Search Results - "Belle, Roman"

Investigations on small molecule inhibitors targeting the histone H3K4 tri-methyllysine binding PHD-finger of JmjC histone demethylases by Bhushan, Bhaskar, Erdmann, Alexandre, Zhang, Yijia, Belle, Roman, Johannson, Catrine, Oppermann, Udo, Hopkinson, Richard J., Schofield, Christopher J., Kawamura, Akane

“…[Display omitted] Plant homeodomain (PHD) containing proteins are important epigenetic regulators and are of interest as potential drug targets. Inspired by…”
Get full text

Thioether Macrocyclic Peptides Selected against TET1 Compact Catalytic Domain Inhibit TET1 Catalytic Activity by Nishio, Kosuke, Belle, Roman, Katoh, Takayuki, Kawamura, Akane, Sengoku, Toru, Hanada, Kazuharu, Ohsawa, Noboru, Shirouzu, Mikako, Yokoyama, Shigeyuki, Suga, Hiroaki

“…The ten–eleven translocation (TET) protein family, consisting of three isoforms (TET1/2/3), have been found in mammalian cells and have a crucial role in…”
Get full text

The Role of Electrostatic Interactions in Binding of Histone H3K4me2/3 to the Sgf29 Tandem Tudor Domain by Pieters, Bas J G E, Meulenbroeks, Erik, Belle, Roman, Mecinović, Jasmin

“…Several reader domain proteins that specifically recognize methyllysine-containing histones contain the negatively-charged aspartate or glutamate residues as…”
Get full text

Reading and erasing of the phosphonium analogue of trimethyllysine by epigenetic proteins by Belle, Roman, Kamps, Jos J. A. G., Poater, Jordi, Kumar, Kiran, Pieters, Bas J. G. E., Salah, Eidarus, Claridge, Timothy D. W., Paton, Robert S., Bickelhaupt, F. Matthias, Kawamura, Akane, Schofield, Christopher J., Mecinović, Jasmin

“…N ε -Methylation of lysine residues in histones plays an essential role in the regulation of eukaryotic transcription. The ‘highest’ methylation mark, N ε…”
Get full text

Expanding the chemical functionality of DNA nanomaterials generated by rolling circle amplification by Baker, Ysobel R, Yuan, Liyiwen, Chen, Jinfeng, Belle, Roman, Carlisle, Robert, El-Sagheer, Afaf H, Brown, Tom

“…Abstract Rolling circle amplification (RCA) is a powerful tool for the construction of DNA nanomaterials such as hydrogels, high-performance scaffolds and DNA…”
Get full text

Focused Screening Identifies Different Sensitivities of Human TET Oxygenases to the Oncometabolite 2‑Hydroxyglutarate by Belle, Roman, Saraç, Hilal, Salah, Eidarus, Bhushan, Bhaskar, Szykowska, Aleksandra, Roper, Grace, Tumber, Anthony, Kriaucionis, Skirmantas, Burgess-Brown, Nicola, Schofield, Christopher J., Brown, Tom, Kawamura, Akane

“…Ten-eleven translocation enzymes (TETs) are Fe­(II)/2-oxoglutarate (2OG) oxygenases that catalyze the sequential oxidation of 5-methylcytosine to…”
Get full text

Selective targeting of human TET1 by cyclic peptide inhibitors: Insights from biochemical profiling by Šimelis, Klemensas, Saraç, Hilal, Salah, Eidarus, Nishio, Kosuke, McAllister, Tom E., Corner, Thomas P., Tumber, Anthony, Belle, Roman, Schofield, Christopher J., Suga, Hiroaki, Kawamura, Akane

“…[Display omitted] Ten-Eleven Translocation (TET) enzymes are Fe(II)/2OG-dependent oxygenases that play important roles in epigenetic regulation, but selective…”
Get full text

Dual LSD1 and HDAC6 Inhibition Induces Doxorubicin Sensitivity in Acute Myeloid Leukemia Cells by Bulut, Ipek, Lee, Adam, Cevatemre, Buse, Ruzic, Dusan, Belle, Roman, Kawamura, Akane, Gul, Sheraz, Nikolic, Katarina, Ganesan, A, Acilan, Ceyda

“…Defects in epigenetic pathways are key drivers of oncogenic cell proliferation. We developed a LSD1/HDAC6 multitargeting inhibitor (iDual), a hydroxamic acid…”
Get full text

Histone Lysine and Dna Methylation : Dynamic Marks in the Chromatin by Belle, Roman

“…Ten-eleven translocation (TET) enzymes are epigenetic enzymes that are responsible for the iterative oxidation of 5-methylcytosine (5mC) to…”
Get full text

Enantioselective Allylation of Selected ortho-Substituted Benzaldehydes: A Comparative Study by Hessler, Filip, Betík, Robert, Kadlčíková, Aneta, Belle, Roman, Kotora, Martin

“…We report a systematic study of the allylation of ortho‐substituted benzaldehydes under catalysis of a Lewis base (N,N‐dioxide), a Lewis acid (Keck…”
Get full text

Investigating d-lysine stereochemistry for epigenetic methylation, demethylation and recognition by Belle, Roman, Al Temimi, Abbas H K, Kumar, Kiran, Pieters, Bas J G E, Tumber, Anthony, Dunford, James E, Johansson, Catrine, Oppermann, Udo, Brown, Tom, Schofield, Christopher J, Hopkinson, Richard J, Paton, Robert S, Kawamura, Akane, Mecinović, Jasmin

“…Histone lysine methylation is regulated by N -methyltransferases, demethylases, and N -methyl lysine binding proteins. Thermodynamic, catalytic and…”
Get more information

The Effect of the Length of Histone H3K4me3 on Recognition by Reader Proteins by Pieters, Bas, Belle, Roman, Mecinović, Jasmin

“…Thermodynamic analyses of associations between reader domain proteins and histone H3K4me3 peptides demonstrated that the shortest recognised histone substrate…”
Get full text

Small-molecules that covalently react with a human prolyl hydroxylase - towards activity modulation and substrate capture by Bush, Jacob T, Leśniak, Robert K, Yeh, Tzu-Lan, Belle, Roman, Kramer, Holger, Tumber, Anthony, Chowdhury, Rasheduzzaman, Flashman, Emily, Mecinović, Jasmin, Schofield, Christopher J

“…We describe covalently binding modulators of the activity of human prolyl hydroxylase domain 2 (PHD2) and studies towards a strategy for photocapture of PHD2…”
Get more information

Hydroxylamine as an oxygen nucleophile: substitution of sulfonamide by a hydroxyl group in benzothiazole-2-sulfonamides by Kamps, Jos J A G, Belle, Roman, Mecinović, Jasmin

“…Benzothiazole-2-sulfonamides react with an excess of hydroxylamine in aqueous solutions to form 2-hydroxybenzothiazole, sulfur dioxide, and the corresponding…”
Get more information

Human histone demethylase KDM6B can catalyse sequential oxidations by Hopkinson, Richard J, Langley, Gareth W, Belle, Roman, Walport, Louise J, Dunne, Kate, Münzel, Martin, Salah, Eidarus, Kawamura, Akane, Claridge, Timothy D W, Schofield, Christopher J

“…Jumonji domain-containing demethylases (JmjC-KDMs) catalyse demethylation of Nε-methylated lysines on histones and play important roles in gene regulation. We…”
Get more information

Reading and erasing of the phosphonium analogue of trimethyllysine by epigenetic proteins by Belle, Roman, Kamps, Jos J A G, Poater, Jordi, Kumar, Kiran, Pieters, Bas J G E, Salah, Eidarus, Claridge, Timothy D W, Paton, Robert S, Bickelhaupt, F Matthias, Kawamura, Akane, Schofield, Christopher J, Mecinović, Jasmin

“…N -Methylation of lysine residues in histones plays an essential role in the regulation of eukaryotic transcription. The 'highest' methylation mark, N…”
Get full text