نتایج جستجو برای: dependent kinetics

تعداد نتایج: 772907  

Journal: :Proceedings of the National Academy of Sciences of the United States of America 2013
Andreas Rinne Alexandra Birk Moritz Bünemann

The present study demonstrates that agonist-mediated activation of α2A adrenergic receptors (α(2A)AR) is voltage-dependent. By resolving the kinetics of conformational changes of α(2A)AR at defined membrane potentials, we show that negative membrane potentials in the physiological range promote agonist-mediated activation of α(2A)AR. We discovered that the conformational change of α(2A)AR by vo...

Journal: :Annals of oncology : official journal of the European Society for Medical Oncology 2011
D Mahadevan R Plummer M S Squires D Rensvold S Kurtin C Pretzinger T Dragovich J Adams V Lock D M Smith D Von Hoff H Calvert

BACKGROUND AT7519 is an inhibitor of multiple cyclin-dependent kinases (CDKs). Based on potent antitumor activity in preclinical models, a first-in-human clinical trial in refractory solid tumors investigated its safety, tolerability, pharmacokinetics (PK) and pharmacodynamics (PD). PATIENTS AND METHODS AT7519 was administered in a '3 + 3' dose- escalation scheme on 5 consecutive days every 3...

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