Results 41 to 50 of about 16,709 (213)

Gene regulation and tumor suppression by the bromodomain-containing protein BRD7 [PDF]

Cell Cycle, 2010
Oncogene-induced senescence (OIS) is a cellular defense mechanism against excessive mitogenic signaling and tumorigenesis. One of the major pathways required for OIS is the p53 tumor suppressor pathway. Consequently, many human tumors harbor p53 mutations while others show a dysfunctional p53 pathway, frequently by unknown mechanisms.
MANTOVANI, FIAMMA, Drost J., Voorhoeve P. M., DEL SAL, GIANNINO, Agami R.   +4 more
openaire   +3 more sources

BRD4 PROTAC degrader MZ1 exhibits anti-B-cell acute lymphoblastic leukemia effects via targeting CCND3

Hematology, 2023
Introduction B-cell acute lymphoblastic leukemia (B-ALL) is the most prevalent malignant tumor affecting children. While the majority of B-ALL patients (90%) experience successful recovery, early relapse cases of B-ALL continue to exhibit high mortality ...
Li Ma, Jianwei Wang, Yang Yang, Jun Lu, Jing Ling, Xinran Chu, Zimu Zhang, Yanfang Tao, Xiaolu Li, Yuanyuan Tian, Zhiheng Li, Yongping Zhang, Xu Sang, Lihui Lu, Xiaomei Wan, Kunlong Zhang, Yanling Chen, Juanjuan Yu, Ran Zhuo, Shuiyan Wu, Jian Pan, Xiuxia Zhou, Yixin Hu, Shaoyan Hu   +23 more
doaj   +1 more source

Solution structure of the extraterminal domain of the bromodomain‐containing protein BRD4 [PDF]

Protein Science, 2008
AbstractBRD4, which is a member of the BET (bromodomains and extraterminal) protein family, interacts preferentially with acetylated chromatin and possesses multiple cellular functions in meiosis, embryonic development, the cell cycle, and transcription.
Yi-Jan, Lin, Takashi, Umehara, Makoto, Inoue, Kohei, Saito, Takanori, Kigawa, Moon-Kyoo, Jang, Keiko, Ozato, Shigeyuki, Yokoyama, Balasundaram, Padmanabhan, Peter, Güntert   +9 more
openaire   +2 more sources

Bromodomain dimers: A case study of BRD4 and family-wide AlphaFold predictions [PDF]

Structural Dynamics
Bromodomains are conserved acetyl-lysine reader domains that play a central role in the assembly of transcriptional regulatory complexes. While generally presumed to function as monomers, bromodomain homo-dimers have been identified, and several ...
Alisa S. Dengler, Lara Lunglmeir, Matthias J. Brandl, T. Reid Alderson   +3 more
doaj   +1 more source

Genome-wide survey of D/E repeats in human proteins uncovers their instability and aids in identifying their role in the chromatin regulator ATAD2

iScience, 2022
Summary: D/E repeats are stretches of aspartic and/or glutamic acid residues found in over 150 human proteins. We examined genomic stability of D/E repeats and functional characteristics of D/E repeat-containing proteins vis-à-vis the proteins with poly ...
Shalabh Shukla, Pavlo Lazarchuk, Maria N. Pavlova, Julia M. Sidorova   +3 more
doaj   +1 more source

Rational design and development of selective BRD7 bromodomain inhibitors and their activity in prostate cancer

, 2023
Bromodomain-containing proteins are readers of acetylated lysine and play important roles in cancer. Bromo-domain-containing protein 7 (BRD7) has been implicated in multiple malignancies; however, there are no selective chemical probes to study its ...
Sandra, Ordonez, Surbhi, Sood, Alexander, McQuade, Brian , Smith, Sijie, Wang, Emily, Dykhuizen, Brayden, Strohmier, Chad, Maschinot   +7 more
core   +1 more source

Multicomponent Stapling of Glucagon‐Like Peptide‐1 Enables Receptor‐Guided PROTAC Delivery

Angewandte Chemie, EarlyView.
We report a stapled glucagon‐like peptide‐1 (GLP‐1) analogue created via multicomponent tryptophan‐mediated Petasis reaction (TMPR). This strategy yields a stabilised peptide with superior helicity and improved potency. Conjugation to a bromodomain‐containing protein 4 (BRD4) degrader creates the first GLP‐1‐guided targeted protein degrader (PROTAC ...
Jan L. Venne, Sona Krajcovicova, Graeme Davies, Hannah Bolt, Jefferson Revell, David R. Spring   +5 more
wiley   +2 more sources

BRD4 Inhibitor GNE-987 Exerts Anticancer Effects by Targeting Super-Enhancer-Related Gene LYL1 in Acute Myeloid Leukemia

Journal of Immunology Research, 2022
Background. AML (acute myeloid leukemia) is a common hematological malignancy in children with poor treatment effects and poor prognosis. Recent studies have shown that as a novel BRD4 (bromodomain containing 4) PROTACs (proteolysis targeting chimeras ...
Xu Sang, Yongping Zhang, Fang Fang, Li Gao, Yanfang Tao, Xiaolu Li, Zimu Zhang, Jianwei Wang, Yuanyuan Tian, Zhiheng Li, Di Yao, Yumeng Wu, Xinran Chu, Kunlong Zhang, Li Ma, Lihui Lu, Yanling Chen, Juanjuan Yu, Ran Zhuo, Shuiyan Wu, Zhen Zhang, Jian Pan, Shaoyan Hu   +22 more
doaj   +1 more source

Design of a chemical probe for the Bromodomain and Plant Homeodomain Finger-containing (BRPF) family of proteins [PDF]

, 2017
The bromodomain and PHD finger-containing (BRPF) family are scaffolding proteins important for the recruitment of histone acetyltransferases of the MYST family to chromatin.
Boyd, H, Savitsky, P, Meier, JC, Cheasty, A, Brennan, PE, Stefan Knapp, Catherine Rogers, David M. Andrews, Müller, S, Yannick Morias, Cunoosamy, D, Anne Cheasty, Fedorov, Oleg, Helen Boyd, Danen Cunoosamy, Elliott D. Bayle, Müller, Susanne, Oleg Fedorov, Rogers, C, Niall Igoe, Scholze, S, Knapp, Stefan, Cynthia Tallant, Sarah Scholze, Julia C. Meier, Tallant, C, Knapp, S, Tallant, Cynthia, Paul E. Brennan, Morias, Y, Susanne Müller, Rogers, Catherine, Brennan, Paul, Pavel Savitsky, Bayle, ED, Igoe, N, Savitsky, Pavel, Andrews, DM, Paul V. Fish, Fedorov, O, Meier, Julia C, Fish, PV   +41 more
core   +1 more source

A Nutrient-Based Cellular Model to Characterize Acetylation-Dependent Protein-Protein Interactions

Frontiers in Molecular Biosciences, 2022
Cellular homeostasis requires the orderly expression of thousands of transcripts. Gene expression is regulated by numerous proteins that recognize post-translational modifications—in particular, the acetylation of lysine residues (Kac) on histones.
Jérémy Loehr, Jérémy Loehr, Pata-Eting Kougnassoukou Tchara, Pata-Eting Kougnassoukou Tchara, Pata-Eting Kougnassoukou Tchara, Kevin Gonthier, Kevin Gonthier, Chahinez Noufi, Chahinez Noufi, Naomie Linteau, Naomie Linteau, Étienne Audet-Walsh, Étienne Audet-Walsh, Jean-Philippe Lambert, Jean-Philippe Lambert, Jean-Philippe Lambert   +15 more
doaj   +1 more source