Results 171 to 180 of about 137,279 (309)

De Novo Design of Multivalent α/β‐Peptides Mimicking Transcription Factors Targeting the CBP KIX Domain

Chemistry – A European Journal, EarlyView.
A modular, de novo α/β‐peptide design strategy allows fine‐tuning of ligand properties, resulting in multivalent ligands that simultaneously target separate binding sites on the protein surface. ABSTRACT Protein‐protein interactions that regulate gene expression in the nucleus are increasingly recognized as potential therapeutic targets but present ...
Márk V. Tresztián, Vencel L. Petrovicz, Edit Wéber, Tamás A. Martinek, Zsófia Hegedüs   +4 more
wiley   +1 more source

Positive allosteric modulator activity of ginsenosides is restricted to P2X7 and P2X4 receptors. [PDF]

Purinergic Signal
Allum E, Stokes L.
europepmc   +1 more source

Substrate‐Selective Inhibition of the SARS‐CoV‐2 Papain‐Like Protease: Inhibition of Hydrolysis of Human Over Viral Substrates

Chemistry – A European Journal, EarlyView.
The SARS‐CoV‐2 papain‐like protease (PLpro) is a medicinal chemistry target. Here we report mass spectrometry assays employing oligopeptide substrates based on the sequences of the viral polyproteins 1a/1ab and on an ISG15‐modified human protein, which enabled the identification of substrate‐selective PLpro inhibitors.
Sakshi Sharma, Peter A. C. Wing, Wojtek Trede, Shyam Basak, Simeon D. Draganov, Taylah Andrews‐Clark, Eidarus Salah, Petra Lukacik, Claire Strain‐Damerell, Adán Pinto‐Fernández, Martin A. Walsh, Fernanda Duarte, Christopher J. Schofield, Lennart Brewitz   +13 more
wiley   +1 more source

Exploring allosteric efflux pump inhibitors and the role of bacterial membrane potential in modulating drug resistance. [PDF]

Front Microbiol
Hada APS, Meena KR, Jitendra, Singh G, Arya H, Kumar A.   +5 more
europepmc   +1 more source

A Systematic Review on Disease‐Modifying Therapies in Parkinsonian Disorders

Clinical Pharmacology &Therapeutics, EarlyView.
Parkinsonian disorders, including Parkinson's disease, Lewy body dementia, multiple system atrophy, and progressive supranuclear palsy, are progressive neurodegenerative conditions with no treatment options to slow disease progression. This systematic review provides an overview of evidence of disease‐modifying therapies that have been evaluated in ...
Pepijn P.N.M. Eijsvogel, Lars M.G. Smits, Philip H.C. Kremer, Geert Jan Groeneveld   +3 more
wiley   +1 more source

Structural basis of Fumosorinone-mediated allosteric inhibition of PTP1B for cancer immunotherapy. [PDF]

Commun Biol
Zhang J, Lin L, Gong N, Li W, Liu Y, Sundarraj R, Li Y, Dong M, Ma J, Woycechowsky K, Mei K, Ge Y, Yuchi Z, Luo D.   +13 more
europepmc   +1 more source

Transcranial Magnetic Stimulation as a Translational Biomarker in Early‐Phase Anti‐Seizure Medication Development: A Randomized, Double‐Blind, Placebo‐Controlled Study in Generalized Epilepsy

Clinical Pharmacology &Therapeutics, EarlyView.
One‐third of epilepsy patients remain treatment‐resistant, underscoring the need for novel anti‐seizure medications (ASMs) and reliable biomarkers of central target engagement. Cortical hyperexcitability is a hallmark of epilepsy, making excitability a valuable pharmacodynamic biomarker for early‐phase drug development supporting go/no‐go decision ...
Catherine M. E. de Cuba, Titia Q. Ruijs, Annika A. de Goede, Robert J. Doll, Maria Juachon, Michel J. A. M. van Putten, Geert Jan Groeneveld, Jules A. A. C. Heuberger   +7 more
wiley   +1 more source

Mapping the SHP2 Allosteric Pocket With Target-Biased Covalent Fragments. [PDF]

Chembiochem
Efrém NL, Csorba N, Amoussa M, Ábrányi-Balogh P, Guo Z, Petri L, Bo F, Di Lorenzo V, Roske Y, Szalai TV, Mihalovits L, Simon J, Li J, Daumke O, Keserű GM, Nazaré M.   +15 more
europepmc   +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

Effectiveness and safety of cenobamate after conversion to monotherapy or dual therapy in real‐world clinical practice

Epileptic Disorders, EarlyView.
Abstract Objective Patients with drug‐resistant epilepsy (DRE) typically take multiple anti‐seizure medications (ASMs) and are at risk of treatment‐related adverse events (AEs). This study assessed the impact of cenobamate monotherapy or dual therapy in patients with drug‐resistant epilepsy.
Álvaro Sánchez‐Guijo Benavente, Guillermina García Martín, Estuardo Daniel Castro Ruiz, Pablo Cabezudo García, Yolanda López Moreno, José Carlos Estévez María, Irene Lorite Fuentes, Sergio Navarro Conti, Raquel Calle Calle, Alejandro Fernández Cabrera, Isabel Ros González, Dulce Campos Blanco, María Isabel Chamorro Muñoz, Pedro Jesús Serrano Castro   +13 more
wiley   +1 more source