Introduction: Cutaneous squamous cell carcinoma (cSCC) is the second most frequent cancer; it can be locally invasive and metastatic. cSCC is an immense clinical and economic problem given its sheer incidence and potential morbidity and mortality, particularly in the elderly and immunocompromised. Epigenetics has emerged as one of the most exciting areas of human biology, impacting virtually all areas of cellular physiology. Inhibition of an epigenetic enzyme is a potential treatment of cSCC.
Areas Covered: We provide an overview of the development of inhibitors targeting the lysine demethylase, LSD1 (KDM1A), the first histone demethylase discovered. We summarize current treatment modalities for cSCC and provide a rationale for why epigenome-targeting therapies, and particularly LSD1 inhibitors, may be a novel and effective approach for treating pre-malignant and malignant cSCCs. A search was conducted in PubMed utilizing the combination of 'LSD1' with keywords such as 'epidermis,' 'squamous cell carcinoma,' or 'skin.' Relevant papers from 2000 to 2020 were reviewed.
Expert Opinion: Given the ability of LSD1 inhibitors to promote epidermal differentiation and enhance anti-tumor immune responses, LSD1 inhibitors may offer a highly effective therapeutic approach for the prevention and treatment of these ubiquitous cancers.
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http://dx.doi.org/10.1080/14728222.2020.1762175 | DOI Listing |
Life Med
June 2023
Department of Pathology, Immunology and Laboratory Medicine, College of Medicine, University of Florida, Gainesville, FL 32610, USA.
Immune checkpoint inhibitors (ICIs) use antibodies that block cell surface immune checkpoint proteins with great efficacy in treating immunogenic or "immune hot" tumors such as melanoma, kidney, and lung adenocarcinoma. ICIs have limited response rates to other non-immunogenic cancers. The tumor microenvironment (TME) consists of many cell types that collectively promote tumor progression.
View Article and Find Full Text PDFBiomed Pharmacother
January 2025
Ph.D. Program in Medical Neuroscience, Taipei Medical University and National Health Research Institutes, Taipei 11031, Taiwan; TMU Research Center for Drug Discovery, Taipei Medical University, Taipei 11031, Taiwan; International Master Program in Medical Neuroscience, Taipei Medical University, New Taipei City 23564, Taiwan; TMU Research Center of Neuroscience, Taipei Medical University, Taipei 11031, Taiwan; Department of Biomedical Science and Environmental Biology, Kaohsiung Medical University, Kaohsiung 80780, Taiwan. Electronic address:
Traumatic brain injury (TBI) constitutes a significant burden on global healthcare systems, especially affecting younger populations, where it is a leading cause of disability and mortality. Current treatments for TBI mainly focus on preventing further brain damage and controlling symptoms. However, despite these approaches, several clinical needs remain unmet.
View Article and Find Full Text PDFChin J Cancer Res
December 2024
Department of Oncology, the Affiliated Cancer Hospital of Zhengzhou University & Henan Cancer Hospital, Henan Engineering Research Center of Precision Therapy of Gastrointestinal Cancer and Zhengzhou Key Laboratory for Precision Therapy of Gastrointestinal Cancer, Zhengzhou 450008, China.
Gastric cancer (GC) ranks 3rd in incidence rate and mortality rate among malignant tumors in China, and the age-standardized five-year net survival rate of patients with GC was 35.9% from 2010 to 2014. The tumor immune microenvironment (TIME), which includes T cells, macrophages, natural killer (NK) cells and B cells, significantly affects tumor progression, immunosuppression and drug resistance in patients with GC.
View Article and Find Full Text PDFEur J Med Chem
January 2025
School of Medical and Information Engineering, School of Pharmacy, Gannan Medical University, Ganzhou, 341000, PR China; Jiangxi Provincial Key Laboratory of Tissue Engineering, Gannan Medical University, Ganzhou, 341000, PR China. Electronic address:
Epigenetic dysregulation plays a pivotal role in the initiation and progression of various cancers, influencing critical processes such as tumor growth, invasion, migration, survival, apoptosis, and angiogenesis. Consequently, targeting epigenetic pathways has emerged as a promising strategy for anticancer drug discovery in recent years. However, the clinical efficacy of epigenetic inhibitors, such as HDAC inhibitors, has been limited, often accompanied by resistance.
View Article and Find Full Text PDFBackground: Atypical teratoid rhabdoid tumor (ATRT) is the most common malignant brain tumor in infants, and more than 60% of children with ATRT die from their tumor. ATRT is associated with mutational inactivation/deletion of , a member of the SWI/SNF chromatin remodeling complex, suggesting that epigenetic events play a critical role in tumor development and progression. Moreover, disruption of SWI/SNF allows unopposed activity of epigenetic repressors, which contribute to tumorigenicity.
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