Structural and molecular modeling features of P2X receptors

• Published in: International journal of molecular sciences Vol. 15; no. 3; pp. 4531 - 4549
• Main Authors: Alves, Luiz Anastacio, da Silva, João Herminio Martins, Ferreira, Dinarte Neto Moreira, Fidalgo-Neto, Antonio Augusto, Teixeira, Pedro Celso Nogueira, de Souza, Cristina Alves Magalhães, Caffarena, Ernesto Raúl, de Freitas, Mônica Santos
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI AG 14-03-2014; Molecular Diversity Preservation International (MDPI)
• Subjects: Adenosine triphosphatase; Adenosine Triphosphate - chemistry; Adenosine Triphosphate - metabolism; Animals; Crystallography; Crystallography, X-Ray; Humans; ion channel activity; Ions; Magnetic Resonance Spectroscopy; Models, Molecular; Neurotransmitters; P2X7 receptor; patch-clamp; Protein Isoforms - chemistry; Protein Isoforms - metabolism; Protein Multimerization; Protein Structure, Tertiary; Proteins; Receptors, Purinergic P2X - chemistry; Receptors, Purinergic P2X - metabolism; Review
• ISSN: 1422-0067; 1661-6596; 1422-0067
• DOI: 10.3390/ijms15034531

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.