Search Results - "Bondeson, Daniel P."
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Targeted Protein Degradation by Small Molecules
Published in Annual review of pharmacology and toxicology (06-01-2017)“…Protein homeostasis networks are highly regulated systems responsible for maintaining the health and productivity of cells. Whereas therapeutics have been…”
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Targeting BCR-ABL1 in Chronic Myeloid Leukemia by PROTAC-Mediated Targeted Protein Degradation
Published in Cancer research (Chicago, Ill.) (15-09-2019)“…Although the use of ATP-competitive tyrosine kinase inhibitors of oncoprotein BCR-ABL1 has enabled durable responses in patients with chronic myeloid leukemia…”
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Systematic profiling of conditional degron tag technologies for target validation studies
Published in Nature communications (20-09-2022)“…Conditional degron tags (CDTs) are a powerful tool for target validation that combines the kinetics and reversible action of pharmacological agents with the…”
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Lessons in PROTAC Design from Selective Degradation with a Promiscuous Warhead
Published in Cell chemical biology (18-01-2018)“…Inhibiting protein function selectively is a major goal of modern drug discovery. Here, we report a previously understudied benefit of small molecule…”
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Ion and solute transport by Prestin in Drosophila and Anopheles
Published in Journal of insect physiology (01-04-2012)“…[Display omitted] ► One Drosophila and two A. gambiae orthologues have high homology with mammalian Slc26a5 and Slc26a6. ► dPrestin and AgPrestin-B show…”
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Scaffold hopping enables direct access to more potent PROTACs with in vivo activity
Published in Chemical communications (Cambridge, England) (23-06-2020)“…Herein we employ a scaffold hopping approach to enhance the activity of a previously reported BCR-Abl PROTAC. This represents a significant advance in the…”
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Catalytic in vivo protein knockdown by small-molecule PROTACs
Published in Nature chemical biology (01-08-2015)“…The use of a high-affinity VHL ligand allows the development of chimeric molecules that promote the association of ERRα or RIPK2 with the VHL E3 ubiquitin…”
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An In Vitro Pull-down Assay of the E3 Ligase:PROTAC:Substrate Ternary Complex to Identify Effective PROTACs
Published in Methods in molecular biology (Clifton, N.J.) (2021)“…Assessing the specificity of PROTACs and confirming their proposed mechanism of action are critical for a robust targeted protein degradation program. Owing to…”
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The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study
Published in Cell chemical biology (18-01-2018)“…Proteolysis targeting chimera (PROTAC) technology has emerged over the last two decades as a powerful tool for targeted degradation of endogenous proteins…”
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In vivo Drosophilia genetic model for calcium oxalate nephrolithiasis
Published in American journal of physiology. Renal physiology (01-12-2012)“…Nephrolithiasis is a major public health problem with a complex and varied etiology. Most stones are composed of calcium oxalate (CaOx), with dietary excess a…”
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Phosphate dysregulation via the XPR1-KIDINS220 protein complex is a therapeutic vulnerability in ovarian cancer
Published in Nature cancer (18-04-2022)“…Despite advances in precision medicine, the clinical prospects for patients with ovarian and uterine cancers have not substantially improved. Here, we analyzed…”
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Real‐time visualization of calcium oxalate crystals in Drosophila ‐ a gut and renal model of kidney stones
Published in The FASEB journal (01-04-2012)“…Abstract only Background Kidney stones (nephrolithiasis) are an expensive and painful health problem with a complex etiology with ~70% of stones composed of…”
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