Search Results - "HARMS, John F"
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Facilitation of corticostriatal transmission following pharmacological inhibition of striatal phosphodiesterase 10A: role of nitric oxide-soluble guanylyl cyclase-cGMP signaling pathways
Published in The Journal of neuroscience (08-04-2015)“…The striatum contains a rich variety of cyclic nucleotide phosphodiesterases (PDEs), which play a critical role in the regulation of cAMP and cGMP signaling…”
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Inhibition of the striatum-enriched phosphodiesterase PDE10A: A novel approach to the treatment of psychosis
Published in Neuropharmacology (01-08-2006)“…Phosphodiesterase 10A (PDE10A) is a recently identified cyclic nucleotide phosphodiesterase expressed primarily in dopaminoreceptive medium spiny neurons of…”
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Chronic suppression of phosphodiesterase 10A alters striatal expression of genes responsible for neurotransmitter synthesis, neurotransmission, and signaling pathways implicated in Huntington's disease
Published in The Journal of pharmacology and experimental therapeutics (01-01-2011)“…Inhibition of phosphodiesterase 10A (PDE10A) promotes cyclic nucleotide signaling, increases striatal activation, and decreases behavioral activity. Enhanced…”
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CCK Receptor Inhibition Reduces Pancreatic Tumor Fibrosis and Promotes Nanoparticle Delivery
Published in Biomedicines (01-05-2024)“…The poor prognosis for pancreatic ductal adenocarcinoma (PDAC) patients is due in part to the highly fibrotic nature of the tumors that impedes delivery of…”
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Utilizing Peptide Ligand GPCRs to Image and Treat Pancreatic Cancer
Published in Biomedicines (02-06-2018)“…It is estimated that early detection of pancreatic ductal adenocarcinoma (PDAC) could increase long-term patient survival by as much as 30% to 40%…”
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Phosphodiesterase 9A in Brain Regulates cGMP Signaling Independent of Nitric-Oxide
Published in Frontiers in neuroscience (23-08-2019)“…PDE9A is a cGMP-specific phosphodiesterase expressed in neurons throughout the brain that has attracted attention as a therapeutic target to treat cognitive…”
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Kinetics of Metastatic Breast Cancer Cell Trafficking in Bone
Published in Clinical cancer research (01-03-2006)“…Purpose: In vivo studies have focused on the latter stages of the bone metastatic process (osteolysis), whereas little is known about earlier events, e.g.,…”
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Behavioral characterization of mice deficient in the phosphodiesterase-10A (PDE10A) enzyme on a C57/Bl6N congenic background
Published in Neuropharmacology (01-02-2008)“…The phenotype of genetically modified animals is strongly influenced by both the genetic background of the animal as well as environmental factors. We have…”
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Phosphodiesterase 10A Inhibition Improves Cortico-Basal Ganglia Function in Huntington’s Disease Models
Published in Neuron (Cambridge, Mass.) (21-12-2016)“…Huntington’s disease (HD) symptoms are driven to a large extent by dysfunction of the basal ganglia circuitry. HD patients exhibit reduced striatal…”
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Discovery of a Novel Class of Phosphodiesterase 10A Inhibitors and Identification of Clinical Candidate 2-[4-(1-Methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the Treatment of Schizophrenia
Published in Journal of medicinal chemistry (27-08-2009)“…By utilizing structure-based drug design (SBDD) knowledge, a novel class of phosphodiesterase (PDE) 10A inhibitors was identified. The structure-based drug…”
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Discovery of a Novel Class of Phosphodiesterase 10A Inhibitors and Identification of Clinical Candidate 2-[4-(1-Methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the Treatment of Schizophrenia † Coordinates of the PDE10A crystal structures have been deposited in the Protein Data Bank for compound 1 (3HQW), 2 (3HQY), 3 (3HQW) and 9 (3HR1)
Published in Journal of medicinal chemistry (27-08-2009)“…By utilizing structure-based drug design (SBDD) knowledge, a novel class of phosphodiesterase (PDE) 10A inhibitors was identified. The structure-based drug…”
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Identification of a Potent, Highly Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor Clinical Candidate
Published in Journal of medicinal chemistry (08-02-2018)“…Computational modeling was used to direct the synthesis of analogs of previously reported phosphodiesterase 2A (PDE2A) inhibitor 1 with an imidazotriazine core…”
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Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor
Published in Journal of medicinal chemistry (13-07-2017)“…Phosphodiesterase 2A (PDE2A) inhibitors have been reported to demonstrate in vivo activity in preclinical models of cognition. To more fully explore the…”
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Phosphodiesterase 9A regulates central cGMP and modulates responses to cholinergic and monoaminergic perturbation in vivo
Published in The Journal of pharmacology and experimental therapeutics (01-05-2012)“…Cyclic nucleotides are critical regulators of synaptic plasticity and participate in requisite signaling cascades implicated across multiple neurotransmitter…”
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Maintaining GFP tissue fluorescence through bone decalcification and long-term storage
Published in BioTechniques (01-12-2002)Get full text
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Tu1923 A Single Nucleotide Polymorphism of the CCK-B Receptor Does Not Effect Survival in Colon & Gastric Cancer
Published in Gastroenterology (New York, N.Y. 1943) (01-05-2013)Get full text
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Vagotomy enhances experimental metastases of 4THMpc breast cancer cells and alters Substance P level
Published in Regulatory peptides (29-11-2008)“…We have previously demonstrated that inactivation of capsaicin-sensitive sensory neurons enhances lung and heart metastases of breast carcinoma. Because a…”
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Role of endogenous cholecystokinin on growth of human pancreatic cancer
Published in International journal of oncology (01-03-2011)“…Cholecystokinin (CCK) and gastrin stimulate growth of pancreatic cancer. Although down-regulation of gastrin inhibits growth of pancreatic cancer, the…”
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Endogenous osteonectin/SPARC/BM-40 expression inhibits MDA-MB-231 breast cancer cell metastasis
Published in Cancer research (Chicago, Ill.) (15-08-2005)“…Skeletal metastases occur with high incidence in patients with breast cancer and cause long-term skeletal morbidity. Osteonectin (SPARC, BM-40) is a bone…”
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