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Activation of β2-adrenergetic receptor by mutation in the cholesterol binding site: molecular dynamics simulation

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Abstract

The results of molecular dynamics simulation of the mutated β2-adrenergic receptor in the hydrated lipid bilayer in the presence and in the absence of cholesterol molecules are presented. The simultaneous action of two factors, namely, the presence of cholesterol and mutation in the cholesterol binding site, induces receptor activation.

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References

  1. Y. Xiang, V. O. Rybin, S. F. Steinberg, B. Kobilka, J. Biol. Chem., 2002, 277, 34280.

    Article  CAS  Google Scholar 

  2. M. A. Hanson, V. Cherezov, M. T. Griffith, C. B. Roth, V.-P. Jaakola, E. Y. T. Chien, J. Velasquez, P. Kuhn, R. C. Stevens, Structure, 2008, 16, 897.

    Article  CAS  Google Scholar 

  3. V. Cherezov, D. M. Rosenbaum, M. A. Hanson, S. G. Rasmussen, F. S. Thian, T. S. Kobilka, H. J. Choi, P. Kuhn, W. I. Weis, B. K. Kobilka, R. C. Stevens, Science, 2007, 318, 1258.

    Article  CAS  Google Scholar 

  4. E. S. Alekseev, T. V. Bogdan, Russ. Chem. Bull. (Int. Ed.), 2013, 62, 2567 [Izv. Akad. Nauk, Ser. Khim., 2013, 2567].

    Article  CAS  Google Scholar 

  5. L. Adamian, H. Naveed, J. Liang, Biochim. Biophys. Acta, 2011, 1808, 1092.

    Article  CAS  Google Scholar 

  6. S. Jo, J. B. Lim, J. B. Klauda, W. Im, Biophys. J., 2009, 97, 50.

    Article  CAS  Google Scholar 

  7. H. J. C. Berendsen, D. Spoel, R. Drunen, Comp. Phys. Comm., 1995, 91, 43.

    Article  CAS  Google Scholar 

  8. K. Vanommeslaeghe, E. Hatcher, C. Acharya, S. Kundu, S. Zhong, J. Shim, E. Darian, O. Guvench, P. Lopes, I. Vorobyov, A. D. MacKerell, Jr., J. Comp. Chem., 2010, 31, 671.

    CAS  Google Scholar 

  9. R. O. Dror, D. H. Arlow, D. W. Borhani, M. O. Jensen, S. Piana, D. E. Shaw, Proc. Natl. Acad. Sci. USA, 2009, 106, 4689.

    Article  CAS  Google Scholar 

  10. B. A. Hall, J. P. Armitage, M. S. P. Sansom, PLoS Comp. Biol., 2012, 8, e1002685.

    Article  CAS  Google Scholar 

  11. R. O. Dror, D. H. Arlow, P. Maragakis, T. J. Mildorf, A. C. Pan, H. Xua, D. W. Borhani, D. E. Shaw, Proc. Natl. Acad. Sci. USA, 2011, 108, 18684.

    Article  CAS  Google Scholar 

  12. J. A. Ballesteros, A. D. Jensen, G. Liapakis, S. G. Rasmussen, L. Shi, U. Gether, J. A. Javitch, J. Biol. Chem., 2001, 276, 29171.

    Article  CAS  Google Scholar 

  13. S. G. F. Rasmussen, H. J. Choi, J. J. Fung, E. Pardon, P. Casarosa, P. S. Chae, B. T. DeVree, D. M. Rosenbaum, F. S. Thian, T. S. Kobilka, A. Schnapp, I. Konetzki, R. K. Sunahara, S. H. Gellman, A. Pautsch, J. Steyaert, W. I. Weis, B. K. Kobilka, Nature, 2011, 469, 175.

    Article  CAS  Google Scholar 

  14. G. Milligan, Mol. Pharmacol., 2003, 64, 1271.

    Article  CAS  Google Scholar 

  15. T. Costa, S. Cotecchia, Trends Pharmacol. Sci., 2005, 26, 618.

    Article  CAS  Google Scholar 

  16. D. M. Rosenbaum, C. Zhang, J. A. Lyons, R. Holl, D. Aragao, D. H. Arlow, S. G. F. Rasmussen, H. J. Choi, B. T. DeVree, R. K. Sunahara, P. S. Chae, S. H. Gellman, R. O. Dror, D. E. Shaw, W. I. Weis, M. Caffrey, P. Gmeiner, B. K. Kobilka, Nature, 2011, 469, 236.

    Article  CAS  Google Scholar 

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Authors and Affiliations

  1. Department of Chemistry, M. V. Lomonosov Moscow State University, Build. 3, 1 Leninskie Gory, 119991, Moscow, Russian Federation

    E. S. Alekseev & T. V. Bogdan

Authors
  1. E. S. Alekseev
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  2. T. V. Bogdan
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Correspondence to T. V. Bogdan.

Additional information

Published in Russian in Izvestiya Akademii Nauk. Seriya Khimicheskaya, No. 5, pp. 1095–1101, May, 2014.

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Alekseev, E.S., Bogdan, T.V. Activation of β2-adrenergetic receptor by mutation in the cholesterol binding site: molecular dynamics simulation. Russ Chem Bull 63, 1095–1101 (2014). https://doi.org/10.1007/s11172-014-0554-2

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  • DOI: https://doi.org/10.1007/s11172-014-0554-2

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