Results 201 to 210 of about 222,027 (284)

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

Prime Editing-Based Functional Characterization Supports a Likely Pathogenic Interpretation of <i>NF1</i> c.6394T>C (p.Ser2132Pro). [PDF]

Genes (Basel)
Wu J, Li G, Liu S, Ma C, Wang X.
europepmc   +1 more source

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

Cell polarity control by an unconventional G-protein complex in bacteria. [PDF]

Nat Commun
Dinet C, Sebban-Kreuzer C, Byrne-Kodjabachian D, Lhospice S, Herrou J, Durbesson F, Vincentelli R, Calvez V, Sturgis J, Michelot A, Mignot T.   +10 more
europepmc   +1 more source

Potentiation effects of the positive allosteric modulator PTC‐174 on NMDA receptors in neonatal male rat substantia nigra dopaminergic neurons

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Positive allosteric modulators bind to secondary binding sites on the receptor and alter receptor conformation and activation, changing agonist potency and efficacy. PTC‐174 is a novel NMDA receptor positive allosteric modulator that particularly enhances activity of receptors containing GluN2C or GluN2D subunits.
Bangyuan Liu, Alasdair J. Gibb
wiley   +1 more source

The ERK MAPK pathway in mesenchymal glioblastoma: tumorigenesis, microenvironmental reprogramming, and the therapeutic promise of RAS(ON) multi-selective inhibition. [PDF]

Front Mol Neurosci
Basole UM, Fitzpatric MM, Donohoe J, Obulasetti S, Snider W, Haugen E, Garcia D, Gonzalez-Manteiga A, Sertorio M, Oria M.   +9 more
europepmc   +1 more source

NMDA receptor subunit‐dependent analysis of radiprodil inhibition in neonatal male rat substantia nigra dopaminergic neurons

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Radiprodil is a GluN2B subunit selective NMDA receptor negative allosteric modulator which is currently under clinical investigation as a possible anti‐epileptic drug for paediatric use. Our goal was to investigate the inhibition of dopaminergic neuron NMDA responses by radiprodil.
Bangyuan Liu, Alasdair J. Gibb
wiley   +1 more source

GDP-Loaded K-Ras Transiently Binds to Effector B-Raf RBD, Mirroring the Structure of the Active GTP-Loaded Complex. [PDF]

J Am Chem Soc
Xiang X, Basnet M, Yuan C, Bruschweiler-Li L, Brüschweiler R.   +4 more
europepmc   +1 more source

Phase II Trial of Nivolumab in Advanced Solid Tumors Based on Genomic Profiling: BELIEVE Trial (NCCH1901) Subcohort

Cancer Science, EarlyView.
Off‐label nivolumab treatment guided by CGP results was evaluated in 56 patients with advanced solid tumors. TMB‐High was the predominant biomarker leading to nivolumab treatment. Nivolumab showed limited clinical benefit in 50 patients with measurable disease, with an ORR of 16.0%, DCR of 40.0%, median PFS of 2.7 months, and median OS of 7.2 months ...
Masashi Kanai, Kuniko Sunami, Tatsunori Shimoi, Satoshi Nishiwaki, Ichiro Kinoshita, Tetsuhiro Yoshinami, Chigusa Morizane, Yusuke Sato, Toshio Kubo, Mamoru Ito, Hiroshi Nishihara, Toru Mukohara, Hidekazu Shirota, Ryo Ko, Taro Shibata, Manabu Muto, Noboru Yamamoto   +16 more
wiley   +1 more source

Structure and dynamics of a four-protofilament microtubule from Heimdallarchaeales α/β-tubulin. [PDF]

Sci Adv
Tran LT, Ali S, Matsumoto T, Yamazaki Y, Narita A, Miyazaki M, Robinson RC.   +6 more
europepmc   +1 more source