Results 61 to 70 of about 33,428 (239)

Tumor-Promoting ATAD2 and Its Preclinical Challenges

Biomolecules, 2022
ATAD2 has received extensive attention in recent years as one prospective oncogene with tumor-promoting features in many malignancies. ATAD2 is a highly conserved bromodomain family protein that exerts its biological functions by mainly AAA ATPase and ...
Haicheng Liu, Qianghai Wen, Sheng Yan, Weikun Zeng, Yuhua Zou, Quanliang Liu, Guoxi Zhang, Junrong Zou, Xiaofeng Zou   +8 more
doaj   +1 more source

Selective Targeting of Bromodomains of the Bromodomain-PHD Fingers Family Impairs Osteoclast Differentiation [PDF]

ACS Chemical Biology, 2017
Histone acetyltransferases of the MYST family are recruited to chromatin by BRPF scaffolding proteins. We explored functional consequences and the therapeutic potential of inhibitors targeting acetyl-lysine dependent protein interaction domains (bromodomains) present in BRPF1-3 in bone maintenance.
Julia C. Meier, Cynthia Tallant, Oleg Fedorov, Hanna Witwicka, Sung-Yong Hwang, Ruud G. van Stiphout, Jean-Philippe Lambert, Catherine Rogers, Clarence Yapp, Brian S. Gerstenberger, Vita Fedele, Pavel Savitsky, David Heidenreich, Danette L. Daniels, Dafydd R. Owen, Paul V. Fish, Niall M. Igoe, Elliott D. Bayle, Bernard Haendler, Udo C.T. Oppermann, Francesca Buffa, Paul E. Brennan, Susanne Müller, Anne Claude Gingras, Paul R. Odgren, Mark J. Birnbaum, Stefan Knapp   +26 more
openaire   +4 more sources

Ferritinophagy is required for the induction of ferroptosis by the bromodomain protein BRD4 inhibitor (+)-JQ1 in cancer cells

Cell Death and Disease, 2019
(+)-JQ1 is an inhibitor of the tumor-driver bromodomain protein BRD4 and produces satisfactory effects because it efficiently increases apoptosis. Ferroptosis is an oxidative cell death program differing from apoptosis.
Shiyao Sui, Jian Zhang, Shouping Xu, Qin Wang, Peiyuan Wang, D. Pang   +5 more
semanticscholar   +1 more source

Inhibitors of bromodomain and extra‐terminal proteins for treating multiple human diseases

Medicinal research reviews (Print), 2020
Clinical development of bromodomain and extra‐terminal (BET) protein inhibitors differs from the traditional course of drug development. These drugs are simultaneously being evaluated for treating a wide spectrum of human diseases due to their novel ...
E. Kulikowski, B. Rakai, N. Wong
semanticscholar   +1 more source

Bromodomains as therapeutic targets in cancer [PDF]

Briefings in Functional Genomics, 2013
The malleability of the epigenome has long been recognized as a unique opportunity for therapeutic intervention. Interest in targeting components of the epigenetic machinery for therapeutic gain had initially been aimed at chromatin modifying enzymes.
Barbieri, I., Cannizzaro, E., Dawson, M. A.   +2 more
openaire   +2 more sources

Bioactivation of Isoxazole-Containing Bromodomain and Extra-Terminal Domain (BET) Inhibitors

Metabolites, 2021
The 3,5-dimethylisoxazole motif has become a useful and popular acetyl-lysine mimic employed in isoxazole-containing bromodomain and extra-terminal (BET) inhibitors but may introduce the potential for bioactivations into toxic reactive metabolites.
Noah R. Flynn, Michael D. Ward, Mary A. Schleiff, Corentine M. C. Laurin, Rohit Farmer, Stuart J. Conway, Gunnar Boysen, S. Joshua Swamidass, Grover P. Miller   +8 more
doaj   +1 more source

Histone Recognition and Large-Scale Structural Analysis of the Human Bromodomain Family

Cell, 2012
Summary Bromodomains (BRDs) are protein interaction modules that specifically recognize ε-N-lysine acetylation motifs, a key event in the reading process of epigenetic marks.
P. Filippakopoulos, S. Picaud, M. Mangos, T. Keates, Jean-Philippe Lambert, Dalia Barsyte-Lovejoy, I. Felletár, R. Volkmer, S. Müller, T. Pawson, A. Gingras, C. Arrowsmith, S. Knapp   +12 more
semanticscholar   +1 more source

Developing inhibitors of bromodomain-histone interactions

, 2014
Lysine acetylation is a widespread protein post-translational modification that influences diverse cellular processes. An association between acetylation of histone N-terminal tails and transcriptional activation has been recognised since the 1960s ...
Hewings, David Stephen, Conway, Stuart J, Brennan, Paul E   +2 more
core   +2 more sources

Unveiling the folding mechanism of the Bromodomains

Biochemistry and Biophysics Reports, 2017
Bromodomains (BRDs) are small protein domains often present in large multidomain proteins involved in transcriptional regulation in eukaryotic cells. They currently represent valuable targets for the development of inhibitors of aberrant transcriptional processes in a variety of human diseases.
Petrosino, Maria, Bonetti, Daniela, Pasquo, Alessandra, Lori, Laura, Chiaraluce, Roberta, Consalvi, Valerio, Travaglini-allocatelli, Carlo   +6 more
openaire   +4 more sources

Bromodomains on the brain [PDF]

Science-Business eXchange, 2013
A Dana-Farber–led team has found that MYCN amplification provides a marker for sensitivity to BET bromodomain inhibition in neuroblastomas. GSK is using the marker as one criterion to select patients for a Phase I trial of its BET bromodomain inhibitor in cancer.
openaire   +1 more source