Results 111 to 120 of about 1,519,714 (391)

New Insights into Key Determinants for Adenosine 1 Receptor Antagonists Selectivity Using Supervised Molecular Dynamics Simulations

Biomolecules, 2020
Adenosine receptors (ARs), like many otherGprotein-coupledreceptors (GPCRs), are targets of primary interest indrug design. However, one of the main limits for the development of drugs for this class of GPCRs is the complex selectivity profile usually ...
Giovanni Bolcato, Maicol Bissaro, Giuseppe Deganutti, Mattia Sturlese, Stefano Moro   +4 more
doaj   +1 more source

B cell mechanobiology in health and disease: emerging techniques and insights into therapeutic responses

FEBS Letters, EarlyView.
B cells sense external mechanical forces and convert them into biochemical signals through mechanotransduction. Understanding how malignant B cells respond to physical stimuli represents a groundbreaking area of research. This review examines the key mechano‐related molecules and pathways in B lymphocytes, highlights the most relevant techniques to ...
Marta Sampietro, Marco Cellani, Cristina Scielzo   +2 more
wiley   +1 more source

Thrombin-receptor antagonist vorapaxar in acute coronary syndromes.

New England Journal of Medicine, 2012
BACKGROUND Vorapaxar is a new oral protease-activated-receptor 1 (PAR-1) antagonist that inhibits thrombin-induced platelet activation. METHODS In this multinational, double-blind, randomized trial, we compared vorapaxar with placebo in 12,944 patients
P. Tricoci, Zhen Huang, C. Held, D. Moliterno, P. Armstrong, F. Van de Werf, H. White, P. Aylward, L. Wallentin, E. Chen, Y. Lokhnygina, J. Pei, S. Leonardi, Tyrus L. Rorick, A. Kilian, L. Jennings, G. Ambrosio, C. Bode, Á. Cequier, J. Cornel, R. Diaz, A. Erkan, K. Huber, M. Hudson, Lixin Jiang, J. Jukema, B. Lewis, A. Lincoff, G. Montalescot, J. Nicolau, H. Ogawa, M. Pfisterer, J. Prieto, W. Rużyłło, P. Sinnaeve, R. Storey, M. Valgimigli, D. Whellan, P. Widimsky, J. Strony, R. Harrington, K. Mahaffey   +41 more
semanticscholar   +1 more source

Allosteric Antagonism of the A_2A Adenosine Receptor by a Series of Bitopic Ligands

Cells, 2020
Allosteric antagonism by bitopic ligands, as reported for many receptors, is a distinct modulatory mechanism. Although several bitopic A2A adenosine receptor (A2AAR) ligand classes were reported as pharmacological tools, their receptor binding and ...
Zhan-Guo Gao, Kiran S. Toti, Ryan Campbell, R. Rama Suresh, Huijun Yang, Kenneth A. Jacobson   +5 more
doaj   +1 more source

New and developing non-adrenoreceptor small molecule drugs for the treatment of asthma [PDF]

, 2017
Introduction: Inhaled corticosteroids (ICS) alone or in combination with an inhaled long-acting beta2-agonist (LABA) are the preferred long-term treatment for adults and adolescents with symptomatic asthma.
Thomson, Neil C.
core   +1 more source

P‐glycoprotein modulates the fluidity gradient of the plasma membrane of multidrug resistant CHO cells

FEBS Letters, EarlyView.
To explore the impact of the overexpression of the multidrug‐transporter P‐glycoprotein (ABCB1) on membrane fluidity, we compared the transversal gradient of mobility and microviscosity in plasma membranes of drug‐sensitive Chinese hamster ovary cells (AuxB1) and their multidrug‐resistant derivatives (B30) using the fluorescent n‐(9‐anthroyloxy) fatty ...
Roger Busche, John R. Riordan, Burkhard Tümmler   +2 more
wiley   +1 more source

Behavioral and pharmacological characterization of a mouse model of palatable diet alternation [PDF]

, 2017
Obesity and eating disorders represent a severe problem in Western societies. Both the increased availability of highly palatable foods and dieting are major risk factors contributing to the epidemic disorders of feeding. The purpose of this study was to
Schlain, Gabrielle Star
core  

Disinhibition of hippocampal CA3 neurons induced by suppression of an adenosine A1 receptor-mediated inhibitory tonus: Pre- and postsynaptic components [PDF]

, 1993
Intracellular recordings were performed on hippocampal CA3 neuronsin vitro to investigate the inhibitory tonus generated by endogenously produced adenosine in this brain region.
Alzheimer, Alzheimer, Alzheimer, Alzheimer, Andreasen, Arai, Ault, Ault, B. Sutor, Bauer, Beavo, Beavo, Ben-Ari, Bruns, Bruns, C. Alzheimer, Chamberlin, Daly, Dragunow, Dragunow, Dunwiddie, Dunwiddie, Dunwiddie, Fredholm, G. Ten Bruggencate, Gerber, Greene, Greene, Haas, Hablitz, Hablitz, Jackisch, Johnston, Linden, Linden, Llinás, Lohse, Madison, Malenka, Meghji, Miles, Moraidis, Nicholson, Pockett, Prestwich, Prince, Scholz, Schubert, Schubert, Smellie, Smellie, Smith, Snyder, Snyder, Sutor, Tanaka, Thompson, Thompson, Van Calker, Williams, Zetterström   +60 more
core   +1 more source

Evolutionary interplay between viruses and R‐loops

FEBS Letters, EarlyView.
Viruses interact with specialized nucleic acid structures called R‐loops to influence host transcription, epigenetic states, latency, and immune evasion. This Perspective examines the roles of R‐loops in viral replication, integration, and silencing, and how viruses co‐opt or avoid these structures.
Zsolt Karányi, Zita Képes, Zoltán Szabó, Eszter Csoma, Lóránt Székvölgyi   +4 more
wiley   +1 more source

Interleukin-1-receptor antagonist in type 2 diabetes mellitus.

New England Journal of Medicine, 2007
BACKGROUND The expression of interleukin-1-receptor antagonist is reduced in pancreatic islets of patients with type 2 diabetes mellitus, and high glucose concentrations induce the production of interleukin-1beta in human pancreatic beta cells, leading ...
C. Larsen, M. Faulenbach, A. Vaag, A. Vølund, J. Ehses, B. Seifert, T. Mandrup-Poulsen, M. Donath   +7 more
semanticscholar   +2 more sources