Cereblon|Recruiting PROTACs

Cereblon-Recruiting PROTACs: Will New Drugs Have to Face Old ...

The PROTACs contained wogonin as a ligand for CDK9 and pomalidomide to recruit CRBN E3 ligase. The results of cellular assays showed that ...

Cereblon-Recruiting PROTACs: Will New Drugs Have to Face Old ...

The classical low-molecular-weight drugs are designed to bind with high affinity to the biological targets endowed with receptor or ...

Discovery of the cereblon-recruiting tubulin PROTACs effective in ...

We report the discovery of W13 as the first PROTAC against tubulin, which was created by connecting a CRBN ligand to the widely recognized microtubule- ...

Discovery and Characterization of a Novel Cereblon-Recruiting ...

Bridged PROTAC is a novel protein complex degrader strategy that exploits the target protein's binding partner to degrade undruggable proteins.

Development of a covalent cereblon-based PROTAC employing a ...

Many cereblon (CRBN) ligands have been used to develop proteolysis targeting chimeras (PROTACs), but all are reversible binders of the E3 ubiquitin ligase.

Cereblon-recruiting proteolysis targeting chimeras (PROTACs) can ...

Cereblon-recruiting proteolysis targeting chimeras (PROTACs) can determine the selective degradation of HDAC1 over HDAC3†.

Modeling the CRL4A ligase complex to predict target protein ...

Modeling the CRL4A ligase complex to predict target protein ubiquitination induced by cereblon-recruiting PROTACs

Solid-Phase Synthesis of Cereblon-Recruiting Selective Histone ...

The PROTACs were either based on an unselective vorinostat-like HDAC ligand or derived from a selective HDAC6 inhibitor. Notably, both PROTAC ...

PROTAC targeted protein degraders: the past is prologue - Nature

These are heterobifunctional small molecules consisting of two ligands joined by a linker: one ligand recruits and binds a protein of interest ( ...

Protein degraders - from thalidomide to new PROTACs

cereblon, molecular glue degrader, PROTACs, protein degrader, thalidomide, ubiquitin. Topic: technology; thalidomide; proteolysis targeting ...

Cereblon-Based Small-Molecule Compounds to Control Neural ...

... (PROTACs) for target protein knockdown. These studies raise the ... A novel cereblon modulator recruits GSPT1 to the CRL4(CRBN) ubiquitin ligase.

PROTAC® Optimization Kit for BET Bromodomain-Cereblon Binding

The PROTAC® Optimization Kit for BET Bromodomain-Cereblon Binding is designed for testing and profiling of PROTACs® directed against BET Bromodomain family ...

A selective and orally bioavailable VHL-recruiting PROTAC ... - Nature

Our tool compound, ACBI2, shows selective degradation of SMARCA2 over SMARCA4 in ex vivo human whole blood assays and in vivo efficacy in SMARCA4-deficient ...

E3 Ligase Ligands in Successful PROTACs: An Overview ... - Frontiers

Cereblon. CRBN is a 442-amino acid protein that forms a Cullin-4-RING E3 ubiquitin ligase (CRL4) complex and interacts with the adaptor ...

Solid-phase synthesis of cereblon-recruiting selective histone ...

Solid-phase synthesis of cereblon-recruiting selective histone deacetylase 6 degraders (HDAC6 PROTACs) with anti-leukemic activity.

Homo-protac cereblon degrader 1 82033 - BPS Bioscience

Homo-protac cereblon degrader 1 Homo-PROTAC Cereblon Degrader 1 is a highly potent and efficient Cereblon (CRBN) degrader with minimal effects on IKZF1 and ...

(PDF) Cereblon-Recruiting PROTACs: Will New Drugs Have to Face ...

value of 8.0 [24]. ... drug resistance [25]. ... expressed, and contributes to various cancers such as pancreatic, prostate and breast cancer. ... a triazole group in ...

Ubiquitin recruiting chimera: more than just a PROTAC - Biology Direct

Artificially targeted ubiquitin-dependent degradation of various proteins has evolved into the therapeutically relevant PROTAC technology.

Cereblon versus VHL: Hijacking E3 Ligases Against Each Other ...

VHL and CRBN are also the two most popular E3 ligases being recruited by bifunctional Proteolysis-targeting chimeras (PROTACs) to induce ubiquitination and ...

HTRF Cereblon Binding Kit, 500 Assay Points - Revvity

Cereblon is also one of the two most popular E3 ligases which is recruited by bifunctional Proteolysis-targeting chimeras (PROTACs) to induce ubiquitination and ...