Results 131 to 140 of about 142,607 (261)
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 +3 more
wiley +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 +4 more
wiley +1 more source
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
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
Cancer Science, EarlyView.Comparison of extracellular vesicles with parental cells through proteomic profiling, followed by an integrated bioinformatic pipeline including disease association and transcriptomic analyses, identifies candidate biomarkers for multiple myeloma. Among these, MIF emerges as a clinically relevant marker, supported by validation in patient samples and ...
Natalia Platonova +13 more
wiley +1 more source
New Treatment Strategy and Future Research Direction for BRAF‐Mutated Cancer
Cancer Science, EarlyView.Treatment with BRAF inhibitor plus MEK inhibitor is currently used in BRAF‐mutated various malignancies except colorectal cancer, and treatments with BRAF and/or MEK inhibitors and anti‐EGFR antibody are used in BRAF‐mutated colorectal cancer. Despite recent advances in BRAF‐targeted therapies, their efficacy is still limited.
Masanobu Takahashi +2 more
wiley +1 more source
Cancer Science, EarlyView.Chemically modified siR‐PTBP1 disrupts the Warburg effect by reprogramming pyruvate kinase splicing from PKM2 to PKM1. This metabolic shift activates the TCA cycle, increases ATP production, and excessive ROS generation, and ultimately induces apoptotic cell death in colorectal cancer cells.
Keita Matsumoto +19 more
wiley +1 more source
Non-canonical and constitutive activation of small GTPases: more than an exception to the rule? [PDF]
Biochem JKiers J, Hordijk PL.
europepmc +1 more source
m6A‐Mediated Stabilization of MRPS23 Drives NSCLC Progression Via HSPA8 and ERK Signaling Modulation
Cancer Science, EarlyView.MRPS23 mRNA is m6A‐methylated by WTAP and stabilized by IGF2BP3, leading to increased MRPS23 protein. MRPS23 physically interacts with HSPA8, and this interaction is functionally associated with activation of the RAS–RAF–MEK–ERK pathway, ultimately promoting NSCLC cell proliferation and tumor progression.
Sihong Le +4 more
wiley +1 more source