Search Results - "Schwarz, Daniel M. C."
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Temperature-jump solution X-ray scattering reveals distinct motions in a dynamic enzyme
Published in Nature chemistry (01-11-2019)“…Correlated motions of proteins are critical to function, but these features are difficult to resolve using traditional structure determination techniques…”
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Hsp70 and Hsp40 inhibit an inter-domain interaction necessary for transcriptional activity in the androgen receptor
Published in Nature communications (08-08-2019)“…Molecular chaperones such as Hsp40 and Hsp70 hold the androgen receptor (AR) in an inactive conformation. They are released in the presence of androgens,…”
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Revisiting the “Art of the Chemical Probe”
Published in ACS chemical biology (18-05-2018)Get full text
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A Phosphoramidate Strategy Enables Membrane Permeability of a Non-nucleotide Inhibitor of the Prolyl Isomerase Pin1
Published in ACS medicinal chemistry letters (10-09-2020)“…The membrane permeability of nucleotide-based drugs, such as sofosbuvir (Sovaldi), requires installation of phosphate-caging groups. One strategy, termed…”
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Design, Synthesis, and Evaluation of Nonretinoid Retinol Binding Protein 4 Antagonists for the Potential Treatment of Atrophic Age-Related Macular Degeneration and Stargardt Disease
Published in Journal of medicinal chemistry (25-09-2014)“…Accumulation of lipofuscin in the retina is associated with pathogenesis of atrophic age-related macular degeneration and Stargardt disease. Lipofuscin…”
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Bicyclic [3.3.0]-Octahydrocyclopenta[c]pyrrolo Antagonists of Retinol Binding Protein 4: Potential Treatment of Atrophic Age-Related Macular Degeneration and Stargardt Disease
Published in Journal of medicinal chemistry (13-08-2015)“…Antagonists of retinol-binding protein 4 (RBP4) impede ocular uptake of serum all-trans retinol (1) and have been shown to reduce cytotoxic bisretinoid…”
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Robust Sequence Determinants of α‑Synuclein Toxicity in Yeast Implicate Membrane Binding
Published in ACS chemical biology (21-08-2020)“…Protein conformations are shaped by cellular environments, but how environmental changes alter the conformational landscapes of specific proteins in vivo…”
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Author Correction: Hsp70 and Hsp40 inhibit an inter-domain interaction necessary for transcriptional activity in the androgen receptor
Published in Nature communications (07-10-2019)“…An amendment to this paper has been published and can be accessed via a link at the top of the paper…”
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Inhibitors of heat shock protein 70 (Hsp70) with enhanced metabolic stability reduce tau levels
Published in Bioorganic & medicinal chemistry letters (01-06-2021)“…[Display omitted] •Two series of YM-08 analogs were designed to remove metabolic liabilities.•Optimization resulted in JG-23, which is 12-fold more…”
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