Results 41 to 50 of about 20,494 (185)

Differential Water Networks Guide Selectivity Optimization of a Cell Active BPTF Inhibitor in Neuroblastoma

Angewandte Chemie, EarlyView.
BZ2 is a second‐generation Bromodomain PHD finger Transcription Factor (BPTF) inhibitor with improved selectivity over Class I and Class IV BRD off‐targets identified in our previously reported inhibitor, BZ1. Structural analyses reveal that water network engagement is key to this selectivity.
Kesavan Babu, Chun‐Ju Tsou, Sourav Das, Liying Fan, Anasuya Pal, Molly Sneddon, Timothy R. Stachowski, Priyanka Samanta, Stanley Nithianantham, Caroline Buchholz, Shi Zhang, Xiang Fu, Rahul S. Kathayat, Wenwei Lin, Yongtao Li, Lei Yang, Taosheng Chen, Marcus Fischer, Anang A. Shelat, William C. K. Pomerantz   +19 more
wiley   +2 more sources

Targeting transcription factors associated with hemoglobinopathies: Lessons from successful interventions and implications for cancer

Molecular Oncology, EarlyView.
This review summarizes the transcription factors, repressive chromatin‐modifying complexes, and epigenetic mechanisms that control fetal hemoglobin repression. Notably, many regulators of γ‐globin silencing also function in transcriptional and epigenetic networks that drive cancer, highlighting opportunities to translate advances in hemoglobinopathy ...
Meigen Yu, Puspa Das, Xing Zhang, Xiaodong Cheng   +3 more
wiley   +1 more source

Should I Stay or Should I Go—Leveraging an Overlooked Feature of Click‐to‐Release Chemistry for Affinity Labeling

Angewandte Chemie, EarlyView.
Click‐to‐release (C2R) chemistry is redirected from payload liberation toward ligand‐directed covalent protein labeling through a transient dihydropyridazine methide (DHP‐methide). This concept opens the way to dual‐functional systems combining covalent target engagement with controlled effector release.
Dóra Kern, Krisztina Németh, Tímea Imre, József Simon, Kitti Meggyes, Gergő Bárdos, László Petri, Márton Bojtár, Attila Kormos, Péter Kele   +9 more
wiley   +2 more sources

Arginine methylation as a regulatory ratchet in cancer: From substrate selection to malignant‐state stabilization

Molecular Oncology, EarlyView.
Arginine methylation can be viewed as a persistence‐prone post‐translational modification regulated by a network of PRMTs. Competitive and compensatory interactions among PRMTs can redistribute methylation across substrate pools shaped by sequence, structural, spatial, and environmental layers, reinforcing RNA‐processing, chromatin, and signaling ...
So Hyun Kwon, Ji Min Lee
wiley   +1 more source

Selective Antagonists of the Bronchiolar Epithelial NF-κB-Bromodomain-Containing Protein 4 Pathway in Viral-Induced Airway Inflammation

Cell Reports, 2018
Summary: The mechanisms by which the mammalian airway detects invading viral pathogens to trigger protective innate neutrophilic inflammation are incompletely understood.
Bing Tian, Zhiqing Liu, Jun Yang, Hong Sun, Yingxin Zhao, Maki Wakamiya, Haiying Chen, Erik Rytting, Jia Zhou, Allan R. Brasier   +9 more
doaj   +1 more source

SPHINX31 acts as a SRPK1 inhibitor targeting the ATR/DNA‐PKcs/CHK1 replicative checkpoint to inhibit cell growth in non‐small cell lung cancer

Molecular Oncology, EarlyView.
The kinase SRPK1 directly interacts with the protein TOPBP1 and regulates the pre‐mRNA splicing of WIZ thereby contributing to the activation of the ATR/CHK1 replicative checkpoint in response to replicative stress. This allows cancer cells' genomic stability and survival.
Amani Shreim, Aurelie Genoux, Nadiia Zubchuk, Haoyang Zheng, Perla Salameh, Theo Ziegelmeyer, Fabien Dalonneau, Margot Rouchette, Christiane Oddou, Simona Miron, Helene Polveche, Adiilah Mamode Cassim, Carmen Garrido, Eleni Nikolakaki, Didier Auboeuf, Tao Jia, Sophie Zinn‐Justin, Beatrice Eymin   +17 more
wiley   +1 more source

Brd4 471-730 functions as a DNI of the MCV LT and Brd4 interaction.

, 2012
A. Brd4 471-730 inhibits MCV LT and Brd4 Co-IP. 293T cells were co-transfected with pcDNA4C-MCV LT together with a pCDNA4C plasmid encoding Xpress-tagged Brd4 471-730 or the empty vector.
Jianxin You (121729), Christopher B. Buck (121726), Jing Li (10611), Rachel M. Schowalter (121719), Xin Wang (91924), Jing Jiao (121723)   +5 more
core   +1 more source

Molecular Dynamic Simulations of Bromodomain and Extra-Terminal Protein 4 Bonded to Potent Inhibitors

Molecules, 2021
Bromodomain and extra-terminal domain (BET) subfamily is the most studied subfamily of bromodomain-containing proteins (BCPs) family which can modulate acetylation signal transduction and produce diverse physiological functions.
Siao Chen, Yi He, Yajiao Geng, Zhi Wang, Lu Han, Weiwei Han   +5 more
doaj   +1 more source

Advanced Materials for Biologics Delivery to Brain Tumors

Advanced Materials, EarlyView.
Material innovation is central to unlocking the therapeutic potential of biologics against many central nervous system diseases, including brain cancer. By engineering carriers with controlled transport, targeting, and release properties, advanced materials can overcome the blood–brain barrier and tumor microenvironment, improving the delivery of ...
Yuran Feng, Yuxue Cao, Maria Kavallaris, Taskeen Janjua, Amirali Popat   +4 more
wiley   +1 more source

BRD4 Structure–Activity Relationships of Dual PLK1 Kinase/BRD4 Bromodomain Inhibitor BI-2536

, 2016
A focused library of analogues of the dual PLK1 kinase/BRD4 bromodomain inhibitor BI-2536 was prepared and then analyzed for BRD4 and PLK1 inhibitory activities.
Maryanna E. Lanning (1621531), Makoto Yoshioka (1668034), Rachel N. Fountain (1668022), Mithun Raje (1668031), Lijia Chen (1621525), Jeremy L. Yap (1621519), Steven Fletcher (1621516), Jeffrey W. Strovel (1668025), Jacob A. Scheenstra (1668028)   +8 more
core   +1 more source