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Protection from amyloid β peptide-induced memory, biochemical and morphological deficits by a phosphodiesterase-4D (PDE4D) allosteric inhibitor.

Cui SY, Yang MX, Zhang YH, Zheng V, Zhang HT, Gurney ME, Xu Y, O'Donnell JM.

J Pharmacol Exp Ther. 2019 Sep 5. pii: jpet.119.259986. doi: 10.1124/jpet.119.259986. [Epub ahead of print]


Design and Synthesis of Selective Phosphodiesterase 4D (PDE4D) Allosteric Inhibitors for the Treatment of Fragile X Syndrome and Other Brain Disorders.

Gurney ME, Nugent RA, Mo X, Sindac JA, Hagen TJ, Fox D 3rd, O'Donnell JM, Zhang C, Xu Y, Zhang HT, Groppi VE, Bailie M, White RE, Romero DL, Vellekoop AS, Walker JR, Surman MD, Zhu L, Campbell RF.

J Med Chem. 2019 May 23;62(10):4884-4901. doi: 10.1021/acs.jmedchem.9b00193. Epub 2019 Apr 23.


Genetic Association of Phosphodiesterases With Human Cognitive Performance.

Gurney ME.

Front Mol Neurosci. 2019 Feb 8;12:22. doi: 10.3389/fnmol.2019.00022. eCollection 2019. Review.


Memory enhancing effects of BPN14770, an allosteric inhibitor of phosphodiesterase-4D, in wild-type and humanized mice.

Zhang C, Xu Y, Chowdhary A, Fox D 3rd, Gurney ME, Zhang HT, Auerbach BD, Salvi RJ, Yang M, Li G, O'Donnell JM.

Neuropsychopharmacology. 2018 Oct;43(11):2299-2309. doi: 10.1038/s41386-018-0178-6. Epub 2018 Aug 14.


The Use of Facebook Advertising to Recruit Healthy Elderly People for a Clinical Trial: Baseline Metrics.

Cowie JM, Gurney ME.

JMIR Res Protoc. 2018 Jan 24;7(1):e20. doi: 10.2196/resprot.7918.


A negative allosteric modulator of PDE4D enhances learning after traumatic brain injury.

Titus DJ, Wilson NM, Alcazar O, Calixte DA, Dietrich WD, Gurney ME, Atkins CM.

Neurobiol Learn Mem. 2018 Feb;148:38-49. doi: 10.1016/j.nlm.2017.12.008. Epub 2017 Dec 30.


Multiple Behavior Phenotypes of the Fragile-X Syndrome Mouse Model Respond to Chronic Inhibition of Phosphodiesterase-4D (PDE4D).

Gurney ME, Cogram P, Deacon RM, Rex C, Tranfaglia M.

Sci Rep. 2017 Nov 7;7(1):14653. doi: 10.1038/s41598-017-15028-x.


Therapeutic benefits of phosphodiesterase 4B inhibition after traumatic brain injury.

Wilson NM, Gurney ME, Dietrich WD, Atkins CM.

PLoS One. 2017 May 19;12(5):e0178013. doi: 10.1371/journal.pone.0178013. eCollection 2017.


Comparison of the Pharmacological Profiles of Selective PDE4B and PDE4D Inhibitors in the Central Nervous System.

Zhang C, Xu Y, Zhang HT, Gurney ME, O'Donnell JM.

Sci Rep. 2017 Jan 5;7:40115. doi: 10.1038/srep40115.


Chronic Cognitive Dysfunction after Traumatic Brain Injury Is Improved with a Phosphodiesterase 4B Inhibitor.

Titus DJ, Wilson NM, Freund JE, Carballosa MM, Sikah KE, Furones C, Dietrich WD, Gurney ME, Atkins CM.

J Neurosci. 2016 Jul 6;36(27):7095-108. doi: 10.1523/JNEUROSCI.3212-15.2016.


Phosphodiesterase-4 (PDE4) molecular pharmacology and Alzheimer's disease.

Gurney ME, D'Amato EC, Burgin AB.

Neurotherapeutics. 2015 Jan;12(1):49-56. doi: 10.1007/s13311-014-0309-7. Review.


Discovery of triazines as selective PDE4B versus PDE4D inhibitors.

Hagen TJ, Mo X, Burgin AB, Fox D 3rd, Zhang Z, Gurney ME.

Bioorg Med Chem Lett. 2014 Aug 15;24(16):4031-4. doi: 10.1016/j.bmcl.2014.06.002. Epub 2014 Jun 12.


The effect of diet on the protective action of D156844 observed in spinal muscular atrophy mice.

Butchbach ME, Singh J, Gurney ME, Burghes AH.

Exp Neurol. 2014 Jun;256:1-6. doi: 10.1016/j.expneurol.2014.03.005. Epub 2014 Mar 25.


Structural basis for the design of selective phosphodiesterase 4B inhibitors.

Fox D 3rd, Burgin AB, Gurney ME.

Cell Signal. 2014 Mar;26(3):657-63. doi: 10.1016/j.cellsig.2013.12.003. Epub 2013 Dec 19.


Blocking the EP3 receptor for PGE2 with DG-041 decreases thrombosis without impairing haemostatic competence.

Tilly P, Charles AL, Ludwig S, Slimani F, Gross S, Meilhac O, Geny B, Stefansson K, Gurney ME, Fabre JE.

Cardiovasc Res. 2014 Mar 1;101(3):482-91. doi: 10.1093/cvr/cvt276. Epub 2013 Dec 9.


Small molecule allosteric modulators of phosphodiesterase 4.

Gurney ME, Burgin AB, Magnusson OT, Stewart LJ.

Handb Exp Pharmacol. 2011;(204):167-92. doi: 10.1007/978-3-642-17969-3_7. Review.


Limitations of current therapies to prevent thrombosis: a need for novel strategies.

Fabre JE, Gurney ME.

Mol Biosyst. 2010 Feb;6(2):305-15. doi: 10.1039/b914375k. Epub 2009 Oct 26. Review.


Design of phosphodiesterase 4D (PDE4D) allosteric modulators for enhancing cognition with improved safety.

Burgin AB, Magnusson OT, Singh J, Witte P, Staker BL, Bjornsson JM, Thorsteinsdottir M, Hrafnsdottir S, Hagen T, Kiselyov AS, Stewart LJ, Gurney ME.

Nat Biotechnol. 2010 Jan;28(1):63-70. doi: 10.1038/nbt.1598. Epub 2009 Dec 27.


Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor antagonist, as a novel antiplatelet agent that does not prolong bleeding.

Singh J, Zeller W, Zhou N, Hategan G, Mishra RK, Polozov A, Yu P, Onua E, Zhang J, Ramírez JL, Sigthorsson G, Thorsteinnsdottir M, Kiselyov AS, Zembower DE, Andrésson T, Gurney ME.

J Med Chem. 2010 Jan 14;53(1):18-36. doi: 10.1021/jm9005912.


Discovery of 4-[(2S)-2-{[4-(4-chlorophenoxy)phenoxy]methyl}-1-pyrrolidinyl]butanoic acid (DG-051) as a novel leukotriene A4 hydrolase inhibitor of leukotriene B4 biosynthesis.

Sandanayaka V, Mamat B, Mishra RK, Winger J, Krohn M, Zhou LM, Keyvan M, Enache L, Sullins D, Onua E, Zhang J, Halldorsdottir G, Sigthorsdottir H, Thorlaksdottir A, Sigthorsson G, Thorsteinnsdottir M, Davies DR, Stewart LJ, Zembower DE, Andresson T, Kiselyov AS, Singh J, Gurney ME.

J Med Chem. 2010 Jan 28;53(2):573-85. doi: 10.1021/jm900838g.


Effects of 2,4-diaminoquinazoline derivatives on SMN expression and phenotype in a mouse model for spinal muscular atrophy.

Butchbach ME, Singh J, Thorsteinsdóttir M, Saieva L, Slominski E, Thurmond J, Andrésson T, Zhang J, Edwards JD, Simard LR, Pellizzoni L, Jarecki J, Burghes AH, Gurney ME.

Hum Mol Genet. 2010 Feb 1;19(3):454-67. doi: 10.1093/hmg/ddp510. Epub 2009 Nov 6.


Heterocyclic 1,7-disubstituted indole sulfonamides are potent and selective human EP3 receptor antagonists.

Hategan G, Polozov AM, Zeller W, Cao H, Mishra RK, Kiselyov AS, Ramirez J, Halldorsdottir G, Andrésson T, Gurney ME, Singh J.

Bioorg Med Chem Lett. 2009 Dec 1;19(23):6797-800. doi: 10.1016/j.bmcl.2009.09.084. Epub 2009 Sep 27.


Discovery of leukotriene A4 hydrolase inhibitors using metabolomics biased fragment crystallography.

Davies DR, Mamat B, Magnusson OT, Christensen J, Haraldsson MH, Mishra R, Pease B, Hansen E, Singh J, Zembower D, Kim H, Kiselyov AS, Burgin AB, Gurney ME, Stewart LJ.

J Med Chem. 2009 Aug 13;52(15):4694-715. doi: 10.1021/jm900259h. Erratum in: J Med Chem. 2010 Mar 11;53(5):2330-1.


Antagonists of the EP3 receptor for prostaglandin E2 are novel antiplatelet agents that do not prolong bleeding.

Singh J, Zeller W, Zhou N, Hategen G, Mishra R, Polozov A, Yu P, Onua E, Zhang J, Zembower D, Kiselyov A, Ramírez JL, Sigthorsson G, Bjornsson JM, Thorsteinsdottir M, Andrésson T, Bjarnadottir M, Magnusson O, Fabre JE, Stefansson K, Gurney ME.

ACS Chem Biol. 2009 Feb 20;4(2):115-26. doi: 10.1021/cb8002094.


3-Acrylamide-4-aryloxyindoles: synthesis, biological evaluation and metabolic stability of potent and selective EP3 receptor antagonists.

Zhou N, Zeller W, Zhang J, Onua E, Kiselyov AS, Ramirez J, Palsdottir G, Halldorsdottir G, Andrésson T, Gurney ME, Singh J.

Bioorg Med Chem Lett. 2009 Mar 1;19(5):1528-31. doi: 10.1016/j.bmcl.2008.12.112. Epub 2009 Jan 8.


Peri-substituted hexahydro-indolones as novel, potent and selective human EP3 receptor antagonists.

O'Connell M, Zeller W, Burgeson J, Mishra RK, Ramirez J, Kiselyov AS, Andrésson T, Gurney ME, Singh J.

Bioorg Med Chem Lett. 2009 Feb 1;19(3):778-82. doi: 10.1016/j.bmcl.2008.12.027. Epub 2008 Dec 10.


3,4-Disubstituted indole acylsulfonamides: a novel series of potent and selective human EP3 receptor antagonists.

Zhou N, Zeller W, Krohn M, Anderson H, Zhang J, Onua E, Kiselyov AS, Ramirez J, Halldorsdottir G, Andrésson T, Gurney ME, Singh J.

Bioorg Med Chem Lett. 2009 Jan 1;19(1):123-6. doi: 10.1016/j.bmcl.2008.11.007. Epub 2008 Nov 6.


DcpS as a therapeutic target for spinal muscular atrophy.

Singh J, Salcius M, Liu SW, Staker BL, Mishra R, Thurmond J, Michaud G, Mattoon DR, Printen J, Christensen J, Bjornsson JM, Pollok BA, Kiledjian M, Stewart L, Jarecki J, Gurney ME.

ACS Chem Biol. 2008 Nov 21;3(11):711-22. doi: 10.1021/cb800120t.


Synthesis and biological evaluation of novel 2,4-diaminoquinazoline derivatives as SMN2 promoter activators for the potential treatment of spinal muscular atrophy.

Thurmond J, Butchbach ME, Palomo M, Pease B, Rao M, Bedell L, Keyvan M, Pai G, Mishra R, Haraldsson M, Andresson T, Bragason G, Thosteinsdottir M, Bjornsson JM, Coovert DD, Burghes AH, Gurney ME, Singh J.

J Med Chem. 2008 Feb 14;51(3):449-69. doi: 10.1021/jm061475p. Epub 2008 Jan 19.


Neuregulin1 (NRG1) signaling through Fyn modulates NMDA receptor phosphorylation: differential synaptic function in NRG1+/- knock-outs compared with wild-type mice.

Bjarnadottir M, Misner DL, Haverfield-Gross S, Bruun S, Helgason VG, Stefansson H, Sigmundsson A, Firth DR, Nielsen B, Stefansdottir R, Novak TJ, Stefansson K, Gurney ME, Andresson T.

J Neurosci. 2007 Apr 25;27(17):4519-29.


Screening for presenilin inhibitors using the free-living nematode, Caenorhabditis elegans.

Ellerbrock BR, Coscarelli EM, Gurney ME, Geary TG.

J Biomol Screen. 2004 Mar;9(2):147-52.


The gene encoding 5-lipoxygenase activating protein confers risk of myocardial infarction and stroke.

Helgadottir A, Manolescu A, Thorleifsson G, Gretarsdottir S, Jonsdottir H, Thorsteinsdottir U, Samani NJ, Gudmundsson G, Grant SF, Thorgeirsson G, Sveinbjornsdottir S, Valdimarsson EM, Matthiasson SE, Johannsson H, Gudmundsdottir O, Gurney ME, Sainz J, Thorhallsdottir M, Andresdottir M, Frigge ML, Topol EJ, Kong A, Gudnason V, Hakonarson H, Gulcher JR, Stefansson K.

Nat Genet. 2004 Mar;36(3):233-9. Epub 2004 Feb 8.


SEL-10 interacts with presenilin 1, facilitates its ubiquitination, and alters A-beta peptide production.

Li J, Pauley AM, Myers RL, Shuang R, Brashler JR, Yan R, Buhl AE, Ruble C, Gurney ME.

J Neurochem. 2002 Sep;82(6):1540-8.


Neuregulin 1 and susceptibility to schizophrenia.

Stefansson H, Sigurdsson E, Steinthorsdottir V, Bjornsdottir S, Sigmundsson T, Ghosh S, Brynjolfsson J, Gunnarsdottir S, Ivarsson O, Chou TT, Hjaltason O, Birgisdottir B, Jonsson H, Gudnadottir VG, Gudmundsdottir E, Bjornsson A, Ingvarsson B, Ingason A, Sigfusson S, Hardardottir H, Harvey RP, Lai D, Zhou M, Brunner D, Mutel V, Gonzalo A, Lemke G, Sainz J, Johannesson G, Andresson T, Gudbjartsson D, Manolescu A, Frigge ML, Gurney ME, Kong A, Gulcher JR, Petursson H, Stefansson K.

Am J Hum Genet. 2002 Oct;71(4):877-92. Epub 2002 Jul 23.


Disease mechanisms revealed by transcription profiling in SOD1-G93A transgenic mouse spinal cord.

Olsen MK, Roberds SL, Ellerbrock BR, Fleck TJ, McKinley DK, Gurney ME.

Ann Neurol. 2001 Dec;50(6):730-40.


Human apolipoprotein E4 accelerates beta-amyloid deposition in APPsw transgenic mouse brain.

Carter DB, Dunn E, McKinley DD, Stratman NC, Boyle TP, Kuiper SL, Oostveen JA, Weaver RJ, Boller JA, Gurney ME.

Ann Neurol. 2001 Oct;50(4):468-75.


Immunohistochemical study on the distribution of Bcl-2 and Bax in the central nervous system of the transgenic mice expressing a human Cu/Zn SOD mutation.

Shin CM, Chung YH, Kim MJ, Shin DH, Kim YS, Gurney ME, Lee KW, Cha CI.

Brain Res. 2000 Dec 29;887(2):309-15.


Measurement of o- and m-tyrosine as markers of oxidative damage in motor neuron disease.

Poljak A, Pamphlett R, Gurney ME, Duncan MW.

Redox Rep. 2000;5(2-3):137-40. No abstract available.


Tau phosphorylation at serine 396 and serine 404 by human recombinant tau protein kinase II inhibits tau's ability to promote microtubule assembly.

Evans DB, Rank KB, Bhattacharya K, Thomsen DR, Gurney ME, Sharma SK.

J Biol Chem. 2000 Aug 11;275(32):24977-83.


Neurobiology. Stay the executioner's hand.

Gurney ME, Tomasselli AG, Heinrikson RL.

Science. 2000 Apr 14;288(5464):283-4. No abstract available.


Reactive astrocytes express p53 in the spinal cord of transgenic mice expressing a human Cu/Zn SOD mutation.

Cho KJ, Chung YH, Shin C, Shin DH, Kim YS, Gurney ME, Lee KW, Cha CI.

Neuroreport. 1999 Dec 16;10(18):3939-43.


What transgenic mice tell us about neurodegenerative disease.

Gurney ME.

Bioessays. 2000 Mar;22(3):297-304. Review.


Immunocytochemical study on the distribution of nitrotyrosine in the brain of the transgenic mice expressing a human Cu/Zn SOD mutation.

Cha CI, Chung YH, Shin CM, Shin DH, Kim YS, Gurney ME, Lee KW.

Brain Res. 2000 Jan 17;853(1):156-61.


Membrane-anchored aspartyl protease with Alzheimer's disease beta-secretase activity.

Yan R, Bienkowski MJ, Shuck ME, Miao H, Tory MC, Pauley AM, Brashier JR, Stratman NC, Mathews WR, Buhl AE, Carter DB, Tomasselli AG, Parodi LA, Heinrikson RL, Gurney ME.

Nature. 1999 Dec 2;402(6761):533-7.


Lack of involvement of neuronal nitric oxide synthase in the pathogenesis of a transgenic mouse model of familial amyotrophic lateral sclerosis.

Facchinetti F, Sasaki M, Cutting FB, Zhai P, MacDonald JE, Reif D, Beal MF, Huang PL, Dawson TM, Gurney ME, Dawson VL.

Neuroscience. 1999;90(4):1483-92.


Enhanced oxygen radical production in a transgenic mouse model of familial amyotrophic lateral sclerosis.

Liu R, Althaus JS, Ellerbrock BR, Becker DA, Gurney ME.

Ann Neurol. 1998 Nov;44(5):763-70.


Protein oxidative damage in a transgenic mouse model of familial amyotrophic lateral sclerosis.

Andrus PK, Fleck TJ, Gurney ME, Hall ED.

J Neurochem. 1998 Nov;71(5):2041-8.


Mutant CuZn superoxide dismutase in motor neuron disease.

Gurney ME, Liu R, Althaus JS, Hall ED, Becker DA.

J Inherit Metab Dis. 1998 Aug;21(5):587-97. Review.


Relationship of oxygen radical-induced lipid peroxidative damage to disease onset and progression in a transgenic model of familial ALS.

Hall ED, Andrus PK, Oostveen JA, Fleck TJ, Gurney ME.

J Neurosci Res. 1998 Jul 1;53(1):66-77.


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