Results 61 to 70 of about 128,101 (191)

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

Design, synthesis, and characterization of I-BET567, a pan-bromodomain and extra terminal (BET) bromodomain oral candidate [PDF]

, 2022
Through regulation of the epigenome, the bromodomain and extra terminal (BET) family of proteins represent important therapeutic targets for the treatment of human disease. Through mimicking the endogenous N-acetyl-lysine group and disrupting the protein–
Henley, Nick, Ferrie, Alan, Bamborough, Paul, Hirst, David J., Lovatt, Cerys, McCleary, Scott, Osmani, Qendresa, Prinjha, Rab K., Davis, Rob, Zhu, Linrong, Tomkinson, Nicholas C. O., Watson, Robert J., Lugo, David, Lindon, Matthew J., Gray, Matthew, Haynes, Andrea, Craggs, Peter D., Humphreys, Philip G., Harrison, Lee A., Molnar, Judit, Bit, Rino A., Rioja, Inmaculada, Tang, Dalin, Theodoulou, Natalie H., Atkinson, Stephen J., Cutler, Leanne, Holyer, Ian D., Thomas, Clare, Patten, Chris, Chung, Chun-wa, Gong, GangLi, Hayhow, Thomas G., Gordon, Laurie J., Preston, Alex, Taylor, Simon, Sun, Fenglai, Wellaway, Christopher R., Smithers, Nicholas, Seal, Jonathan T.   +38 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

Targeting bromodomain and extra-terminal proteins to inhibit neuroblastoma tumorigenesis through regulating MYCN

Frontiers in Cell and Developmental Biology, 2022
Bromodomain and extra-terminal domain (BET) family proteins play important roles in regulating the expression of multiple proto-oncogenes by recognizing acetylation of histones and non-histone proteins including transcription factors, which subsequently ...
Xiyao Shi, Xiyao Shi, Ying Wang, Longhui Zhang, Longhui Zhang, Wenjie Zhao, Wenjie Zhao, Xiangpeng Dai, Xiangpeng Dai, Yong-Guang Yang, Yong-Guang Yang, Yong-Guang Yang, Xiaoling Zhang, Xiaoling Zhang   +13 more
doaj   +1 more source

The role of BET attenuation in melanoma [PDF]

, 2022
Bromodomain and extra-terminal (BETs) proteins function as epigenetic readers by docking onto acetylated lysine residues (Kac) on histone tails via tandem bromodomains (BRDs), and recruiting protein binding partners via an extra-terminal recruitment ...
Henderson, Elizabeth K
core   +1 more source

BET Bromodomain as a Target of Epigenetic Therapy

CHEMICAL & PHARMACEUTICAL BULLETIN, 2016
Acetylation of histone is a key epigenetic modification, and contributes to many DNA-dependent cellular processes. The bromodomain structure, which consists of approximately 110 amino acid residues, serves as a 'reader' that recognizes acetylated lysine in histones, leading to recruitment of positive transcriptional elongation factor b (P-TEFb), and ...
openaire   +3 more sources

Bromodomain Protein Inhibitors Reorganize the Chromatin of Synovial Fibroblasts

Cells, 2023
Bromodomain- and extra-terminal domain (BET) proteins are epigenetic reader proteins that regulate transcription of their target genes by binding to acetylated histone side chains.
Monika Krošel, Larissa Moser, Miranda Houtman, Jasna Friščić, Matija Tomšič, Oliver Distler, Markus H. Hoffmann, Caroline Ospelt, Kerstin Klein   +8 more
doaj   +1 more source

Efficacy, safety and cost‐effectiveness of CAR‐T therapy

British Journal of Clinical Pharmacology, EarlyView.
CAR T‐cells demonstrate high efficacy in blood cancers, including ALL, MM and DLBCL. Innovations target solid tumours despite challenges such as antigen escape. Combination therapies enhance the delivery and infiltration of CAR T cells. Toxicity, cost and resistance remain major barriers to clinical use.
Emina Karahmet Sher, Amina Džidić‐Krivić, Emma Pinjic, Nejra Selak, Kanita Omerbasic, Alexandar Chupin, Andrej Belancic, Almir Fajkic   +7 more
wiley   +1 more source

Apabetalone, a Clinical-Stage, Selective BET Inhibitor, Opposes DUX4 Target Gene Expression in Primary Human FSHD Muscle Cells

Biomedicines, 2023
Facioscapulohumeral dystrophy (FSHD) is a muscle disease caused by inappropriate expression of the double homeobox 4 (DUX4) gene in skeletal muscle, and its downstream activation of pro-apoptotic transcriptional programs.
Christopher D. Sarsons, Dean Gilham, Laura M. Tsujikawa, Sylwia Wasiak, Li Fu, Brooke D. Rakai, Stephanie C. Stotz, Agostina Carestia, Michael Sweeney, Ewelina Kulikowski   +9 more
doaj   +1 more source

Harnessing ferroptosis from multilayer defense networks to nanoplatforms for specific cancer therapy

BMEMat, EarlyView.
Nanomaterials target metabolically‐regulated ferroptosis for cancer therapy. Iron‐based or alternative nanoplatforms integrate ferroptosis with chemotherapy, immunotherapy, or radiotherapy. They enable stimulus‐responsive therapies (photothermal, photodynamic, sonodynamic) activated by near‐infrared, light, or ultrasound, achieving potent synergistic ...
Xinyue Xu, Xuejian Wang, Wenyan Jiang, Wan Hairul Anuar Kamaruddin, Chunyan Fang, Pengfei Zhang   +5 more
wiley   +1 more source