期刊
FUTURE MEDICINAL CHEMISTRY
卷 8, 期 11, 页码 1349-1372出版社
FUTURE SCI LTD
DOI: 10.4155/fmc-2016-0010
关键词
allosteric; bitopic; bivalent; D2R; designed multiple ligands; dopamine D-2 receptor; multivalent; orthosteric
资金
- Faculty of Pharmacy and Pharmaceutical Sciences, Monash University
The dopamine D-2 receptor (D2R) has been implicated in the symptomology of disorders such as schizophrenia and Parkinson's disease. Multivalent ligands provide useful tools to investigate emerging concepts of G protein-coupled receptor drug action such as allostery, bitopic binding and receptor dimerization. This review focuses on the approaches taken toward the development of multivalent ligands for the D2R recently and highlights the challenges associated with each approach, their utility in probing D2R function and approaches to develop new D2R-targeting drugs. Furthermore, we extend our discussion to the possibility of designing multitarget ligands. The insights gained from such studies may provide the basis for improved therapeutic targeting of the D2R.
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