Modeling β-Adrenergic Receptor Activation: the Work of Robert J. Lefkowitz
نویسندگان
چکیده
منابع مشابه
Profile of Brian K. Kobilka and Robert J. Lefkowitz, 2012 Nobel laureates in chemistry.
Those of us that had been hammering away in the field for 40 years or more cannot deny the excitement in learning that Brian Kobilka, a former postdoctoral fellow of Robert Lefkowitz, in collaboration with Roger Sunahara, had determined the structure of the agonist-bound β2-adrenergic receptor-Gs protein complex (1). To borrow a phrase from Henry Bourne, this is “the Big Enchilada” for the G pr...
متن کاملAn interview with Professor Robert J. Lefkowitz, M.D. Interview by Vicki Glaser.
Robert J. Lefkowitz, M.D., is James B. Duke Professor of Medicine and Professor of Biochemistry at the Duke University Medical Center. He has been an Investigator of the Howard Hughes Medical Institute since 1976. Dr. Lefkowitz received a Bachelor's degree from Columbia College and an M.D. degree from Columbia University College of Physicians and Surgeons. After serving an internship and one ye...
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Normal hearts have increased contractility in response to catecholamines. Because several lipids activate PKCs, we hypothesized that excess cellular lipids would inhibit cardiomyocyte responsiveness to adrenergic stimuli. Cardiomyocytes treated with saturated free fatty acids, ceramide, and diacylglycerol had reduced cellular cAMP response to isoproterenol. This was associated with increased PK...
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A third of marketed drugs act by binding to a G-protein-coupled receptor (GPCR) and either triggering or preventing receptor activation. Although recent crystal structures have provided snapshots of both active and inactive functional states of GPCRs, these structures do not reveal the mechanism by which GPCRs transition between these states. Here we propose an activation mechanism for the β(2)...
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Optogenetics has provided a revolutionary approach to dissecting biological phenomena. However, the generation and use of optically active GPCRs in these contexts is limited and it is unclear how well an opsin-chimera GPCR might mimic endogenous receptor activity. Here we show that a chimeric rhodopsin/β2 adrenergic receptor (opto-β2AR) is similar in dynamics to endogenous β2AR in terms of: cAM...
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ژورنال
عنوان ژورنال: Journal of Biological Chemistry
سال: 2007
ISSN: 0021-9258
DOI: 10.1016/s0021-9258(20)76740-2