Results 111 to 120 of about 24,956 (275)

BET inhibitors potentiate melanoma ferroptosis and immunotherapy through AKR1C2 inhibition. [PDF]

Mil Med Res, 2023
Meng Y, Sun HY, He Y, Zhou Q, Liu YH, Su H, Yin MZ, Zeng FR, Chen X, Deng GT.   +9 more
europepmc   +1 more source

Rapid screening of staphylokinase protein variants using an unpurified cell‐free expression system

FEBS Open Bio, EarlyView.
An unpurified cell‐free protein synthesis (CFPS) platform enables rapid functional screening of staphylokinase variants. Direct plasminogen‐activation assays performed in microplate format provide real‐time activity readouts, allowing rapid identification and ranking of variants with improved or reduced fibrinolytic activity without protein ...
Maria Tomková, Veronika Hovanová, Jiri Damborsky, Erik Sedlák   +3 more
wiley   +1 more source

Design and synthesis of small molecule BET inhibitors

The confidentiality statement on each page of this thesis DOES NOT apply.Previously held under moratorium in Chemistry department (GSK) from 11/3/2020 until 20/03/2025.Small molecule Bromodomain and Extra-Terminal (BET) inhibitors have shown promising ...
Kessedjian, Hripsimée
core   +1 more source

Blood‐based proteomic profiling reveals context‐dependent changes in BCL2‐associated signaling during taxane therapy in breast cancer patients

FEBS Open Bio, EarlyView.
Chemotherapy side effects significantly impact cancer survivors' quality of life. Using protein levels in blood samples from breast cancer patients before and after 12 weeks of taxane treatment, we detected treatment‐dependent changes in calcium signaling and aging pathways associated with cancer recurrence.
Saira Munshani, Eiman Y. Ibrahim, Rozalyn L. Rodwin, Leah M. Ferrucci, Kim Blenman, Maryam Lustberg, Barbara E. Ehrlich   +6 more
wiley   +1 more source

Recent progress and structural analyses of domain-selective BET inhibitors. [PDF]

Med Res Rev, 2023
Divakaran A, Harki DA, Pomerantz WCK.
europepmc   +1 more source

Long‐term hippocampal alterations and cognitive impairment in a murine model of surgical sepsis

FEBS Open Bio, EarlyView.
Using a mouse model of surgical sepsis, we tested long‐term memory and analyzed the transcriptome of single cells isolated from the hippocampus. Survivor mice showed worse memory, loss of certain brain cell subpopulations, and abnormal immune cell activity—suggesting that post‐sepsis brain alterations may be linked to cognitive deficits.
Dong Seong Cho, Rebecca Schmitt, Aneesha Dasgupta, Alexandra Ducharme, Jason Doles   +4 more
wiley   +1 more source

Current landscape of BRD4 inhibitors: Selective targeting and protein degradation for enhanced efficacy

Results in Chemistry
The bromodomain and extra-terminal domain (BET) family of proteins has been implicated as a crucial factor in the pathogenesis of numerous diseases by regulating gene expression and chromatin dynamics through its bromodomains, which bind to acetylated ...
Linlin Deng, Erkang Tian, Ting Ma, Shaojie Liang, Sijia Hu, Linwei Li, Juan Li   +6 more
doaj   +1 more source

Molecular dynamics simulations of positively selected codons in FcγRI reveal novel biochemical binding properties

FEBS Open Bio, EarlyView.
Evolutionary analysis across 32 placental mammals identified positive selection at residues H148 and W149 in the immune receptor FcγR1. Ancestral reconstruction combined with molecular dynamics simulations reveals how these mutations may influence receptor structure and dynamics, providing insight into the evolution of antibody recognition and immune ...
David A. Young, Omar Arias‐Gaguancela, Fiona Gibson, Morgan Grainger, Jodie Score, Amit Nathubhai, Mauricio Cafiero, Lee Richard Machado   +7 more
wiley   +1 more source

Design and synthesis of dimethylisoxazole quinolines as BET inhibitors

Previously held under moratorium in Chemistry department (GSK) from 1/6/15 until 3 September 2021.The confidentiality statement on each page of this thesis DOES NOT applyGene regulation is governed by the assembly of protein complexes capable of reading ...
Wellaway, Christopher Roland
core   +1 more source

Optimizing photoactivation of PA‐mCherry for optical pooled CRISPR screens

FEBS Open Bio, EarlyView.
Photoactivatable PA‐mCherry finds widespread use to optically tag individual cells. However, confocal 405 nm UV laser‐scanning (normal scan) is much less efficient than widefield UV illumination, limiting the use of PA‐mCherry on confocal instruments. We remedy this limitation by reporting that rapid and repeated confocal scanning with a low‐intensity,
Sravasti Mukherjee, Giulia Zanetti, Bram van den Broek, Kees Jalink   +3 more
wiley   +1 more source