Results 11 to 20 of about 37,262 (190)
Translational Neuroscience, 2023 Brain vascular inflammation is characterized by endothelial activation and immune cell recruitment to the blood vessel wall, potentially causing a breach in the blood – brain barrier, brain parenchyma inflammation, and a decline of cognitive function ...
Wasiak Sylwia +14 more
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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
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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
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The BRPF1 bromodomain is a molecular reader of di-acetyllysine
Current Research in Structural Biology, 2020 Bromodomain-containing proteins are often part of chromatin-modifying complexes, and their activity can lead to altered expression of genes that drive cancer, inflammation and neurological disorders in humans.
Juliet O. Obi +10 more
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Bromodomains as therapeutic targets [PDF]
Expert Reviews in Molecular Medicine, 2011 Acetylation of lysine residues is a post-translational modification with broad relevance to cellular signalling and disease biology. Enzymes that ‘write’ (histone acetyltransferases, HATs) and ‘erase’ (histone deacetylases, HDACs) acetylation sites are an area of extensive research in current drug development, but very few potent inhibitors that ...
Muller, S, Filippakopoulos, P, Knapp, S
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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
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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
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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
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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
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BRD4 associates with p53 in DNMT3A-mutated leukemia cells and is implicated in apoptosis by the bromodomain inhibitor JQ1 [PDF]
, 2013 The bromodomain and extra terminal (BET) family protein bromodomain containing protein 4 (BRD4) is an epigenetic regulator recently identified as a therapeutic target for several hematological cancers, notably mixed lineage leukemia-fusion acute myeloid ...
Bastow, Sarah +3 more
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