Search results for: Matthias Groh

Items from 1 to 12 out of 12 results

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RNA/DNA Hybrid Interactome Identifies DXH9 as a Molecular Player in Transcriptional Termination and R-Loop-Associated DNA Damage

Agnese Cristini, Matthias Groh, Maiken S. Kristiansen, Natalia Gromak

Cell Reports > 2018 > 23 > 6 > 1891-1905

R-loops comprise an RNA/DNA hybrid and displaced single-stranded DNA. They play important biological roles and are implicated in pathology. Even so, proteins recognizing these structures are largely undefined. Using affinity purification with the S9.6 antibody coupled to mass spectrometry, we defined the RNA/DNA hybrid interactome in HeLa cells. This consists of known R-loop-associated factors SRSF1,...

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Senataxin: Genome Guardian at the Interface of Transcription and Neurodegeneration

Matthias Groh, Laura Oana Albulescu, Agnese Cristini, Natalia Gromak

Journal of Molecular Biology > 2017 > 429 > 21 > 3181-3195

R-loops comprise an RNA/DNA hybrid and a displaced single-stranded DNA. They play crucial biological functions and are implicated in neurological diseases, including ataxias, amyotrophic lateral sclerosis, nucleotide expansion disorders (Friedreich ataxia and fragile X syndrome), and cancer. Currently, it is unclear which mechanisms cause R-loop structures to become pathogenic. The RNA/DNA helicase...

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Exploring the chemical space of ureidothiophene-2-carboxylic acids as inhibitors of the quorum sensing enzyme PqsD from Pseudomonas aeruginosa

J. Henning Sahner, Martin Empting, Ahmed Kamal, Elisabeth Weidel, more

European Journal of Medicinal Chemistry > 2015 > 96 > C > 14-21

Pseudomonas aeruginosa employs a quorum sensing (QS) communication system that makes use of small diffusible molecules. Among other effects, the QS system coordinates the formation of biofilm which decisively contributes to difficulties in the therapy of Pseudomonas infections. The present work deals with the structure-activity exploration of ureidothiophene-2-carboxylic acids as inhibitors of PqsD,...

article

Cooking enhances curcumin anti-cancerogenic activity through pyrolytic formation of “deketene curcumin”

Indra N. Dahmke, Stefan P. Boettcher, Matthias Groh, Ulrich Mahlknecht

Food Chemistry > 2014 > 151 > Complete > 514-519

Curcumin is widely used in traditional Asian kitchen as a cooking ingredient. Despite its low bioavailability, epidemiological data, on low cancer incidence in Asia, suggest beneficial health effects of this compound. Therefore, the question arose whether cooking modifies the anti-cancerogenic effects of curcumin. To evaluate this, we pyrolysed curcumin with and without coconut fat or olive oil, and...

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Benzamidobenzoic acids as potent PqsD inhibitors for the treatment of Pseudomonas aeruginosa infections

Stefan Hinsberger, Johannes C. de Jong, Matthias Groh, Jörg Haupenthal, more

European Journal of Medicinal Chemistry > 2014 > 76 > Complete > 343-351

Targeting PqsD is a promising novel approach to disrupt bacterial cell-to-cell-communication in Pseudomonas aeruginosa. In search of selective PqsD inhibitors, two series of benzamidobenzoic acids – one published as RNAP inhibitors and the other as PqsD inhibitors – were investigated for inhibitory activity toward the respective other enzyme. Additionally, novel derivatives were synthesized and biologically...

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Novel small molecule inhibitors targeting the “switch region” of bacterial RNAP: Structure-based optimization of a virtual screening hit

J. Henning Sahner, Matthias Groh, Matthias Negri, Jörg Haupenthal, more

European Journal of Medicinal Chemistry > 2013 > 65 > Complete > 223-231

Rising resistance against current antibiotics necessitates the development of antibacterial agents with alternative targets. The “switch region” of RNA polymerase (RNAP), addressed by the myxopyronins, could be such a novel target site. Based on a hit candidate discovered by virtual screening, a small library of 5-phenyl-3-ureidothiophene-2-carboxylic acids was synthesized resulting in compounds with...

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A Detective Story in Drug Discovery: Elucidation of a Screening Artifact Reveals Polymeric Carboxylic Acids as Potent Inhibitors of RNA Polymerase

Weixing Zhu, Matthias Groh, Jörg Haupenthal, Rolf W. Hartmann

Chemistry – A European Journal > 19 > 26 > 8397 - 8400

Chasing the active impurity: In the validation of a screening hit it was discovered that a polymeric trace impurity was responsible for the biological activity. Such a side product can be formed with similar compounds. During the investigations it was discovered that the negatively charged macromolecule interacts very efficiently with the protein surface of E. coli RNAP via electrostatic interactions.

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Enantiopure isoplagiochin C by directed deracemization through axis-to-axis chirality transfer

Gerhard Bringmann, Dominik Hager, Anu Schaumlöffel, Matthias Groh, more

Tetrahedron: Asymmetry > 2013 > 24 > 9-10 > 575-581

Isoplagiochin C 1 was prepared for the first time in enantiopure form from synthetic racemic material, using a novel stereochemical concept. This macrocyclic bisbibenzyl contains two biaryl axes. Of these, axis A is configurationally stable by its fixation within the macrocyclic framework, while axis B is stereochemically unstable. By diesterification of rac-1 with enantiopure (P)-1,1′-binaphthyl-2,2′-dicarboxylic...

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Configurational Assignment of Cyclic Bisbibenzyls by HPLC‐CD and Quantum‐Chemical CD Calculations

Anu Schaumlöffel, Matthias Groh, Michael Knauer, Andreas Speicher, more

European Journal of Organic Chemistry > 2012 > 35 > 6878 - 6887

Macrocyclic bisbibenzyls are intriguing natural products that are obtained from liverworts. Recently, they have received growing interest due to the discovery of novel representatives and because of their antitumoral and antifungal activities. Depending on the individual coupling type, these structures can possess one or two biaryl axes, which, with larger ortho substituents or increased ring strain...

article

[(Bi₈²⁺)Ru²⁺(Bi₈²⁺)] – Coordination Chemistry of Bismuth Polycations

Matthias Groh, Michael Ruck

Zeitschrift für anorganische und allgemeine Chemie > 638 > 10 > 1568 - 1568

article

Syntheses of Macrocyclic Bis(bibenzyl) Compounds Derived from Perrottetin E

Andreas Speicher, Matthias Groh, Markus Hennrich, Anh‐Minh Huynh

European Journal of Organic Chemistry > 2010 > 35 > 6760 - 6778

Macrocyclic bis(bibenzyl) compounds are natural products from liverworts and are of growing interest due to recent reports on new isolated compounds and on their remarkable biological activities. We report here on a flexible and general approach to the total set of nine bis(bibenzyl) compounds of the riccardin and plagiochin type derived from perrottetin E. The structures were confirmed through their...

article

Room‐Temperature Synthesis of the Highly Polar Cluster Compound Sn[SnCl][W₃Cl₁₃]

Ejaz Ahmed, Matthias Groh, Michael Ruck

European Journal of Inorganic Chemistry > 2010 > 33 > 5294 - 5297

A new synthetic strategy is employed to synthesize a tungsten trinuclear cluster compound with an ionic liquid (IL) as the reaction medium. Dark brown block‐shaped crystals of Sn[SnCl][W₃Cl₁₃] were obtained at room temperature by reacting tin and WCl₆ in Lewis acidic ionic liquid [BMIM]Cl/AlCl₃ ([BMIM]⁺ = 1‐butyl‐3‐methylimidazolium). Compound Sn[SnCl][W₃Cl₁₃] crystallizes in the polar hexagonal space...

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