Analysis of the conserved Asp(114) residue of the dopamine D2 receptor in schizophrenic patient

  title={Analysis of the conserved Asp(114) residue of the dopamine D2 receptor in schizophrenic patient},
  author={S. Shaikh and Steve Hodgkinson and L. Pilowsk and Jim van Os and Homero Vallada and David A. Collier and Michael Gill},
  journal={Psychiatric Genetics},
The factors that influence response to antipsychotics treatment in chlorpromazine remain difficult to delineate but are thought to include genetic factors. Site-directed mutagenesis studies have demonstrated that substitution of the conserved residues Asp(113) to an Asn or Glu greatly reduces the binding affinity of propranolol in the β-adrenergic receptor and the substitution of an Asp(114) has similar effects in the dopamine D2 receptor. In this study we have found the Asp(114) in the… 
A QM protein–ligand investigation of antipsychotic drugs with the dopamine D2 Receptor (D2R)
It is concluded that although H-bond interactions of ligands with Asp114 are the most dominant interaction in the binding site, if van der Waals and steric interactions ofligands which have cumulative effect on the ligand binding are not included in the calculations, the interaction energies are overestimated.
Receptor pharmacogenetics: relevance to CNS syndromes.
The aim of this review is to summarize the most significant findings in pharmacogenetic research in relation to CNS drugs and to outline how these studies could lead to the individualization of drug treatment.