Results 31 to 40 of about 33,428 (239)
TRPM3-Induced Gene Transcription Is under Epigenetic Control
Pharmaceuticals, 2022 Transient receptor potential M3 (TRPM3) cation channels regulate numerous biological functions, including gene transcription. Stimulation of TRPM3 channels with pregnenolone sulfate activates stimulus-responsive transcription factors, which bind to short
Gerald Thiel, Oliver G. Rössler
doaj +1 more source
Hydrophobic Waters in Bromodomains [PDF]
The 2nd Molecules Medicinal Chemistry Symposium (MMCS): Facing Novel Challenges in Drug Discovery, 2019 Targeting epigenetic proteins is a rapidly growing area for medicinal chemistry and drug discovery. Recent years have seen an explosion of interest in developing small molecules binding to bromodomains due to their implication in cancer, inflammation, and a plethora of diseases.
Serena G. Piticchio +8 more
openaire +3 more sources
Frontiers in Cell and Developmental Biology, 2022 Epigenetic regulation is a critical mechanism in controlling virulence, differentiation, and survival of the human malaria parasite Plasmodium (P.) falciparum.
Jennifer E. Quinn +10 more
doaj +1 more source
Binding hotspots of BAZ2B bromodomain:histone interaction revealed by solution NMR driven docking [PDF]
, 2014 Bromodomains are epigenetic reader domains, which have come under increasing scrutiny both from academic and pharmaceutical research groups. Effective targeting of the BAZ2B bromodomain by small molecule inhibitors has been recently reported, but no ...
Ferguson, Fleur M. +26 more
core +1 more source
The bromodomain interaction module [PDF]
FEBS Letters, 2012 ε‐N‐acetylation of lysine residues (Kac) is one of the most abundant post‐translation modifications (PTMs) in the human proteome. In the nucleus, acetylation of histones has been linked to transcriptional activation of genes but the functional consequences of most acetylation events and proteins recruited to these sites remains largely unknown ...
Filippakopoulos, P, Knapp, S
openaire +2 more sources
Pharmaceuticals, 2022 Crescentic glomerulonephritis is a devastating autoimmune disease that without early and properly treatment may rapidly progress to end-stage renal disease and death.
Lucia Tejedor-Santamaria +13 more
doaj +1 more source
BET bromodomain inhibition as a therapeutic strategy to target c-Myc
Cell, 2011 SUMMARY MYC contributes to the pathogenesis of a majority of human cancers, yet strategies to modulate the function of the c-Myc oncoprotein do not exist.
Citation Delmore +25 more
semanticscholar +1 more source
Molecules and Cells, 2020 SUMMARY BET bromodomain inhibitors (BBDI) are candidate therapeutic agents in triple-negative breast cancer (TNBC) and other cancer types, but inherent and acquired resistance to BBDIs limit their potential clinical use.
Shaokun Shu +41 more
semanticscholar +1 more source
Design and Synthesis of Hybrid Compounds as Epigenetic Modifiers
Pharmaceuticals, 2021 Epigenetic modifiers acting through polypharmacology mechanisms are promising compounds with which to treat several infectious diseases. Histone deacetylase (HDAC) enzymes, mainly class I, and extra-terminal bromodomains (BET) are involved in viral ...
Juliana Romano Lopes +4 more
doaj +1 more source
Proceedings of the National Academy of Sciences of the United States of America, 2022 Significance BET bromodomain inhibition is therapeutic in multiple diseases; however, pan-BET inhibitors have induced significant myelosuppression and gastrointestinal toxicity, perhaps due to inhibition of both tandem bromodomains (BD) of all BET family
Ramkumar Modukuri +20 more
semanticscholar +1 more source