Search Results - "Dellsén, Anita"
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Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor‑1 Agonists
Published in Journal of medicinal chemistry (13-10-2022)“…In this work, cysteine staples were used as a late-stage functionalization strategy to diversify peptides and build conjugates targeting the melanocortin…”
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Macrocyclic Modalities Combining Peptide Epitopes and Natural Product Fragments
Published in Journal of the American Chemical Society (11-03-2020)“…“Hot loop” protein segments have variable structure and conformation and contribute crucially to protein–protein interactions. We describe a new hot loop…”
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Discovery and Early Clinical Development of an Inhibitor of 5‑Lipoxygenase Activating Protein (AZD5718) for Treatment of Coronary Artery Disease
Published in Journal of medicinal chemistry (09-05-2019)“…5-Lipoxygenase activating protein (FLAP) inhibitors attenuate 5-lipoxygenase pathway activity and reduce the production of proinflammatory and vasoactive…”
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Melanocortin 1 Receptor Agonists Based on a Bivalent, Bicyclic Peptide Framework
Published in Journal of medicinal chemistry (22-07-2021)“…We have designed a new class of highly potent bivalent melanocortin receptor ligands based on the nature-derived bicyclic peptide sunflower trypsin inhibitor 1…”
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Development of Novel Melanocortin Receptor Agonists Based on the Cyclic Peptide Framework of Sunflower Trypsin Inhibitor‑1
Published in Journal of medicinal chemistry (26-04-2018)“…Ultrastable cyclic peptide frameworks offer great potential for drug design due to their improved bioavailability compared to their linear analogues. Using the…”
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Discovery of retinoic acid receptor agonists as proliferators of cardiac progenitor cells through a phenotypic screening approach
Published in Stem cells translational medicine (01-01-2020)“…Identification of small molecules with the potential to selectively proliferate cardiac progenitor cells (CPCs) will aid our understanding of the signaling…”
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Discovery of novel class 1 phosphatidylinositide 3-kinases (PI3K) fragment inhibitors through structure-based virtual screening
Published in Bioorganic & medicinal chemistry letters (15-01-2011)“…The identification of novel class 1 phosphatidylinositide 3-kinases (PI3K) inhibitors by fragment-based virtual screening is described. The discovery of ligand…”
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Structure‐Based Drug Design of Mineralocorticoid Receptor Antagonists to Explore Oxosteroid Receptor Selectivity
Published in ChemMedChem (05-01-2017)“…The mineralocorticoid receptor (MR) is a nuclear hormone receptor involved in the regulation of body fluid and electrolyte homeostasis. In this study we…”
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RAR-related orphan receptor A isoform 1 (RORa1) is disrupted by a balanced translocation t(4;15)(q22.3;q21.3) associated with severe obesity
Published in European journal of human genetics : EJHG (01-08-2005)“…We have identified a family comprising a mother and two children with idiopathic and profound obesity body mass index (BMI) 41-49 kg/m(2). The three family…”
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Exploring Binding Mechanisms in Nuclear Hormone Receptors by Monte Carlo and X-ray-derived Motions
Published in Biophysical journal (28-03-2017)“…In this study, we performed an extensive exploration of the ligand entry mechanism for members of the steroid nuclear hormone receptor family (androgen…”
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Human 4-hydroxyphenylpyruvate dioxygenase : primary structure and chromosomal localization of the gene
Published in European journal of biochemistry (01-05-1993)“…We report the primary structure of 4-hydroxyphenylpyruvate dioxygenase [4-hydroxyphenyl-pyruvate:oxygen oxidoreductase (hydroxylating, decarboxylating)]. The…”
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Human 4‐hydroxyphenylpyruvate dioxygenase
Published in European journal of biochemistry (01-05-1993)“…We report the primary structure of 4‐hydroxyphenylpyruvate dioxygenase [4‐hydroxyphenylpyruvate: oxygen oxidoreductase (hydroxylating, decarboxylating)]. The…”
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