Results 71 to 80 of about 5,434 (195)
Discovery of SKP2‐Recruiting PROTACs for Target Protein Degradation
Based on the SKP2‐targeting ligand SL1, we designed non‐covalent PROTACs by linking it with the BRD4 inhibitor JQ1 and the AR antagonist AL through a linker. These PROTACs successfully induced the ubiquitination of BRD4 and AR, followed by proteasome‐mediated degradation.
Guanjun Dong +13 more
wiley +1 more source
LYAR potentiates rRNA synthesis by recruiting BRD2/4 and the MYST-type acetyltransferase KAT7 to rDNA [PDF]
Activation of ribosomal RNA (rRNA) synthesis is pivotal during cell growth and proliferation, but its aberrant upregulation may promote tumorigenesis. Here, we demonstrate that the candidate oncoprotein, LYAR, enhances ribosomal DNA (rDNA) transcription.
Tachikawa, Hiroyuki +13 more
core +1 more source
We identify an antagonistic ubiquitin circuit that controls cellular permissiveness to multiple coronaviruses. The deubiquitinase USP7 stabilizes the epigenetic regulator KDM6A to upregulate viral receptors, while the E3 ligase RNF40 degrades KDM6A by catalyzing K6/K11‐ubiquitin chains of KDM6A for autophagic degradation.
Meng‐Zhuo Huang +9 more
wiley +1 more source
Binding analysis of L10 towards BRD2-BD2.
SPR sensorgrams obtained by running different concentrations of L10 over immobilized BRD2-BD2. The figure in the inset shows fitting of data points at equilibrium (Req) for the interaction of different concentrations of L10 to immobilized BD2.
Balasundaram Padmanabhan (3165435) +4 more
core +1 more source
This article outlines recent findings on genetics of juvenile myoclonic epilepsy (JME), where JME occurrence is associated with polymorphic allelic variants in BRD2 gene (locus EJM3) and GJD2 gene (locus EJM2).Objective: To establish risk factors for ...
O. S. Shilkina +4 more
doaj
Metamorphosis and lncRNAs: A Close Relationship
ABSTRACT The classical definition of metamorphosis is a post‐embryonic transformation, such as from a tadpole to a froglet. However, recent studies suggest this process occurs to some degree in all vertebrates, as the underlying endocrine and molecular pathways are highly conserved. With the advent of high‐throughput sequencing, transcriptomic data for
H. Herrera‐Orozco +1 more
wiley +1 more source
Interaction of BRD2 and BRD4 with KSHV latent episomes.
(A) Schematic of KSHV genome regulatory regions tested by ChIP assay and primer positions a-i. Red triangles represent CTCF binding sites and TR is terminal repeats. Open reading frames for KSHV gene are indicated.
Horng-Shen Chen (473322) +5 more
core +1 more source
Analysis of Brd2 influence on PPARγ and C/EBPα expression.
(A) PPARγ and C/EBPα mRNA expression in Brd2 knockdown 3T3-L1 cells, and (B) in Brd2 overexpression 3T3-L1 cells, as detected by reverse transcription PCR at different time points during adipogenic differentiation.
Jingyu Wang (292122) +9 more
core +1 more source
Molecular Glue Degraders Redefining Targeted Therapies From Discovery to Therapeutic Applications
Molecular glue degraders (MGDs) constitute an emerging class of therapeutic agents poised to revolutionize the paradigm of targeted drug discovery. By reprogramming E3 ubiquitin ligases to degrade proteins of interest (POI) via a transient formation of a ternary complex mediated by protein–protein interactions, MGDs surpass the intrinsic limitations of
Jinfeng Wen +3 more
wiley +1 more source
The bromodomain and extra-terminal domain (BET) proteins are promising drug targets for cancer and immune diseases. However, BET inhibition effects have been studied more in the context of bromodomain-containing protein 4 (BRD4) than BRD2, and the BET ...
Takayoshi Matsuda +13 more
core +1 more source

