Results 61 to 70 of about 27,094 (219)

Chemical Inhibition of Bromodomain Proteins in Insect-Stage African Trypanosomes Perturbs Silencing of the Variant Surface Glycoprotein Repertoire and Results in Widespread Changes in the Transcriptome

Microbiology Spectrum, 2023
The eukaryotic protozoan parasite Trypanosoma brucei is transmitted by the tsetse fly to both humans and animals, where it causes a fatal disease called African trypanosomiasis.
Ethan C. Ashby, Jennifer L. Havens, Lindsey M. Rollosson, Johanna Hardin, Danae Schulz   +4 more
doaj   +1 more source

Supramolecular Degraders: An Emerging Paradigm in Targeted Protein Degradation

Advanced Science, EarlyView.
Dynamic supramolecular assembly reshapes targeted protein degradation by coordinating modular degrader construction, delivery, functional integration, and intracellular assembly or activation across proteasomal, endosomal–lysosomal, and autophagy–lysosomal pathways.
Kongjun Liu, Xue Yuan, Yan Zhou, Rui Yuan, Shaocheng Xie, Yong Chen, Peiyi Wang, Jianmei Gao, Qihai Gong   +8 more
wiley   +1 more source

1,3,4-oxadiazoles as inhibitors of the atypical member of the BET family bromodomain factor 3 from Trypanosoma cruzi (TcBDF3)

Frontiers in Microbiology
Chagas disease, caused by the protozoan parasite Trypanosoma cruzi, affects millions globally, with increasing urban cases outside of Latin America. Treatment is based on two compounds, namely, benznidazole (BZ) and nifurtimox, but chronic cases pose ...
Victoria L. Alonso, Victoria L. Alonso, Andrea M. Escalante, Elvio Rodríguez Araya, Elvio Rodríguez Araya, Gianfranco Frattini, Gianfranco Frattini, Luis E. Tavernelli, Diego M. Moreno, Diego M. Moreno, Ricardo L. E. Furlan, Esteban Serra, Esteban Serra   +12 more
doaj   +1 more source

Synthesis and Structure–Activity Relationships of Aristoyagonine Derivatives as Brd4 Bromodomain Inhibitors with X-ray Co-Crystal Research

Molecules, 2021
Epigenetic regulation is known to play a key role in progression of anti-cancer therapeutics. Lysine acetylation is an important mechanism in controlling gene expression.
Minjin Yoo, Tae Hyun Park, Miyoun Yoo, Yeongrin Kim, Joo-Youn Lee, Kyu Myung Lee, Seong Eon Ryu, Byung Il Lee, Kwan-Young Jung, Chi Hoon Park   +9 more
doaj   +1 more source

AS‐TLC‐Based High‐Throughput Screening Integrated with CuAAC Optimization Strategy Facilitates the Rapid Discovery of YTHDC1 Inhibitor

Advanced Science, EarlyView.
We developed Affinity Selection Thin‐Layer Chromatography (AS‐TLC) as a method for high‐throughput screening (HTS) of compound mixtures. Furthermore, we integrated activity assays with AS‐TLC and identified a YTH domain‐containing protein 1 (YTHDC1) inhibitor. Building on this hit, we applied copper(I)‐catalyzed azide–alkyne cycloaddition (CuAAC) click
Mingchen Wang, Shuiping Fu, Ye Xu, Jia Gao, Jiwei Ren, Xu Yang, Hesong Xu, Ge Sun, Yanjie Li, Yanlin Wang, Lu Jin, Peijuan Chen, Ying Xu, Jianhao Li, Hua Lin, Chujiao Hu, Kaixian Chen, Huan Xiong, Cheng Luo, Shijie Chen   +19 more
wiley   +1 more source

Spotlight on Plant Bromodomain Proteins

Biology, 2023
Bromodomain-containing proteins (BRD-proteins) are the “readers” of histone lysine acetylation, translating chromatin state into gene expression. They act alone or as components of larger complexes and exhibit diverse functions to regulate gene expression; they participate in chromatin remodeling complexes, mediate histone modifications, serve as ...
Eirini Bardani, Paraskevi Kallemi, Martha Tselika, Konstantina Katsarou, Kriton Kalantidis   +4 more
openaire   +3 more sources

Glucose and Glutamine Deprivation Promotes Breast Cancer Lung Metastasis via BRD4‐Dependent Enhancer Activation

Advanced Science, EarlyView.
To model a nutrient‐restricted tumor microenvironment, breast cancer cells were adapted to low glucose and glutamine levels. In the adapted cells, BRD4‐driven enhancer activation increases pro‐invasive EDN1 expression, facilitated by ATF3/c‐JUN and reinforced by enhancer RNA.
Poshan Yugal Bhattarai, Arathy Vasukutty, Yujin Na, Sung‐Chul Lim, Hong Seok Choi   +4 more
wiley   +1 more source

A Versatile DNA‐Encoded Library Platform for the Discovery of Highly Cooperative Chemical Inducers of Proximity

Advanced Science, EarlyView.
We present a versatile DNA‐encoded library (DEL) platform designed for rapid library synthesis and subsequent screening for chemical inducers of proximity (CIPs) across various presenter proteins of choice. Applying this approach, we discovered a novel molecular glue‐like compound mediating CRBN‐BRD9 ternary complex formation with remarkable ...
Bingqi Tong, Sunny A. Tang, Yifan Deng, Zhihan Nan, Alison X. Gao, Gregory A. Michaud, Simone Bonazzi, Frédéric Berst, Frédéric J. Zécri, Shuang Liu, William J. Gibson, Stuart L. Schreiber   +11 more
wiley   +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

A Chemical Probe for the ATAD2 Bromodomain [PDF]

Angewandte Chemie, 2016
AbstractATAD2 is a cancer‐associated protein whose bromodomain has been described as among the least druggable of that target class. Starting from a potent lead, permeability and selectivity were improved through a dual approach: 1) using CF2 as a sulfone bio‐isostere to exploit the unique properties of fluorine, and 2) using 1,3‐interactions to ...
Paul Bamborough, Chun‐wa Chung, Emmanuel H. Demont, Rebecca C. Furze, Andrew J. Bannister, Ka Hing Che, Hawa Diallo, Clement Douault, Paola Grandi, Tony Kouzarides, Anne‐Marie Michon, Darren J. Mitchell, Rab K. Prinjha, Christina Rau, Samuel Robson, Robert J. Sheppard, Richard Upton, Robert J. Watson   +17 more
openaire   +3 more sources