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Angiotensin and biased analogs induce structurally distinct active conformations within a GPCR.

Wingler LM, Skiba MA, McMahon C, Staus DP, Kleinhenz ALW, Suomivuori CM, Latorraca NR, Dror RO, Lefkowitz RJ, Kruse AC.

Science. 2020 Feb 21;367(6480):888-892. doi: 10.1126/science.aay9813.


Molecular mechanism of biased signaling in a prototypical G protein-coupled receptor.

Suomivuori CM, Latorraca NR, Wingler LM, Eismann S, King MC, Kleinhenz ALW, Skiba MA, Staus DP, Kruse AC, Lefkowitz RJ, Dror RO.

Science. 2020 Feb 21;367(6480):881-887. doi: 10.1126/science.aaz0326.


Structure of the M2 muscarinic receptor-β-arrestin complex in a lipid nanodisc.

Staus DP, Hu H, Robertson MJ, Kleinhenz ALW, Wingler LM, Capel WD, Latorraca NR, Lefkowitz RJ, Skiniotis G.

Nature. 2020 Mar;579(7798):297-302. doi: 10.1038/s41586-020-1954-0. Epub 2020 Jan 16.


Structure of an endosomal signaling GPCR-G protein-β-arrestin megacomplex.

Nguyen AH, Thomsen ARB, Cahill TJ 3rd, Huang R, Huang LY, Marcink T, Clarke OB, Heissel S, Masoudi A, Ben-Hail D, Samaan F, Dandey VP, Tan YZ, Hong C, Mahoney JP, Triest S, Little J 4th, Chen X, Sunahara R, Steyaert J, Molina H, Yu Z, des Georges A, Lefkowitz RJ.

Nat Struct Mol Biol. 2019 Dec;26(12):1123-1131. doi: 10.1038/s41594-019-0330-y. Epub 2019 Nov 18.


Detergent- and phospholipid-based reconstitution systems have differential effects on constitutive activity of G-protein-coupled receptors.

Staus DP, Wingler LM, Pichugin D, Prosser RS, Lefkowitz RJ.

J Biol Chem. 2019 Sep 6;294(36):13218-13223. doi: 10.1074/jbc.AC119.009848. Epub 2019 Jul 30.


Mechanism of β2AR regulation by an intracellular positive allosteric modulator.

Liu X, Masoudi A, Kahsai AW, Huang LY, Pani B, Staus DP, Shim PJ, Hirata K, Simhal RK, Schwalb AM, Rambarat PK, Ahn S, Lefkowitz RJ, Kobilka B.

Science. 2019 Jun 28;364(6447):1283-1287. doi: 10.1126/science.aaw8981. Epub 2019 Jun 27.


Distinctive Activation Mechanism for Angiotensin Receptor Revealed by a Synthetic Nanobody.

Wingler LM, McMahon C, Staus DP, Lefkowitz RJ, Kruse AC.

Cell. 2019 Jan 24;176(3):479-490.e12. doi: 10.1016/j.cell.2018.12.006. Epub 2019 Jan 10.


Angiotensin Analogs with Divergent Bias Stabilize Distinct Receptor Conformations.

Wingler LM, Elgeti M, Hilger D, Latorraca NR, Lerch MT, Staus DP, Dror RO, Kobilka BK, Hubbell WL, Lefkowitz RJ.

Cell. 2019 Jan 24;176(3):468-478.e11. doi: 10.1016/j.cell.2018.12.005. Epub 2019 Jan 10.


β-arrestin 1 regulates β2-adrenergic receptor-mediated skeletal muscle hypertrophy and contractility.

Kim J, Grotegut CA, Wisler JW, Li T, Mao L, Chen M, Chen W, Rosenberg PB, Rockman HA, Lefkowitz RJ.

Skelet Muscle. 2018 Dec 27;8(1):39. doi: 10.1186/s13395-018-0184-8.


Manifold roles of β-arrestins in GPCR signaling elucidated with siRNA and CRISPR/Cas9.

Luttrell LM, Wang J, Plouffe B, Smith JS, Yamani L, Kaur S, Jean-Charles PY, Gauthier C, Lee MH, Pani B, Kim J, Ahn S, Rajagopal S, Reiter E, Bouvier M, Shenoy SK, Laporte SA, Rockman HA, Lefkowitz RJ.

Sci Signal. 2018 Sep 25;11(549). pii: eaat7650. doi: 10.1126/scisignal.aat7650.


G protein-coupled receptor kinases (GRKs) orchestrate biased agonism at the β2-adrenergic receptor.

Choi M, Staus DP, Wingler LM, Ahn S, Pani B, Capel WD, Lefkowitz RJ.

Sci Signal. 2018 Aug 21;11(544). pii: eaar7084. doi: 10.1126/scisignal.aar7084.


GPCR signaling: conformational activation of arrestins.

Kahsai AW, Pani B, Lefkowitz RJ.

Cell Res. 2018 Aug;28(8):783-784. doi: 10.1038/s41422-018-0067-x. No abstract available.


Biased G Protein-Coupled Receptor Signaling: Changing the Paradigm of Drug Discovery.

Wisler JW, Rockman HA, Lefkowitz RJ.

Circulation. 2018 May 29;137(22):2315-2317. doi: 10.1161/CIRCULATIONAHA.117.028194. Review. No abstract available.


Small-Molecule Positive Allosteric Modulators of the β2-Adrenoceptor Isolated from DNA-Encoded Libraries.

Ahn S, Pani B, Kahsai AW, Olsen EK, Husemoen G, Vestergaard M, Jin L, Zhao S, Wingler LM, Rambarat PK, Simhal RK, Xu TT, Sun LD, Shim PJ, Staus DP, Huang LY, Franch T, Chen X, Lefkowitz RJ.

Mol Pharmacol. 2018 Aug;94(2):850-861. doi: 10.1124/mol.118.111948. Epub 2018 May 16.


Sortase ligation enables homogeneous GPCR phosphorylation to reveal diversity in β-arrestin coupling.

Staus DP, Wingler LM, Choi M, Pani B, Manglik A, Kruse AC, Lefkowitz RJ.

Proc Natl Acad Sci U S A. 2018 Apr 10;115(15):3834-3839. doi: 10.1073/pnas.1722336115. Epub 2018 Mar 26.


Biased signalling: from simple switches to allosteric microprocessors.

Smith JS, Lefkowitz RJ, Rajagopal S.

Nat Rev Drug Discov. 2018 Apr;17(4):243-260. doi: 10.1038/nrd.2017.229. Epub 2018 Jan 5. Review.


β-Arrestin2 mediates progression of murine primary myelofibrosis.

Rein LA, Wisler JW, Kim J, Theriot B, Huang L, Price T, Yang H, Chen M, Chen W, Sipkins D, Fedoriw Y, Walker JK, Premont RT, Lefkowitz RJ.

JCI Insight. 2017 Dec 21;2(24). pii: 98094. doi: 10.1172/jci.insight.98094.


Mechanism of intracellular allosteric β2AR antagonist revealed by X-ray crystal structure.

Liu X, Ahn S, Kahsai AW, Meng KC, Latorraca NR, Pani B, Venkatakrishnan AJ, Masoudi A, Weis WI, Dror RO, Chen X, Lefkowitz RJ, Kobilka BK.

Nature. 2017 Aug 24;548(7668):480-484. doi: 10.1038/nature23652. Epub 2017 Aug 16.


A Serendipitous Scientist.

Lefkowitz RJ.

Annu Rev Pharmacol Toxicol. 2018 Jan 6;58:17-32. doi: 10.1146/annurev-pharmtox-010617-053149. Epub 2017 Jul 17.


β-Arrestin2 Couples Metabotropic Glutamate Receptor 5 to Neuronal Protein Synthesis and Is a Potential Target to Treat Fragile X.

Stoppel LJ, Auerbach BD, Senter RK, Preza AR, Lefkowitz RJ, Bear MF.

Cell Rep. 2017 Mar 21;18(12):2807-2814. doi: 10.1016/j.celrep.2017.02.075.


Distinct conformations of GPCR-β-arrestin complexes mediate desensitization, signaling, and endocytosis.

Cahill TJ 3rd, Thomsen AR, Tarrasch JT, Plouffe B, Nguyen AH, Yang F, Huang LY, Kahsai AW, Bassoni DL, Gavino BJ, Lamerdin JE, Triest S, Shukla AK, Berger B, Little J 4th, Antar A, Blanc A, Qu CX, Chen X, Kawakami K, Inoue A, Aoki J, Steyaert J, Sun JP, Bouvier M, Skiniotis G, Lefkowitz RJ.

Proc Natl Acad Sci U S A. 2017 Mar 7;114(10):2562-2567. doi: 10.1073/pnas.1701529114. Epub 2017 Feb 21.


Allosteric "beta-blocker" isolated from a DNA-encoded small molecule library.

Ahn S, Kahsai AW, Pani B, Wang QT, Zhao S, Wall AL, Strachan RT, Staus DP, Wingler LM, Sun LD, Sinnaeve J, Choi M, Cho T, Xu TT, Hansen GM, Burnett MB, Lamerdin JE, Bassoni DL, Gavino BJ, Husemoen G, Olsen EK, Franch T, Costanzi S, Chen X, Lefkowitz RJ.

Proc Natl Acad Sci U S A. 2017 Feb 14;114(7):1708-1713. doi: 10.1073/pnas.1620645114. Epub 2017 Jan 27.


GPCR-G Protein-β-Arrestin Super-Complex Mediates Sustained G Protein Signaling.

Thomsen ARB, Plouffe B, Cahill TJ 3rd, Shukla AK, Tarrasch JT, Dosey AM, Kahsai AW, Strachan RT, Pani B, Mahoney JP, Huang L, Breton B, Heydenreich FM, Sunahara RK, Skiniotis G, Bouvier M, Lefkowitz RJ.

Cell. 2016 Aug 11;166(4):907-919. doi: 10.1016/j.cell.2016.07.004. Epub 2016 Aug 4.


Allosteric nanobodies reveal the dynamic range and diverse mechanisms of G-protein-coupled receptor activation.

Staus DP, Strachan RT, Manglik A, Pani B, Kahsai AW, Kim TH, Wingler LM, Ahn S, Chatterjee A, Masoudi A, Kruse AC, Pardon E, Steyaert J, Weis WI, Prosser RS, Kobilka BK, Costa T, Lefkowitz RJ.

Nature. 2016 Jul 21;535(7612):448-52. Epub 2016 Jul 13.


Conformationally selective RNA aptamers allosterically modulate the β2-adrenoceptor.

Kahsai AW, Wisler JW, Lee J, Ahn S, Cahill Iii TJ, Dennison SM, Staus DP, Thomsen AR, Anasti KM, Pani B, Wingler LM, Desai H, Bompiani KM, Strachan RT, Qin X, Alam SM, Sullenger BA, Lefkowitz RJ.

Nat Chem Biol. 2016 Sep;12(9):709-16. doi: 10.1038/nchembio.2126. Epub 2016 Jul 11.


Alfred Goodman Gilman (1941-2015).

Lefkowitz RJ.

Nature. 2016 Jan 21;529(7586):284. doi: 10.1038/529284a. No abstract available.


The role of β-arrestin2-dependent signaling in thoracic aortic aneurysm formation in a murine model of Marfan syndrome.

Wisler JW, Harris EM, Raisch M, Mao L, Kim J, Rockman HA, Lefkowitz RJ.

Am J Physiol Heart Circ Physiol. 2015 Nov;309(9):H1516-27. doi: 10.1152/ajpheart.00291.2015. Epub 2015 Sep 14.


Inspiring the next generation of physician-scientists.

Lefkowitz RJ.

J Clin Invest. 2015 Aug 3;125(8):2905-7. doi: 10.1172/JCI83222. Epub 2015 Aug 3.


Allosteric modulation of β-arrestin-biased angiotensin II type 1 receptor signaling by membrane stretch.

Tang W, Strachan RT, Lefkowitz RJ, Rockman HA.

J Biol Chem. 2014 Oct 10;289(41):28271-83. doi: 10.1074/jbc.M114.585067. Epub 2014 Aug 28.


Visualization of arrestin recruitment by a G-protein-coupled receptor.

Shukla AK, Westfield GH, Xiao K, Reis RI, Huang LY, Tripathi-Shukla P, Qian J, Li S, Blanc A, Oleskie AN, Dosey AM, Su M, Liang CR, Gu LL, Shan JM, Chen X, Hanna R, Choi M, Yao XJ, Klink BU, Kahsai AW, Sidhu SS, Koide S, Penczek PA, Kossiakoff AA, Woods VL Jr, Kobilka BK, Skiniotis G, Lefkowitz RJ.

Nature. 2014 Aug 14;512(7513):218-222. doi: 10.1038/nature13430. Epub 2014 Jun 22.


Recent developments in biased agonism.

Wisler JW, Xiao K, Thomsen AR, Lefkowitz RJ.

Curr Opin Cell Biol. 2014 Apr;27:18-24. doi: 10.1016/ Epub 2013 Nov 20. Review.


Divergent transducer-specific molecular efficacies generate biased agonism at a G protein-coupled receptor (GPCR).

Strachan RT, Sun JP, Rominger DH, Violin JD, Ahn S, Rojas Bie Thomsen A, Zhu X, Kleist A, Costa T, Lefkowitz RJ.

J Biol Chem. 2014 May 16;289(20):14211-24. doi: 10.1074/jbc.M114.548131. Epub 2014 Mar 25.


Discovery of β2 Adrenergic Receptor Ligands Using Biosensor Fragment Screening of Tagged Wild-Type Receptor.

Aristotelous T, Ahn S, Shukla AK, Gawron S, Sassano MF, Kahsai AW, Wingler LM, Zhu X, Tripathi-Shukla P, Huang XP, Riley J, Besnard J, Read KD, Roth BL, Gilbert IH, Hopkins AL, Lefkowitz RJ, Navratilova I.

ACS Med Chem Lett. 2013 Oct 10;4(10):1005-1010. Epub 2013 Sep 3.


Regulation of β2-adrenergic receptor function by conformationally selective single-domain intrabodies.

Staus DP, Wingler LM, Strachan RT, Rasmussen SG, Pardon E, Ahn S, Steyaert J, Kobilka BK, Lefkowitz RJ.

Mol Pharmacol. 2014 Mar;85(3):472-81. doi: 10.1124/mol.113.089516. Epub 2013 Dec 6.


β-Arrestin regulation of myosin light chain phosphorylation promotes AT1aR-mediated cell contraction and migration.

Simard E, Kovacs JJ, Miller WE, Kim J, Grandbois M, Lefkowitz RJ.

PLoS One. 2013 Nov 8;8(11):e80532. doi: 10.1371/journal.pone.0080532. eCollection 2013.


Arrestins come of age: a personal historical perspective.

Lefkowitz RJ.

Prog Mol Biol Transl Sci. 2013;118:3-18. doi: 10.1016/B978-0-12-394440-5.00001-2. Review.


A brief history of G-protein coupled receptors (Nobel Lecture).

Lefkowitz RJ.

Angew Chem Int Ed Engl. 2013 Jun 17;52(25):6366-78. doi: 10.1002/anie.201301924. Epub 2013 May 6. No abstract available.


Structure of active β-arrestin-1 bound to a G-protein-coupled receptor phosphopeptide.

Shukla AK, Manglik A, Kruse AC, Xiao K, Reis RI, Tseng WC, Staus DP, Hilger D, Uysal S, Huang LY, Paduch M, Tripathi-Shukla P, Koide A, Koide S, Weis WI, Kossiakoff AA, Kobilka BK, Lefkowitz RJ.

Nature. 2013 May 2;497(7447):137-41. doi: 10.1038/nature12120. Epub 2013 Apr 21.


Conformation guides molecular efficacy in docking screens of activated β-2 adrenergic G protein coupled receptor.

Weiss DR, Ahn S, Sassano MF, Kleist A, Zhu X, Strachan R, Roth BL, Lefkowitz RJ, Shoichet BK.

ACS Chem Biol. 2013 May 17;8(5):1018-26. doi: 10.1021/cb400103f. Epub 2013 Mar 21.


Pharmacological blockade of a β(2)AR-β-arrestin-1 signaling cascade prevents the accumulation of DNA damage in a behavioral stress model.

Hara MR, Sachs BD, Caron MG, Lefkowitz RJ.

Cell Cycle. 2013 Jan 15;12(2):219-24. doi: 10.4161/cc.23368. Epub 2012 Jan 15.


β-Arrestin2 mediates the initiation and progression of myeloid leukemia.

Fereshteh M, Ito T, Kovacs JJ, Zhao C, Kwon HY, Tornini V, Konuma T, Chen M, Lefkowitz RJ, Reya T.

Proc Natl Acad Sci U S A. 2012 Jul 31;109(31):12532-7. doi: 10.1073/pnas.1209815109. Epub 2012 Jul 5.


Competing G protein-coupled receptor kinases balance G protein and β-arrestin signaling.

Heitzler D, Durand G, Gallay N, Rizk A, Ahn S, Kim J, Violin JD, Dupuy L, Gauthier C, Piketty V, Crépieux P, Poupon A, Clément F, Fages F, Lefkowitz RJ, Reiter E.

Mol Syst Biol. 2012 Jun 26;8:590. doi: 10.1038/msb.2012.22.


An interview with Robert J. Lefkowitz.

Lefkowitz RJ.

Trends Pharmacol Sci. 2012 Feb;33(2):51-2. No abstract available.


A tale of two callings.

Lefkowitz RJ.

J Clin Invest. 2011 Oct;121(10):4201-3. doi: 10.1172/JCI60817. Epub 2011 Oct 3. No abstract available.


Molecular mechanism of β-arrestin-biased agonism at seven-transmembrane receptors.

Reiter E, Ahn S, Shukla AK, Lefkowitz RJ.

Annu Rev Pharmacol Toxicol. 2012;52:179-97. doi: 10.1146/annurev.pharmtox.010909.105800. Epub 2011 Sep 19. Review.


Distinct phosphorylation sites on the β(2)-adrenergic receptor establish a barcode that encodes differential functions of β-arrestin.

Nobles KN, Xiao K, Ahn S, Shukla AK, Lam CM, Rajagopal S, Strachan RT, Huang TY, Bressler EA, Hara MR, Shenoy SK, Gygi SP, Lefkowitz RJ.

Sci Signal. 2011 Aug 9;4(185):ra51. doi: 10.1126/scisignal.2001707.


A stress response pathway regulates DNA damage through β2-adrenoreceptors and β-arrestin-1.

Hara MR, Kovacs JJ, Whalen EJ, Rajagopal S, Strachan RT, Grant W, Towers AJ, Williams B, Lam CM, Xiao K, Shenoy SK, Gregory SG, Ahn S, Duckett DR, Lefkowitz RJ.

Nature. 2011 Aug 21;477(7364):349-53. doi: 10.1038/nature10368.


Multiple ligand-specific conformations of the β2-adrenergic receptor.

Kahsai AW, Xiao K, Rajagopal S, Ahn S, Shukla AK, Sun J, Oas TG, Lefkowitz RJ.

Nat Chem Biol. 2011 Aug 21;7(10):692-700. doi: 10.1038/nchembio.634.


Emerging paradigms of β-arrestin-dependent seven transmembrane receptor signaling.

Shukla AK, Xiao K, Lefkowitz RJ.

Trends Biochem Sci. 2011 Sep;36(9):457-69. doi: 10.1016/j.tibs.2011.06.003. Epub 2011 Jul 20. Review.


Introduction to the series on novel aspects of cardiovascular G-protein-coupled receptor signaling.

Rockman HA, Lefkowitz RJ.

Circ Res. 2011 Jul 8;109(2):202-4. doi: 10.1161/CIRCRESAHA.110.231126. No abstract available.

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