Results 51 to 60 of about 15,396 (289)

Unveiling New Triazoloquinoxaline‐Based PROTACs Designed for the Selective Degradation of the ncBAF Chromatin Remodeling Subunit BRD9

Chemistry – A European Journal, EarlyView.
We present new BRD9‐targeting degraders featuring a chemical warhead and E3 ligase ligand that distinctly differ from the typical chemical units used for BRD9 degradation. Specifically, we identified two VHL‐based PROTACs (2 and 9) based on a [1,2,4]triazolo[4,3‐a]quinoxaline scaffold that effectively and selectively degrade BRD9 and exhibit ...
Martina Pierri, Guglielmo Bove, Erica Gazzillo, Ester Colarusso, Francesca Scala, Giacomo Pepe, Stefania Terracciano, Maria Giovanna Chini, Nicla Simonelli, Ines Bruno, Angela Nebbioso, Pietro Campiglia, Giuseppe Bifulco, Lucia Altucci, Nunzio Del Gaudio, Gianluigi Lauro   +15 more
wiley   +1 more source

Aromatic Amines Exert Contrasting Effects on the Anticoagulant Effect of Acetaldehyde upon APTT

Advances in Hematology, 2014
The pharmacological effects of amphetamine, procaine, procainamide, DOPA, isoproterenol, and atenolol upon activated partial thromboplastin time in the absence and presence of acetaldehyde have been investigated.
La'Teese Hall, Sarah J. Murrey, Arthur S. Brecher   +2 more
doaj   +1 more source

New Pyridobenothiazolone Derivatives Display Nanomolar Pan‐Serotype Anti‐Dengue Virus Activity

ChemMedChem, EarlyView.
A ligand‐based strategy is employed, starting from hit compound 2, to develop the C‐2 modified pyridobenzothiazolone 19 as a pan‐serotype nanomolar DENV‐1‐4 inhibitor. Investigations of the mechanism reveal the peculiar ability to abolish the infectivity of virions in a second infection.
Tommaso Felicetti, Chin Piaw Gwee, Kitti Wing Ki Chan, Giacomo Pepe, Ciro Milite, Pietro Campiglia, Satoru Watanabe, Muhammad Danial Bin Mohd Mazlan, Stefano Sabatini, Serena Massari, Oriana Tabarrini, Gianluca Sbardella, Subhash G. Vasudevan, Giuseppe Manfroni   +13 more
wiley   +1 more source

Wolff-Parkinson-White Syndrome: Electrocardiogram

Journal of Education and Teaching in Emergency Medicine, 2016
History of present illness: A 26-year-old male with no significant past medical history presented to the emergency department with palpitations. The patient experienced these symptoms five times before in his life, but they had self-resolved with ...
Brianna Miner, Jonathan Patane, Carrie Chandwani   +2 more
doaj   +1 more source

Frequency Analysis of Atrial Fibrillation From the Surface Electrocardiogram [PDF]

, 2004
Atrial fibrillation (AF) is the most common arrhythmia encountered in clinical practice. Neither the natural history of AF nor its response to therapy are sufficiently predictable by clinical and echocardiographic parameters.
Bollmann, Andreas, Husser, Daniela, Olsson, Bertil, Sornmo, Leif, Stridh, Martin   +4 more
core  

Characterization of double potentials in human atrial flutter: Studies during transient entrainment [PDF]

, 1990
Double potentials, defined as atrial electrograms with two discrete deflections per beat separated by an isoelectric interval or a low amplitude baseline, have been observed during right atrial endocardial mapping of human atrial flutter.
Henthorn, Richard W., Okumura, Ken, Olshansky, Brian, Waldo, Albert L.   +3 more
core   +1 more source

Novel Para‐Phenylenediamine‐Based Derivatives as Receptor Tyrosine Kinase‐like Orphan Receptor 1 (ROR1) Inhibitors: An In Vitro Preliminary Characterization

ChemMedChem, EarlyView.
ROR1 represents a promising target for the development of novel antiproliferative compounds, giving its high expression in different cancer cell lines. The present study describes the workflow leading to the design, synthesis, and characterization of a series of para‐phenylenediamine‐based compounds able to interact with the target kinase, inhibiting ...
Gerardina Smaldone, Maria Rosaria Miranda, Francesca Di Matteo, Valeria Napolitano, Michela Aliberti, Simona Musella, Veronica Di Sarno, Gianluigi Lauro, Giuseppe Bifulco, Giacomo Pepe, Giovanna Aquino, Mario Felice Tecce, Isabel Maria Gomez‐Monterrey, Pietro Campiglia, Carmine Ostacolo, Alessia Bertamino, Vincenzo Vestuto, Tania Ciaglia   +17 more
wiley   +1 more source

The Pharmacology and Clinical Use of Lidocaine and Procainamide [PDF]

, 1973
Both procainamide and lidocaine are useful for acutely treating cardiac arrhythmias, and procainamide can be useful in chronic antiarrhythmic regimens.
Bigger, J. Thomas, Jr., Giardina, Elsa-Grace V.   +1 more
core   +1 more source

771-3 Direct Characterization of F1ecalnide Binding Rates from Use-Dependent Conduction Delay In Canine Purkinje Fibers [PDF]

, 1995
To quantitatively characterize flecainide-induced channel blockade from usedependent conduction delay (CD), 12 canine purkinje fibers were studied using a dual microelectrode technique. During 60 sec of pacing at interstimulus intervals (ISI) of 1.25–0.4
Cragun, Kevin T., Johnson, Susan B., Packer, Douglas L.   +2 more
core   +1 more source

Predicting OCT2/MATEs‐Mediated Drug Interactions in Healthy Volunteers and Patients with Chronic Kidney Disease: Insights from Extended Clearance Concept, Endogenous Biomarkers, and In Vitro Inhibition Studies (Perspectives from the International Transporter Consortium)

Clinical Pharmacology &Therapeutics, EarlyView.
Organic cation transporter (OCT) 2 and multidrug and toxin extrusion (MATE) transporters play significant roles in the renal secretion of organic cations and drug–drug interactions (DDIs). Recent in vitro studies indicate that the Ki values for OCT2 exhibit substrate dependency and increase in potency with pre‐incubation.
Satoshi Asano, Aleksandra Galetin, Yoshiko Tomita, Kathleen M. Giacomini, Xiaoyan Chu, Xinning Yang, Toshimichi Nakamura, Hiroyuki Kusuhara, Yuichi Sugiyama   +8 more
wiley   +1 more source