Results 111 to 120 of about 33,428 (239)

Brd4 BD1 Domain Antagonism of MS436 Preserves Blood‐Brain Barrier Integrity via Rnf43/β‐Catenin Signaling Pathway

Advanced Science
Blood‐brain barrier (BBB) disruption is central to neurodegenerative and cerebrovascular diseases, but its causal role and therapeutic targeting remain challenging.
Chenxiao Li, Xiaochen Zhang, Jiangwei Xia, Shuang Liu, Yushan Du, Sihan Li, Shukui Zhang, Yong Zhang, Fen Ji, Jianwei Jiao, Jingjing Zhang   +10 more
doaj   +1 more source

PAX3-FOXO1 establishes myogenic super enhancers and confers BET bromodomain vulnerability

Cancer Discovery, 2017
Alveolar rhabdomyosarcoma is a life-threatening myogenic cancer of children and adolescent young adults, driven primarily by the chimeric transcription factor PAX3-FOXO1 (P3F). The mechanisms by which P3F dysregulates chromatin are unknown.
B. Gryder, M. Yohe, Hsien-Chao Chou, Xiaohu Zhang, Joana G Marques, Marco Wachtel, B. Schaefer, Nirmalya Sen, Y. Song, A. Gualtieri, S. Pomella, R. Rota, Abigail H. Cleveland, Xinyu Wen, Sivasish Sindiri, Jun S. Wei, F. Barr, Sudipto Das, T. Andresson, R. Guha, M. Lal-Nag, M. Ferrer, J. Shern, K. Zhao, Craig J. Thomas, J. Khan   +25 more
semanticscholar   +1 more source

Epigenetic Reader BRD4 (Bromodomain-Containing Protein 4) Governs Nucleus-Encoded Mitochondrial Transcriptome to Regulate Cardiac Function

Circulation, 2020
Supplemental Digital Content is available in the text. Background: BET (bromodomain and extraterminal) epigenetic reader proteins, in particular BRD4 (bromodomain-containing protein 4), have emerged as potential therapeutic targets in a number of ...
S. Kim, Xin Zhang, G. Schiattarella, Francisco Altamirano, Thaís A. R. Ramos, Kristin M. French, Nan Jiang, P. Szweda, Bret M. Evers, Herman I. May, Xiang Luo, Hongliang Li, L. Szweda, Vinicius Maracaja-Coutinho, S. Lavandero, T. Gillette, Joseph A. Hill   +16 more
semanticscholar   +1 more source

Targeting MYCN in Neuroblastoma by BET Bromodomain Inhibition [PDF]

, 2013
Bromodomain inhibition comprises a promising therapeutic strategy in cancer, particularly for hematologic malignancies. To date, however, genomic biomarkers to direct clinical translation have been lacking. We conducted a cell-based screen of genetically
Bassil, Christopher F, Gustafson, William Clay, Nekritz, Erin A, Kung, Andrew L, Weiss, William A, Garnett, Matthew J, Puissant, Alexandre, Frumm, Stacey M, Chanthery, Yvan H, Benes, Cyril H, Zeid, Rhamy, Qi, Jun, Stegmaier, Kimberly, McDermott, Ultan, Bradner, James E, Greninger, Patricia, Alexe, Gabriela   +16 more
core   +1 more source

A Novel Family of Bromodomain Genes

Genomics, 2000
The bromodomain is a structural motif characteristic of proteins involved in chromatin-dependent regulation of transcription. Bromodomain proteins have been identified as integral components of chromatin remodeling complexes and frequently possess histone acetyltransferase activity. Their encoding genes have been identified at translocation breakpoints,
M H, Jones, N, Hamana, J i, Nezu, M, Shimane   +3 more
openaire   +2 more sources

Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression

Journal of Medicinal Chemistry, 2018
Proteins of the bromodomain and extra-terminal (BET) family are epigenetics “readers” and promising therapeutic targets for cancer and other human diseases.
Chong Qin, Yang Hu, Bing Zhou, E. Fernández-Salas, Chao-Yie Yang, Liu Liu, D. McEachern, S. Przybranowski, Mi Wang, J. Stuckey, J. Meagher, Longchuan Bai, Zhuo Chen, Mei Lin, Jiuling Yang, Danya Ziazadeh, Fuming Xu, Jiantao Hu, Weiguo Xiang, Liyue Huang, Siwei Li, Bo Wen, Duxin Sun, Shaomeng Wang   +23 more
semanticscholar   +1 more source

Chemical probes targeting epigenetic proteins: Applications beyond oncology

Epigenetics, 2017
Epigenetic chemical probes are potent, cell-active, small molecule inhibitors or antagonists of specific domains in a protein; they have been indispensable for studying bromodomains and protein methyltransferases. The Structural Genomics Consortium (SGC),
Suzanne Ackloo, Peter J. Brown, Susanne Müller   +2 more
doaj   +1 more source

Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands.

, 2013
The bromodomain protein module, which binds to acetylated lysine, is emerging as an important epigenetic therapeutic target. We report the structure-guided optimization of 3,5-dimethylisoxazole derivatives to develop potent inhibitors of the BET ...
Knapp, Stefan, Olcina, MM, Gill, A, Sheppard, DW, Wells, C, Tumber, A, Ritchie, AJ, Freeman, K, Brennan, Paul, Filippakopoulos, Panagis, Picaud, S, Conway, Stuart, Fedorov, O, Hammond, Ester, Hewings, DS, Martin, S, Russell, Angela   +16 more
core   +1 more source

Optimization of 3,5-Dimethylisoxazole Derivatives as Potent Bromodomain Ligands

, 2015
The bromodomain protein module, which binds to acetylated lysine, is emerging as an important epigenetic therapeutic target. We report the structure-guided optimization of 3,5-dimethylisoxazole derivatives to develop potent inhibitors of the BET ...
Stuart J. Conway (1280553), Oleg Fedorov (244326), Stefan Knapp (244328), Sarah Picaud (1280562), Andrew Gill (1295037), Angela J. Russell (106482), Monica M. Olcina (1295040), Christopher Wells (1295034), David S. Hewings (1295028), David W. Sheppard (1295046), Ester M. Hammond (233098), Anthony Tumber (765317), Paul E. Brennan (1290474), Alison J. Ritchie (1295043), Katherine Freeman (239943), Panagis Filippakopoulos (1280556), Sarah Martin (1295031)   +16 more
core   +1 more source

Structural Activity Relationship Analysis of New Diphenyl PFI-3 Analogues Targeting for the Treatment of Glioblastoma

Pharmaceuticals
Background/Objectives: Human glioblastoma (GBM) is the most aggressive brain cancer in adults and a highly treatment-refractory malignancy. The overall prognosis for the GBM is extremely poor, with a median survival of 12–14 months after initial ...
Dong-Jin Hwang, Chuanhe Yang, Yinan Wang, Hannah Kelso, Satyanarayana Pochampally, Lawrence M. Pfeffer, Duane D. Miller   +6 more
doaj   +1 more source