Results 31 to 40 of about 56,924 (160)

Mechanisms altering airway smooth muscle cell Ca(2+) homeostasis in two asthma models [PDF]

, 2008
Background: Asthma is characterized by airway remodeling, altered mucus production and airway smooth muscle cell (ASMC) contraction causing extensive airway narrowing. In particular, alterations of ASMC contractility seem to be of crucial importance. The
Bergner, Albrecht, Edelmann, Martin, Fischer, Rainald, Huber, Rudolf M., Kellner, Julia, Oelmez, Hamza, Tantzscher, Juliane   +6 more
core   +1 more source

BET Bromodomain Inhibitors Suppress Inflammatory Activation of Gingival Fibroblasts and Epithelial Cells From Periodontitis Patients

Frontiers in Immunology, 2019
BET bromodomain proteins are important epigenetic regulators of gene expression that bind acetylated histone tails and regulate the formation of acetylation-dependent chromatin complexes.
Anna Maksylewicz, Agnieszka Bysiek, Katarzyna B. Lagosz, Justyna M. Macina, Malgorzata Kantorowicz, Grzegorz Bereta, Maja Sochalska, Katarzyna Gawron, Maria Chomyszyn-Gajewska, Jan Potempa, Jan Potempa, Aleksander M. Grabiec   +11 more
doaj   +1 more source

BET inhibitor suppresses migration of human hepatocellular carcinoma by inhibiting SMARCA4

Scientific Reports, 2021
Hepatocellular carcinoma (HCC) is one of the most prevalent and poorly responsive cancers worldwide. Bromodomain and extraterminal (BET) inhibitors, such as JQ1 and OTX-015, inhibit BET protein binding to acetylated residues in histones.
Hae In Choi, Ga Yeong An, Mina Baek, Eunyoung Yoo, Jin Choul Chai, Young Seek Lee, Kyoung Hwa Jung, Young Gyu Chai   +7 more
doaj   +1 more source

BRD3 Regulates the Inflammatory and Stress Response in Rheumatoid Arthritis Synovial Fibroblasts

Biomedicines, 2023
Background: Individual functions of members of the bromodomain (BRD) and extra-terminal (BET) protein family underlying the anti-inflammatory effects of BET inhibitors in rheumatoid arthritis (RA) are incompletely understood.
Tanja Seifritz, Matthias Brunner, Eva Camarillo Retamosa, Malgorzata Maciukiewicz, Monika Krošel, Larissa Moser, Thomas Züllig, Matija Tomšič, Oliver Distler, Caroline Ospelt, Kerstin Klein   +10 more
doaj   +1 more source

Optimization of a “Bump-and-Hole” Approach to Allele-Selective BET Bromodomain Inhibition [PDF]

, 2018
Allele-specific chemical genetics enables selective inhibition within families of highly-conserved proteins. The four BET (bromodomain & extra-terminal domain) proteins – BRD2, BRD3, BRD4 and BRDT bind acetylated chromatin via their bromodomains and ...
Albrecht, Amorim, Anders, Andrieu, Arrowsmith, Bamborough, Bamborough, Baud, Baud, Bishop, Bolden, Bunnage, Cheung, Clackson, Conery, Dawson, Deeney, Delmore, Dubocovich, Filippakopoulos, Filippakopoulos, Gacias, Gadd, Galdeano, Gamsjaeger, Huang, Islam, Lamonica, Li, Lin, Lu, Miller, Mirguet, Muller, Nassar, Nguyen, Nicholls, Nicodeme, Philpott, Picaud, Raina, Raux, Runcie, Sander, Schroder, Shi, Shi, Smith, Stathis, Stonestrom, Tanaka, Theodoulou, Theodoulou, Wang, Winter, Yang, Zengerle, Zhou, Zou, Zuber   +59 more
core   +2 more sources

Neuronal differentiation and cell-cycle programs mediate response to BET-bromodomain inhibition in MYC-driven medulloblastoma

Nature Communications, 2019
BET-bromodomain inhibitors could be used to treat medulloblastoma tumors with Myc amplifications. Here, the authors show that both the response and resistance to BET inhibitors in mice is mediated by bHLH/homeobox transcription factors.
Pratiti Bandopadhayay, Federica Piccioni, Ryan O’Rourke, Patricia Ho, Elizabeth M. Gonzalez, Graham Buchan, Kenin Qian, Gabrielle Gionet, Emily Girard, Margo Coxon, Matthew G. Rees, Lisa Brenan, Frank Dubois, Ofer Shapira, Noah F. Greenwald, Melanie Pages, Amanda Balboni Iniguez, Brenton R. Paolella, Alice Meng, Claire Sinai, Giovanni Roti, Neekesh V. Dharia, Amanda Creech, Benjamin Tanenbaum, Prasidda Khadka, Adam Tracy, Hong L. Tiv, Andrew L. Hong, Shannon Coy, Rumana Rashid, Jia-Ren Lin, Glenn S. Cowley, Fred C. Lam, Amy Goodale, Yenarae Lee, Kathleen Schoolcraft, Francisca Vazquez, William C. Hahn, Aviad Tsherniak, James E. Bradner, Michael B. Yaffe, Till Milde, Stefan M. Pfister, Jun Qi, Monica Schenone, Steven A. Carr, Keith L. Ligon, Mark W. Kieran, Sandro Santagata, James M. Olson, Prafulla C. Gokhale, Jacob D. Jaffe, David E. Root, Kimberly Stegmaier, Cory M. Johannessen, Rameen Beroukhim   +55 more
doaj   +1 more source

BET Bromodomain Proteins Brd2, Brd3 and Brd4 Selectively Regulate Metabolic Pathways in the Pancreatic β-Cell. [PDF]

PLoS ONE, 2016
Displacement of Bromodomain and Extra-Terminal (BET) proteins from chromatin has promise for cancer and inflammatory disease treatments, but roles of BET proteins in metabolic disease remain unexplored.
Jude T Deeney, Anna C Belkina, Orian S Shirihai, Barbara E Corkey, Gerald V Denis   +4 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

Beyond the BET family:targeting CBP/p300 with 4-acyl pyrroles [PDF]

, 2017
BET bromodomain inhibitors are widely used both as chemical tools to study the biological role of their targets in living organisms, and as candidates for drug development against several cancer variants and human disorders. However, non-BET bromodomains
Breit, Bernhard, Einsle, Oliver, Gerhardt, Stefan, Günther, Stefan, Hau, Mirjam, Hügle, Martin, Jung, Manfred, Lucas, Xavier, Ostrovskyi, Dmytro, Regenass, Pierre, Wohlwend, Daniel   +10 more
core   +2 more sources

High-Resolution Mapping of RNA Polymerases Identifies Mechanisms of Sensitivity and Resistance to BET Inhibitors in t(8;21) AML

Cell Reports, 2016
Bromodomain and extra-terminal domain (BET) family inhibitors offer an approach to treating hematological malignancies. We used precision nuclear run-on transcription sequencing (PRO-seq) to create high-resolution maps of active RNA polymerases across ...
Yue Zhao, Qi Liu, Pankaj Acharya, Kristy R. Stengel, Quanhu Sheng, Xiaofan Zhou, Hojoong Kwak, Melissa A. Fischer, James E. Bradner, Stephen A. Strickland, Sanjay R. Mohan, Michael R. Savona, Bryan J. Venters, Ming-Ming Zhou, John T. Lis, Scott W. Hiebert   +15 more
doaj   +1 more source