Current drug treatments targeting dopamine D3 receptor

GM Leggio, C Bucolo, CBM Platania… - Pharmacology & …, 2016 - Elsevier
Dopamine receptors (DR) have been extensively studied, but only in recent years they
became object of investigation to elucidate the specific role of different subtypes (D1R, D2R …

Computational modeling approaches to structure− function analysis of G protein-coupled receptors

F Fanelli, PG De Benedetti - Chemical reviews, 2005 - ACS Publications
Any aspect of cell activity is regulated by extracellular signals that are recognized, decoded,
and transduced inside the cell via different classes of plasma membrane receptors. 1-3 G …

Targeted rescue of a destabilized mutant of p53 by an in silico screened drug

FM Boeckler, AC Joerger, G Jaggi… - Proceedings of the …, 2008 - National Acad Sciences
The tumor suppressor p53 is mutationally inactivated in≈ 50% of human cancers.
Approximately one-third of the mutations lower the melting temperature of the protein …

Discovery and Characterization of a G Protein–Biased Agonist That Inhibits β-Arrestin Recruitment to the D2 Dopamine Receptor

RB Free, LS Chun, AE Moritz, BN Miller, TB Doyle… - Molecular …, 2014 - ASPET
A high-throughput screening campaign was conducted to interrogate a 380,000+ small-
molecule library for novel D2 dopamine receptor modulators using a calcium mobilization …

Homology modeling and docking evaluation of aminergic G protein-coupled receptors

FM McRobb, B Capuano, IT Crosby… - Journal of chemical …, 2010 - ACS Publications
We report the development of homology models of dopamine (D2, D3, and D4), serotonin (5-
HT1B, 5-HT2A, 5-HT2B, and 5-HT2C), histamine (H1), and muscarinic (M1) receptors …

Dopamine D2, D3, and D4 Selective Phenylpiperazines as Molecular Probes To Explore the Origins of Subtype Specific Receptor Binding

K Ehrlich, A Gotz, S Bollinger… - Journal of medicinal …, 2009 - ACS Publications
Assembling phenylpiperazines with 7a-azaindole via different spacer elements, we
developed subtype selective dopamine receptor ligands of types 1a, c, 2a, and 3a …

[PDF][PDF] Update 1 of: computational modeling approaches to structure–function analysis of G protein-coupled receptors

F Fanelli, PG De Benedetti - Chemical Reviews-Columbus, 2011 - researchgate.net
Any aspect of cell activity is regulated by extracellular signals that are recognized, decoded,
and transduced inside the cell via different classes of plasma membrane receptors. 1À3 G …

The structural evolution of dopamine D3 receptor ligands: structure–activity relationships and selected neuropharmacological aspects

F Boeckler, P Gmeiner - Pharmacology & therapeutics, 2006 - Elsevier
“Evolution consists largely of molecular tinkering.”—Following the famous concept of the
molecular geneticist and medicine Nobel laureate François Jacob, in this review we …

Homology modeling of G-protein-coupled receptors and implications in drug design

A Patny, PV Desai, MA Avery - Current medicinal chemistry, 2006 - ingentaconnect.com
G-protein-coupled receptors (GPCRs) are considered therapeutically important due to their
involvement in a variety of processes governing several cellular functions, and their …

Structural basis for Na+-sensitivity in dopamine D2 and D3 receptors

M Michino, RB Free, TB Doyle, DR Sibley… - Chemical …, 2015 - pubs.rsc.org
To understand the structural basis for the Na+-sensitivity of ligand binding to dopamine D2-
like receptors, using computational analysis in combination with binding assays, we …