Results 71 to 80 of about 13,129 (191)

A Vanillin‐Derived Inhibitor of Aggregates via Targeting Intrinsically Disordered Regions of Phytoviral Nucleocapsid Protein

Aggregate
Phase separation (PS) plays a fundamental role in organizing aggregates during the viral lifecycle, providing significant opportunities for in viral disease treatment by inhibiting PS. Intrinsically disordered regions (IDRs) have been extensively studied
Yanju Wang, Yuqin Luo, Xin Li, Feifei Chen, Xingjie Zhang, Lu Yu, Runjiang Song, Baoan Song   +7 more
doaj   +1 more source

Agonist‐specific conformational dynamics at the β2‐adrenoceptor dictate allosteric modulation of Gαs signalling and bronchodilation

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose β2‐adrenoceptor (β2AR) agonists are the cornerstone of asthma therapy and promote bronchodilation through Gαs signalling in airway smooth muscle (ASM), but their efficacy is limited by β‐arrestin‐mediated β2AR desensitization.
Sushrut D. Shah, Joshua Richard, Suvankar Ghosh, Jillian Jerwick, Joice T. Gavali, Raymond B. Penn, Alexander D. MacKerell Jr, Deepak A. Deshpande   +7 more
wiley   +1 more source

The chemokine receptor‐like fourth extracellular loop of the apelin receptor differentially regulates apelin and elabela binding and signalling

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Apelin and Elabela are endogenous ligands of the apelin receptor (apelin receptor/APJ), a GPCR involved in cardiovascular regulation and body fluid homeostasis. The human receptor contains a conserved disulfide bridge linking the N‐terminal domain to extracellular loop 3 (ECL3) via Cys19 and Cys281, forming a structural ...
Chloé Bonef, Hela Bouhsine, Carine Huynh, Marion Chaigneau, Steven Dubois, Mikel Garcia‐Marcos, Catherine Llorens‐Cortes, Denis Servent, Philippe Robin, Hervé Nozach, Isabel Alves, Xavier Iturrioz   +11 more
wiley   +1 more source

Molecular cloning, characterization, and expression analysis of a gene encoding a Ran binding protein (RanBP) in Cucumis melo L. [PDF]

, 2011
Ran binding proteins (RanBPs) are highly conserved members of the GTP-binding protein family that are involved in nuclear protein export between the nucleus and the cytoplasm.
Baloglu, Mehmet Cengiz, Yücel, Ayşe Meral, Öktem, Hüseyin Avni, Zakharov, Florence Negre   +3 more
core   +1 more source

Inhibition of late sodium current prevents pathological hyperactivation of calcium/calmodulin‐dependent protein kinase IIδ in a murine model of acute doxorubicin‐related cardiotoxicity

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Doxorubicin (DOX) is a highly effective anthracycline, whose clinical application for cancer is limited by cardiotoxicity. The mechanisms underlying doxorubicin‐induced toxic cardiomyopathy (DICM) involve electrophysiological remodelling with intracellular Na+ overload because of increased late INa and hyperactivation of
Anna‐Lena Feder, Anna‐Maria Pfützenreuter, Lea Maria Funke, Maria Johanna Baier, Daniel Tarnowski, Laura Stengel, Lars Siegfried Maier, Can Martin Sag   +7 more
wiley   +1 more source

Dualsteric and dual‐acting modulation of muscarinic receptors by antagonist KH‐5

British Journal of Pharmacology, EarlyView.
Abstract Background and purpose Muscarinic acetylcholine receptors are key therapeutic targets, and ligands engaging both orthosteric and allosteric sites may offer improved selectivity and efficacy. Here, we investigated whether the muscarinic antagonist KH‐5 acts as a dualsteric antagonist and defined its mode of interaction with muscarinic receptors.
Alena Janoušková‐Randáková, Eva Dolejší, Nikolai Chetverikov, Jan Jakubík   +3 more
wiley   +1 more source

An ATM and ATR dependent checkpoint inactivates spindle assembly by targeting CEP63 [PDF]

, 2010
The effects of ATM and ATR signalling induced by chromosomal breakage have been described extensively in modulating cell cycle progression up to the onset of mitosis.
Smith, E.A.
core  

Thermodynamic characterisation of covalent ligand binding

British Journal of Pharmacology, EarlyView.
Background and Purpose Differential scanning fluorimetry (DSF) is a common and straightforward method to evaluate the thermal stability of proteins and has been heavily used for ligand binding characterisation as well as for screening. One class of compounds that is less typically evaluated by DSF are covalent binders.
Rebecca Hertzman, Maayan Lavie, Almog Nadir, Ronen Gabizon, Nir London   +4 more
wiley   +1 more source

The nuclear export receptor Xpo1p forms distinct complexes with NES transport substrates and the yeast ran binding protein 1 (Yrb1p) [PDF]

, 2001
Xpo1p (Crm1p) is the nuclear export receptor for proteins containing a leucine-rich nuclear export signal (NES). Xpo1p, the NES-containing protein, and GTP-bound Ran form a complex in the nucleus that translocates across the nuclear pore.
Stade, K., Mann, M., Schlenstedt, G., Redd, M., Maurer, P., Solsbacher, J., Bischoff, F.R., Greiner, M., Podtelejnikov, A.V., Weis, K.   +9 more
core  

MiR‐375 in CAFs‐Derived EVs Promotes HCC Progression via Regulating RASA1 and May Potentially Serve as a Biomarker for HCC

Cancer Science, EarlyView.
CAFs could transfer EVs miR‐375 into endothelial cells with a low level of RASA1 and further promote EC angiogenesis. Plasma EVs miR‐375 have the potential values as a novel diagnostic and prognostic biomarker for HCC. ABSTRACT Cancer‐associated fibroblasts (CAFs) in the tumor microenvironment play an important role in cancer initiation and progression
Wei Qin, Li Wang, Beiyuan Hu, Cuicui Xiao, XiaoYing Wu, Huan Tian, Songlin Peng   +6 more
wiley   +1 more source