Search Results - "Donovan, Katherine"
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Doing social volcanology: exploring volcanic culture in Indonesia
Published in Area (London 1969) (01-03-2010)“…Social volcanology refers to the integration of social science research methods into the traditionally physical domain of volcanology. This emerging…”
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2
Optimized libraries for CRISPR-Cas9 genetic screens with multiple modalities
Published in Nature communications (21-12-2018)“…The creation of genome-wide libraries for CRISPR knockout (CRISPRko), interference (CRISPRi), and activation (CRISPRa) has enabled the systematic interrogation…”
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3
Plasticity in binding confers selectivity in ligand-induced protein degradation
Published in Nature chemical biology (01-07-2018)“…Heterobifunctional small-molecule degraders that induce protein degradation through ligase-mediated ubiquitination have shown considerable promise as a new…”
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4
Development of Dual and Selective Degraders of Cyclin‐Dependent Kinases 4 and 6
Published in Angewandte Chemie International Edition (06-05-2019)“…Cyclin‐dependent kinases 4 and 6 (CDK4/6) are key regulators of the cell cycle, and there are FDA‐approved CDK4/6 inhibitors for treating patients with…”
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Optimized sgRNA design to maximize activity and minimize off-target effects of CRISPR-Cas9
Published in Nature biotechnology (01-02-2016)“…Genome-wide sgRNA libraries based on rules for on-target activity improve results of Cas9-based screens and facilitate a further refinement of on- and…”
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6
Structural complementarity facilitates E7820-mediated degradation of RBM39 by DCAF15
Published in Nature chemical biology (01-01-2020)“…The investigational drugs E7820, indisulam and tasisulam (aryl-sulfonamides) promote the degradation of the splicing factor RBM39 in a proteasome-dependent…”
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Homolog-Selective Degradation as a Strategy to Probe the Function of CDK6 in AML
Published in Cell chemical biology (21-02-2019)“…The design of selective small molecules is often stymied by similar ligand binding pockets. Here, we report BSJ-03-123, a phthalimide-based degrader that…”
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Small molecule degraders of the hepatitis C virus protease reduce susceptibility to resistance mutations
Published in Nature communications (01-08-2019)“…Targeted protein degradation is a promising drug development paradigm. Here we leverage this strategy to develop a new class of small molecule antivirals that…”
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Thalidomide promotes degradation of SALL4, a transcription factor implicated in Duane Radial Ray syndrome
Published in eLife (01-08-2018)“…In historical attempts to treat morning sickness, use of the drug thalidomide led to the birth of thousands of children with severe birth defects. Despite…”
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Bruton tyrosine kinase degradation as a therapeutic strategy for cancer
Published in Blood (28-02-2019)“…The covalent Bruton tyrosine kinase (BTK) inhibitor ibrutinib is highly efficacious against multiple B-cell malignancies. However, it is not selective for BTK,…”
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11
Chemo-proteomics exploration of HDAC degradability by small molecule degraders
Published in Cell chemical biology (21-10-2021)“…Targeted protein degradation refers to the use of small molecules that recruit a ubiquitin ligase to a target protein for ubiquitination and subsequent…”
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12
Discovery of an AKT Degrader with Prolonged Inhibition of Downstream Signaling
Published in Cell chemical biology (16-01-2020)“…The PI3K/AKT signaling cascade is one of the most commonly dysregulated pathways in cancer, with over half of tumors exhibiting aberrant AKT activation…”
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The CDK inhibitor CR8 acts as a molecular glue degrader that depletes cyclin K
Published in Nature (London) (10-09-2020)“…Molecular glue compounds induce protein–protein interactions that, in the context of a ubiquitin ligase, lead to protein degradation 1 . Unlike traditional…”
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14
Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK)
Published in Journal of medicinal chemistry (10-05-2018)“…We present the development of the first small molecule degraders that can induce anaplastic lymphoma kinase (ALK) degradation, including in non-small-cell lung…”
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15
Orthologous CRISPR–Cas9 enzymes for combinatorial genetic screens
Published in Nature biotechnology (01-02-2018)“…Combinatorial CRISPR screens are improved by using Cas9 enzymes from two different organisms. Combinatorial genetic screening using CRISPR–Cas9 is a useful…”
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pSILAC mass spectrometry reveals ZFP91 as IMiD-dependent substrate of the CRL4 CRBN ubiquitin ligase
Published in Nature communications (22-05-2017)“…Thalidomide and its derivatives lenalidomide and pomalidomide (IMiDs) are effective treatments of haematologic malignancies. It was shown that IMiDs impart…”
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Mapping the Degradable Kinome Provides a Resource for Expedited Degrader Development
Published in Cell (10-12-2020)“…Targeted protein degradation (TPD) refers to the use of small molecules to induce ubiquitin-dependent degradation of proteins. TPD is of interest in drug…”
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Small-molecule-induced polymerization triggers degradation of BCL6
Published in Nature (London) (03-12-2020)“…Effective and sustained inhibition of non-enzymatic oncogenic driver proteins is a major pharmacological challenge. The clinical success of thalidomide…”
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Targeted degradation of aberrant tau in frontotemporal dementia patient-derived neuronal cell models
Published in eLife (25-03-2019)“…Tauopathies are neurodegenerative diseases characterized by aberrant forms of tau protein accumulation leading to neuronal death in focal brain areas. Positron…”
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Discovery of a Potent Degrader for Fibroblast Growth Factor Receptor 1/2
Published in Angewandte Chemie International Edition (12-07-2021)“…Aberrant activation of FGFR signaling occurs in many cancers, and ATP‐competitive FGFR inhibitors have received regulatory approval. Despite demonstrating…”
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