Results 141 to 150 of about 81,932 (256)

2-(Trihydroxyphenyl)thienopyrimidinones as Key Scaffolds for Targeting a Novel Allosteric Site of HIV-1 Integrase. [PDF]

Molecules
Tocco G, Laus A, Casula M, Caboni P, Beutler JA, Tramontano E, Esposito F.   +6 more
europepmc   +1 more source

A Conserved Allosteric Site on Drug-Metabolizing CYPs: A Systematic Computational Assessment. [PDF]

Int J Mol Sci, 2021
Fischer A, Smieško M.
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

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

De novo design of protein condensation inhibitors by targeting an allosteric site of cGAS. [PDF]

Nat Commun
Zhao W, Chen G, He J, Shen X, Xiong M, Xiong L, Qi Z, Xie H, Li W, Li J, Dou H, Hu H, Su H, Shao Q, Li M, Sun H, Xu Y.   +16 more
europepmc   +1 more source

Identification of Potential Allosteric Site Binders of Indoleamine 2,3-Dioxygenase 1 from Plants: A Virtual and Molecular Dynamics Investigation. [PDF]

Pharmaceuticals (Basel), 2022
de Almeida VM, Santos-Filho OA.
europepmc   +1 more source

Soticlestat as an adjunctive therapy in children and young adults with Dravet syndrome

Epilepsia, EarlyView.
Overview of the phase 3 trial evaluating soticlestat as adjunctive therapy in children and young adults with Dravet syndrome. Abstract Objective This study evaluated the efficacy, safety, and tolerability of soticlestat as adjunctive therapy in children and young adults with Dravet syndrome (DS).
Joseph Sullivan, Kette Valente, Vicente Villanueva, Adam Strzelczyk, Rima Nabbout, Eiji Nakagawa, Yuehua Zhang, Marta Zolnowska, Yasir Khan, Cheng Dong, Samuel Hsiao, Sarah I. Sheikh, Philipp von Rosenstiel, Mahnaz Asgharnejad, Venkatesha Murthy   +14 more
wiley   +1 more source

Support Vector Machine Identification of Small Molecule Binders to an Understudied Allosteric Site of SARS-CoV-2 Mpro for Next-Generation PROTAC-Based Therapeutics. [PDF]

Arch Pharm (Weinheim)
Fassi EMA, Mekni N, Albani M, Maehrlein S, Weldert AC, Schirmeister T, Langer T, Razioso G.   +7 more
europepmc   +1 more source

Integration of In Silico Strategies for Drug Repositioning towards P38α Mitogen-Activated Protein Kinase (MAPK) at the Allosteric Site. [PDF]

Pharmaceutics, 2022
Suriya U, Mahalapbutr P, Rungrotmongkol T.   +2 more
europepmc   +1 more source

A phase 3, randomized clinical trial of soticlestat as adjunctive therapy for Lennox–Gastaut syndrome

Epilepsia, EarlyView.
Soticlestat as adjunctive therapy for Lennox–Gastaut syndrome. Abstract Objective There remains a need for new treatments for Lennox–Gastaut syndrome (LGS), a developmental and epileptic encephalopathy with a heterogenous patient population that often requires polytherapy. The phase 3, randomized SKYWAY study (NCT04938427) investigated the efficacy and
Renzo Guerrini, Eric D. Marsh, Wei‐Ping Liao, Katsumi Imai, Ruzica Kravljanac, Anna Altmann, Cecil D. Hahn, Stéphane Auvin, Jimmy Schiemann, Yasir Khan, Pranab Mitra, Sarah I. Sheikh, Philipp von Rosenstiel, Mahnaz Asgharnejad, Dennis Dlugos, Venkatesha Murthy   +15 more
wiley   +1 more source