Search Results - "Lefkowitz, Robert J"

A Brief History of G-Protein Coupled Receptors (Nobel Lecture) by Lefkowitz, Robert J.

“…The idea of receptors has fascinated scientists for more than a century. Today it is known that the G‐protein coupled receptors (GPCRs) represent by far the…”
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Conformational Basis of G Protein-Coupled Receptor Signaling Versatility by Wingler, Laura M., Lefkowitz, Robert J.

“…G protein-coupled receptors (GPCRs) are privileged structural scaffolds in biology that have the versatility to regulate diverse physiological processes…”
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Teaching old receptors new tricks: biasing seven-transmembrane receptors by Lefkowitz, Robert J, Rajagopal, Sudarshan, Rajagopal, Keshava

“…Key Points Seven-transmembrane receptors (7TMRs), also known as G protein-couple receptors, are the largest class of transmembrane receptors and a common…”
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Distinctive Activation Mechanism for Angiotensin Receptor Revealed by a Synthetic Nanobody by Wingler, Laura M., McMahon, Conor, Staus, Dean P., Lefkowitz, Robert J., Kruse, Andrew C.

“…The angiotensin II (AngII) type 1 receptor (AT1R) is a critical regulator of cardiovascular and renal function and is an important model for studies of…”
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Molecular mechanism of biased signaling in a prototypical G protein-coupled receptor by Suomivuori, Carl-Mikael, Latorraca, Naomi R, Wingler, Laura M, Eismann, Stephan, King, Matthew C, Kleinhenz, Alissa L W, Skiba, Meredith A, Staus, Dean P, Kruse, Andrew C, Lefkowitz, Robert J, Dror, Ron O

“…Biased signaling, in which different ligands that bind to the same G protein-coupled receptor preferentially trigger distinct signaling pathways, holds great…”
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Angiotensin and biased analogs induce structurally distinct active conformations within a GPCR by Wingler, Laura M, Skiba, Meredith A, McMahon, Conor, Staus, Dean P, Kleinhenz, Alissa L W, Suomivuori, Carl-Mikael, Latorraca, Naomi R, Dror, Ron O, Lefkowitz, Robert J, Kruse, Andrew C

“…Biased agonists of G protein-coupled receptors (GPCRs) preferentially activate a subset of downstream signaling pathways. In this work, we present crystal…”
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Loss of biased signaling at a G protein-coupled receptor in overexpressed systems by Li, Angus, Liu, Samuel, Huang, Rennica, Ahn, Seungkirl, Lefkowitz, Robert J

“…G protein-coupled receptors (GPCRs) regulate cellular signaling pathways by coupling to two classes of transducers: heterotrimeric G proteins and β-arrestins…”
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Allosteric nanobodies reveal the dynamic range and diverse mechanisms of G-protein-coupled receptor activation by Staus, Dean P., Strachan, Ryan T., Manglik, Aashish, Pani, Biswaranjan, Kahsai, Alem W., Kim, Tae Hun, Wingler, Laura M., Ahn, Seungkirl, Chatterjee, Arnab, Masoudi, Ali, Kruse, Andrew C., Pardon, Els, Steyaert, Jan, Weis, William I., Prosser, R. Scott, Kobilka, Brian K., Costa, Tommaso, Lefkowitz, Robert J.

“…Stabilization of an active and inactive conformation of the β 2 -adrenergic receptor by allosteric nanobodies reveals differential ligand-dependent regulation…”
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β-Arrestin- but Not G Protein-Mediated Signaling by the "Decoy" Receptor CXCR7 by Rajagopal, Sudarshan, Kim, Jihee, Ahn, Seungkirl, Craig, Stewart, Lam, Christopher M., Gerard, Norma P., Gerard, Craig, Lefkowitz, Robert J.

“…Ubiquitously expressed seven-transmembrane receptors (7TMRs) classically signal through heterotrimeric G proteins and are commonly referred to as G…”
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Mechanism of β2AR regulation by an intracellular positive allosteric modulator by Liu, Xiangyu, Masoudi, Ali, Kahsai, Alem W, Li-Yin, Huang, Pani Biswaranjan, Staus, Dean P, Shim, Paul J, Hirata Kunio, Simhal, Rishabh K, Schwalb, Allison M, Rambarat, Paula K, Ahn Seungkirl, Lefkowitz, Robert J, Kobilka, Brian

“…Positive reinforcement in a GPCRMany drug discovery efforts focus on G protein–coupled receptors (GPCRs), a class of receptors that regulate many physiological…”
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Visualization of arrestin recruitment by a G-protein-coupled receptor by Shukla, Arun K., Westfield, Gerwin H., Xiao, Kunhong, Reis, Rosana I., Huang, Li-Yin, Tripathi-Shukla, Prachi, Qian, Jiang, Li, Sheng, Blanc, Adi, Oleskie, Austin N., Dosey, Anne M., Su, Min, Liang, Cui-Rong, Gu, Ling-Ling, Shan, Jin-Ming, Chen, Xin, Hanna, Rachel, Choi, Minjung, Yao, Xiao Jie, Klink, Bjoern U., Kahsai, Alem W., Sidhu, Sachdev S., Koide, Shohei, Penczek, Pawel A., Kossiakoff, Anthony A., Woods Jr, Virgil L., Kobilka, Brian K., Skiniotis, Georgios, Lefkowitz, Robert J.

“…Single-particle electron microscopy and hydrogen–deuterium exchange mass spectrometry are used to characterize the structure and dynamics of a…”
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Historical review: A brief history and personal retrospective of seven-transmembrane receptors by Lefkowitz, Robert J.

“…Pharmacologists have studied receptors for more than a century but a molecular understanding of their properties has emerged only during the past 30–35 years…”
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Selective Engagement of G Protein Coupled Receptor Kinases (GRKs) Encodes Distinct Functions of Biased Ligands by Zidar, David A., Violin, Jonathan D., Whalen, Erin J., Lefkowitz, Robert J.

“…CCL19 and CCL21 are endogenous agonists for the seven-transmembrane receptor CCR7. They are equally active in promoting G protein stimulation and chemotaxis…”
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Multiple ligand-specific conformations of the β2-adrenergic receptor by Kahsai, Alem W, Xiao, Kunhong, Rajagopal, Sudarshan, Ahn, Seungkirl, Shukla, Arun K, Sun, Jinpeng, Oas, Terrence G, Lefkowitz, Robert J

“…A quantitative covalent labeling strategy reveals that multiple ligand-specific conformational states are present in the G protein–coupled β 2 -adrenergic…”
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unique mechanism of β-blocker action: Carvedilol stimulates β-arrestin signaling by Wisler, James W, DeWire, Scott M, Whalen, Erin J, Violin, Jonathan D, Drake, Matthew T, Ahn, Seungkirl, Shenoy, Sudha K, Lefkowitz, Robert J

“…For many years, β-adrenergic receptor antagonists (β-blockers or βAR antagonists) have provided significant morbidity and mortality benefits in patients who…”
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Trafficking of G Protein–Coupled Receptors by Drake, Matthew T, Shenoy, Sudha K, Lefkowitz, Robert J

“…G protein–coupled receptors (GPCRs) play an integral role in the signal transduction of an enormous array of biological phenomena, thereby serving to modulate…”
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Allosteric “beta-blocker” isolated from a DNA-encoded small molecule library by Ahn, Seungkirl, Kahsai, Alem W., Pani, Biswaranjan, Wang, Qin-Ting, Zhao, Shuai, Wall, Alissa L., Strachan, Ryan T., Staus, Dean P., Wingler, Laura M., Sun, Lillian D., Sinnaeve, Justine, Choi, Minjung, Cho, Ted, Xu, Thomas T., Hansen, Gwenn M., Burnett, Michael B., Lamerdin, Jane E., Bassoni, Daniel L., Gavino, Bryant J., Husemoen, Gitte, Olsen, Eva K., Franch, Thomas, Costanzi, Stefano, Chen, Xin, Lefkowitz, Robert J.

“…The β₂-adrenergic receptor (β₂AR) has been a model system for understanding regulatory mechanisms of G-protein–coupled receptor (GPCR) actions and plays a…”
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Allosteric modulator potentiates β2AR agonist-promoted bronchoprotection in asthma models by Ahn, Seungkirl, Maarsingh, Harm, Walker, Julia Kl, Liu, Samuel W, Hegde, Akhil, Sumajit, Hyeje C, Kahsai, Alem W, Lefkowitz, Robert J

“…Asthma is a chronic inflammatory disease associated with episodic airway narrowing. Inhaled β2-adrenergic receptor (β2AR) agonists (β2-agonists) promote…”
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A beta-arrestin-biased agonist of the parathyroid hormone receptor (PTH1R) promotes bone formation independent of G protein activation by Gesty-Palmer, Diane, Flannery, Pat, Yuan, Ling, Corsino, Leonor, Spurney, Robert, Lefkowitz, Robert J, Luttrell, Louis M

“…About 40% of the therapeutic agents in use today exert their effects through seven-transmembrane receptors (7TMRs). When activated by ligands, these receptors…”
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Functional specialization of β-arrestin interactions revealed by proteomic analysis by Xiao, Kunhong, McClatchy, Daniel B, Shukla, Arun K, Zhao, Yang, Chen, Minyong, Shenoy, Sudha K, Yates, John R. III, Lefkowitz, Robert J

“…β-arrestins are cytosolic proteins that form complexes with seven-transmembrane receptors after agonist stimulation and phosphorylation by the G…”
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