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Search for "histone" in Full Text gives 38 result(s) in Beilstein Journal of Organic Chemistry.

Investigation of the action of poly(ADP-ribose)-synthesising enzymes on NAD+ analogues

  • Sarah Wallrodt,
  • Edward L. Simpson and
  • Andreas Marx

Beilstein J. Org. Chem. 2017, 13, 495–501, doi:10.3762/bjoc.13.49

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  • -step procedure (Supporting Information File 1, Scheme S1). Next, NAD+ substrate properties were investigated in ADP-ribosylation assays with histone H1.2 as acceptor and in ARTD automodification. For a better comparison, the assay conditions for ARTD2, ARTD5 and ARTD6 were chosen to be similar and were
  • derived from previously established ARTD1 catalysed ADP-ribosylation [21]. Incubation of NAD+ or NAD+ analogues with ARTD enzyme in reaction buffer and with or without histone H1.2 as additional acceptor protein were performed at 30 °C to decrease the reported NADase activity of tankyrases [15]. Reaction
  • [25] and can be detected by some minor staining of the involved proteins, which is also visible in some of the investigated reactions. As expected from the close structural similarity between ARTD1 and ARTD2 (panel a and b), both enzymes behave similarly in histone ADP-ribosylation (Supporting
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Published 10 Mar 2017

Synthesis of spiro[isoindole-1,5’-isoxazolidin]-3(2H)-ones as potential inhibitors of the MDM2-p53 interaction

  • Salvatore V. Giofrè,
  • Santa Cirmi,
  • Raffaella Mancuso,
  • Francesco Nicolò,
  • Giuseppe Lanza,
  • Laura Legnani,
  • Agata Campisi,
  • Maria A. Chiacchio,
  • Michele Navarra,
  • Bartolo Gabriele and
  • Roberto Romeo

Beilstein J. Org. Chem. 2016, 12, 2793–2807, doi:10.3762/bjoc.12.278

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  • , chilenine, lennoxamine, magallanesine and nuevamine [20][21][22][23][24][25]. These compounds possess a lot of pharmacological activities such as anxiolytic/anticonvulsant, TNFα-inhibitory, antiangiogenic, 5-HT antagonistic/antidepressant [26][27][28][29][30], PARP-1-inhibitory [31], histone deacetylase
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Published 20 Dec 2016

From supramolecular chemistry to the nucleosome: studies in biomolecular recognition

  • Marcey L. Waters

Beilstein J. Org. Chem. 2016, 12, 1863–1869, doi:10.3762/bjoc.12.175

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  • -helices; aromatic interactions; β-hairpin peptides; cation–π interactions; dynamic combinatorial chemistry; histone; molecular recognition in water; nucleosome; π–π-stacking; post-translational modification; supramolecular chemistry; Review Childhood influences When thinking about how to start writing
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Published 17 Aug 2016

Diversity-oriented synthesis of analogues of the novel macrocyclic peptide FR-225497 through late stage functionalization

  • Jyotiprasad Mukherjee,
  • Suman Sil and
  • Shital Kumar Chattopadhyay

Beilstein J. Org. Chem. 2015, 11, 2487–2492, doi:10.3762/bjoc.11.270

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  • which involves a late-stage functionalization of a macrocyclic scaffold through cross metathesis in an attempt to create diversity. The utility of this protocol is demonstrated through the preparation of three structural analogues of the important naturally occurring histone deacetylase inhibitor FR
  • peptides of the general structure 1 (Figure 1) displays important histone deacetylase inhibition property relevant to drug design against a number of diseases ranging from antifungal, antimicrobial to arrest of proliferation of several cell types of epithelial and hematological origin [13]. The compounds
  • of the spacer region as well as the metal-binding domain attached to a particular surface recognition part present in the class of these compounds since histone deacetylase activity has been correlated to zinc-binding ability of the 8-oxo moiety in some of such compounds [25]. Moreover, the
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Published 08 Dec 2015

Regulation of integrin and growth factor signaling in biomaterials for osteodifferentiation

  • Qiang Wei,
  • Theresa L. M. Pohl,
  • Anja Seckinger,
  • Joachim P. Spatz and
  • Elisabetta A. Cavalcanti-Adam

Beilstein J. Org. Chem. 2015, 11, 773–783, doi:10.3762/bjoc.11.87

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  • , which significantly improve cell reprogramming [34]. The regulated cell adhesion can decrease histone deacetylase activity and upregulate the expression of WD repeat domain 5 (WDR5). As a result, the mechanomodulation of the epigenetic state of cells can be controlled. Cell reprogramming allows the
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Published 13 May 2015

Synthesis of antibacterial 1,3-diyne-linked peptoids from an Ugi-4CR/Glaser coupling approach

  • Martin C. N. Brauer,
  • Ricardo A. W. Neves Filho,
  • Bernhard Westermann,
  • Ramona Heinke and
  • Ludger A. Wessjohann

Beilstein J. Org. Chem. 2015, 11, 25–30, doi:10.3762/bjoc.11.4

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  • structures as well as simple Ugi products exhibit promising biological profiles, e.g., cytotoxicity [13][19][20], fungicidal [21][22] and antibacterial properties [23][24][25][26], or inhibition of histone deacetylases [27]. The Ugi post-modification strategy has also been employed in the synthesis of
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Published 07 Jan 2015

Synthesis of novel derivatives of 5-hydroxymethylcytosine and 5-formylcytosine as tools for epigenetics

  • Anna Chentsova,
  • Era Kapourani and
  • Athanassios Giannis

Beilstein J. Org. Chem. 2014, 10, 7–11, doi:10.3762/bjoc.10.2

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  • -enzymes; Introduction Epigenetic modifications play a crucial role in cell differentiation and cell development [1]. They control gene expression through several mechanisms such as non-coding RNAs, histone modifications (acetylation, methylation, phosphorylation, etc.) [2], and DNA methylation [3][4][5
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Published 03 Jan 2014

SF002-96-1, a new drimane sesquiterpene lactone from an Aspergillus species, inhibits survivin expression

  • Silke Felix,
  • Louis P. Sandjo,
  • Till Opatz and
  • Gerhard Erkel

Beilstein J. Org. Chem. 2013, 9, 2866–2876, doi:10.3762/bjoc.9.323

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  • -1β and treatment of the cells with the fungal compound (Figure 5), corroborating the results obtained in the reporter gene assays. As a control, we investigated the influence of the compound on the binding of lysine9 acetylated histone H3 (H3K9Ac) to the constitutive gapdh promoter as a marker for
  • -lysine9 acetylated histone H3 antibody (9671, New England Biolabs, Frankfurt/M) at dilutions recommended by the manufacturers (1:50). The immunoprecipitates were pelleted and incubated at 65 °C overnight to reverse cross-links. The DNA was extracted by phenol–chloroform extraction and precipitated with
  • IL-6 (for Stat3) and 10 ng/mL TNF-α, 5 ng/mL IL-1β (for NF-κB) for 30 min. Chromatin was cross-linked and immunoprecipitated using antibodies against Stat3, NF-κB p65, acetylated histone 3 (H3K9Ac) or rabbit IgG. DNA isolated from immunoprecipitates or from total chromatin preparation before
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Published 13 Dec 2013

Recent progress in the discovery of small molecules for the treatment of amyotrophic lateral sclerosis (ALS)

  • Allison S. Limpert,
  • Margrith E. Mattmann and
  • Nicholas D. P. Cosford

Beilstein J. Org. Chem. 2013, 9, 717–732, doi:10.3762/bjoc.9.82

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  • compounds modestly reduced intercellular levels of TDP-43 [43] as well as histone deacetylase 6 (HDAC-6) and autophagy-related protein 7 (ATG-7), proteins known to be regulated by TDP-43 [45][46]. Since reduction of TDP-43 levels in motor neurons may prove to be beneficial to ALS treatment, further
  • , treatment with 32 prolonged the post-onset survival of SOD1 H46R animals [68]. These studies indicate that the attenuation of oxidative-stress pathways through the upregulation of antioxidant genes can reduce disease progression in ALS models. Novel mechanisms Histone deacetylase (HDAC) inhibitors: Several
  • gene analysis studies have discovered distinct gene expression profiles in ALS patients [69][70], indicating that transcriptional dysfunction may contribute to ALS pathology [71]. One mechanism of eliciting changes in gene expression is through the acetylation of histone proteins, which allows access
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Published 15 Apr 2013

Thioester derivatives of the natural product psammaplin A as potent histone deacetylase inhibitors

  • Matthias G. J. Baud,
  • Thomas Leiser,
  • Vanessa Petrucci,
  • Mekala Gunaratnam,
  • Stephen Neidle,
  • Franz-Josef Meyer-Almes and
  • Matthew J. Fuchter

Beilstein J. Org. Chem. 2013, 9, 81–88, doi:10.3762/bjoc.9.11

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  • . Keywords: epigenetics; histone deacetylase; natural product; prodrug; psammaplin A; thioester; Introduction Chromatin is a macromolecular complex consisting of DNA, histone and nonhistone proteins. The epigenetic control of chromatin organization plays a major role in the regulation of gene expression
  • epigenetic modifications, their biological outcomes, and how their misregulation is involved in diseases such as cancer [1][2]. The dynamic post-translational acetylation/deacetylation of histone proteins is one of the most commonly studied epigenetic events, and occurs at specific lysine residues on the N
  • -terminal histone tails, which project out from the nucleosome (the fundamental repeating unit of chromatin). Acetylation/deacetylation of such lysine residues is achieved by the action of histone acetyltransferases (HATs) and histone deacetylases (HDACs), respectively. Histone deacetylation by HDACs causes
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Published 15 Jan 2013

Synthesis and in silico screening of a library of β-carboline-containing compounds

  • Kay M. Brummond,
  • John R. Goodell,
  • Matthew G. LaPorte,
  • Lirong Wang and
  • Xiang-Qun Xie

Beilstein J. Org. Chem. 2012, 8, 1048–1058, doi:10.3762/bjoc.8.117

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  • NIH Molecular Repository (MLSMR) and may target proteins such as histone deacetylase 4, endothelial nitric oxide synthase, 5-hydroxytryptamine receptor 6 and mitogen-activated protein kinase 1. These in silico screening results aim to add value to the β-carboline library of compounds for those
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Published 10 Jul 2012

RAFT polymers for protein recognition

  • Alan F. Tominey,
  • Julia Liese,
  • Sun Wei,
  • Klaus Kowski,
  • Thomas Schrader and
  • Arno Kraft

Beilstein J. Org. Chem. 2010, 6, No. 66, doi:10.3762/bjoc.6.66

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  • could be detected for the short version, indicating that size matters and promotes multivalent or cooperative binding. Finally, the protein series was extended to lysine-rich histone (pI 10), lysozyme (pI 9), proteinase K (pI 8) and bovine serum albumin or BSA (pI 6). Again, the strong binders B20CH15
  • – admittedly much weaker – 2:1 complex. Histone association with B20CH15 is an illustrative example. The first Kd value is 16 nM, followed by very weak binding at a second site with a Kd of 1 mM. With respect to varying pI values, both RAFT polymers display little selectivity: From lysozyme (pI > 9) down to
  • -containing RAFT copolymer and lysine–rich histone (Kd = 16 nM). In the future, we intend to investigate if it is possible to interrupt the nucleosome complex formation by noncovalent detachment of ds-DNA from its “own” histone proteins using histone-binding RAFT copolymers. Structures of monomers 1–7 and
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Published 17 Jun 2010

Molecular recognition of organic ammonium ions in solution using synthetic receptors

  • Andreas Späth and
  • Burkhard König

Beilstein J. Org. Chem. 2010, 6, No. 32, doi:10.3762/bjoc.6.32

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Published 06 Apr 2010
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