Search Results - "Friemann, Rosmarie"
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Subangstrom Resolution X-Ray Structure Details Aquaporin-Water Interactions
Published in Science (American Association for the Advancement of Science) (14-06-2013)“…Aquaporins are membrane channels that facilitate the flow of water across biological membranes. Two conserved regions are central for selective function: the…”
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Transcription factor clusters regulate genes in eukaryotic cells
Published in eLife (25-08-2017)“…Transcription is regulated through binding factors to gene promoters to activate or repress expression, however, the mechanisms by which factors find targets…”
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Mechanism of NanR gene repression and allosteric induction of bacterial sialic acid metabolism
Published in Nature communications (31-03-2021)“…Bacteria respond to environmental changes by inducing transcription of some genes and repressing others. Sialic acids, which coat human cell surfaces, are a…”
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Inhibitor binding mode and allosteric regulation of Na+-glucose symporters
Published in Nature communications (07-12-2018)“…Sodium-dependent glucose transporters (SGLTs) exploit sodium gradients to transport sugars across the plasma membrane. Due to their role in renal sugar…”
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Potent and selective aldo-keto reductase 1C3 (AKR1C3) inhibitors based on the benzoisoxazole moiety: application of a bioisosteric scaffold hopping approach to flufenamic acid
Published in European journal of medicinal chemistry (25-04-2018)“…The aldo-keto reductase 1C3 (AKR1C3) isoform plays a vital role in the biosynthesis of androgens and is considered an attractive target in prostate cancer…”
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Substrate-bound outward-open structure of a Na+-coupled sialic acid symporter reveals a new Na+ site
Published in Nature communications (01-05-2018)“…Many pathogenic bacteria utilise sialic acids as an energy source or use them as an external coating to evade immune detection. As such, bacteria that colonise…”
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Structure and mechanism of a tripartite ATP-independent periplasmic TRAP transporter
Published in Nature communications (27-02-2023)“…In bacteria and archaea, tripartite ATP-independent periplasmic (TRAP) transporters uptake essential nutrients. TRAP transporters receive their substrates via…”
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Correction: Transcription factor clusters regulate genes in eukaryotic cells
Published in eLife (06-02-2019)Get full text
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Bioisosteres of Indomethacin as Inhibitors of Aldo-Keto Reductase 1C3
Published in ACS medicinal chemistry letters (11-04-2019)“…Aldo-keto reductase 1C3 (AKR1C3) is an attractive target in drug design for its role in resistance to anticancer therapy. Several nonsteroidal…”
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Structural snapshots along the reaction pathway of ferredoxin-thioredoxin reductase
Published in Nature (05-07-2007)“…Oxygen-evolving photosynthetic organisms regulate carbon metabolism through a light-dependent redox signalling pathway. Electrons are shuttled from photosystem…”
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Structural and biophysical analysis of a Haemophilus influenzae tripartite ATP-independent periplasmic (TRAP) transporter
Published in eLife (13-02-2024)“…Tripartite ATP-independent periplasmic (TRAP) transporters are secondary-active transporters that receive their substrates via a soluble-binding protein to…”
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Structures of the multicomponent Rieske non-heme iron toluene 2,3-dioxygenase enzyme system
Published in Acta crystallographica. Section D, Biological crystallography. (01-01-2009)“…Bacterial Rieske non‐heme iron oxygenases catalyze the initial hydroxylation of aromatic hydrocarbon substrates. The structures of all three components of one…”
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The Sodium Sialic Acid Symporter From Staphylococcus aureus Has Altered Substrate Specificity
Published in Frontiers in chemistry (2018)“…Mammalian cell surfaces are decorated with complex glycoconjugates that terminate with negatively charged sialic acids. Commensal and pathogenic bacteria can…”
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Crystal structure of the HIV-2 neutralizing Fab fragment 7C8 with high specificity to the V3 region of gp125
Published in PloS one (26-04-2011)“…7C8 is a mouse monoclonal antibody specific for the third hypervariable region (V3) of the human immunodeficiency virus type 2 (HIV-2)-associated protein…”
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Structure of the Fab fragment of the anti-murine EGFR antibody 7A7 and exploration of its receptor binding site
Published in Molecular immunology (01-07-2011)“…► The crystal structure of the 7A7 Fab was solved at high resolution (1.4 Å). ► 7A7 was raised against the murine EGFR, but cross-reacts with the human…”
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Targeting Myeloid Differentiation Using Potent 2‑Hydroxypyrazolo[1,5‑a]pyridine Scaffold-Based Human Dihydroorotate Dehydrogenase Inhibitors
Published in Journal of medicinal chemistry (26-07-2018)“…Human dihydroorotate dehydrogenase (hDHODH) catalyzes the rate-limiting step in de novo pyrimidine biosynthesis, the conversion of dihydroorotate to orotate…”
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On the function of TRAP substrate-binding proteins: Conformational variation of the sialic acid binding protein SiaP
Published in The Journal of biological chemistry (30-09-2024)“…Tripartite ATP-independent periplasmic (TRAP) transporters are analogous to ABC transporters in that they use a substrate-binding protein to scavenge…”
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Design, synthesis, biological evaluation and X-ray structural studies of potent human dihydroorotate dehydrogenase inhibitors based on hydroxylated azole scaffolds
Published in European journal of medicinal chemistry (31-03-2017)“…A new generation of potent hDHODH inhibitors designed by a scaffold-hopping replacement of the quinolinecarboxylate moiety of brequinar, one of the most potent…”
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Hydroxyazole scaffold-based Plasmodium falciparum dihydroorotate dehydrogenase inhibitors: Synthesis, biological evaluation and X-ray structural studies
Published in European journal of medicinal chemistry (01-02-2019)“…Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH) has been clinically validated as a target for antimalarial drug discovery, as a triazolopyrimidine…”
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Nimotuzumab, an Antitumor Antibody that Targets the Epidermal Growth Factor Receptor, Blocks Ligand Binding while Permitting the Active Receptor Conformation
Published in Cancer research (Chicago, Ill.) (15-07-2009)“…Overexpression of the epidermal growth factor (EGF) receptor (EGFR) in cancer cells correlates with tumor malignancy and poor prognosis for cancer patients…”
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