Results 51 to 60 of about 81,753 (307)
Bifunctional HDAC Therapeutics: One Drug to Rule Them All?
Molecules, 2020 Histone deacetylase (HDAC) enzymes play crucial roles in epigenetic gene expression and are an attractive therapeutic target. Five HDAC inhibitors have been approved for cancer treatment to date, however, clinical applications have been limited due to ...
Joshua P. Smalley +2 more
doaj +1 more source
Clinical Epigenetics, 2012 The zinc-dependent mammalian histone deacetylase (HDAC) family comprises 11 enzymes, which have specific and critical functions in development and tissue homeostasis.
Delcuve Geneviève P +2 more
doaj +1 more source
Targeting phosphoinositide 3-kinase (PI3K) in head and neck squamous cell carcinoma (HNSCC). [PDF]
, 2018 The landscape of head and neck squamous cell carcinoma (HNSCC) has been changing rapidly due to growing proportion of HPV-related disease and development of new therapeutic agents.
Jung, Kyungsuk +2 more
core +2 more sources
FEBS Letters, EarlyView.This perspective highlights emerging insights into how the circadian transcription factor CLOCK:BMAL1 regulates chromatin architecture, cooperates with other transcription factors, and coordinates enhancer dynamics. We propose an updated framework for how circadian transcription factors operate within dynamic and multifactorial chromatin landscapes ...
Xinyu Y. Nie, Jerome S. Menet
wiley +1 more source
Thermal shift engagement assay for Class IIA histone deacetylase inhibitor screening
Results in ChemistryHistone deacetylase (HDAC) proteins are the targets of several anti-cancer clinical drugs, which motivates future inhibitor development. Class IIA HDAC proteins, HDAC4, HDAC5, HDAC7, and HDAC9, are pseudodeacetylases that lack a key catalytic amino acid ...
Lauren N. Kotsull, Mary Kay H. Pflum
doaj +1 more source
The Role of HDACs and HDACi in Cartilage and Osteoarthritis
Frontiers in Cell and Developmental Biology, 2020 Epigenetics plays an important role in the pathogenesis and treatment of osteoarthritis (OA). In recent decades, HDAC family members have been associated with OA.
He Zhang +5 more
doaj +1 more source
ING1 inhibits Twist1 expression to block EMT and is antagonized by the HDAC inhibitor vorinostat
European Journal of Cell Biology, 2023 ING1 is a chromatin targeting subunit of the Sin3a histone deacetylase (HDAC) complex that alters chromatin structure to subsequently regulate gene expression.
Yang Yang +14 more
doaj +1 more source
The role of histone modifications in transcription regulation upon DNA damage
FEBS Letters, EarlyView.This review discusses the critical role of histone modifications in regulating gene expression during the DNA damage response (DDR). By modulating chromatin structure and recruiting repair factors, these post‐translational modifications fine‐tune transcriptional programmes to maintain genomic stability.
Angelina Job Kolady, Siyao Wang
wiley +1 more source
Molecular Oncology, EarlyView.HDAC4 is degraded by the E3 ligase FBXW7. In colorectal cancer, FBXW7 mutations prevent HDAC4 degradation, leading to oxaliplatin resistance. Forced degradation of HDAC4 using a PROTAC compound restores drug sensitivity by resetting the super‐enhancer landscape, reprogramming the epigenetic state of FBXW7‐mutated cells to resemble oxaliplatin ...
Vanessa Tolotto +13 more
wiley +1 more source
Disease Models & Mechanisms, 2016 Clinical management of abdominal aortic aneurysm (AAA) is currently limited to elective surgical repair because an effective pharmacotherapy is still awaited.
María Galán +8 more
doaj +1 more source