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Int J Mol Sci. 2014 Mar 14;15(3):4531-49. doi: 10.3390/ijms15034531.

Structural and molecular modeling features of P2X receptors.

Author information

  • 1Cell Communication Laboratory, Oswaldo Cruz Institute, Oswaldo Cruz Foundation (FIOCRUZ), 4365 Brazil ave, Rio de Janeiro 21045-900, Brazil. alveslaa@ioc.fiocruz.br.
  • 2Oswaldo Cruz Foundation (FIOCRUZ) Ceará Avenida Santos Dumont, 5753, Torre Saúde, Sala 1303, Papicu, Fortaleza-CE, CEP 60180-900, Brazil. jhms@fiocruz.br.
  • 3Cell Communication Laboratory, Oswaldo Cruz Institute, Oswaldo Cruz Foundation (FIOCRUZ), 4365 Brazil ave, Rio de Janeiro 21045-900, Brazil. dinarteneto@yahoo.com.br.
  • 4Cell Communication Laboratory, Oswaldo Cruz Institute, Oswaldo Cruz Foundation (FIOCRUZ), 4365 Brazil ave, Rio de Janeiro 21045-900, Brazil. fidalgo@kftox.com.
  • 5Cell Communication Laboratory, Oswaldo Cruz Institute, Oswaldo Cruz Foundation (FIOCRUZ), 4365 Brazil ave, Rio de Janeiro 21045-900, Brazil. teixeirapcn@yahoo.com.
  • 6Cell Communication Laboratory, Oswaldo Cruz Institute, Oswaldo Cruz Foundation (FIOCRUZ), 4365 Brazil ave, Rio de Janeiro 21045-900, Brazil. souzacam@ioc.fiocruz.br.
  • 7Scientific Computation Program, Oswaldo Cruz Foundation (FIOCRUZ), 4365 Brazil ave, Rio de Janeiro 21045-900, Brazil. ernesto@fiocruz.br.
  • 8Jiri Jonas Nuclear Magnetic Resonance Center, Science and Technology Institute of Structural Biology and Bioimaging, Leopoldo de Meis Medical Biochemistry Institute, Rio de Janeiro Federal University (UFRJ), Carlos Chagas Filho ave, 373, Rio de Janeiro 21941-901, Brazil. msfreitas@bioqmed.ufrj.br.

Abstract

Currently, adenosine 5'-triphosphate (ATP) is recognized as the extracellular messenger that acts through P2 receptors. P2 receptors are divided into two subtypes: P2Y metabotropic receptors and P2X ionotropic receptors, both of which are found in virtually all mammalian cell types studied. Due to the difficulty in studying membrane protein structures by X-ray crystallography or NMR techniques, there is little information about these structures available in the literature. Two structures of the P2X4 receptor in truncated form have been solved by crystallography. Molecular modeling has proven to be an excellent tool for studying ionotropic receptors. Recently, modeling studies carried out on P2X receptors have advanced our knowledge of the P2X receptor structure-function relationships. This review presents a brief history of ion channel structural studies and shows how modeling approaches can be used to address relevant questions about P2X receptors.

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