The BET family in immunity and disease

N Wang, R Wu, D Tang, R Kang - Signal transduction and targeted …, 2021 - nature.com
Innate immunity serves as the rapid and first-line defense against invading pathogens, and
this process can be regulated at various levels, including epigenetic mechanisms. The …

[HTML][HTML] PROTACs technology for treatment of Alzheimer's disease: Advances and perspectives

H Inuzuka, J Liu, W Wei, AH Rezaeian - Acta materia medica, 2022 - ncbi.nlm.nih.gov
Neurodegenerative diseases (NDs) are characteristic with progression of neuron
degeneration, resulting in dysfunction of cognition and mobility. Many neurodegenerative …

Discovery of QCA570 as an exceptionally potent and efficacious proteolysis targeting chimera (PROTAC) degrader of the bromodomain and extra-terminal (BET) …

C Qin, Y Hu, B Zhou, E Fernandez-Salas… - Journal of medicinal …, 2018 - ACS Publications
Proteins of the bromodomain and extra-terminal (BET) family are epigenetics “readers” and
promising therapeutic targets for cancer and other human diseases. We describe herein a …

[HTML][HTML] Inhibition of HDAC3 reverses Alzheimer's disease-related pathologies in vitro and in the 3xTg-AD mouse model

KJ Janczura, CH Volmar, GC Sartor… - Proceedings of the …, 2018 - pmc.ncbi.nlm.nih.gov
Alzheimer's disease (AD) is the leading cause of age-related dementia. Neuropathological
hallmarks of AD include brain deposition of β-amyloid (Aβ) plaques and accumulation of …

Bromodomain drug discovery–the past, the present, and the future

M Pervaiz, P Mishra, S Günther - The Chemical Record, 2018 - Wiley Online Library
With the bromodomain (BRD) inhibitor JQ1, a remarkable success story of BRD4 as a novel
drug target has been set off that yielded many anti‐cancer drugs that are now in clinical …

Basal cell carcinoma pathogenesis and therapy involving hedgehog signaling and beyond

A Bakshi, SC Chaudhary, M Rana… - Molecular …, 2017 - Wiley Online Library
Basal cell carcinoma (BCC) of the skin is driven by aberrant hedgehog signaling. Thus
blocking this signaling pathway by small molecules such as vismodegib inhibits tumor …

Alzheimer's disease-related epigenetic changes: novel therapeutic targets

A Paniri, MM Hosseini, H Akhavan-Niaki - Molecular Neurobiology, 2024 - Springer
Aging is a significant risk factor for Alzheimer's disease (AD), although the precise
mechanism and molecular basis of AD are not yet fully understood. Epigenetic mechanisms …

BRD4 inhibition attenuates inflammatory pain by ameliorating NLRP3 inflammasome-induced pyroptosis

T Hua, H Wang, X Fan, N An, J Li, H Song… - Frontiers in …, 2022 - frontiersin.org
Chronic pain, such as persistent inflammatory pain, remains a public health problem that
has no effective treatment at present. Bromodomain-containing protein 4 (BRD4) inhibition …

A human Tau expressing zebrafish model of progressive supranuclear palsy identifies Brd4 as a regulator of microglial synaptic elimination

Q Bai, E Shao, D Ma, B Jiao, SD Scheetz… - Nature …, 2024 - nature.com
Progressive supranuclear palsy (PSP) is an incurable neurodegenerative disease
characterized by 4-repeat (0N/4R)-Tau protein accumulation in CNS neurons. We generated …

Small molecule modulators of chromatin remodeling: from neurodevelopment to neurodegeneration

D Jiang, T Li, C Guo, TS Tang, H Liu - Cell & Bioscience, 2023 - Springer
The dynamic changes in chromatin conformation alter the organization and structure of the
genome and further regulate gene transcription. Basically, the chromatin structure is …