Results 91 to 100 of about 15,581 (231)
SPR-measured dissociation kinetics of PROTAC ternary complexes influence target degradation rate [PDF]
, 2019 Bifunctional degrader molecules, known as proteolysis-targeting chimeras (PROTACs), function by recruiting a target to an E3 ligase, forming a target/PROTAC/ligase ternary complex.
Ciulli, Alessio +7 more
core +3 more sources
BRD9 inhibition as potential treatment option for testicular germ cell tumors
Andrology, EarlyView.Abstract Background Testicular germ cell tumors (TGCT) are the predominant tumor in younger males. Usually, 5‐year survival rates are quite high, but 15–20% of patients with metastatic non‐seminomas are resistant to standard cisplatin‐based therapy.
Aylin Hansen +5 more
wiley +1 more source
Pharmacological ResearchThe bromodomain and extraterminal domain (BET) family proteins serve as primary readers of acetylated lysine residues and play crucial roles in cell proliferation and differentiation.
Nan Liu +11 more
doaj +1 more source
Targeting the epigenetic readers in Ewing Sarcoma inhibits the oncogenic transcription factor EWS/Fli1. [PDF]
, 2016 Ewing Sarcoma is a rare bone and soft tissue malignancy affecting children and young adults. Chromosomal translocations in this cancer produce fusion oncogenes as characteristic molecular signatures of the disease.
Alonso +56 more
core +2 more sources
Intrinsic specificity of a ‘core’ TIP60 acetyltransferase complex in Drosophila
The FEBS Journal, EarlyView.The intrinsic substrate selectivity of the Drosophila TIP60‐core acetyltransferase was determined using synthetic nucleosome arrays. Targeted mass spectrometry revealed site‐specific acetylation of histones H2A, H2A.V, and H4, uncovering distinct acetylation rates and patterns across individual lysines.
Silke Krause +5 more
wiley +1 more source
Epigenetics and chromatin remodeling play a role in lung disease [PDF]
, 2011 Epigenetics is defined as heritable changes that affect gene expression without altering the DNA sequence. Epigenetic regulation of gene expression is facilitated through different mechanisms such as DNA methylation, histone modifications and RNA ...
Adcock, IM +3 more
core +1 more source
BET bromodomain inhibitors synergize with ATR inhibitors in melanoma [PDF]
Cell Death & Disease, 2017 AbstractMetastatic malignant melanoma continues to be a challenging disease despite clinical translation of the comprehensive understanding of driver mutations and how melanoma cells evade immune attack. In Myc-driven lymphoma, efficacy of epigenetic inhibitors of the bromodomain and extra-terminal domain (BET) family of bromodomain proteins can be ...
Somsundar Veppil Muralidharan +10 more
openaire +3 more sources
The FEBS Journal, EarlyView.Genetic rearrangements resulting in the expression of KMT2A fusion alleles can lead to dramatic transcriptional disturbances that contribute to the onset of acute leukaemias. Fortunately, menin inhibition has emerged as a promising new class of targeted therapy.
Lydia Elaine Roets +2 more
wiley +1 more source
Structural and Atropisomeric Factors Governing the Selectivity of Pyrimido-benzodiazipinones as Inhibitors of Kinases and Bromodomains [PDF]
, 2018 Bromodomains have been pursued intensively over the past several years as emerging targets for the development of anticancer and anti-inflammatory agents.
Alessi, Dario R. +27 more
core +3 more sources
MedComm, Volume 7, Issue 4, April 2026.E1A is an important protein for adenovirus to initiate viral replication. Previous reports have shown that E1A binds to p300 as a regulatory factor. However, our study provides a new perspective that E1A promotes oncolytic adenovirus replication by degrading p300.
Boduan Xiao +7 more
wiley +1 more source