Results 1 to 10 of about 4,858 (185)

Hydrophobic Waters in Bromodomains [PDF]

Proceedings, 2019
Targeting epigenetic proteins is a rapidly growing area for medicinal chemistry and drug [...]
Serena G. Piticchio, Miriam Martínez-Cartró, Salvatore Scaffidi, Sergio Rodríguez-Arévalo, Andrea Bagán, Ainoa Sánchez-Arfelis, Carmen Escolano, Carles Galdeano, Xavier Barril   +8 more
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Development of a PET Probe Targeting Bromodomain and Extra-Terminal Proteins for In Vitro and In Vivo Visualization [PDF]

Pharmaceuticals
Background: Bromodomain and extra-terminal (BET) proteins are critical regulators of gene transcription, as they recognize acetylated lysine residues. The BD1 bromodomain of BRD4, a member of the BET family, has emerged as a promising therapeutic target ...
Yongle Wang, Yanli Wang, Yulong Xu, Hua Cheng, Tewodros Mulugeta Dagnew, Leyi Kang, Darcy Tocci, Iris Z. Shen, Can Zhang, Changning Wang   +9 more
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A novel carboxamide bromodomain inhibitor attenuates osteoarthritis via epigenetic repression of NF-κB and MAPK signaling [PDF]

Frontiers in Immunology
Bromodomains are epigenetic readers that modulate gene expression linked to inflammation and cartilage degeneration. Emerging evidence suggests their dysregulation plays a pivotal role in osteoarthritis (OA) pathogenesis, making them promising ...
Hyemi Lee, Seong Jae Han, Subin Ok, Kwang Min Lee, Seungseok Choi, Injoo Yoon, Somang Choi, Jina Kim, Serim Ryu, Min-Hee Son, In-Hyun Lee, Chanmi Cho, Siyoung Yang   +12 more
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Protein dynamics and structural waters in bromodomains. [PDF]

PLoS ONE, 2017
Bromodomains are epigenetic readers of acetylated lysines that are integral parts of histone tails. The 61 bromodomains in humans are structurally highly conserved but specifically bind to widely varying recognition motifs, suggesting that dynamic rather
Xiaoxiao Zhang, Kai Chen, Yun-Dong Wu, Olaf Wiest   +3 more
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Biochemical profiling of histone binding selectivity of the yeast bromodomain family. [PDF]

PLoS ONE, 2010
It has been shown that molecular interactions between site-specific chemical modifications such as acetylation and methylation on DNA-packing histones and conserved structural modules present in transcriptional proteins are closely associated with ...
Qiang Zhang, Suvobrata Chakravarty, Dario Ghersi, Lei Zeng, Alexander N Plotnikov, Roberto Sanchez, Ming-Ming Zhou   +6 more
doaj   +1 more source

Deep-learning analysis of micropattern-based organoids enables high-throughput drug screening of Huntington’s disease models

Cell Reports: Methods, 2022
Summary: Organoids are carrying the promise of modeling complex disease phenotypes and serving as a powerful basis for unbiased drug screens, potentially offering a more efficient drug-discovery route.
Jakob J. Metzger, Carlota Pereda, Arjun Adhikari, Tomomi Haremaki, Szilvia Galgoczi, Eric D. Siggia, Ali H. Brivanlou, Fred Etoc   +7 more
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Reprogramming by De-bookmarking the Somatic Transcriptional Program through Targeting of BET Bromodomains

Cell Reports, 2016
One critical event in reprogramming to pluripotency is erasure of the somatic transcriptional program of starting cells. Here, we present the proof of principle of a strategy for reprogramming to pluripotency facilitated by small molecules that interfere
Zhicheng Shao, Chunping Yao, Alireza Khodadadi-Jamayran, Weihua Xu, Tim M. Townes, Michael R. Crowley, Kejin Hu   +6 more
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Euryops pectinatus L. Flower Extract Inhibits P-glycoprotein and Reverses Multi-Drug Resistance in Cancer Cells: A Mechanistic Study

Molecules, 2020
Euryops pectinatus is a South African ornamental plant belonging to family Asteraceae. The present work evaluates the cytotoxic activity and phytochemical profile of the flower extract. Metabolite profiling was performed using HPLC-PDA-ESI-MS/MS.
Wafaa M. Elkady, Iriny M. Ayoub, Yousra Abdel-Mottaleb, Mohamed F. ElShafie, Michael Wink   +4 more
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The Aggregation of ATAD2 Bromodomain in Solution

Chinese Journal of Magnetic Resonance, 2023
ATPase family AAA domain-containing protein 2 (ATAD2) is a chromatin regulator, also known as an oncogenic transcription cofactor. Its abnormal expression is closely related to the occurrence and development of various malignant tumors. ATAD2 consists of
WANG Yuanfang, WANG Xiaohua, SHU Chang, ZHANG Xu, LIU Maili, ZENG Danyun   +5 more
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Crystal structure of [1,2,4] triazolo[4,3- b ]pyridazine derivatives as BRD4 bromodomain inhibitors and structure–activity relationship study

Scientific Reports, 2023
BRD4 contains two tandem bromodomains (BD1 and BD2) that recognize acetylated lysine for epigenetic reading, and these bromodomains are promising therapeutic targets for treating various diseases, including cancers.
Jung-Hoon Kim, Navin Pandit, Miyoun Yoo, Tae Hyun Park, Ji U Choi, Chi Hoon Park, Kwan-Young Jung, Byung Il Lee   +7 more
doaj   +1 more source