New pyrrole derivatives as DNA gyrase and 14α-demethylase inhibitors: Design, synthesis, antimicrobial evaluation, and molecular docking.
Sign Up to like & getrecommendations! Published in 2023 at "Drug development research"
DOI: 10.1002/ddr.22080
Abstract: An efficient one-pot reaction utilizing readily available chemical reagents was used to prepare novel 2-amino-1,5-diaryl-1H-pyrrole-3-carbonitrile derivatives and the structures of these compounds were validated by spectroscopic data and elemental analyses. All the synthetic compounds were… read more here.
Keywords: demethylase; dna gyrase; ic50; gyrase demethylase ... See more keywords
Antiproliferative effect of the histone demethylase inhibitor GSK‐J4 in chondrosarcomas
Sign Up to like & getrecommendations! Published in 2019 at "IUBMB Life"
DOI: 10.1002/iub.2110
Abstract: Chondrosarcoma (CS) is the second most common malignant bone sarcoma. Its treatment remains an issue, because this tumor is radio‐ and chemo‐resistant. In the present study, we investigated the antitumoral potential of GSK‐J4, a small… read more here.
Keywords: demethylase; antiproliferative effect; cisplatin; proliferation ... See more keywords
Glutathione-Bioimprinted Nanoparticles Targeting of N6-methyladenosine FTO Demethylase as a Strategy against Leukemic Stem Cells.
Sign Up to like & getrecommendations! Published in 2022 at "Small"
DOI: 10.1002/smll.202106558
Abstract: The N6-methyladenosine (m6 A) demethylase FTO plays an oncogenic role in acute myeloid leukemia (AML). Despite the promising recent progress for developing some small-molecule FTO inhibitors, the clinical potential remains limited due to mild biological… read more here.
Keywords: fto; methyladenosine; stem cells; leukemic stem ... See more keywords
Biological roles of LSD1 beyond its demethylase activity
Sign Up to like & getrecommendations! Published in 2020 at "Cellular and Molecular Life Sciences"
DOI: 10.1007/s00018-020-03489-9
Abstract: It is well-established that Lysine-specific demethylase 1 (LSD1, also known as KDM1A) roles as a lysine demethylase canonically acting on H3K4me1/2 and H3K9me1/2 for regulating gene expression. Though the discovery of non-histone substrates methylated by… read more here.
Keywords: demethylase activity; roles lsd1; demethylase; lsd1 beyond ... See more keywords
Novel inhibitors of lysine (K)-specific Demethylase 4A with anticancer activity
Sign Up to like & getrecommendations! Published in 2017 at "Investigational New Drugs"
DOI: 10.1007/s10637-017-0496-2
Abstract: SummaryLysine (K)-specific demethylase 4A (KDM4A) is a histone demethylase that removes methyl residues from trimethylated or dimethylated histone 3 at lysines 9 and 36. Overexpression of KDM4A is found in various cancer types. To identify… read more here.
Keywords: demethylase; ldd2269; kdm4a; novel inhibitors ... See more keywords
Probing the interaction of the p53 C-terminal domain to the histone demethylase LSD1.
Sign Up to like & getrecommendations! Published in 2017 at "Archives of biochemistry and biophysics"
DOI: 10.1016/j.abb.2017.07.021
Abstract: The p53 transcription factor plays a central role in the regulation of the expression of several genes, and itself is post-translationally regulated through its different domains. Of particular relevance for p53 function is its intrinsically… read more here.
Keywords: terminal domain; demethylase; lsd1; p53 ... See more keywords
Mechanism of Crosstalk between the LSD1 Demethylase and HDAC1 Deacetylase in the CoREST Complex
Sign Up to like & getrecommendations! Published in 2020 at "Cell Reports"
DOI: 10.1016/j.celrep.2020.01.091
Abstract: Summary The transcriptional corepressor complex CoREST is one of seven histone deacetylase complexes that regulate the genome through controlling chromatin acetylation. The CoREST complex is unique in containing both histone demethylase and deacetylase enzymes, LSD1… read more here.
Keywords: deacetylase; demethylase; corest complex; corest ... See more keywords
It takes two to tango - The case of thebaine 6-O-demethylase.
Sign Up to like & getrecommendations! Published in 2020 at "International journal of biological macromolecules"
DOI: 10.1016/j.ijbiomac.2020.07.030
Abstract: Thebaine 6-O-demethylase (T6ODM) is an Fe(II)/2-oxoglutarate-dependent dioxygenase catalysing two oxidative O-demethylation reactions in morphine biosynthesis. Its crystal structure revealed a large active site pocket which is at least two times larger than necessary to accommodate… read more here.
Keywords: tango case; takes two; demethylase; two tango ... See more keywords
Thebaine is Selectively Demethylated by Thebaine 6-O-Demethylase and Codeine-3-O-demethylase at Distinct Binding Sites: A Computational Study.
Sign Up to like & getrecommendations! Published in 2021 at "Inorganic chemistry"
DOI: 10.1021/acs.inorgchem.1c00468
Abstract: Two homologous 2-oxoglutarate-dependent (ODD) nonheme enzymes thebaine 6-O-demethylase (T6ODM) and codeine-3-O-demethylase (CODM), are involved in the morphine biosynthesis pathway from thebaine, catalyzing the O-demethylation reaction with precise regioselectivity at C6 and C3 positions of thebaine… read more here.
Keywords: regioselectivity; codeine demethylase; demethylase; thebaine demethylase ... See more keywords
Discovery of CC-90011: A Potent and Selective Reversible Inhibitor of Lysine Specific Demethylase 1 (LSD1).
Sign Up to like & getrecommendations! Published in 2020 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.0c00978
Abstract: Histone demethylase LSDl (KDMlA) belongs to the flavin adenine dinucleotide (FAD) dependent family of monoamine oxidases and is vital in regulation of mammalian biology. Dysregulation and overexpression of LSD1 are hallmarks of a number of… read more here.
Keywords: potent selective; discovery 90011; demethylase; selective reversible ... See more keywords
Rational Design and Optimization of m6A-RNA Demethylase FTO Inhibitors as Anticancer Agents
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.1c02075
Abstract: Aberrant regulation of N6-methyladenosine (m6A) RNA modification has been implicated in the progression of multiple diseases, including cancer. Previously, we identified a small molecule inhibitor of the m6A demethylase fat mass- and obesity-associated protein (FTO),… read more here.
Keywords: m6a rna; demethylase; fto; m6a ... See more keywords