Robert J. Lefkowitz

Mar 1, 2024 | jci.org | Howard A. Rockman |Robert J. Lefkowitz

G protein–coupled receptors (GPCRs) represent by far the largest, most versatile, and ubiquitous class of cellular receptors, comprising more than 800 distinct receptors. They represent the largest class of targets for therapeutic drugs, comprising almost one-third of all FDA-approved agents, amounting to some 700 different drugs. Yet when one of us (Lefkowitz) began his career, there was no concrete evidence that drug and hormone receptors actually existed as independent molecular entities.

Nov 30, 2023 | nature.com | Robert J. Lefkowitz |Howard A. Rockman |Paul J. Shim |Samuel E. Liu |Seungkirl Ahn |Sudarshan Rajagopal | +3 more

arising from T. Benkel et al. Nature Communications https://doi.org/10.1038/s41467-022-34765-w (2022)The introduction of β-adrenergic receptor blockers, “β-blockers”, as a treatment for heart failure decades ago was a major advance in cardiovascular medicine1,2,3,4. Moreover, it has been clear for a number of years that some β-blockers with “intrinsic sympathomimetic activity” (ISA) due to weak partial agonist activity mediated through G protein stimulation did not share this salutary effect5,6.