2006
DOI: 10.1208/aapsj080237
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Computational Methods in Drug Design: Modeling G Protein-Coupled Receptor Monomers, Dimers, and Oligomers

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Cited by 8 publications
(9 citation statements)
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References 120 publications
(129 reference statements)
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“…59 Characterization of the CXCR4 crystal structure in the presence of small antagonists also supports the hypothesis of receptor dimerization, and suggests that additional interactions between CXCR4 dimers generate higher order complexes. 60 According to structural data, dimer association is driven mostly by hydrophobic interactions between residues included in transmembrane (TM)-V and -VI, 60 in contrast to previous models of GPCR, which suggest contacts through TM-I, TM-IV, and TM-V. [61][62][63] In silico analysis on CCR5 identified Val64 in TM-I and I164 in TM-IV as key residues for dimerization and function. Mutation of these residues in CCR5 blocks dimerization and the response to CCL5 stimulus.…”
Section: Chemokine Receptor Dimerization/oligomerization: a Potentialmentioning
confidence: 97%
“…59 Characterization of the CXCR4 crystal structure in the presence of small antagonists also supports the hypothesis of receptor dimerization, and suggests that additional interactions between CXCR4 dimers generate higher order complexes. 60 According to structural data, dimer association is driven mostly by hydrophobic interactions between residues included in transmembrane (TM)-V and -VI, 60 in contrast to previous models of GPCR, which suggest contacts through TM-I, TM-IV, and TM-V. [61][62][63] In silico analysis on CCR5 identified Val64 in TM-I and I164 in TM-IV as key residues for dimerization and function. Mutation of these residues in CCR5 blocks dimerization and the response to CCL5 stimulus.…”
Section: Chemokine Receptor Dimerization/oligomerization: a Potentialmentioning
confidence: 97%
“…58 Complete details on the generation of the activated state models were published and properly described by them in the literature. 43,46,59,60 Docking Studies. Minimum energy conformers of each ligand were selected for the initial docking.…”
Section: ■ Associated Contentmentioning
confidence: 99%
“…However, cannabinoid receptors share only 20-21% sequence identity with bovine rhodopsin. Despite this, modelling has contributed a great deal to current understanding of cannabinoid ligand-receptor interactions [159][160][161][162][163][164][165], including CBII [166][167][168], and have helped explain why some ligands are selective for one receptor over another [160,166,167,169].…”
Section: The Development Of Cbii-selective Ago-nistsmentioning
confidence: 99%