Results 181 to 190 of about 121,181 (303)

SAG1.3-derived Frizzled-targeting negative allosteric modulators

Abstract Exaggerated Wingless/Int1 (WNT)/Frizzled (FZD) signaling contributes to pathologies including fibrosis and different forms of cancers. Thus, targeting FZDs as WNT receptors for therapeutic purposes constitutes a promising intervention if the imminent risk of unwanted side effects caused by the involvement of WNT/FZD signaling in stem ...
Gunnar Schulte, Lukas Grätz, Ainoleena Turku, Pawel Kozielewicz, Carl-Fredrik Bowin, Magdalena Scharf, Jan Voss, Julia Kinsolving, Rawan Shekhani, Nuria Oliva-Vilarnau, Tobias Koolmeister, Marlies Körber, Volker Lauschke, Stefan Löber, Peter Gmeiner   +14 more
openaire   +1 more source

Considerations for drug trials in hypertrophic cardiomyopathy

ESC Heart Failure, Volume 12, Issue 2, Page 1095-1112, April 2025.
Abstract Hypertrophic cardiomyopathy (HCM) is a heterogeneous condition with potentially serious manifestations. Management has traditionally comprised therapies to palliate symptoms and implantable cardioverter‐defibrillators to prevent sudden cardiac death. The need for disease‐modifying therapies has been recognized for decades.
John P. Farrant, Matthias Schmitt, Anna B. Reid, Clifford J. Garratt, William G. Newman, Aneil Malhotra, Rhys Beynon, Masliza Mahmod, Betty Raman, Robert M. Cooper, Dana Dawson, Thomas Green, Sanjay K. Prasad, Anvesha Singh, Susanna Dodd, Hugh Watkins, Stefan Neubauer, Christopher A. Miller   +17 more
wiley   +1 more source

Effects of fenfluramine and sigma‐1‐dependent pharmacological and genetic modulation in a mouse kindling model

Epilepsia, EarlyView.
Abstract Objective Sigma‐1 is a chaperone protein that serves as a key homeostatic regulator, implicated in neuronal excitability and seizure control. Positive allosteric modulators offer a use‐dependent means to enhance Sigma‐1 activity, potentially with favorable tolerability compared to direct agonists.
Eva‐Lotta von Rüden, Verena Buchecker, Amelie Wagner, Victoria M. Stocker, Liga Zvejniece, Heidrun Potschka   +5 more
wiley   +1 more source

Effects of GABAAR modulators CL218872 and MRK-016 on neural repair and synaptic plasticity in mice with Intracerebral hemorrhage.

PLoS ONE
BackgroundIntracerebral hemorrhage (ICH) is a devastating condition characterized by rapid onset, high rates of disability and mortality, and prolonged recovery.
Tingting Chen, Hongxia He, Fei Huang, Junwu Liu, Hongli Zhou, Lei Xu   +5 more
doaj   +1 more source

Influence of the TARP γ8-Selective Negative Allosteric Modulator JNJ-55511118 on AMPA Receptor Gating and Channel Conductance. [PDF]

Mol Pharmacol, 2022
Coombs ID, Sexton CA, Cull-Candy SG, Farrant M.   +3 more
europepmc   +1 more source

Add‐on treatment with vinpocetine reduces seizure frequency and improves comorbidities in patients with loss‐of‐function γ‐aminobutyric acid type A receptor variants

Epilepsia, EarlyView.
Abstract Objective The semisynthetic compound vinpocetine has gained attention as a potential precision medicine for developmental and epileptic encephalopathies caused by loss‐of‐function (LoF) variants in γ‐aminobutyric acid type A (GABAA) receptor genes. As a positive allosteric modulator of GABAA receptors, case reports suggest that vinpocetine can
Cathrine E. Gjerulfsen, Vivian W. Y. Liao, Tomasz S. Mieszczanek, Anne V. Jakobsen, Elena Gardella, Kern Olofsson, Marina Nikanorova, Allan Bayat, Sebastian Ortiz, Sarah Weckhuysen, Cecilie Johannessen Landmark, Orrin Devinsky, Mary Chebib, Philip K. Ahring, Guido Rubboli, Rikke S. Møller   +15 more
wiley   +1 more source

Precision therapies for genetic epilepsies in 2025: Promises and pitfalls

Epilepsia Open, EarlyView.
Abstract By targeting the underlying etiology, precision therapies offer an exciting paradigm shift to improve the stagnant outcomes of drug‐resistant epilepsies, including developmental and epileptic encephalopathies. Unlike conventional antiseizure medications (ASMs) which only treat the symptoms (seizures) but have no effect on the underlying ...
Shuyu Wang, Emilio Perucca, Samuel F. Berkovic, Piero Perucca   +3 more
wiley   +1 more source

Impact of cenobamate on cortical responses to transcranial magnetic stimulation in people with drug‐resistant focal epilepsy

Epilepsia Open, EarlyView.
Abstract Objective Cenobamate (CNB) is an effective antiseizure medication, though its mechanisms of efficacy remain incompletely understood. We assessed changes in cortical responses to transcranial magnetic stimulation (TMS) following CNB treatment.
Silvano R. Gefferie, Diego Jiménez‐Jiménez, Gerhard H. Visser, Robert M. Helling, Arn M. J. M. van den Maagdenberg, Josemir W. Sander, Simona Balestrini, Roland D. Thijs   +7 more
wiley   +1 more source

Optical control of pain in vivo with a photoactive mGlu receptor negative allosteric modulator

Altres ajuts: ICREA (ICREA Academia-2010), Fundació la Marató de TV3 (Grant 20152031) and IWT (SBO-140028).Light-operated drugs constitute a major target in drug discovery, since they may provide spatiotemporal resolution for the treatment of complex ...
Bresolí-Obach, Roger, Font, Joan, López-Cano, Marc, Ciruela, Francisco, Llebaria, Amadeu, Scarselli, Pamela, Fernández-Dueñas, Víctor, Nonell, Santi, Goudet, Cyril, Catena, Juanlo, Malhaire, Fanny, Di Pietro, Paola, Battaglia, Giuseppe, Giraldo, Jesús, Pin, Jean-Philippe, Nicoletti, Ferdinando, Rovira, Xavier, Notartomaso, Serena   +17 more
core  

AKT, ATR, and Notch Inhibitors Radiosensitize a Preclinical Model of Adenoid Cystic Carcinoma

Head &Neck, EarlyView.
ABSTRACT Background Adenoid Cystic Carcinoma (ACC) is a rare and lethal type of head and neck cancer. Standard therapy involves surgery followed by radiation therapy. The majority of ACC has MYB overexpression and MYB‐NFIB gene fusions, while Notch mutations are associated with aggressive behavior.
Shivani Thoidingjam, Sushmitha Sriramulu, Asya Haider Muratoglu, Stephen Brown, Oudai Hassan, Benjamin Movsas, Haythem Ali, Steven Chang, Patrick Ha, Farzan Siddiqui, Shyam Nyati   +10 more
wiley   +1 more source