Published in J Med Chem on January 25, 2007
Pharmacological validation of Trypanosoma brucei phosphodiesterases B1 and B2 as druggable targets for African sleeping sickness. J Med Chem (2011) 1.24
The structure of the GAF A domain from phosphodiesterase 6C reveals determinants of cGMP binding, a conserved binding surface, and a large cGMP-dependent conformational change. J Biol Chem (2008) 1.15
Cross-couplings between benzylic and aryl halides "on water": synthesis of diarylmethanes. Chem Commun (Camb) (2009) 1.03
Modeling Protein-Ligand Binding by Mining Minima. J Chem Theory Comput (2010) 0.92
The multiple roles of computational chemistry in fragment-based drug design. J Comput Aided Mol Des (2009) 0.85
Structures of the PelD cyclic diguanylate effector involved in pellicle formation in Pseudomonas aeruginosa PAO1. J Biol Chem (2012) 0.85
Improving MM-GB/SA Scoring through the Application of the Variable Dielectric Model. J Chem Theory Comput (2011) 0.83
Phosphodiesterase 10A: a novel target for selective inhibition of colon tumor cell growth and β-catenin-dependent TCF transcriptional activity. Oncogene (2014) 0.81
Synthesis and in vitro evaluation of new analogues as inhibitors for phosphodiesterase 10A. Eur J Med Chem (2011) 0.79
Structure-Based Design of a Potent, Selective, and Brain Penetrating PDE2 Inhibitor with Demonstrated Target Engagement. ACS Med Chem Lett (2014) 0.79
Radiosynthesis and Radiotracer Properties of a 7-(2-[18F]Fluoroethoxy)-6-methoxypyrrolidinylquinazoline for Imaging of Phosphodiesterase 10A with PET. Pharmaceuticals (Basel) (2012) 0.77
Identification of small molecules that improve ATP synthesis defects conferred by Leber's hereditary optic neuropathy mutations. Mitochondrion (2016) 0.76
Acid-Facilitated Debenzylation of N-Boc, N-Benzyl Double Protected 2-Aminopyridinomethylpyrrolidine Derivatives. Tetrahedron (2011) 0.75
The single cyclic nucleotide-specific phosphodiesterase of the intestinal parasite Giardia lamblia represents a potential drug target. PLoS Negl Trop Dis (2017) 0.75
Glutamate receptor ion channels: structure, regulation, and function. Pharmacol Rev (2010) 11.25
Varenicline: an alpha4beta2 nicotinic receptor partial agonist for smoking cessation. J Med Chem (2005) 6.13
An innovative design to establish proof of concept of the antidepressant effects of the NR2B subunit selective N-methyl-D-aspartate antagonist, CP-101,606, in patients with treatment-refractory major depressive disorder. J Clin Psychopharmacol (2008) 3.90
The future of peptide-based drugs. Chem Biol Drug Des (2013) 3.41
Phosphodiesterases in the CNS: targets for drug development. Nat Rev Drug Discov (2006) 2.10
Phosphodiesterase 10A inhibitors: a novel approach to the treatment of the symptoms of schizophrenia. Curr Opin Investig Drugs (2007) 1.95
On-resin N-methylation of cyclic peptides for discovery of orally bioavailable scaffolds. Nat Chem Biol (2011) 1.82
Immunohistochemical localization of PDE10A in the rat brain. Brain Res (2003) 1.61
Immunohistochemical localization of phosphodiesterase 10A in multiple mammalian species. J Histochem Cytochem (2006) 1.60
Cyclic GMP signaling is involved in the luteinizing hormone-dependent meiotic maturation of mouse oocytes. Biol Reprod (2009) 1.59
Genetic deletion of the striatum-enriched phosphodiesterase PDE10A: evidence for altered striatal function. Neuropharmacology (2006) 1.53
Molecular mechanism of AMPA receptor noncompetitive antagonism. Neuron (2005) 1.51
Inhibition of the striatum-enriched phosphodiesterase PDE10A: a novel approach to the treatment of psychosis. Neuropharmacology (2006) 1.44
The impact of P-glycoprotein on the disposition of drugs targeted for indications of the central nervous system: evaluation using the MDR1A/1B knockout mouse model. Drug Metab Dispos (2004) 1.43
PDE4B polymorphisms and decreased PDE4B expression are associated with schizophrenia. Schizophr Res (2008) 1.32
Mechanism for the allosteric regulation of phosphodiesterase 2A deduced from the X-ray structure of a near full-length construct. Proc Natl Acad Sci U S A (2009) 1.30
Allosteric modulators for the treatment of schizophrenia: targeting glutamatergic networks. Curr Top Med Chem (2013) 1.28
Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. J Med Chem (2012) 1.19
A 3-month clinical trial comparing the IOP-lowering efficacy of bimatoprost and latanoprost in patients with normal-tension glaucoma. Adv Ther (2006) 1.19
A patient preference comparison of Azarga (brinzolamide/timolol fixed combination) vs Cosopt (dorzolamide/timolol fixed combination) in patients with open-angle glaucoma or ocular hypertension. Clin Ophthalmol (2008) 1.19
Glycine transporter type 1 blockade changes NMDA receptor-mediated responses and LTP in hippocampal CA1 pyramidal cells by altering extracellular glycine levels. J Physiol (2004) 1.14
Inhibition of the striatal specific phosphodiesterase PDE10A ameliorates striatal and cortical pathology in R6/2 mouse model of Huntington's disease. PLoS One (2010) 1.11
Bimatoprost 0.03% versus travoprost 0.004% in black Americans with glaucoma or ocular hypertension. Adv Ther (2003) 1.09
Inhibition of Phosphodiesterase 10A Increases the Responsiveness of Striatal Projection Neurons to Cortical Stimulation. J Pharmacol Exp Ther (2008) 1.09
Effects of a NR2B selective NMDA glutamate antagonist, CP-101,606, on dyskinesia and Parkinsonism. Mov Disord (2008) 1.08
3,5-Bicyclic aryl piperidines: a novel class of alpha4beta2 neuronal nicotinic receptor partial agonists for smoking cessation. Bioorg Med Chem Lett (2005) 1.06
Optimizing PK properties of cyclic peptides: the effect of side chain substitutions on permeability and clearance(). Medchemcomm (2012) 1.05
Development of a computational approach to predict blood-brain barrier permeability. Drug Metab Dispos (2004) 1.04
Discovery and SAR of 2-aminothiazole inhibitors of cyclin-dependent kinase 5/p25 as a potential treatment for Alzheimer's disease. Bioorg Med Chem Lett (2004) 1.03
Role of estrogen receptors in neuroprotection by estradiol against MPTP toxicity. Neuropharmacology (2007) 1.02
Discovery of cytotoxic dolastatin 10 analogues with N-terminal modifications. J Med Chem (2014) 1.01
Chronic suppression of phosphodiesterase 10A alters striatal expression of genes responsible for neurotransmitter synthesis, neurotransmission, and signaling pathways implicated in Huntington's disease. J Pharmacol Exp Ther (2010) 1.00
Blockade of cannabinoid type 1 receptors augments the antiparkinsonian action of levodopa without affecting dyskinesias in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-treated rhesus monkeys. J Pharmacol Exp Ther (2007) 0.99
Structural basis for the catalytic mechanism of human phosphodiesterase 9. Proc Natl Acad Sci U S A (2008) 0.99
Synthesis and structure based optimization of novel Akt inhibitors. Bioorg Med Chem Lett (2008) 0.97
Activation mechanism of the CO sensor CooA. Mutational and resonance Raman spectroscopic studies. J Biol Chem (2003) 0.97
Glycine transporter inhibition reverses ketamine-induced working memory deficits. Neuroreport (2010) 0.96
Cyclic nucleotide binding GAF domains from phosphodiesterases: structural and mechanistic insights. Structure (2009) 0.96
Phosphodiesterase 9A regulates central cGMP and modulates responses to cholinergic and monoaminergic perturbation in vivo. J Pharmacol Exp Ther (2012) 0.96
Immunohistochemical localization of phosphodiesterase 2A in multiple mammalian species. J Histochem Cytochem (2009) 0.93
Design of selective, ATP-competitive inhibitors of Akt. J Med Chem (2010) 0.93
Structural basis for effectiveness of siderophore-conjugated monocarbams against clinically relevant strains of Pseudomonas aeruginosa. Proc Natl Acad Sci U S A (2010) 0.92
Fmoc-based synthesis of disulfide-rich cyclic peptides. J Org Chem (2014) 0.92
Anilinoquinazoline inhibitors of fructose 1,6-bisphosphatase bind at a novel allosteric site: synthesis, in vitro characterization, and X-ray crystallography. J Med Chem (2002) 0.90
Design and discovery of a selective small molecule κ opioid antagonist (2-methyl-N-((2'-(pyrrolidin-1-ylsulfonyl)biphenyl-4-yl)methyl)propan-1-amine, PF-4455242). J Med Chem (2011) 0.89
Utilizing structures of CYP2D6 and BACE1 complexes to reduce risk of drug-drug interactions with a novel series of centrally efficacious BACE1 inhibitors. J Med Chem (2015) 0.89
Crystal structures of interleukin 17A and its complex with IL-17 receptor A. Nat Commun (2013) 0.89
Repeated estradiol treatment prevents MPTP-induced dopamine depletion in male mice. Neuroendocrinology (2003) 0.88
Phosphodiesterase 10 inhibition reduces striatal excitotoxicity in the quinolinic acid model of Huntington's disease. Neurobiol Dis (2009) 0.88
Medicinal chemistry design principles for liver targeting through OATP transporters. Curr Top Med Chem (2013) 0.88
Pramipexole inhibits MPTP toxicity in mice by dopamine D3 receptor dependent and independent mechanisms. Eur J Pharmacol (2003) 0.88
Comparative α-helicity of cyclic pentapeptides in water. Angew Chem Int Ed Engl (2014) 0.88
Improving on nature: making a cyclic heptapeptide orally bioavailable. Angew Chem Int Ed Engl (2014) 0.87
Potent and cellularly active 4-aminoimidazole inhibitors of cyclin-dependent kinase 5/p25 for the treatment of Alzheimer's disease. Bioorg Med Chem Lett (2009) 0.87
Modulation of NMDA receptor function by inhibition of D-amino acid oxidase in rodent brain. Neuropharmacology (2011) 0.87
Amelioration of ketamine-induced working memory deficits by dopamine D1 receptor agonists. Psychopharmacology (Berl) (2010) 0.87
Potent pyrimidinetrione-based inhibitors of MMP-13 with enhanced selectivity over MMP-14. Bioorg Med Chem Lett (2005) 0.86
Potent, selective pyrimidinetrione-based inhibitors of MMP-13. Bioorg Med Chem Lett (2006) 0.86
In pursuit of alpha4beta2 nicotinic receptor partial agonists for smoking cessation: carbon analogs of (-)-cytisine. Bioorg Med Chem Lett (2005) 0.86
Pyridone-conjugated monobactam antibiotics with gram-negative activity. J Med Chem (2013) 0.85
Alterations in gene regulation following inhibition of the striatum-enriched phosphodiesterase, PDE10A. Neuropharmacology (2009) 0.85
Functionalization of aromatic amino acids via direct C-H activation: generation of versatile building blocks for accessing novel peptide space. Org Lett (2010) 0.85
Discovery of small molecule isozyme non-specific inhibitors of mammalian acetyl-CoA carboxylase 1 and 2. Bioorg Med Chem Lett (2009) 0.85
3-(2-carboxyethyl)-4,6-dichloro-1H-indole-2-carboxylic acid: an allosteric inhibitor of fructose-1,6-bisphosphatase at the AMP site. Bioorg Med Chem Lett (2003) 0.84
PDE4 as a target for cognition enhancement. Expert Opin Ther Targets (2013) 0.84
Short Hydrophobic Peptides with Cyclic Constraints Are Potent Glucagon-like Peptide-1 Receptor (GLP-1R) Agonists. J Med Chem (2015) 0.84
Discovery of a novel series of 6-azauracil-based thyroid hormone receptor ligands: potent, TR beta subtype-selective thyromimetics. Bioorg Med Chem Lett (2003) 0.84
Biaryl-bridged macrocyclic peptides: conformational constraint via carbogenic fusion of natural amino acid side chains. J Org Chem (2012) 0.84
PDE inhibition and cognition enhancement. Expert Opin Ther Pat (2012) 0.84
Use of 3D properties to characterize beyond rule-of-5 property space for passive permeation. J Chem Inf Model (2012) 0.83
Identification of a brain penetrant PDE9A inhibitor utilizing prospective design and chemical enablement as a rapid lead optimization strategy. J Med Chem (2009) 0.83
Prevention of ketamine-induced working memory impairments by AMPA potentiators in a nonhuman primate model of cognitive dysfunction. Behav Brain Res (2010) 0.83