Search Results - "Alexander, Leslie D"
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Synthesis of sansalvamide A peptidomimetics: triazole, oxazole, thiazole, and pseudoproline containing compounds
Published in Tetrahedron (28-01-2012)“…Peptidomimetic-based macrocycles typically have improved pharmacokinetic properties over those observed with peptide analogs. Described are the syntheses of 13…”
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Macrocyclic inhibitors of hsp90
Published in Current topics in medicinal chemistry (01-10-2010)“…Heat shock proteins (HSP) are a family of highly conserved proteins, whose expression increases in response to stresses that may threaten cell survival. Over…”
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3
Towards a predictive framework for biocrust mediation of plant performance: A meta‐analysis
Published in The Journal of ecology (01-11-2019)“…Understanding the importance of biotic interactions in driving the distribution and abundance of species is a central goal of plant ecology. Early vascular…”
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Biocrusts are associated with increased plant biomass and nutrition at seedling stage independently of root-associated fungal colonization
Published in Plant and soil (2020)“…Aims Plant-soil interactions are important drivers of plant productivity and community structure. Biocrusts – soil surface-dwelling biotic communities…”
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Macrocycles That Inhibit the Binding between Heat Shock Protein 90 and TPR-Containing Proteins
Published in ACS chemical biology (16-12-2011)“…Heat shock protein 90 (Hsp90) accounts for 1–2% of the total proteins in normal cells and functions as a molecular chaperone that folds, assembles, and…”
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Design and synthesis of Hsp90 inhibitors: Exploring the SAR of Sansalvamide A derivatives
Published in Bioorganic & medicinal chemistry (15-09-2010)“…Utilizing the structure–activity relationship we have developed during the synthesis of the first two generations and mechanism of action studies that point to…”
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Synthesis and evaluation of biotinylated sansalvamide A analogs and their modulation of Hsp90
Published in Bioorganic & medicinal chemistry letters (15-08-2011)“…Described are the syntheses of three sansalvamide A derivatives that contain biotinylated tags at individual positions around the macrocycle. The tagged…”
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A small molecule that preferentially binds the closed conformation of Hsp90
Published in Bioorganic & medicinal chemistry letters (01-12-2011)“…Described is the synthesis of three different fluorescein-tagged derivatives of a macrocycle, and their binding affinity to heat shock protein 90 (Hsp90)…”
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An Hsp90 modulator that exhibits a unique mechanistic profile
Published in Bioorganic & medicinal chemistry letters (01-05-2012)“…Described is the synthesis of two biotinylated derivatives of a cytotoxic macrocycle. Pull-down assays indicate that this macrocycle targets the N-middle…”
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10
Histone deacetylase inhibitors: synthesis of cyclic tetrapeptides and their triazole analogs
Published in Tetrahedron letters (18-08-2010)“…Synthesis of nine macrocyclic peptide HDAC inhibitors and three triazole derivatives is described. HDAC inhibitory activity of these compounds against HeLa…”
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11
Evaluation of Di-Sansalvamide A Derivatives: Synthesis, Structure−Activity Relationship, and Mechanism of Action
Published in Journal of medicinal chemistry (24-12-2009)“…Described is the SAR of 18 di-sansalvamide A derivatives and the mechanism of action of the most potent compound. We show that this scaffold is a promising…”
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Conformationally based design of macrocycles as antitumor agents
Published in Current opinion in drug discovery & development (01-07-2008)“…A key feature for any chemotherapeutic agent is a favorable conformation when it is presenting itself to its intended target. Numerous macrocycles have been…”
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