Results 1 to 10 of about 4,268 (116)
Antiangiogenic Activity and in Silico Cereblon Binding Analysis of Novel Thalidomide Analogs
Molecules, 2020 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,
Christian Steinebach +2 more
exaly +3 more sources
Synthesis, biological evaluation and clinical trials of Cereblon-based PROTACs [PDF]
Communications ChemistryPROteolysis-Targeting Chimeras (PROTACs) are an emerging class of molecules capable of inducing a forced approximation between a protein of interest (POI) and an E3 ligase enzyme (e.g., Cereblon), leading to the degradation of the POI by the cell’s own ...
André T. S. Vicente +2 more
doaj +2 more sources
A unified platform for the rapid assembly of glutarimides for Cereblon E3 ligase modulatory drugs [PDF]
Nature CommunicationsGlutarimide-containing Cereblon (CRBN) ligands are critical motifs for PROTACs, molecular glue degraders and next-generation Cereblon E3 ligase modulatory drugs (CELMoDs), which represent promising therapeutic modalities in targeted protein degradation ...
David M. Whalley +12 more
doaj +2 more sources
The CB1 receptor interacts with cereblon and drives cereblon deficiency-associated memory shortfalls
EMBO Molecular MedicineCereblon/CRBN is a substrate-recognition component of the Cullin4A-DDB1-Roc1 E3 ubiquitin ligase complex. Destabilizing mutations in the human CRBN gene cause a form of autosomal recessive non-syndromic intellectual disability (ARNSID) that is modelled ...
Manuel Guzmán +2 more
exaly +2 more sources
Frontiers in Cell and Developmental Biology, 2021 Thalidomide, a sedative drug that was once excluded from the market owing to its teratogenic properties, was later found to be effective in treating multiple myeloma.
Tomomi Sato +4 more
doaj +1 more source
3,6′- and 1,6′-Dithiopomalidomide Mitigate Ischemic Stroke in Rats and Blunt Inflammation
Pharmaceutics, 2022 (1) Background: An important concomitant of stroke is neuroinflammation. Pomalidomide, a clinically available immunomodulatory imide drug (IMiD) used in cancer therapy, lowers TNF-α generation and thus has potent anti-inflammatory actions. Well-tolerated
Yan-Rou Tsai +18 more
doaj +1 more source
Scientific Reports, 2023 The design of cereblon-binding molecular glues (MGs) that selectively recruit a desired protein while excluding teratogenic SALL4 is an area of significant interest when designing therapeutic agents.
Xiaolei Ma +12 more
doaj +1 more source
UDP-glucose, cereblon-dependent proinsulin degrader
Scientific Reports, 2022 Insulin secretion is regulated in multiple steps, and one of the main steps is in the endoplasmic reticulum (ER). Here, we show that UDP-glucose induces proinsulin ubiquitination by cereblon, and uridine binds and competes for proinsulin degradation and ...
Jaeyong Cho +6 more
doaj +1 more source
Frontiers in Oncology, 2021 BackgroundCereblon (CRBN) is a direct target of immunomodulatory drugs (IMiDs) and is known to be sensitive and responsive to IMiD therapy. We evaluated CRBN expression in bone marrow plasma cells and analyzed whether CRBN expression was associated with ...
Byung-Hyun Lee +9 more
doaj +1 more source
Cells, 2023 Allergy is a chronic inflammatory disease, and its incidence has increased worldwide in recent years. Thalidomide, which was initially used as an anti-emetic drug but was withdrawn due to its teratogenic effects, is now used to treat blood cancers ...
Hyeun-Wook Chang +2 more
doaj +1 more source