Results 71 to 80 of about 24,939 (257)

Lipid Pocket Binders Impose Allosteric Changes of Protein Dynamics Around the Active Site of the Protein Kinase p38α

Angewandte Chemie International Edition, Volume 65, Issue 15, 6 April 2026.
Used in search of novel allosteric sites in the serine/threonine kinase p38α, NMR spectroscopy reveals a dynamic coupling between the catalytic and lipid pockets. The findings uncover a motional interdependence that links distant regions of the enzyme, highlighting the lipid pocket as a promising site for allosteric intervention.
Sara Medina Gómez, Laurin T. Homberg, Mike Bührmann, Daniel Rauh, Rasmus Linser   +4 more
wiley   +1 more source

Photoelectron spectra of fluorine substituted diazanaphthalenes: “Even cases” [PDF]

, 1975
The high resolution He 584 Å photoelectron spectra of three diazanaphthalenes and some of their fluorine derivatives are presented.
Beerlage, M., Feil, D., Ham, D.M.W. van den, Meer, D. van der   +3 more
core   +2 more sources

ATF4‐mediated stress response as a therapeutic vulnerability in chordoma

Molecular Oncology, Volume 20, Issue 4, Page 1008-1021, April 2026.
We screened 5 chordoma cell lines against 100+ inhibitors of epigenetic and metabolic pathways and kinases and identified halofuginone, a tRNA synthetase inhibitor. Mechanistically halofuginone induces an integrated stress response, with eIF2alpha phosphorylation, activation of ATF4 and its target genes CHOP, ASNS, INHBE leading to cell death ...
Lucia Cottone, James Dunford, Eleanor Calcutt, Vicki Gamble, Filiz Senbabaoglu Aksu, Lorena Ligammari, Georgina Wherry, Giorgia Gaeta, John C. Christianson, Adrienne M. Flanagan, Udo Oppermann, Adam P. Cribbs   +11 more
wiley   +1 more source

Biological evaluation of novel 6-Arylbenzimidazo [1,2-c] quinazoline derivatives as inhibitors of LPS-induced TNF- alpha secretion

Biological Research, 2008
This study describes the effect of novel 6-Arylbenzimidazo [1,2-c] quinazoline derivatives as tumor necrosis factor alpha (TNF-á) production inhibitors.
GLORIA D GALARCE, ROCÍO E FONCEA, ANA M EDWARDS, HERNÁN PESSOA-MAHANA, CARLOS D PESSOA-MAHANA, ROBERTO A EBENSPERGER   +5 more
doaj  

High-Yield Synthesis of N⁴-(3-Chloro-4-fluorophenyl)-7-((4-methoxybenzyl)thio)quinazoline-4,6-diamine via N-(3-Chloro-4-fluorophenyl)-7-((4-methoxybenzyl)thio)-6-nitroquinazolin-4-amine

Molbank
The target compound, N4-(3-chloro-4-fluorophenyl)-7-((4-methoxybenzyl)thio)quinazoline-4,6-diamine, was synthesized in two steps from N-(3-chloro-4-fluorophenyl)-7-fluoro-6-nitroquinazolin-4-amine by a nucleophilic aromatic substitution, yielding N-(3 ...
Susila Thapa, Jeanne L. Bolliger
doaj   +1 more source

Benzothiadiazine dioxide human cytomegalovirus inhibitors: Synthesis and antiviral evaluation of main heterocycle modified derivatives [PDF]

, 2013
The benzothiadiazine dioxide derivatives are potent non-nucleoside human cytomegalovirus (HCMV) inhibitors. As part of our comprehensive structure-activity relationship (SAR) study of these compounds, we have now proposed structural modifications on the ...
Bruno, Ana M., Castro, Ana, Gil, Carmen, Martínez, Ana, Otero, Joaquín, Prieto, Columbiana, Pérez, Concepción   +6 more
core   +2 more sources

Prevention of Weight Regain After GLP1RA Cessation With Oral TIX100

Diabetes, Obesity and Metabolism, EarlyView.
SeongHo Jo, Junqin Chen, Gu Jing, Guanlan Xu, Peng Li, Anath Shalev   +5 more
wiley   +1 more source

Synthetic Cathepsin B Sensitive Adjuvant‐Peptide Conjugates to Target Intracellular Toll‐Like Receptors 7 and 8

ChemistryEurope, Volume 4, Issue 4, April 2026.
Cathepsin B‐sensitive peptide–adjuvant conjugates are designed, synthesized, and evaluated to deliver an antigenic peptid and an adjuvant targeting Toll‐like receptors 7 and 8 (TLR7/8) to antigen presenting cells. The adjuvant is released by cathepsin B resulting in antigen presentation and TLR mediated T cell activation.
Marjolein M. E. Isendoorn, Giulia Castello, Nico J. Meeuwenoord, Martijn Verdoes, Jeroen D. C. Codée, Ferry Ossendorp, Dmitri V. Filippov   +6 more
wiley   +1 more source

Signaling events involved in cytokine and chemokine production induced by secretory phospholipase A2 in human lung macrophages. [PDF]

, 2006
7openopenGranata F; Frattini A; Loffredo S; Del Prete A; Sozzani S; Marone G; Triggiani M.Granata, F; Frattini, A; Loffredo, S; DEL PRETE, Annalisa; Sozzani, Silvano; Marone, G; Triggiani ...
DEL PRETE A, FRATTINI A, GRANATA F, LOFFREDO S, M. TRIGGIANI, MARONE G, SOZZANI S   +6 more
core   +1 more source

Copper‐ and Silver‐Catalyzed Reactions of Active Methylene Isocyanides: Facile Access to Highly Substituted Five‐ and Six‐Membered Heterocycles

Chemistry – A European Journal, Volume 32, Issue 13, 1 April 2026.
This review summarizes recent advances in copper‐ and silver‐catalyzed reactions of active methylene isocyanides for the synthesis of highly substituted five‐ and six‐membered heterocycles. Emphasis is placed on [3+n] cycloadditions, annulations, and asymmetric strategies, highlighting current limitations and future opportunities in heterocycle ...
Jimil George, Kyungsoo Oh
wiley   +1 more source