Results 71 to 80 of about 767,969 (287)

The novel BET‐CBP/p300 dual inhibitor NEO2734 is active in SPOP mutant and wild‐type prostate cancer

EMBO Molecular Medicine, 2019
CULLIN3‐based E3 ubiquitin ligase substrate‐binding adaptor gene SPOP is frequently mutated in prostate cancer (PCa). PCa harboring SPOP hotspot mutants (e.g., F133V) are resistant to BET inhibitors because of aberrant elevation of BET proteins. Here, we
Yuqian Yan, Jian Ma, Dejie Wang, Dong Lin, Xiaodong Pang, Shangqian Wang, Yu Zhao, Lei Shi, Hui Xue, Yunqian Pan, Jun Zhang, Claes Wahlestedt, Francis J Giles, Yu Chen, Martin E Gleave, Collin C Collins, Dingwei Ye, Yuzhuo Wang, Haojie Huang   +18 more
doaj   +1 more source

Epigenetic reprogramming of lineage switching in cancer

FEBS Letters, EarlyView.
Cancer cells rarely commit to a single identity. Epigenetic mechanisms and tumor microenvironment cues push epithelial cells toward flexible, hybrid states that can shift into mesenchymal, neuroendocrine, or stem‐like fates, driving metastasis, drug resistance, and tumor heterogeneity. Targeting the epigenetic regulators behind these transitions, using
Ezgi Boyvatlı, Burcu Akman, Ezgi Bağırsakçı, Nese Atabey, Serap Erkek‐Ozhan   +4 more
wiley   +1 more source

Autophagy and mitophagy in pancreatic β‐cell homeostasis and their involvement in diabetes pathophysiology

FEBS Letters, EarlyView.
This review focuses on the role of autophagy and mitophagy in maintaining pancreatic β‐cell function and homeostasis. We discuss how genetic defects affecting these pathways contribute to the development of type 1, type 2, monogenic, and gestational diabetes. We further explore their potential as therapeutic targets. Created in BioRender.
Yunkyeong Lee, Mingming Tong, Anna L. Gloyn   +2 more
wiley   +1 more source

The Commonly Used PI3-Kinase Probe LY294002 Is an Inhibitor of BET Bromodomains

, 2016
A commonly used small-molecule probe in cell-signaling research is the phosphoinositide 3-kinase inhibitor LY294002. Quantitative chemoproteomic profiling shows that LY294002 and LY303511, a close analogue devoid of PI3K activity, inhibit the BET ...
Gitte Neubauer (1843147), Chun-Wa Chung (153155), Carsten Hopf (1643689), Mikhail M. Savitski (1843150), Thilo Werner (1355949), Maria Fälth Savitski (1843144), Paola Grandi (1343472), Gerard Drewes (1290381), Matthew Lindon (1355946), Rabinder K. Prinjha (1843153), Antje Dittmann (1357548), Marcus Bantscheff (1290387)   +11 more
core   +1 more source

Partial depletion of plasminogen activator inhibitor‐1 decreases subcutaneous fat cell hypertrophy and liver cholesterol in high‐fat‐fed female mice

FEBS Letters, EarlyView.
Obesity raises blood levels of PAI‐1, a protein linked to metabolic dysfunction‐associated steatotic liver disease in people with obesity. In female mice fed a high‐fat diet, partially lowering PAI‐1 led to smaller subcutaneous fat cells and lower liver cholesterol, without changing body weight or insulin sensitivity.
Claudia E. Ramirez Bustamante, Robert Sharp, Pradip K. Saha, Elizabeth S. Anaya, Elizabeth L. Lieu, Evelyn L. de Groot, Pooja Patel, Mi Jeong Heo, Aaron R. Cox, Kang Ho Kim, Sean M. Hartig   +10 more
wiley   +1 more source

BET inhibition silences expression of MYCN and BCL2 and induces cytotoxicity in neuroblastoma tumor models.

PLoS ONE, 2013
BET family proteins are epigenetic regulators known to control expression of genes involved in cell growth and oncogenesis. Selective inhibitors of BET proteins exhibit potent anti-proliferative activity in a number of hematologic cancer models, in part ...
Anastasia Wyce, Gopinath Ganji, Kimberly N Smitheman, Chun-Wa Chung, Susan Korenchuk, Yuchen Bai, Olena Barbash, BaoChau Le, Peter D Craggs, Michael T McCabe, Karen M Kennedy-Wilson, Lydia V Sanchez, Romain L Gosmini, Nigel Parr, Charles F McHugh, Dashyant Dhanak, Rab K Prinjha, Kurt R Auger, Peter J Tummino   +18 more
doaj   +1 more source

BET inhibitor resistance emerges from leukaemia stem cells

, 2015
Bromodomain and extra terminal protein (BET) inhibitors are first-in-class targeted therapies that deliver a new therapeutic opportunity by directly targeting bromodomain proteins that bind acetylated chromatin marks.
Stanley, Kym, Papenfuss, Anthony T., Prinjha, Rab K., Huntly, Brian J.P., Kouzarides, Tony, Lee, Stanley Chun-Wei, Dawson, Sarah-Jane, Gilan, Omer, Ramsay, Robert G., Tyler, Dean, Rubin, Alan F., Lane, Steven W., Abdel-Wahab, Omar, Fong, Chun Yew, Lugo, Dave, Lam, Enid Y.N., Sinha, Devbarna, Johnstone, Ricky W., Giotopoulos, George, Dawson, Mark A., Ftouni, Sarah, Gregory, Richard, Morison, Jessica, Jeffrey, Philip, Yeh, Paul, Carpenter, Christopher   +25 more
core   +1 more source

Structures of mycobacterial 3‐methylcrotonyl‐CoA carboxylase reveal carrier‐domain translocation between catalytic sites

FEBS Letters, EarlyView.
Mycobacterial 3‐methylcrotonyl‐CoA carboxylase uses a mobile biotin‐carrying domain to shuttle a carboxyl group between two catalytic sites, enabling carboxylation of 3‐methylcrotonyl‐CoA during leucine breakdown. Cryo‐electron microscopy captures the carrier at both sites and reveals an inward loop movement that may prevent futile rebinding to the ...
Ajit Yadav, Bogdan I. Florea, Sebastian Geibel   +2 more
wiley   +1 more source

[News Clip: Another Election Bet]

, 1960
Video footage from the WBAP-TV television station in Fort Worth, Texas, to accompany a news story about a lost bet where Carl Thompson has to push a peanut one block from the drug store to the grocery ...
WBAP-TV (Television station : Fort Worth, Tex.)
core   +1 more source

The heterodimeric amino acid transporters (HAT) of the SLC7/SLC3 family: A structure−function relationships and relevance to human pathology

FEBS Letters, EarlyView.
Heterodimeric amino acid transporters consist of SLC7 and SLC3 family proteins arranged in a conserved structural organization. They regulate nutrient transport across cell membranes, supporting essential cellular functions. These transporters also contribute to xenobiotic/drug uptake and distribution.
Mariafrancesca Scalise, Tiziano Mazza, Raffaella Scanga, Lara Console, Michele Galluccio, Cesare Indiveri   +5 more
wiley   +1 more source