, Franz-Josef Meyer-Almes
Summary: HDACs play a role in many diseases, and the hydroxamate group in HDACis may cause toxic side effects, leading to exploration of non-hydroxamic HDACis. These new inhibitors have alternative ZBGs to replace the hydroxamate group, maintaining high potency and high selectivity.
Article
Oncology
Stephen W. Booth, Toby A. Eyre, John Whittaker, Leticia Campo, Lai Mun Wang, Elizabeth Soilleux, Daniel Royston, Gabrielle Rees, Murali Kesavan, Catherine Hildyard, Farasat Kazmi, Nick La Thangue, David Kerr, Mark R. Middleton, Graham P. Collins
Summary: This Phase 2a study assessed the safety, tolerability, and efficacy of oral HDAC inhibitor CXD101 in patients with relapsed/refractory lymphoma or advanced solid organ cancers. The results showed efficacy in lymphoma patients, but no responses in solid organ cancers. Further studies on combination approaches are needed.
Review
Medical Laboratory Technology
Jehan Mohammad Nazri, Katerina Oikonomopoulou, Elvin D. de Araujo, Dziyana Kraskouskaya, Patrick T. Gunning, Vinod Chandran
Summary: Psoriasis and psoriatic arthritis (PsA) are inflammatory diseases that affect the skin and musculoskeletal system. Current treatments for these conditions are not fully effective, leading to a reduced quality of life for patients. Histone deacetylase (HDAC) inhibitors, originally investigated as anti-cancer agents, have shown promise as a new anti-inflammatory treatment for inflammatory diseases. However, more research is needed to determine their effectiveness for PsA patients. This review provides an overview of psoriatic disease, HDACs, and discusses the potential use of HDAC inhibitors in managing persistent inflammation in psoriatic disease.
CRITICAL REVIEWS IN CLINICAL LABORATORY SCIENCES
(2023)
