Results 131 to 140 of about 37,458 (256)

Dissociation kinetics of G proteins from G protein-coupled receptors and effects of allosteric modulation. [PDF]

Proc Natl Acad Sci U S A
Wang J, Nguyen ATN, Adediwura VA, Lu CS, McNeill SM, Jörg M, Scammells PJ, Christopoulos A, May LT, Miao Y.   +9 more
europepmc   +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

Recent Advances in GPCR Ligand Discovery Using DNA-Encoded Library Technology: From Affinity Binding to Functional Bias and Allosteric Modulation. [PDF]

ACS Med Chem Lett
Zhou R, Wang J, Li X, An Y.
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

Allosteric Modulation of Pathological Ataxin-3 Aggregation: A Path to Spinocerebellar Ataxia Type-3 Therapies. [PDF]

Adv Sci (Weinh)
Silva A, Duarte-Silva S, Martins PM, Rodrigues B, Serrenho D, Vilasboas-Campos D, Teixeira-Castro A, Vieyto-Nuñez J, Mieres-Perez J, Figueiredo F, Podlasiak M, Van-der-Kellen T, Fraga J, Noble J, Lantz C, Sepanj N, Monteiro-Fernandes D, Guerreiro S, Neves-Carvalho A, Pereira-Sousa J, Klärner FG, Schrader T, Loo JA, Pastore A, Sanchez-Garcia E, Bitan G, Carvalho AL, Maciel P, Macedo-Ribeiro S.   +28 more
europepmc   +1 more source

Huntingtin as an Actin Organizer: Structural and Functional Insights

Cytoskeleton, EarlyView.
M. Capizzi, S. Humbert
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

Activation of a Secondary-Messenger Receptor via Allosteric Modulation of a Dynamic Conformational Ensemble. [PDF]

Angew Chem Int Ed Engl
Söldner B, Singh H, Akoury E, Witte G, Linser R.   +4 more
europepmc   +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

Enhancement of hippocampal interneuron excitability by NMDA receptor positive allosteric modulation. [PDF]

J Physiol
Xing H, Banke TG, Zhang L, Yu K, Camp CR, Fritzemeier RG, Akins NS, Paladugu S, Arcoria PJ, Brady BR, Prikhodko O, Kennedy MJ, Liotta DC, Yuan H, Traynelis SF.   +14 more
europepmc   +1 more source