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   Articles with "cereblon" as a keyword



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Comparative analysis of dermal collagen and lipids in cereblon ablated mice using a multimodal nonlinear optical system

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recommendations! Published in 2022 at "Journal of Biophotonics"

DOI: 10.1002/jbio.202200139

Abstract: By utilizing a multimodal nonlinear optical system that combines coherent anti‐Stokes Raman scattering and second harmonic generation to investigate biological characteristics of dermal tissues ex vivo, we demonstrate the potential feasibility of using this optical… read more here.

Keywords: system; cereblon; nonlinear optical; collagen ... See more keywords
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Cereblon Modulators Target ZBTB16 and Its Oncogenic Fusion Partners for Degradation via Distinct Structural Degrons.

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recommendations! Published in 2020 at "ACS chemical biology"

DOI: 10.1021/acschembio.0c00674

Abstract: There is a growing interest in using targeted protein degradation as a therapeutic modality in view of its potential to expand the druggable proteome. One avenue to using this modality is via molecular glue based… read more here.

Keywords: degradation; cereblon; cereblon modulators; structural degrons ... See more keywords
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Cereblon gene variants and clinical outcome in multiple myeloma patients treated with lenalidomide

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recommendations! Published in 2019 at "Scientific Reports"

DOI: 10.1038/s41598-019-51446-9

Abstract: Carfilzomib-lenalidomide-dexamethasone (KRd) therapy has yielded promising results in patients with newly diagnosed multiple myeloma (NDMM). Cereblon (CRBN) is the direct molecular target of lenalidomide and genetic polymorphisms in CRBN have been associated with lenalidomide efficacy.… read more here.

Keywords: therapy; cereblon; multiple myeloma; crbn ... See more keywords
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3-Aminophthalic acid, a new cereblon ligand for targeted protein degradation by O'PROTAC.

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recommendations! Published in 2022 at "Chemical communications"

DOI: 10.1039/d1cc06525d

Abstract: In this study, we identified 3-aminophthalic acid as a new ligand of cereblon (CRBN) E3 ubiquitin ligase and developed a phthalic acid-based O'PROTAC for degradation of the ERG transcription factor. This phthalic acid-based O'PROTAC presented… read more here.

Keywords: cereblon; ligand; phthalic acid; degradation ... See more keywords

Cereblon contributes to cardiac dysfunction by degrading Cav1.2α.

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recommendations! Published in 2022 at "European heart journal"

DOI: 10.1093/eurheartj/ehac072

Abstract: AIMS Cereblon (CRBN) is a substrate receptor of the E3 ubiquitin ligase complex that was reported to target ion channel proteins. L-type voltage-dependent Ca2+ channel (LTCC) density and dysfunction is a critical player in heart… read more here.

Keywords: cereblon; cav1; hfref; cardiac dysfunction ... See more keywords
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Molecular glue CELMoD compounds are regulators of cereblon conformation

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recommendations! Published in 2022 at "Science"

DOI: 10.1126/science.add7574

Abstract: Cereblon (CRBN) is a ubiquitin ligase (E3) substrate receptor protein co-opted by CRBN E3 ligase modulatory drug (CELMoD) agents that target therapeutically relevant proteins for degradation. Prior crystallographic studies defined the drug-binding site within CRBN’s… read more here.

Keywords: cereblon; celmod compounds; conformation; drug ... See more keywords
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Interactome of Aiolos/Ikaros Reveals Combination Rationale of Cereblon Modulators with HDAC Inhibitors in DLBCL

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recommendations! Published in 2022 at "Clinical Cancer Research"

DOI: 10.1158/1078-0432.ccr-21-3347

Abstract: Abstract Purpose: Cereblon (CRBN), a substrate receptor of the E3 ubiquitin ligase complex CRL4CRBN, is the target of the small molecules lenalidomide and avadomide. Upon binding of the drugs, Aiolos and Ikaros are recruited to… read more here.

Keywords: cereblon; transcription; dlbcl; aiolos ikaros ... See more keywords
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UDP-Glucose: A Cereblon-Dependent Glucokinase Protein Degrader

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recommendations! Published in 2022 at "International Journal of Molecular Sciences"

DOI: 10.3390/ijms23169094

Abstract: We previously reported that glucokinase is ubiquitinated and degraded by cereblon with an unknown endogenous glucokinase protein degrader. Here, we show that UDP-glucose is a glucokinase protein degrader. We identified that both glucose and UDP-glucose… read more here.

Keywords: cereblon; protein degrader; udp glucose; glucokinase ... See more keywords
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Antiangiogenic Activity and in Silico Cereblon Binding Analysis of Novel Thalidomide Analogs

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recommendations! Published in 2020 at "Molecules"

DOI: 10.3390/molecules25235683

Abstract: Due to its antiangiogenic and anti-immunomodulatory activity, thalidomide continues to be of clinical interest despite its teratogenic actions, and efforts to synthesize safer, clinically active thalidomide analogs are continually underway. In this study, a cohort… read more here.

Keywords: antiangiogenic activity; cereblon binding; cereblon; thalidomide analogs ... See more keywords