Search Results - "SPITZFADEN, Claus"
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Type IIA topoisomerase inhibition by a new class of antibacterial agents
Published in Nature (London) (19-08-2010)“…Despite the success of genomics in identifying new essential bacterial genes, there is a lack of sustainable leads in antibacterial drug discovery to address…”
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Structural basis of DNA gyrase inhibition by antibacterial QPT-1, anticancer drug etoposide and moxifloxacin
Published in Nature communications (07-12-2015)“…New antibacterials are needed to tackle antibiotic-resistant bacteria. Type IIA topoisomerases (topo2As), the targets of fluoroquinolones, regulate DNA…”
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3
Discovery of functionally distinct anti-C7 monoclonal antibodies and stratification of anti-nicotinic AChR positive Myasthenia Gravis patients
Published in Frontiers in immunology (05-09-2022)“…Myasthenia Gravis (MG) is mediated by autoantibodies against acetylcholine receptors that cause loss of the receptors in the neuromuscular junction…”
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Structural Requirements for Biological Activity of the Ninth and Tenth FIII Domains of Human Fibronectin
Published in The Journal of biological chemistry (07-03-1997)“…The ninth and tenth type III domains of fibronectin each contain specific cell binding sequences, RGD in FIII10 and PHSRN in FIII9, that act synergistically in…”
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A comparison of the folding kinetics and thermodynamics of two homologous fibronectin type III modules
Published in Journal of molecular biology (01-08-1997)“…The homologous ninth and tenth type III modules of human fibronectin share identical topologies and nearly identical core structures. Despite these structural…”
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6
The structure of ribonuclease P protein from Staphylococcus aureus reveals a unique binding site for single-stranded RNA
Published in Journal of molecular biology (07-01-2000)“…Ribonuclease P (RNaseP) catalyses the removal of the 5′-leader sequence from pre-tRNA to produce the mature 5′ terminus. The prokaryotic RNaseP holoenzyme…”
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7
Module-module interactions in the cell binding region of fibronectin: stability, flexibility and specificity
Published in Journal of molecular biology (07-02-1997)“…The structure of mosaic proteins depends on the nature and strength of interactions between individual modules. Here we investigated the structural…”
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8
Destabilization of the complete protein secondary structure on binding to the chaperone GroEL
Published in Nature (London) (17-03-1994)“…Protein folding in vivo is mediated by helper proteins, the molecular chaperones, of which Hsp60 and its Escherichia coli variant GroEL are some of the best…”
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9
Structure of human cyclophilin and its binding site for cyclosporin A determined by X-ray crystallography and NMR spectroscopy
Published in Nature (London) (19-09-1991)“…The protein cyclophilin is the major intracellular receptor for the immunosuppressive drug cyclosporin A. Cyclosporin A acts as an inhibitor of T-cell…”
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Mycobacterium tuberculosis DNA gyrase ATPase domain structures suggest a dissociative mechanism that explains how ATP hydrolysis is coupled to domain motion
Published in Biochemical journal (01-12-2013)“…DNA gyrase, a type II topoisomerase, regulates DNA topology by creating a double-stranded break in one DNA duplex and transporting another DNA duplex [T-DNA…”
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11
Cyclosporin A—cyclophilin complex formation A model based on X-ray and NMR data
Published in FEBS letters (06-04-1992)“…The previously determined 3D NMR solution structure of cyclophilin-bound cyclosporin A (CsA) was docked onto the X-ray crystal structure of cyclophilin…”
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Structurally Diverse Mitochondrial Branched Chain Aminotransferase (BCATm) Leads with Varying Binding Modes Identified by Fragment Screening
Published in Journal of medicinal chemistry (24-03-2016)“…Inhibitors of mitochondrial branched chain aminotransferase (BCATm), identified using fragment screening, are described. This was carried out using a…”
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The Discovery of in Vivo Active Mitochondrial Branched-Chain Aminotransferase (BCATm) Inhibitors by Hybridizing Fragment and HTS Hits
Published in Journal of medicinal chemistry (24-09-2015)“…The hybridization of hits, identified by complementary fragment and high throughput screens, enabled the discovery of the first series of potent inhibitors of…”
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Novel hydroxyl tricyclics (e.g., GSK966587) as potent inhibitors of bacterial type IIA topoisomerases
Published in Bioorganic & medicinal chemistry letters (01-10-2013)“…During the course of our research to find novel mode of action antibacterials, we discovered a series of hydroxyl tricyclic compounds that showed good potency…”
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15
Inhibitors of the DNA-cleavage gate of bacterial type IIA topoisomerases
Published in Acta crystallographica. Section A, Foundations and advances (05-08-2014)“…Abstract only Type IIA topoisomerases resolve topological problems in DNA by making a double-stranded break in one DNA segment, passing another DNA duplex…”
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Crystallization and initial crystallographic analysis of covalent DNA-cleavage complexes of Staphyloccocus aureus DNA gyrase with QPT-1, moxifloxacin and etoposide
Published in Acta crystallographica. Section F, Structural biology communications (01-10-2015)“…Fluoroquinolone drugs such as moxifloxacin kill bacteria by stabilizing the normally transient double‐stranded DNA breaks created by bacterial type IIA…”
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Inhibition of fibril formation in beta-amyloid peptide by a novel series of benzofurans
Published in Biochemical journal (15-05-1999)“…A series of benzofuran derivatives have been identified as inhibitors of fibril formation in the beta-amyloid peptide. The activity of these compounds has been…”
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18
Building proteins with fibronectin type III modules
Published in Structure (London) (15-05-1994)“…Fibronectin type III modules are versatile components of many proteins. Recent structures of module pairs show how these modules are joined together…”
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Rapid Refolding of a Proline-Rich all-$\beta $-sheet Fibronectin Type III Module
Published in Proceedings of the National Academy of Sciences - PNAS (01-10-1996)“…Fibronectin type III modules contain approximately 90 residues and are an extremely common building block of animal proteins. Despite containing a complex…”
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Structural studies on bacterial type IIA topoisomerases - targets for quinolone and coumarin antibiotics
Published in Acta crystallographica. Section A, Foundations of crystallography (16-08-2009)“…Abstract only…”
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