Results 131 to 140 of about 743,371 (240)

From PROTAC to inhibitor: Structure-guided discovery of potent and orally bioavailable BET inhibitors. [PDF]

Eur J Med Chem, 2023
Koravovic M, Mayasundari A, Tasic G, Keramatnia F, Stachowski TR, Cui H, Chai SC, Jonchere B, Yang L, Li Y, Fu X, Hiltenbrand R, Paul L, Mishra V, Klco JM, Roussel MF, Pomerantz WC, Fischer M, Rankovic Z, Savic V.   +19 more
europepmc   +1 more source

Extracellular matrix remodeling and immune reprogramming drive residual tumor progression of liver cancer after incomplete microwave ablation

Molecular Oncology, EarlyView.
Incomplete microwave ablation (iMWA) of liver cancer triggers a biphasic progression in residual tumors. At Day 3, the microenvironment is characterized by acute inflammatory responses and extracellular matrix (ECM) remodeling. By Day 14, a profound shift occurs toward oncogenic signal transduction and immunosuppression, marked by macrophage ...
Yu Liu, Yubei He, Nikolaus Berndt, Michael Mülleder, Kathrin Textoris‐Taube, Jing Guo, Matthias Stechele, Justus Ramtke, Shraga Nahum Goldberg, Lynn Jeanette Savic   +9 more
wiley   +1 more source

BET-inhibitor DYB-41 reduces pulmonary inflammation and local and systemic cytokine levels in LPS-induced acute respiratory distress syndrome: an experimental rodent study

Intensive Care Medicine Experimental
Background Acute respiratory distress syndrome (ARDS) is a form of respiratory failure stemming from various underlying conditions that ultimately lead to inflammation and lung fibrosis.
Manuela Iten, Camille Gschwend, Alessandro Ostini, David Robert Cameron, Christine Goepfert, David Berger, Matthias Haenggi   +6 more
doaj   +1 more source

BET Inhibitors Target the SCLC-N Subtype of Small-Cell Lung Cancer by Blocking NEUROD1 Transactivation. [PDF]

Mol Cancer Res, 2023
Chen H, Gesumaria L, Park YK, Oliver TG, Singer DS, Ge K, Schrump DS.   +6 more
europepmc   +1 more source

Supplementary Figures 1-3 from Induction of MNK Kinase–dependent eIF4E Phosphorylation by Inhibitors Targeting BET Proteins Limits Efficacy of BET Inhibitors

, 2019
Fig. S1 - eIF4E expression and survival data for papillary thyroid. Fig. S2 - Effect of BET inhibitors on genes regulating cytoskeleton Fig.
Brian T. DeCant (15074458), Kazumi Ebine (413354), Maria Matsangou (15074464), Meng Shang (2180498), Samad Z. Munshi (15074461), Hidayatullah G. Munshi (11437026), Krishan Kumar (197868), Thao N.D. Pham (15074455)   +7 more
core   +1 more source

SPHINX31 acts as a SRPK1 inhibitor targeting the ATR/DNA‐PKcs/CHK1 replicative checkpoint to inhibit cell growth in non‐small cell lung cancer

Molecular Oncology, EarlyView.
The kinase SRPK1 directly interacts with the protein TOPBP1 and regulates the pre‐mRNA splicing of WIZ thereby contributing to the activation of the ATR/CHK1 replicative checkpoint in response to replicative stress. This allows cancer cells' genomic stability and survival.
Amani Shreim, Aurelie Genoux, Nadiia Zubchuk, Haoyang Zheng, Perla Salameh, Theo Ziegelmeyer, Fabien Dalonneau, Margot Rouchette, Christiane Oddou, Simona Miron, Helene Polveche, Adiilah Mamode Cassim, Carmen Garrido, Eleni Nikolakaki, Didier Auboeuf, Tao Jia, Sophie Zinn‐Justin, Beatrice Eymin   +17 more
wiley   +1 more source

The multi-CDK inhibitor dinaciclib reverses bromo- and extra-terminal domain (BET) inhibitor resistance in acute myeloid leukemia via inhibition of Wnt/β-catenin signaling

Experimental Hematology & Oncology
Acute myeloid leukemia (AML) is a highly aggressive hematologic cancer with poor survival across a broad range of molecular subtypes. Development of efficacious and well-tolerable therapies encompassing the range of mutations that can arise in AML ...
Alexander R. Marr, Madeline Halpin, Dominique L. Corbin, Yerdanos Asemelash, Steven Sher, Britten K. Gordon, Ethan C. Whipp, Shaneice Mitchell, Bonnie K. Harrington, Shelley Orwick, Samon Benrashid, Virginia M. Goettl, Vedat Yildiz, Andrew D. Mitchell, Olivia Cahn, Alice S. Mims, Karilyn T. M. Larkin, Meixao Long, James Blachly, Jennifer A. Woyach, Rosa Lapalombella, Nicole R. Grieselhuber   +21 more
doaj   +1 more source

Design and Characterization of 1,3-Dihydro-2H-benzo[d]azepin-2-ones as Rule-of-5 Compliant Bivalent BET Inhibitors. [PDF]

ACS Med Chem Lett, 2023
Bamborough P, Chung CW, Goodwin NC, Mitchell DJ, Neipp CE, Phillipou A, Preston A, Prinjha RK, Soden PE, Watson RJ, Demont EH.   +10 more
europepmc   +1 more source

BET and EZH2 Inhibitors: Novel Approaches for Targeting Cancer.

, 2019
PURPOSE OF REVIEW Increasing evidence suggests that epigenome plays a central role in cancer development making it a promising target for anticancer treatments.
Genta S, Pirosa MC, Stathis A
core   +1 more source

Optimizing photoactivation of PA‐mCherry for optical pooled CRISPR screens

FEBS Open Bio, EarlyView.
Photoactivatable PA‐mCherry finds widespread use to optically tag individual cells. However, confocal 405 nm UV laser‐scanning (normal scan) is much less efficient than widefield UV illumination, limiting the use of PA‐mCherry on confocal instruments. We remedy this limitation by reporting that rapid and repeated confocal scanning with a low‐intensity,
Sravasti Mukherjee, Giulia Zanetti, Bram van den Broek, Kees Jalink   +3 more
wiley   +1 more source