Results 71 to 80 of about 5,502 (160)

CRBN Is a Negative Regulator of Bactericidal Activity and Autophagy Activation Through Inhibiting the Ubiquitination of ECSIT and BECN1

open access: yesFrontiers in Immunology, 2019
Cereblon (CRBN) as a multifunctional protein has been extensively studied. Here, we show that CRBN is a negative regulator of bactericidal activity and autophagy activation.
Mi-Jeong Kim   +6 more
doaj   +1 more source

Crbn modulates calcium influx by regulating Orai1 during efferocytosis

open access: yesNature Communications, 2020
Calcium flux must be carefully controlled during the phagocytosis of apoptotic cells (efferocytosis), although how this occurs is not fully understood. Here, the authors show that the Cereblon E3 ligase regulates Orai1 degradation and subsequently SOCE ...
Hyunji Moon   +14 more
doaj   +1 more source

Pediatric Developmental Safety Assessment: Are We Ready for the Next Thalidomide?

open access: yesClinical Pharmacology &Therapeutics, EarlyView.
Pediatric drug development has achieved remarkable success in the last 20 years with over 1,000 products studied in pediatric patients. This success has been driven in part by an increased understanding of pediatric disease processes. The aspect that has been largely overlooked is the potential adverse effect of new drugs on pediatric developmental ...
Gilbert J. Burckart   +6 more
wiley   +1 more source

Mechanism and therapeutic implications of pomalidomide-induced immune surface marker upregulation in EBV-positive lymphomas

open access: yesScientific Reports, 2023
Epstein-Barr virus (EBV) downregulates immune surface markers to avoid immune recognition. Pomalidomide (Pom) was previously shown to increase immune surface marker expression in EBV-infected tumor cells.
Hannah K. Jaeger   +6 more
doaj   +1 more source

Molecular Glue Degraders in Early Development for Cancer Therapy

open access: yesMedicinal Research Reviews, EarlyView.
ABSTRACT Molecular glue degraders are an emerging class of small molecule allosteric modulators that induce or stabilize protein‐protein interactions, enabling targeted degradation of previously intractable proteins. By redirecting E3 ligases to recognize neosubstrates, proteins that are not typically recognized by a specific E3 ubiquitin ligase, they ...
E. Sila Ozdemir   +4 more
wiley   +1 more source

A FRET-Based Assay for the Identification and Characterization of Cereblon Ligands

open access: yes, 2016
Cereblon serves as an ubiquitin ligase substrate receptor that can be tuned toward different target proteins by various cereblon-binding agents. This offers one of the most promising avenues for targeted protein degradation in cancer therapy, but ...
Bär, K.   +4 more
core   +1 more source

Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4 [PDF]

open access: yes, 2015
SummaryBRD4, a bromodomain and extraterminal domain (BET) family member, is an attractive target in multiple pathological settings, particularly cancer.
Altieri, Martha   +10 more
core   +1 more source

The Drug Vehicle and Solvent N-Methylpyrrolidone Is an Immunomodulator and Antimyeloma Compound

open access: yesCell Reports, 2014
N-methyl-2-pyrrolidone (NMP) is a common solvent and drug vehicle. We discovered unexpected antineoplastic and immunomodulatory activity of NMP in a cMYC-driven myeloma model.
Jake Shortt   +20 more
doaj   +1 more source

Arginine methylation as a regulatory ratchet in cancer: From substrate selection to malignant‐state stabilization

open access: yesMolecular Oncology, Volume 20, Issue 10, Page 2466-2489, October 2026.
Arginine methylation can be viewed as a persistence‐prone post‐translational modification regulated by a network of PRMTs. Competitive and compensatory interactions among PRMTs can redistribute methylation across substrate pools shaped by sequence, structural, spatial, and environmental layers, reinforcing RNA‐processing, chromatin, and signaling ...
So Hyun Kwon, Ji Min Lee
wiley   +1 more source

Molecular Glue Degraders Redefining Targeted Therapies From Discovery to Therapeutic Applications

open access: yesMedComm – Oncology
Molecular glue degraders (MGDs) represent an emerging therapy that exploits ubiquitin–proteasome pathways to eliminate otherwise intractable proteins. By stabilizing E3 ligases–target protein interactions, they enable event‐driven degradation, advancing ...
Jinfeng Wen   +3 more
doaj   +1 more source

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