Published in J Med Chem on November 02, 2006
Multifunctional Nanocarriers for diagnostics, drug delivery and targeted treatment across blood-brain barrier: perspectives on tracking and neuroimaging. Part Fibre Toxicol (2010) 1.89
Hot spots in prion protein for pathogenic conversion. Proc Natl Acad Sci U S A (2007) 1.31
2-Aminothiazoles as therapeutic leads for prion diseases. J Med Chem (2011) 1.19
Quinacrine promotes replication and conformational mutation of chronic wasting disease prions. Proc Natl Acad Sci U S A (2014) 0.85
2-Aminothiazoles with improved pharmacotherapeutic properties for treatment of prion disease. ChemMedChem (2013) 0.81
Optimization of Arylamides as Novel, Potent and Brain-penetrant Antiprion Lead Compounds. ACS Med Chem Lett (2013) 0.78
Antiprion compounds that reduce PrP(Sc) levels in dividing and stationary-phase cells. Bioorg Med Chem (2013) 0.78
Prion protein-coated magnetic beads: synthesis, characterization and development of a new ligands screening method. J Chromatogr A (2014) 0.76
Quinpramine ameliorates rat experimental autoimmune neuritis and redistributes MHC class II molecules. PLoS One (2011) 0.75
QSAR study of anti-prion activity of 2-aminothiazoles. EXCLI J (2012) 0.75
Structure and function of an irreversible agonist-β(2) adrenoceptor complex. Nature (2011) 5.35
Activation and allosteric modulation of a muscarinic acetylcholine receptor. Nature (2013) 2.49
Understanding the role of DISC1 in psychiatric disease and during normal development. J Neurosci (2009) 1.89
Genes contributing to prion pathogenesis. J Gen Virol (2008) 1.51
Quinpramine is a novel compound effective in ameliorating brain autoimmune disease. Exp Neurol (2008) 1.44
Interactive SAR studies: rational discovery of super-potent and highly selective dopamine D3 receptor antagonists and partial agonists. J Med Chem (2002) 1.44
The structural evolution of dopamine D3 receptor ligands: structure-activity relationships and selected neuropharmacological aspects. Pharmacol Ther (2006) 1.33
Insolubility of disrupted-in-schizophrenia 1 disrupts oligomer-dependent interactions with nuclear distribution element 1 and is associated with sporadic mental disease. J Neurosci (2008) 1.32
C-terminal fragment of N-cadherin accelerates synapse destabilization by amyloid-β. Brain (2012) 1.20
Rapidly progressive Alzheimer disease. Arch Neurol (2011) 1.19
Disrupted-in-Schizophrenia-1 expression is regulated by beta-site amyloid precursor protein cleaving enzyme-1-neuregulin cascade. Proc Natl Acad Sci U S A (2010) 1.18
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding. J Med Chem (2009) 1.18
The X-ray crystal structure of human beta-hexosaminidase B provides new insights into Sandhoff disease. J Mol Biol (2003) 1.16
alpha-secretase mediated conversion of the amyloid precursor protein derived membrane stub C99 to C83 limits Abeta generation. J Neurochem (2009) 1.15
Tricyclic antidepressants, quinacrine and a novel, synthetic chimera thereof clear prions by destabilizing detergent-resistant membrane compartments. J Neurochem (2006) 1.13
Convergence of two independent mental disease genes on the protein level: recruitment of dysbindin to cell-invasive disrupted-in-schizophrenia 1 aggresomes. Biol Psychiatry (2011) 1.11
Recent advances in the search for D3- and D4-selective drugs: probes, models and candidates. Trends Pharmacol Sci (2011) 1.10
Oligomer assembly of the C-terminal DISC1 domain (640-854) is controlled by self-association motifs and disease-associated polymorphism S704C. Biochemistry (2009) 1.07
Human prion strain selection in transgenic mice. Ann Neurol (2010) 1.06
Rational Molecular Design and EPC Synthesis of a Type VI beta-Turn Inducing Peptide Mimetic This work was supported by the BMBF and the Fonds der Chemischen Industrie. EPC=enantiomerically pure compound. Angew Chem Int Ed Engl (2001) 1.06
Dopamine D2 and D3 receptors in human putamen, caudate nucleus, and globus pallidus. Synapse (2006) 1.05
Labeling and glycosylation of peptides using click chemistry: a general approach to (18)F-glycopeptides as effective imaging probes for positron emission tomography. Angew Chem Int Ed Engl (2010) 1.03
Presenilin-1 but not amyloid precursor protein mutations present in mouse models of Alzheimer's disease attenuate the response of cultured cells to γ-secretase modulators regardless of their potency and structure. J Neurochem (2010) 1.02
Evaluation of lactam-bridged neurotensin analogues adjusting psi(Pro10) close to the experimentally derived bioactive conformation of NT(8-13). J Med Chem (2004) 1.01
Chirospecific synthesis of spirocyclic beta-lactams and their characterization as potent type II beta-turn inducing peptide mimetics. J Org Chem (2006) 1.01
Histidine 6.55 is a major determinant of ligand-biased signaling in dopamine D2L receptor. Mol Pharmacol (2010) 0.98
Oral treatment with the d-enantiomeric peptide D3 improves the pathology and behavior of Alzheimer's Disease transgenic mice. ACS Chem Neurosci (2010) 0.98
Structure-based design of Tet repressor to optimize a new inducer specificity. Biochemistry (2004) 0.97
Argyreia nervosa (Burm. f.): receptor profiling of lysergic acid amide and other potential psychedelic LSD-like compounds by computational and binding assay approaches. J Ethnopharmacol (2013) 0.96
Fancy bioisosteres: novel paracyclophane derivatives as super-affinity dopamine D3 receptor antagonists. J Med Chem (2006) 0.96
Endothelial LRP1 transports amyloid-β1-42 across the blood-brain barrier. J Clin Invest (2015) 0.93
Functionally selective dopamine D₂, D₃ receptor partial agonists. J Med Chem (2014) 0.93
A gene regulation system with four distinct expression levels. J Gene Med (2006) 0.93
Certain 1,4-disubstituted aromatic piperidines and piperazines with extreme selectivity for the dopamine D4 receptor interact with a common receptor microdomain. Mol Pharmacol (2004) 0.92
A novel mass spectrometric assay for the cerebroside sulfate activator protein (saposin B) and arylsulfatase A. J Lipid Res (2005) 0.92
Class A G-protein-coupled receptor (GPCR) dimers and bivalent ligands. J Med Chem (2013) 0.92
Modeling the similarity and divergence of dopamine D2-like receptors and identification of validated ligand-receptor complexes. J Med Chem (2005) 0.90
Saposin A mobilizes lipids from low cholesterol and high bis(monoacylglycerol)phosphate-containing membranes: patient variant Saposin A lacks lipid extraction capacity. J Biol Chem (2006) 0.89
Proteomic, genomic and translational approaches identify CRMP1 for a role in schizophrenia and its underlying traits. Hum Mol Genet (2012) 0.89
Bivalent dopamine D2 receptor ligands: synthesis and binding properties. J Med Chem (2011) 0.89
Novel insights into GPCR-peptide interactions: mutations in extracellular loop 1, ligand backbone methylations and molecular modeling of neurotensin receptor 1. Bioorg Med Chem (2008) 0.89
Phosphatidylinositol-3,5-Bisphosphate is a potent and selective inhibitor of acid sphingomyelinase. Biol Chem (2003) 0.89
In vitro affinities of various halogenated benzamide derivatives as potential radioligands for non-invasive quantification of D(2)-like dopamine receptors. Bioorg Med Chem (2007) 0.88
CoMFA and CoMSIA investigations revealing novel insights into the binding modes of dopamine D3 receptor agonists. J Med Chem (2005) 0.88
Live imaging of prions reveals nascent PrPSc in cell-surface, raft-associated amyloid strings and webs. J Cell Biol (2014) 0.88
SCRF-DFT and NMR comparison of tetracycline and 5a,6-anhydrotetracycline in solution. J Phys Chem B (2006) 0.88
Structure-selectivity investigations of D2-like receptor ligands by CoMFA and CoMSIA guiding the discovery of D3 selective PET radioligands. J Med Chem (2007) 0.88
Muscarinic receptors as model targets and antitargets for structure-based ligand discovery. Mol Pharmacol (2013) 0.87
The expanded octarepeat domain selectively binds prions and disrupts homomeric prion protein interactions. J Biol Chem (2005) 0.87
Functionally selective dopamine D2/D3 receptor agonists comprising an enyne moiety. J Med Chem (2013) 0.87
Active-state models of ternary GPCR complexes: determinants of selective receptor-G-protein coupling. PLoS One (2013) 0.87
18F-Labeled FAUC 346 and BP 897 derivatives as subtype-selective potential PET radioligands for the dopamine D3 receptor. ChemMedChem (2008) 0.87
Dopamine D3 receptor ligands: recent advances in the control of subtype selectivity and intrinsic activity. Biochim Biophys Acta (2006) 0.87
Highly potent 5-aminotetrahydropyrazolopyridines: enantioselective dopamine D3 receptor binding, functional selectivity, and analysis of receptor-ligand interactions. J Med Chem (2011) 0.86
Cellular prion protein participates in amyloid-β transcytosis across the blood-brain barrier. J Cereb Blood Flow Metab (2012) 0.86
Vaccine approaches to prevent and treat prion infection : progress and challenges. BioDrugs (2008) 0.86
Identification of I137M and other mutations that modulate incubation periods for two human prion strains. J Virol (2012) 0.86
Pharmacological prion protein silencing accelerates central nervous system autoimmune disease via T cell receptor signalling. Brain (2010) 0.86
3,4,6-Tri-O-acetyl-2-deoxy-2-[18F]fluoroglucopyranosyl phenylthiosulfonate: a thiol-reactive agent for the chemoselective 18F-glycosylation of peptides. Bioconjug Chem (2007) 0.86
Functional characterization of a partial loss-of-function mutation of the epithelial sodium channel (ENaC) associated with atypical cystic fibrosis. Cell Physiol Biochem (2009) 0.86
PIP3EA and PD-168077, two selective dopamine D4 receptor agonists, induce penile erection in male rats: site and mechanism of action in the brain. Eur J Neurosci (2006) 0.85
Molecular dynamics simulations of the effect of the G-protein and diffusible ligands on the β2-adrenergic receptor. J Mol Biol (2011) 0.85
Similar structure-activity relationships of quinoline derivatives for antiprion and antimalarial effects. J Med Chem (2006) 0.85
Combining independent drug classes into superior, synergistically acting hybrid molecules. Angew Chem Int Ed Engl (2010) 0.84
Complementarity determining regions of an anti-prion protein scFv fragment orchestrate conformation specificity and antiprion activity. Mol Immunol (2008) 0.84
Development of a metabolically stable neurotensin receptor 2 (NTS2) ligand. ChemMedChem (2012) 0.84
Biological effects and use of PrPSc- and PrP-specific antibodies generated by immunization with purified full-length native mouse prions. J Virol (2011) 0.84
Discovery of highly potent and neurotensin receptor 2 selective neurotensin mimetics. J Med Chem (2011) 0.84
Pharmacophore-guided drug discovery investigations leading to bioactive 5-aminotetrahydropyrazolopyridines. Implications for the binding mode of heterocyclic dopamine D3 receptor agonists. J Med Chem (2005) 0.84
Peptide backbone modifications on the C-terminal hexapeptide of neurotensin. Bioorg Med Chem Lett (2008) 0.84
Expansion of the octarepeat domain alters the misfolding pathway but not the folding pathway of the prion protein. Biochemistry (2008) 0.83
Human and rat brain lipofuscin proteome. Proteomics (2012) 0.83
The use of conformation-specific ligands and assays to dissect the molecular mechanisms of neurodegenerative diseases. J Neurosci Res (2007) 0.82
Syntheses, receptor bindings, in vitro and in vivo stabilities and biodistributions of DOTA-neurotensin(8-13) derivatives containing β-amino acid residues - a lesson about the importance of animal experiments. Chem Biodivers (2013) 0.82
Fancy bioisosteres: synthesis, SAR, and pharmacological investigations of novel nonaromatic dopamine D3 receptor ligands. Bioorg Med Chem (2005) 0.82
Click chemistry on solid phase: parallel synthesis of N-benzyltriazole carboxamides as super-potent G-protein coupled receptor ligands. J Comb Chem (2006) 0.82
Click linker: efficient and high-yielding synthesis of a new family of SPOS resins by 1,3-dipolar cycloaddition. Org Lett (2003) 0.82
Synthesis and evaluation of a (18)F-labeled diarylpyrazole glycoconjugate for the imaging of NTS1-positive tumors. J Med Chem (2013) 0.82
Synthesis and radioiodination of selective ligands for the dopamine D3 receptor subtype. Bioorg Med Chem Lett (2004) 0.82
Fancy bioisosteres: metallocene-derived G-protein-coupled receptor ligands with subnanomolar binding affinity and novel selectivity profiles. J Med Chem (2005) 0.82
Dopamine D2-like receptor agonists induce penile erection in male rats: differential role of D2, D3 and D4 receptors in the paraventricular nucleus of the hypothalamus. Behav Brain Res (2011) 0.81
Subtype selective tetracycline agonists and their application for a two-stage regulatory system. Chembiochem (2006) 0.81
Bivalent molecular probes for dopamine D2-like receptors. Bioorg Med Chem (2011) 0.81
Development of a bivalent dopamine D₂ receptor agonist. J Med Chem (2011) 0.81
Cross-receptor interactions between dopamine D2L and neurotensin NTS1 receptors modulate binding affinities of dopaminergics. ACS Chem Neurosci (2011) 0.80
Biotransformation of 21-O-acetyl-deoxycorticosterone by cell suspension cultures of Digitalis lanata (strain W.1.4). Steroids (2012) 0.80
Novel D3 selective dopaminergics incorporating enyne units as nonaromatic catechol bioisosteres: synthesis, bioactivity, and mutagenesis studies. J Med Chem (2008) 0.80
Loss of prion protein leads to age-dependent behavioral abnormalities and changes in cytoskeletal protein expression. Mol Neurobiol (2014) 0.80
Codon 129 polymorphism and the E200K mutation do not affect the cellular prion protein isoform composition in the cerebrospinal fluid from patients with Creutzfeldt-Jakob disease. Eur J Neurosci (2010) 0.80