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GoPubMed Proteins lists recent and important papers and reviews for proteins. Page last changed on 19 Aug 2016.

Phosphodiesterase 10A

PDE10A, Phosphodiesterase 10A
has phosphodiesterase activity for cAMP and has cAMP inhibited activity for cGMP; activity is detected in brain striatum and testis [RGD, Feb 2006] (from NCBI)
Top mentioned proteins: Phosphodiesterase, PDE, CAN, HAD, ACID
Papers on PDE10A
Biochemical and behavioral effects of PDE10A inhibitors: Relationship to target site occupancy.
Lodge et al., Wallingford, United States. In Neuropharmacology, Mar 2016
Phosphodiesterase 10A (PDE10A) inhibitors increase the functionality of striatal medium spiny neurons and produce antipsychotic-like effects in rodents by blocking PDE10A mediated hydrolysis of cAMP and/or cGMP.
Fragment-assisted hit investigation involving integrated HTS and fragment screening: Application to the identification of phosphodiesterase 10A (PDE10A) inhibitors.
Albert et al., Wilmington, United States. In Bioorg Med Chem Lett, Feb 2016
We describe FADD and high-throughput screening (HTS) campaign strategies conducted in parallel against PDE10A where fragment hit co-crystallography was not available.
Development of highly potent phosphodiesterase 10A (PDE10A) inhibitors: Synthesis and in vitro evaluation of 1,8-dipyridinyl- and 1-pyridinyl-substituted imidazo[1,5-a]quinoxalines.
Brust et al., Leipzig, Germany. In Eur J Med Chem, Feb 2016
Herein we report the synthesis of fluorinated inhibitors of phosphodiesterase 10A (PDE10A) which can be used potentially as lead structure for the development of a (18)F-labeled PDE10A imaging agent for positron emission tomography.
Discovery of pyrazolopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
Cox et al., United States. In Bioorg Med Chem Lett, Feb 2016
Herein, we present the identification of a novel class of pyrazolopyrimidine phosphodiesterase 10A (PDE10A) inhibitors.
β-catenin nuclear translocation in colorectal cancer cells is suppressed by PDE10A inhibition, cGMP elevation, and activation of PKG.
Piazza et al., Mobile, United States. In Oncotarget, Jan 2016
UNASSIGNED: Phosphodiesterase 10A (PDE10) is a cGMP and cAMP degrading PDE isozyme that is highly expressed in the brain striatum where it appears to play an important role in cognition and psychomotor activity.
The phosphodiesterase 10A selective inhibitor TAK-063 improves cognitive functions associated with schizophrenia in rodent models.
Kimura et al., Takedamachi, Japan. In J Pharmacol Exp Ther, Jan 2016
TAK-063 [1-[2-fluoro-4-(1H-pyrazol-1-yl)phenyl]-5-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)pyridazin-4(1H)-one] is a potent and selective phosphodiesterase 10A inhibitor that produces antipsychotic-like effects in rodent models of schizophrenia.
Preclinical Characterization of the Phosphodiesterase 10A PET Tracer [(11)C]MK-8193.
Evelhoch et al., United States. In Mol Imaging Biol, Dec 2015
PURPOSE: A positron emission tomography (PET) tracer for the enzyme phosphodiesterase 10A (PDE10A) is desirable to guide the discovery and development of PDE10A inhibitors as potential therapeutics.
The effects of PDE10 inhibition on attentional set-shifting do not depend on the activation of dopamine D1 receptors.
Popik et al., Ludwigshafen am Rhein, Germany. In Behav Pharmacol, Dec 2015
UNASSIGNED: Inhibitors of phosphodiesterase 10A (PDE10A) represent a novel class of potential antipsychotic compounds.
Whole exome sequencing of microdissected splenic marginal zone lymphoma: a study to discover novel tumor-specific mutations.
Hansmann et al., Frankfurt am Main, Germany. In Bmc Cancer, 2014
Screening of 24 additional SMZL for mutations at the same positions found mutated in the WES approach revealed no recurrence of mutations for ZNF608 and PDE10A, whereas the MYD88 L265P missense mutation was identified in 15 % of cases.
Phosphodiesterase 10A inhibitors: analysis of US/EP patents granted since 2012.
García et al., In Pharm Pat Anal, 2014
The unique role of PDE10A, together with its increased pharmacological characterization, have prompted enormous interest in investigating the potential of inhibitors of this enzyme as potential novel therapeutic agents This article reviews PDE10A related patents issued in the period 2012-2014 in the USA and Europe offering also a perspective on potential avenues for the future clinical development of phosphodiesterase 10A inhibitors.
Emerging biology of PDE10A.
Brandon et al., Cambridge, United States. In Curr Pharm Des, 2014
One PDE family, PDE10A, is highly enriched in the brain and its unique expression profile in specific brain regions of interest, in particular to antipsychotic treatment, has made it an attractive therapeutic target for the treatment of schizophrenia.
Treatment of Cognitive Impairment in Schizophrenia: Potential Value of Phosphodiesterase Inhibitors in Prefrontal Dysfunction.
Prickaerts et al., Maastricht, Netherlands. In Curr Pharm Des, 2014
The field is still in its infancy, but nevertheless different PDE-Is seem promising as candidate to optimise neural communication in the prefrontal cortex favouring cognitive functioning in patients diagnosed with schizophrenia, in particular dual inhibitors including PDE1-Is, PDE3-Is and PDE10A-Is.
Phosphodiesterase 10 inhibitors: new disease modifying drugs for Parkinson's disease?
Gil et al., Almozara, Spain. In Curr Med Chem, 2014
The high level of PDE10A expression in the striatal medium spiny neurons suggests a prominent function role for the isoenzyme.
Phosphodiesterase 10A inhibitors: a 2009 - 2012 patent update.
Kehler, Denmark. In Expert Opin Ther Pat, 2013
INTRODUCTION: Inhibitors of the phosphodiesterase enzyme PDE10A have been the target for extensive investigations and huge drug discovery research efforts during the recent years.
Sequencing chromosomal abnormalities reveals neurodevelopmental loci that confer risk across diagnostic boundaries.
Gusella et al., Boston, United States. In Cell, 2012
We sequenced BCAs in patients with autism or related NDDs, revealing disruption of 33 loci in four general categories: (1) genes previously associated with abnormal neurodevelopment (e.g., AUTS2, FOXP1, and CDKL5), (2) single-gene contributors to microdeletion syndromes (MBD5, SATB2, EHMT1, and SNURF-SNRPN), (3) novel risk loci (e.g., CHD8, KIRREL3, and ZNF507), and (4) genes associated with later-onset psychiatric disorders (e.g., TCF4, ZNF804A, PDE10A, GRIN2B, and ANK3).
Discovery of orally active pyrazoloquinolines as potent PDE10 inhibitors for the management of schizophrenia.
Hodgson et al., United States. In Bioorg Med Chem Lett, 2012
analysis of orally active pyrazoloquinolines as potent PDE10 inhibitors for the management of schizophrenia in the rat model
Synthesis, in vivo occupancy, and radiolabeling of potent phosphodiesterase subtype-10 inhibitors as candidates for positron emission tomography imaging.
Bormans et al., Toledo, Spain. In J Med Chem, 2011
Data show that pyridinyl derivatives were less potent than their quinolinyl counterparts, but still exhibited significant PDE10A inhibition potency.
PDE10A and PDE10A-dependent cAMP catabolism are dysregulated oppositely in striatum and nucleus accumbens after lesion of midbrain dopamine neurons in rat: a key step in parkinsonism physiopathology.
Sancesario et al., L'Aquila, Italy. In Neurobiol Dis, 2011
Dopamine loss inversely regulates PDE10A gene expression in the striatum and PDE10A post-transcription in the nucleus accumbens, therein differentially modulating PDE10A-dependent cyclic AMP catabolism.
Phosphodiesterase10A: abundance and circadian regulation in the retina and photoreceptor of the rat.
Spessert et al., Mainz, Germany. In Brain Res, 2011
The findings presented suggest a role of PDE10A in the adaptation of cyclic nucleotide signaling to daily changes in light intensity in retinal neurons including photoreceptors
Phosphodiesterase 10A upregulation contributes to pulmonary vascular remodeling.
Pullamsetti et al., Gießen, Germany. In Plos One, 2010
The present study is the first to demonstrate a central role of PDE10A in progressive pulmonary vascular remodeling.
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