Results 21 to 30 of about 767,969 (287)

The role of BET attenuation in melanoma [PDF]

, 2022
Bromodomain and extra-terminal (BETs) proteins function as epigenetic readers by docking onto acetylated lysine residues (Kac) on histone tails via tandem bromodomains (BRDs), and recruiting protein binding partners via an extra-terminal recruitment ...
Henderson, Elizabeth K
core   +1 more source

Pharmacologic screen identifies active combinations with BET inhibitors and LRRK2 as a novel putative target in lymphoma

eJHaem, 2022
Inhibitors of the Bromo‐ and Extra‐Terminal domain (BET) family proteins have strong preclinical antitumor activity in multiple tumor models, including lymphomas. Limited single‐agent activity has been reported in the clinical setting.
Filippo Spriano, Giulio Sartori, Chiara Tarantelli, Marilia Barreca, Gaetanina Golino, Andrea Rinaldi, Sara Napoli, Michele Mascia, Lorenzo Scalise, Alberto J. Arribas, Luciano Cascione, Emanuele Zucca, Anastasios Stathis, Eugenio Gaudio, Francesco Bertoni   +14 more
doaj   +1 more source

BET Proteins Regulate Expression of Osr1 in Early Kidney Development

Biomedicines, 2021
In utero renal development is subject to maternal metabolic and environmental influences affecting long-term renal function and the risk of developing chronic kidney failure and cardiovascular disease.
Janina Schreiber, Nastassia Liaukouskaya, Lars Fuhrmann, Alexander-Thomas Hauser, Manfred Jung, Tobias B. Huber, Nicola Wanner   +6 more
doaj   +1 more source

Erratum: 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, Berglind Osk Einarsdottir, Joydeep Bhadury, Mattias F Lindberg, Jin Wu, Eric Campeau, Roger Olofsson Bagge, Ulrika Stierner, Lars Ny, Lisa M Nilsson, Jonas A Nilsson   +10 more
openaire   +4 more sources

Potent BRD4 inhibitor suppresses cancer cell-macrophage interaction

Nature Communications, 2020
Inhibitors of the BET family proteins are limited by their potency and oral bio-availability. Here, the authors report a new BET inhibitor, NHWD-870, with improved potency compared to previous BET inhibitors, and show that it suppresses BRD4 and targets ...
Mingzhu Yin, Ying Guo, Rui Hu, Wesley L. Cai, Yao Li, Shiyao Pei, Hongyin Sun, Cong Peng, Jiali Li, Rui Ye, Qiaohong Yang, Nenghui Wang, Yongguang Tao, Xiang Chen, Qin Yan   +14 more
doaj   +1 more source

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

Data on gene and protein expression changes induced by apabetalone (RVX-208) in ex vivo treated human whole blood and primary hepatocytes

Data in Brief, 2016
Apabetalone (RVX-208) inhibits the interaction between epigenetic regulators known as bromodomain and extraterminal (BET) proteins and acetyl-lysine marks on histone tails. Data presented here supports the manuscript published in Atherosclerosis “RVX-208,
Sylwia Wasiak, Dean Gilham, Laura M. Tsujikawa, Christopher Halliday, Karen Norek, Reena G. Patel, Kevin G. McLure, Peter R. Young, Allan Gordon, Ewelina Kulikowski, Jan Johansson, Michael Sweeney, Norman C. Wong   +12 more
doaj   +1 more source

Streamlined DNA-encoded small molecule library screening and validation for the discovery of novel chemotypes targeting BET proteins

Molecular Therapy: Nucleic Acids, 2023
Targeting aberrant epigenetic programs that drive tumorigenesis is a promising approach to cancer therapy. DNA-encoded library (DEL) screening is a core platform technology increasingly used to identify drugs that bind to protein targets.
Seoyeon Jeong, Hwa-Ryeon Kim, June-Ha Shin, Min-Hee Son, In-Hyun Lee, Jae-Seok Roe   +5 more
doaj   +1 more source

BET Inhibition Induces HEXIM1- and RAD51-Dependent Conflicts between Transcription and Replication

Cell Reports, 2018
Summary: BET bromodomain proteins are required for oncogenic transcription activities, and BET inhibitors have been rapidly advanced into clinical trials.
Akhil Bowry, Ann Liza Piberger, Patricia Rojas, Marco Saponaro, Eva Petermann   +4 more
doaj   +1 more source

Genome-wide CRISPR-Cas9 screens identify mechanisms of BET bromodomain inhibitor sensitivity

iScience, 2021
Summary: BET bromodomain inhibitors hold promise as therapeutic agents in diverse indications, but their clinical progression has been challenging and none have received regulatory approval.
David Estoppey, Gabi Schutzius, Christian Kolter, Adrian Salathe, Tiffany Wunderlin, Amandine Meyer, Florian Nigsch, Tewis Bouwmeester, Dominic Hoepfner, Susan Kirkland   +9 more
doaj   +1 more source