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Structures of rhodopsin kinase in different ligand states reveal key elements involved in G protein-coupled receptor kinase activation.

Singh P, Wang B, Maeda T, Palczewski K, Tesmer JJ
J Biol Chem 283 14053-62 (2008)
Related entries: 3c4w, 3c4y, 3c4z, 3c50, 3c51

Cited: 71 times
EuropePMC logo PMID: 18339619

Abstract

G protein-coupled receptor (GPCR) kinases (GRKs) phosphorylate activated heptahelical receptors, leading to their uncoupling from G proteins. Here we report six crystal structures of rhodopsin kinase (GRK1), revealing not only three distinct nucleotide-binding states of a GRK but also two key structural elements believed to be involved in the recognition of activated GPCRs. The first is the C-terminal extension of the kinase domain, which was observed in all nucleotide-bound GRK1 structures. The second is residues 5-30 of the N terminus, observed in one of the GRK1.(Mg2+)2.ATP structures. The N terminus was also clearly phosphorylated, leading to the identification of two novel phosphorylation sites by mass spectral analysis. Co-localization of the N terminus and the C-terminal extension near the hinge of the kinase domain suggests that activated GPCRs stimulate kinase activity by binding to this region to facilitate full closure of the kinase domain.

Reviews - 3c4x mentioned but not cited (1)

  1. Discovery of new GPCR biology: one receptor structure at a time. Hanson MA, Stevens RC. Structure 17 8-14 (2009)

Articles - 3c4x mentioned but not cited (3)

  1. Structures of rhodopsin kinase in different ligand states reveal key elements involved in G protein-coupled receptor kinase activation. Singh P, Wang B, Maeda T, Palczewski K, Tesmer JJ. J Biol Chem 283 14053-14062 (2008)
  2. Modeling Membrane Protein-Ligand Binding Interactions: The Human Purinergic Platelet Receptor. Greene D, Botello-Smith WM, Follmer A, Xiao L, Lambros E, Luo R. J Phys Chem B 120 12293-12304 (2016)
  3. Structure of a monomeric variant of rhodopsin kinase at 2.5 Å resolution. Tesmer JJ, Nance MR, Singh P, Lee H. Acta Crystallogr Sect F Struct Biol Cryst Commun 68 622-625 (2012)


Reviews citing this publication (17)

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Articles citing this publication (50)

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  20. Lecture Chemistry and biology of the initial steps in vision: the Friedenwald lecture. Palczewski K. Invest Ophthalmol Vis Sci 55 6651-6672 (2014)
  21. Conformational Selection in a Protein-Protein Interaction Revealed by Dynamic Pathway Analysis. Chakrabarti KS, Agafonov RV, Pontiggia F, Otten R, Higgins MK, Schertler GFX, Oprian DD, Kern D. Cell Rep 14 32-42 (2016)
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  28. Atomic Structure of GRK5 Reveals Distinct Structural Features Novel for G Protein-coupled Receptor Kinases. Komolov KE, Bhardwaj A, Benovic JL. J Biol Chem 290 20629-20647 (2015)
  29. G Protein-Coupled Receptor Kinase 2 (GRK2) and 5 (GRK5) Exhibit Selective Phosphorylation of the Neurotensin Receptor in Vitro. Inagaki S, Ghirlando R, Vishnivetskiy SA, Homan KT, White JF, Tesmer JJ, Gurevich VV, Grisshammer R. Biochemistry 54 4320-4329 (2015)
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  35. A highly conserved cysteine of neuronal calcium-sensing proteins controls cooperative binding of Ca2+ to recoverin. Ranaghan MJ, Kumar RP, Chakrabarti KS, Buosi V, Kern D, Oprian DD. J Biol Chem 288 36160-36167 (2013)
  36. Structural Determinants Influencing the Potency and Selectivity of Indazole-Paroxetine Hybrid G Protein-Coupled Receptor Kinase 2 Inhibitors. Bouley R, Waldschmidt HV, Cato MC, Cannavo A, Song J, Cheung JY, Yao XQ, Koch WJ, Larsen SD, Tesmer JJG. Mol Pharmacol 92 707-717 (2017)
  37. Phosphorylation of G protein-coupled receptor kinase 1 (GRK1) is regulated by light but independent of phototransduction in rod photoreceptors. Osawa S, Jo R, Xiong Y, Reidel B, Tserentsoodol N, Arshavsky VY, Iuvone PM, Weiss ER. J Biol Chem 286 20923-20929 (2011)
  38. Importance of regions outside the cytoplasmic tail of G-protein-coupled receptors for phosphorylation and dephosphorylation. Gehret AU, Hinkle PM. Biochem J 428 235-245 (2010)
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  40. The regulator of G protein signaling (RGS) domain of G protein-coupled receptor kinase 5 (GRK5) regulates plasma membrane localization and function. Xu H, Jiang X, Shen K, Fischer CC, Wedegaertner PB. Mol Biol Cell 25 2105-2115 (2014)
  41. Design and synthesis of novel 3-(benzo[d]oxazol-2-yl)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine derivatives as selective G-protein-coupled receptor kinase-2 and -5 inhibitors. Cho SY, Lee BH, Jung H, Yun CS, Ha JD, Kim HR, Chae CH, Lee JH, Seo HW, Oh KS. Bioorg Med Chem Lett 23 6711-6716 (2013)
  42. Biochemical and Cellular Specificity of Peptide Inhibitors of G Protein-Coupled Receptor Kinases. Baameur F, Hammitt RA, Friedman J, McMurray JS, Clark RB. Int J Pept Res Ther 20 1-12 (2014)
  43. The Open Question of How GPCRs Interact with GPCR Kinases (GRKs). Cato MC, Yen YC, Francis CJ, Elkins KE, Shareef A, Sterne-Marr R, Tesmer JJG. Biomolecules 11 447 (2021)
  44. The influence of two functional genetic variants of GRK5 on tau phosphorylation and their association with Alzheimer's disease risk. Zhang Y, Zhao J, Yin M, Cai Y, Liu S, Wang Y, Zhang X, Cao H, Chen T, Huang P, Mai H, Liu Z, Tao H, Zhao B, Cui L. Oncotarget 8 72714-72726 (2017)
  45. A New Paroxetine-Based GRK2 Inhibitor Reduces Internalization of the μ-Opioid Receptor. Bouley RA, Weinberg ZY, Waldschmidt HV, Yen YC, Larsen SD, Puthenveedu MA, Tesmer JJG. Mol Pharmacol 97 392-401 (2020)
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  47. Phosphorylation at Serine 21 in G protein-coupled receptor kinase 1 (GRK1) is required for normal kinetics of dark adaption in rod but not cone photoreceptors. Kolesnikov AV, Chrispell JD, Osawa S, Kefalov VJ, Weiss ER. FASEB J 34 2677-2690 (2020)
  48. Structure and Function of the Hypertension Variant A486V of G Protein-coupled Receptor Kinase 4. Allen SJ, Parthasarathy G, Darke PL, Diehl RE, Ford RE, Hall DL, Johnson SA, Reid JC, Rickert KW, Shipman JM, Soisson SM, Zuck P, Munshi SK, Lumb KJ. J Biol Chem 290 20360-20373 (2015)
  49. The rhodopsin-arrestin-1 interaction in bicelles. Chen Q, Vishnivetskiy SA, Zhuang T, Cho MK, Thaker TM, Sanders CR, Gurevich VV, Iverson TM. Methods Mol Biol 1271 77-95 (2015)
  50. Genetic analysis and clinical features of three Chinese patients with Oguchi disease. Wei X, Li H, Wu S, Zhu T, Sui R. Doc Ophthalmol 146 17-32 (2023)


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