Results 71 to 80 of about 15,581 (231)

Targeting bromodomain and extra-terminal proteins to inhibit neuroblastoma tumorigenesis through regulating MYCN

Frontiers in Cell and Developmental Biology, 2022
Bromodomain and extra-terminal domain (BET) family proteins play important roles in regulating the expression of multiple proto-oncogenes by recognizing acetylation of histones and non-histone proteins including transcription factors, which subsequently ...
Xiyao Shi, Xiyao Shi, Ying Wang, Longhui Zhang, Longhui Zhang, Wenjie Zhao, Wenjie Zhao, Xiangpeng Dai, Xiangpeng Dai, Yong-Guang Yang, Yong-Guang Yang, Yong-Guang Yang, Xiaoling Zhang, Xiaoling Zhang   +13 more
doaj   +1 more source

Dual Aptamers‐Based SETDB1 PROTACs as Effective Anti‐Tumor Strategies for Breast Cancer

Advanced Science, EarlyView.
This study establishes dual‐aptamer PROTACs targeting SETDB1 using a SETDB1‐specific aptamer conjugated to AS1411. The designed PROTACs penetrate cells, recruit MDM2 to degrade SETDB1, and inhibit cancer cell proliferation and migration. Remarkably, they also overcome tamoxifen resistance and enhance CD8+ T cell cytotoxicity, suppressing tumor growth ...
Yanxuan Guo, Yingge Lv, Shuyu Huang, Chang Liu, Yan Ouyang, Bei Lan, Chenghao Xuan   +6 more
wiley   +1 more source

Bromodomain Protein Inhibitors Reorganize the Chromatin of Synovial Fibroblasts

Cells, 2023
Bromodomain- and extra-terminal domain (BET) proteins are epigenetic reader proteins that regulate transcription of their target genes by binding to acetylated histone side chains.
Monika Krošel, Larissa Moser, Miranda Houtman, Jasna Friščić, Matija Tomšič, Oliver Distler, Markus H. Hoffmann, Caroline Ospelt, Kerstin Klein   +8 more
doaj   +1 more source

Potent and selective bivalent inhibitors of BET bromodomains [PDF]

Nature Chemical Biology, 2016
Proteins of the bromodomain and extraterminal (BET) family, in particular bromodomain-containing protein 4 (BRD4), are of great interest as biological targets. BET proteins contain two separate bromodomains, and existing inhibitors bind to them monovalently.
Michael J Waring, Huawei Chen, Alfred A Rabow, Graeme Walker, Romel Bobby, Scott Boiko, Rob H Bradbury, Rowena Callis, Edwin Clark, Ian Dale, Danette L Daniels, Austin Dulak, Liz Flavell, Geoff Holdgate, Thomas A Jowitt, Alexey Kikhney, Mark McAlister, Jacqui Méndez, Derek Ogg, Joe Patel, Philip Petteruti, Graeme R Robb, Matthew B Robers, Sakina Saif, Natalie Stratton, Dmitri I Svergun, Wenxian Wang, David Whittaker, David M Wilson, Yi Yao   +29 more
openaire   +3 more sources

Post‐Translational Regulation of CD8+ T Cell Fate and Dysfunction in Tumor Immunity

Advanced Science, EarlyView.
This review delineates how post‐translational modifications (PTMs) function as a central regulatory interface governing CD8+ T cell activation, differentiation, persistence, and exhaustion in antitumor immunity. By integrating antigenic, metabolic, and microenvironmental cues, diverse PTM programs coordinate transcriptional and chromatin states that ...
Zihao Zhou, Xu Chen, Nina Li, Meiyan Zou, Yunfan Lin, Pei Lin, Weiyao Feng, Xinyuan Zhao, Li Cui   +8 more
wiley   +1 more source

Apabetalone, a Clinical-Stage, Selective BET Inhibitor, Opposes DUX4 Target Gene Expression in Primary Human FSHD Muscle Cells

Biomedicines, 2023
Facioscapulohumeral dystrophy (FSHD) is a muscle disease caused by inappropriate expression of the double homeobox 4 (DUX4) gene in skeletal muscle, and its downstream activation of pro-apoptotic transcriptional programs.
Christopher D. Sarsons, Dean Gilham, Laura M. Tsujikawa, Sylwia Wasiak, Li Fu, Brooke D. Rakai, Stephanie C. Stotz, Agostina Carestia, Michael Sweeney, Ewelina Kulikowski   +9 more
doaj   +1 more source

Assessing cellular efficacy of bromodomain inhibitors using fluorescence recovery after photobleaching [PDF]

, 2014
BACKGROUND: Acetylation of lysine residues in histone tails plays an important role in the regulation of gene transcription. Bromdomains are the readers of acetylated histone marks, and, consequently, bromodomain-containing proteins have a variety of ...
Anne-Claude Gingras, Catherine M Rogers, Chris Wells, Claire Strain-Damerell, Clarence Yapp, Jean-Philippe Lambert, Martin Philpott, Nicola A Burgess-Brown, Stefan Knapp, Susanne Müller   +9 more
core   +2 more sources

Efficacy, safety and cost‐effectiveness of CAR‐T therapy

British Journal of Clinical Pharmacology, EarlyView.
CAR T‐cells demonstrate high efficacy in blood cancers, including ALL, MM and DLBCL. Innovations target solid tumours despite challenges such as antigen escape. Combination therapies enhance the delivery and infiltration of CAR T cells. Toxicity, cost and resistance remain major barriers to clinical use.
Emina Karahmet Sher, Amina Džidić‐Krivić, Emma Pinjic, Nejra Selak, Kanita Omerbasic, Alexandar Chupin, Andrej Belancic, Almir Fajkic   +7 more
wiley   +1 more source

A Novel Phenanthridionone Based Scaffold As a Potential Inhibitor of the BRD2 Bromodomain: Crystal Structure of the Complex.

PLoS ONE, 2016
Bromodomain containing proteins recognize the level of histone acetylation and regulate epigenetically controlled processes like gene transcription and chromatin modification.
Shailesh Tripathi, Shruti Mathur, Prashant Deshmukh, Ramu Manjula, Balasundaram Padmanabhan   +4 more
doaj   +1 more source

Multiple Roles of Brd4 in the Infectious Cycle of Human Papillomaviruses

Frontiers in Molecular Biosciences, 2021
Human Papillomaviruses (HPV) reproduce in stratified epithelia by establishing a reservoir of low- level infection in the dividing basal cells and restricting the production of viral particles to terminally differentiated cells.
Alison A. McBride, Alix Warburton, Simran Khurana   +2 more
doaj   +1 more source