Suchergebnisse - "Metivier, Rebecca J"
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Cryo-EM structures of CRAF/MEK1/14-3-3 complexes in autoinhibited and open-monomer states reveal features of RAF regulation
ISSN: 2041-1723, 2041-1723Veröffentlicht: London Nature Publishing Group UK 01.09.2025Veröffentlicht in Nature communications (01.09.2025)“… CRAF (RAF1) is one of three RAF-family kinases that initiate MAP kinase signaling in response to activated RAS and is essential for oncogenic signaling from …”
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Catalytic Degraders Effectively Address Kinase Site Mutations in EML4-ALK Oncogenic Fusions
ISSN: 1520-4804, 1520-4804Veröffentlicht: United States 27.04.2023Veröffentlicht in Journal of medicinal chemistry (27.04.2023)“… Heterobifunctional degraders, known as proteolysis targeting chimeras (PROTACs), theoretically possess a catalytic mode-of-action, yet few studies have either …”
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Unveiling the hidden interactome of CRBN molecular glues
ISSN: 2041-1723, 2041-1723Veröffentlicht: London Nature Publishing Group UK 24.07.2025Veröffentlicht in Nature communications (24.07.2025)“… Induced proximity by molecular glues refers to strategies that leverage the recruitment of proteins to facilitate their modification, regulation or …”
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Discovery of CRBN-Dependent WEE1 Molecular Glue Degraders from a Multicomponent Combinatorial Library
ISSN: 0002-7863, 1520-5126, 1520-5126Veröffentlicht: WASHINGTON Amer Chemical Soc 20.11.2024Veröffentlicht in Journal of the American Chemical Society (20.11.2024)“… Small molecules promoting protein-protein interactions produce a range of therapeutic outcomes. Molecular glue degraders exemplify this concept due to their …”
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Template-assisted covalent modification underlies activity of covalent molecular glues
ISSN: 1552-4450, 1552-4469, 1552-4469Veröffentlicht: New York Nature Publishing Group US 01.12.2024Veröffentlicht in Nature chemical biology (01.12.2024)“… Molecular glues are proximity-inducing small molecules that have emerged as an attractive therapeutic approach. However, developing molecular glues remains …”
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HiBiT-SpyTag: A Minimal Tag for Covalent Protein Capture and Degrader Development
ISSN: 1554-8937, 1554-8937Veröffentlicht: United States 21.04.2023Veröffentlicht in ACS chemical biology (21.04.2023)“… The ability to rapidly and selectively modulate cellular protein levels using small molecules is essential for studying complex biological systems. Degradation …”
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Covalent Stapling of the Cereblon Sensor Loop Histidine Using Sulfur-Heterocycle Exchange
ISSN: 1948-5875, 1948-5875Veröffentlicht: WASHINGTON Amer Chemical Soc 09.11.2023Veröffentlicht in ACS medicinal chemistry letters (09.11.2023)“… Site-specific modification of amino acid residues in protein binding pockets using sulfonyl exchange chemistry expands the druggable proteome by enabling the …”
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Cereblon covalent modulation through structure-based design of histidine targeting chemical probes
ISSN: 2633-0679, 2633-0679Veröffentlicht: RSC 31.08.2022Veröffentlicht in RSC chemical biology (31.08.2022)“… Electrophilic biocompatible warheads, particularly cysteine-reactive acrylamides, have enabled the development of covalent inhibitor drugs and chemical biology …”
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Development of a covalent cereblon-based PROTAC employing a fluorosulfate warhead
ISSN: 2633-0679, 2633-0679Veröffentlicht: England RSC 01.11.2023Veröffentlicht in RSC chemical biology (01.11.2023)“… Many cereblon (CRBN) ligands have been used to develop proteolysis targeting chimeras (PROTACs), but all are reversible binders of the E3 ubiquitin ligase. We …”
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Structure-guided design of a truncated heterobivalent chemical probe degrader of IRE1α
ISSN: 2632-8682, 2632-8682Veröffentlicht: CAMBRIDGE Royal Soc Chemistry 18.03.2025Veröffentlicht in RSC medicinal chemistry (18.03.2025)“… IRE1α is an ER protein involved in the unfolded protein response (UPR) and dysregulation of the ER stress pathway has been implicated in several diseases …”
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Development of sulfonyl fluoride chemical probes to advance the discovery of cereblon modulators
ISSN: 2632-8682, 2632-8682Veröffentlicht: CAMBRIDGE Royal Soc Chemistry 21.02.2024Veröffentlicht in RSC medicinal chemistry (21.02.2024)“… Sulfonyl fluoride EM12-SF was developed previously to covalently engage a histidine residue in the sensor loop of cereblon (CRBN) in the E3 ubiquitin ligase …”
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Characterization of Serine Hydrolases Across Clinical Isolates of Commensal Skin Bacteria Staphylococcus epidermidis Using Activity-Based Protein Profiling
ISSN: 2373-8227, 2373-8227Veröffentlicht: United States 08.05.2020Veröffentlicht in ACS infectious diseases (08.05.2020)“… The bacterial genus comprises diverse species that colonize the skin as commensals but can also cause infection. Previous work identified a family of serine …”
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Discovery of CRBN-dependent WEE1 Molecular Glue Degraders from a Multicomponent Combinatorial Library
ISSN: 2692-8205, 2692-8205Veröffentlicht: United States Cold Spring Harbor Laboratory 05.05.2024Veröffentlicht in bioRxiv (05.05.2024)“… Small molecules promoting protein-protein interactions produce a range of therapeutic outcomes. Molecular glue degraders exemplify this concept due to their …”
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Unveiling the hidden interactome of CRBN molecular glues with chemoproteomics
ISSN: 2692-8205, 2692-8205Veröffentlicht: United States Cold Spring Harbor Laboratory 04.10.2024Veröffentlicht in bioRxiv (04.10.2024)“… Targeted protein degradation and induced proximity refer to strategies that leverage the recruitment of proteins to facilitate their modification, regulation …”
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Chemical Proteomics of Reactive Cysteine Residues in Two Disease Models
ISBN: 1392544041, 9781392544044Veröffentlicht: ProQuest Dissertations & Theses 01.01.2019“… Cysteine residues perform many essential cellular functions, including nucleophilic and redox catalysis, metal coordination, structural stabilization and …”
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Dissertation

