Results 11 to 20 of about 5,540 (198)
Chemical Ligand Space of Cereblon [PDF]
ACS Omega, 2018 The protein cereblon serves as a substrate receptor of a ubiquitin ligase complex that can be tuned toward different target proteins by cereblon-binding agents. This approach to targeted protein degradation is exploited in different clinical settings and
Iuliia Boichenko +7 more
doaj +8 more sources
, 2022 The disclosure provides compds. of formula I,and the salts and solvates thereof. The disclosure also relates to uses of the compds. as cereblon (CRBN) ubiquitination inhibitors, as synthetic intermediates that can be used to prep.
Wang, shaomeng, Rej, Rohan
core +3 more sources
Cereblon: A Protein Crucial to the Multiple Functions of Immunomodulatory Drugs as well as Cell Metabolism and Disease Generation [PDF]
Journal of Immunology Research, 2017 It is well known that cereblon is a key protein in autosomal recessive nonsyndromic mental retardation. Studies have reported that it has an intermediary role in helping immunomodulatory drugs perform their immunomodulatory and tumoricidal effects.
Qinglin Shi, Lijuan Chen
doaj +2 more sources
UBE2G1 governs the destruction of cereblon neomorphic substrates
eLife, 2018 The cereblon modulating agents (CMs) including lenalidomide, pomalidomide and CC-220 repurpose the Cul4-RBX1-DDB1-CRBN (CRL4CRBN) E3 ubiquitin ligase complex to induce the degradation of specific neomorphic substrates via polyubiquitination in ...
Gang Lu +17 more
doaj +3 more sources
Tubulin Resists Degradation by Cereblon-Recruiting PROTACs [PDF]
Cells, 2020 Dysregulation of microtubules and tubulin homeostasis has been linked to developmental disorders, neurodegenerative diseases, and cancer. In general, both microtubule-stabilizing and destabilizing agents have been powerful tools for studies of ...
Ivana Gasic +7 more
doaj +3 more sources
Generalizable Strategies for the Synthesis of Cereblon-Recruiting PROTAC Prodrugs. [PDF]
Angew Chem Int Ed EnglCereblon‐recruiting PROTACs remain challenging to derivatize for prodrug‐based delivery. In this study, three complementary conjugation strategies enabled the efficient synthesis of cleavable PROTAC prodrugs with tunable release kinetics that can be incorporated into a library of PEGylated constructs and bottlebrush prodrugs.
Wang AX +7 more
europepmc +3 more sources
Molecular glues: Recent advances in cereblon substrate identification and mechanistic insights. [PDF]
Smart MolMolecular glues exert diverse core biological functions by inducing or stabilizing protein–protein interactions, extending far beyond the traditional scope of targeted protein degradation. Key breakthroughs include expanded cereblon substrate recognition, sustained G protein‐coupled receptor megacomplex signaling, and the first orthosteric molecular ...
Guan Q +5 more
europepmc +2 more sources
E3 Ligase Ligands in Successful PROTACs: An Overview of Syntheses and Linker Attachment Points
Frontiers in Chemistry, 2021 Proteolysis-targeting chimeras (PROTACs) have received tremendous attention as a new and exciting class of therapeutic agents that promise to significantly impact drug discovery.
Aleša Bricelj +4 more
doaj +1 more source
Tumor and microenvironmental mechanisms of resistance to immunomodulatory drugs in multiple myeloma
Frontiers in Oncology, 2022 Resistance to immunomodulatory drugs (IMiDs®) is a major cause of treatment failure, disease relapse and ultimately poorer outcomes in multiple myeloma (MM). In order to optimally deploy IMiDs and their newer derivates CRBN E3 ligase modulators (CELMoDs®)
Lucia Y. Chen +4 more
doaj +1 more source
Histone deacetylase (HDAC) enzymes 1–3 exist in several corepressor complexes and are viable drug targets. To date, proteolysis targeting chimeras (PROTACs) designed to target HDAC1–3 typically exhibit the selective degradation of HDAC3.
Urvashi Patel (20139240) +7 more
core +5 more sources