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   Articles with "crbn" as a keyword



Discovery of potential novel CRBN modulators by virtual screening and bioassay.

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recommendations! Published in 2022 at "European journal of medicinal chemistry"

DOI: 10.1016/j.ejmech.2022.114355

Abstract: The incidence of malignant tumor with high mortality is increasing yearly. CRBN E3 ubiquitin ligase was proved to be an antitumor target. It was found that thalidomide and its analogs could bind to CRBN E3… read more here.

Keywords: modulators virtual; crbn; virtual screening; crbn modulators ... See more keywords

Novel CRBN-Recruiting Proteolysis-Targeting Chimeras as Degraders of Stimulator of Interferon Genes with In Vivo Anti-Inflammatory Efficacy.

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recommendations! Published in 2022 at "Journal of medicinal chemistry"

DOI: 10.1021/acs.jmedchem.1c01948

Abstract: The activation of the cyclic GMP-AMP synthase-stimulator of interferon gene (STING) pathway has been associated with the pathogenesis of many autoimmune and inflammatory disorders, and small molecules targeting STING have emerged as a new therapeutic… read more here.

Keywords: crbn; stimulator interferon; anti inflammatory; proteolysis targeting ... See more keywords

De-Novo Design of Cereblon (CRBN) Effectors Guided by Natural Hydrolysis Products of Thalidomide Derivatives

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recommendations! Published in 2019 at "Journal of Medicinal Chemistry"

DOI: 10.1021/acs.jmedchem.9b00454

Abstract: Targeted protein degradation via cereblon (CRBN), a substrate receptor of an E3 ubiquitin ligase complex, is an increasingly important strategy in various clinical settings, in which the substrate specificity of CRBN is altered via the… read more here.

Keywords: crbn effectors; crbn; cereblon crbn; substrate ... See more keywords

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

Identification of MORF4L1 as an endogenous substrate of CRBN and its potential role as a therapeutic target in cancer

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recommendations! Published in 2025 at "Scientific Reports"

DOI: 10.1038/s41598-024-82941-3

Abstract: The ubiquitin-proteasome system (UPS) is essential for cellular homeostasis, regulating the degradation of proteins involved in key processes such as cell cycle, apoptosis, and DNA repair. Dysregulation of the UPS is implicated in hepatocellular carcinoma… read more here.

Keywords: cancer; role; substrate crbn; identification morf4l1 ... See more keywords

PLZF and its fusion proteins are pomalidomide-dependent CRBN neosubstrates

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recommendations! Published in 2021 at "Communications Biology"

DOI: 10.1038/s42003-021-02801-y

Abstract: Pomalidomide and lenalidomide are immunomodulatory agents that were derived from thalidomide. Cereblon (CRBN) is a common direct target of thalidomide and related compounds and works as a Cullin Ring 4 E3 ubiquitin ligase (CRL4) with… read more here.

Keywords: crbn; fusion proteins; proteins pomalidomide; pomalidomide dependent ... See more keywords

Discovery of CRBN as a target of thalidomide: a breakthrough for progress in the development of protein degraders.

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recommendations! Published in 2022 at "Chemical Society reviews"

DOI: 10.1039/d2cs00116k

Abstract: Progress in strategies aimed at breaking down therapeutic target proteins has led to a paradigm shift in drug discovery. Thalidomide and its derivatives are the only protein degraders currently used in clinical practice. Our understanding… read more here.

Keywords: thalidomide derivatives; crbn; progress; protein degraders ... 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

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

Mining the CRBN target space redefines rules for molecular glue-induced neosubstrate recognition.

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recommendations! Published in 2025 at "Science"

DOI: 10.1126/science.adt6736

Abstract: The CRL4CRBN E3 ubiquitin ligase is the target of molecular glue degrader compounds that reprogram ligase specificity to induce the degradation of clinically relevant neosubstrate proteins. Known cereblon (CRBN) neosubstrates share a generalizable β-hairpin G-loop… read more here.

Keywords: crbn target; molecular glue; crbn; target ... See more keywords

A Novel Functional Role for Cereblon in Cardiac Cell-Cell Junction Protein Homeostasis, Function and Arrhythmias

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recommendations! Published in 2023 at "Physiology"

DOI: 10.1152/physiol.2023.38.s1.5734511

Abstract: Desmosomes are cell-cell adhesion junctions that function as mechanical anchors between cardiomyocytes. Loss of desmosomal protein levels and integrity due to desmosomal gene mutations are classically linked to arrhythmogenic cardiomyopathy (AC), an inherited cardiac disease… read more here.

Keywords: cell; protein homeostasis; physiology; cell cell ... See more keywords