Abstract
Molecular models of the 5-hydroxytryptamine receptors are reviewed with particular emphasis upon ligand receptor interactions. The use of such models in the areas of drug design and the design and rationalisation of experiments is discussed. It is clear that many groups have modelled the 5-HT receptors using either the bacteriorhodopsin structure, rhodopsin electron density map or rhodopsin α-carbon template. Although it is difficult to assess the accuracy of these models it is expected that the rhodopsin based models show improved accuracy over the bacteriorhodopsin based models. Nevertheless models that are thoroughly validated with experimental mutagenesis and ligand binding data are useful in a qualitative sense providing ideas upon target compounds to synthesise and the design and rationalisation of mutagenesis experiments.
| Original language | English |
|---|---|
| Pages (from-to) | 317-335 |
| Number of pages | 19 |
| Journal | Receptors and Channels |
| Volume | 6 |
| Issue number | 4 |
| Publication status | Published - 27 Jul 1999 |
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Molecular modelling of the 5-hydroxytryptamine receptors. / Wishart, G.; Bremner, D. H.; Sturrock, K. R.
In: Receptors and Channels, Vol. 6, No. 4, 27.07.1999, p. 317-335.Research output: Contribution to journal › Review article
TY - JOUR
T1 - Molecular modelling of the 5-hydroxytryptamine receptors
AU - Wishart, G.
AU - Bremner, D. H.
AU - Sturrock, K. R.
PY - 1999/7/27
Y1 - 1999/7/27
N2 - Molecular models of the 5-hydroxytryptamine receptors are reviewed with particular emphasis upon ligand receptor interactions. The use of such models in the areas of drug design and the design and rationalisation of experiments is discussed. It is clear that many groups have modelled the 5-HT receptors using either the bacteriorhodopsin structure, rhodopsin electron density map or rhodopsin α-carbon template. Although it is difficult to assess the accuracy of these models it is expected that the rhodopsin based models show improved accuracy over the bacteriorhodopsin based models. Nevertheless models that are thoroughly validated with experimental mutagenesis and ligand binding data are useful in a qualitative sense providing ideas upon target compounds to synthesise and the design and rationalisation of mutagenesis experiments.
AB - Molecular models of the 5-hydroxytryptamine receptors are reviewed with particular emphasis upon ligand receptor interactions. The use of such models in the areas of drug design and the design and rationalisation of experiments is discussed. It is clear that many groups have modelled the 5-HT receptors using either the bacteriorhodopsin structure, rhodopsin electron density map or rhodopsin α-carbon template. Although it is difficult to assess the accuracy of these models it is expected that the rhodopsin based models show improved accuracy over the bacteriorhodopsin based models. Nevertheless models that are thoroughly validated with experimental mutagenesis and ligand binding data are useful in a qualitative sense providing ideas upon target compounds to synthesise and the design and rationalisation of mutagenesis experiments.
M3 - Review article
C2 - 10412724
AN - SCOPUS:0032800309
VL - 6
SP - 317
EP - 335
JO - Receptors and Channels
JF - Receptors and Channels
SN - 1060-6823
IS - 4
ER -