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Discovery of potent azaindazole leucine-rich repeat kinase 2 (LRRK2) inhibitors possessing a key intramolecular hydrogen bond - Part 2.

Shore DGM, Sweeney ZK, Beresford A, Chan BK, Chen H, Drummond J, Gill A, Kleinheinz T, Liu X, Medhurst AD, McIver EG, Moffat JG, Zhu H, Estrada AA.

Bioorg Med Chem Lett. 2019 Feb 15;29(4):674-680. doi: 10.1016/j.bmcl.2018.10.017. Epub 2018 Oct 12.


Discovery of highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.

Estrada AA, Chan BK, Baker-Glenn C, Beresford A, Burdick DJ, Chambers M, Chen H, Dominguez SL, Dotson J, Drummond J, Flagella M, Fuji R, Gill A, Halladay J, Harris SF, Heffron TP, Kleinheinz T, Lee DW, Le Pichon CE, Liu X, Lyssikatos JP, Medhurst AD, Moffat JG, Nash K, Scearce-Levie K, Sheng Z, Shore DG, Wong S, Zhang S, Zhang X, Zhu H, Sweeney ZK.

J Med Chem. 2014 Feb 13;57(3):921-36. doi: 10.1021/jm401654j. Epub 2014 Jan 15.


Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.

Wilson DM, Apps J, Bailey N, Bamford MJ, Beresford IJ, Brackenborough K, Briggs MA, Brough S, Calver AR, Crook B, Davis RK, Davis RP, Davis S, Dean DK, Harris L, Heslop T, Holland V, Jeffrey P, Panchal TA, Parr CA, Quashie N, Schogger J, Sehmi SS, Stean TO, Steadman JG, Trail B, Wald J, Worby A, Takle AK, Witherington J, Medhurst AD.

Bioorg Med Chem Lett. 2013 Dec 15;23(24):6890-6. doi: 10.1016/j.bmcl.2013.09.090. Epub 2013 Oct 5.


The discovery of the benzazepine class of histamine H3 receptor antagonists.

Wilson DM, Apps J, Bailey N, Bamford MJ, Beresford IJ, Briggs MA, Calver AR, Crook B, Davis RP, Davis S, Dean DK, Harris L, Heightman TD, Panchal T, Parr CA, Quashie N, Steadman JG, Schogger J, Sehmi SS, Stean TO, Takle AK, Trail BK, White T, Witherington J, Worby A, Medhurst AD.

Bioorg Med Chem Lett. 2013 Dec 15;23(24):6897-901. doi: 10.1016/j.bmcl.2013.09.089. Epub 2013 Oct 5.


Discovery of a Highly Selective, Brain-Penetrant Aminopyrazole LRRK2 Inhibitor.

Chan BK, Estrada AA, Chen H, Atherall J, Baker-Glenn C, Beresford A, Burdick DJ, Chambers M, Dominguez SL, Drummond J, Gill A, Kleinheinz T, Le Pichon CE, Medhurst AD, Liu X, Moffat JG, Nash K, Scearce-Levie K, Sheng Z, Shore DG, Van de Poël H, Zhang S, Zhu H, Sweeney ZK.

ACS Med Chem Lett. 2012 Nov 23;4(1):85-90. doi: 10.1021/ml3003007. eCollection 2013 Jan 10.


Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.

Estrada AA, Liu X, Baker-Glenn C, Beresford A, Burdick DJ, Chambers M, Chan BK, Chen H, Ding X, DiPasquale AG, Dominguez SL, Dotson J, Drummond J, Flagella M, Flynn S, Fuji R, Gill A, Gunzner-Toste J, Harris SF, Heffron TP, Kleinheinz T, Lee DW, Le Pichon CE, Lyssikatos JP, Medhurst AD, Moffat JG, Mukund S, Nash K, Scearce-Levie K, Sheng Z, Shore DG, Tran T, Trivedi N, Wang S, Zhang S, Zhang X, Zhao G, Zhu H, Sweeney ZK.

J Med Chem. 2012 Nov 26;55(22):9416-33. doi: 10.1021/jm301020q. Epub 2012 Oct 15.


Full and partial peroxisome proliferation-activated receptor-γ agonists, but not δ agonist, rescue of dopaminergic neurons in the 6-OHDA parkinsonian model is associated with inhibition of microglial activation and MMP expression.

Sadeghian M, Marinova-Mutafchieva L, Broom L, Davis JB, Virley D, Medhurst AD, Dexter DT.

J Neuroimmunol. 2012 May 15;246(1-2):69-77. doi: 10.1016/j.jneuroim.2012.03.010. Epub 2012 Apr 11.


Preservation of cortical histamine H3 receptors in ischemic vascular and mixed dementias.

Sheng Y, Lee JH, Medhurst AD, Wilcock GK, Esiri M, Wong PT, Chen CP, Lai MK.

J Neurol Sci. 2012 Apr 15;315(1-2):110-4. doi: 10.1016/j.jns.2011.11.013. Epub 2011 Nov 29.


Neuroprotection by the selective iNOS inhibitor GW274150 in a model of Parkinson disease.

Broom L, Marinova-Mutafchieva L, Sadeghian M, Davis JB, Medhurst AD, Dexter DT.

Free Radic Biol Med. 2011 Mar 1;50(5):633-40. doi: 10.1016/j.freeradbiomed.2010.12.026. Epub 2010 Dec 23.


11C-GSK189254: a selective radioligand for in vivo central nervous system imaging of histamine H3 receptors by PET.

Plisson C, Gunn RN, Cunningham VJ, Bender D, Salinas CA, Medhurst AD, Roberts JC, Laruelle M, Gee AD.

J Nucl Med. 2009 Dec;50(12):2064-72. doi: 10.2967/jnumed.109.062919. Epub 2009 Nov 12.


H3 receptor antagonism enhances NCAM PSA-mediated plasticity and improves memory consolidation in odor discrimination and delayed match-to-position paradigms.

Foley AG, Prendergast A, Barry C, Scully D, Upton N, Medhurst AD, Regan CM.

Neuropsychopharmacology. 2009 Nov;34(12):2585-600. doi: 10.1038/npp.2009.89. Epub 2009 Aug 5.


Relationship between microglial activation and dopaminergic neuronal loss in the substantia nigra: a time course study in a 6-hydroxydopamine model of Parkinson's disease.

Marinova-Mutafchieva L, Sadeghian M, Broom L, Davis JB, Medhurst AD, Dexter DT.

J Neurochem. 2009 Aug;110(3):966-75. doi: 10.1111/j.1471-4159.2009.06189.x. Epub 2009 Jun 22.


Heterogeneity of histaminergic neurons in the tuberomammillary nucleus of the rat.

Giannoni P, Passani MB, Nosi D, Chazot PL, Shenton FC, Medhurst AD, Munari L, Blandina P.

Eur J Neurosci. 2009 Jun;29(12):2363-74. doi: 10.1111/j.1460-9568.2009.06765.x. Epub 2009 May 22.


Differential effects of acute and repeat dosing with the H3 antagonist GSK189254 on the sleep-wake cycle and narcoleptic episodes in Ox-/- mice.

Guo RX, Anaclet C, Roberts JC, Parmentier R, Zhang M, Guidon G, Buda C, Sastre JP, Feng JQ, Franco P, Brown SH, Upton N, Medhurst AD, Lin JS.

Br J Pharmacol. 2009 May;157(1):104-17. doi: 10.1111/j.1476-5381.2009.00205.x.


Autoradiographical imaging of PPARgamma agonist effects on PBR/TSPO binding in TASTPM mice.

Roberts JC, Friel SL, Roman S, Perren M, Harper A, Davis JB, Richardson JC, Virley D, Medhurst AD.

Exp Neurol. 2009 Apr;216(2):459-70.


Characterization of histamine H3 receptors in Alzheimer's Disease brain and amyloid over-expressing TASTPM mice.

Medhurst AD, Roberts JC, Lee J, Chen CP, Brown SH, Roman S, Lai MK.

Br J Pharmacol. 2009 May;157(1):130-8. doi: 10.1111/j.1476-5381.2008.00075.x. Epub 2009 Feb 16.


Identification of a novel 5-HT(4) receptor splice variant (r5-HT(4c1)) and preliminary characterisation of specific 5-HT(4a) and 5-HT(4b) receptor antibodies.

Ray AM, Kelsell RE, Houp JA, Kelly FM, Medhurst AD, Cox HM, Calver AR.

Eur J Pharmacol. 2009 Feb 14;604(1-3):1-11. doi: 10.1016/j.ejphar.2008.11.056. Epub 2008 Dec 6.


Tricyclic azepine derivatives as selective brain penetrant 5-HT6 receptor antagonists.

Trani G, Baddeley SM, Briggs MA, Chuang TT, Deeks NJ, Johnson CN, Khazragi AA, Mead TL, Medhurst AD, Milner PH, Quinn LP, Ray AM, Rivers DA, Stean TO, Stemp G, Trail BK, Witty DR.

Bioorg Med Chem Lett. 2008 Oct 15;18(20):5698-700. doi: 10.1016/j.bmcl.2008.08.010. Epub 2008 Aug 7.


Preclinical investigations into the antipsychotic potential of the novel histamine H3 receptor antagonist GSK207040.

Southam E, Cilia J, Gartlon JE, Woolley ML, Lacroix LP, Jennings CA, Cluderay JE, Reavill C, Rourke C, Wilson DM, Dawson LA, Medhurst AD, Jones DN.

Psychopharmacology (Berl). 2009 Jan;201(4):483-94. doi: 10.1007/s00213-008-1310-9. Epub 2008 Sep 3.


The novel cyclooxygenase-2 inhibitor GW637185X protects against l-methyl-4-phenyl-1,2,3,6-tetrahydropyridine toxicity.

Aguirre JA, Leo G, Cueto R, Andbjer B, Naylor A, Medhurst AD, Agnati LF, Fuxe K.

Neuroreport. 2008 Apr 16;19(6):657-60. doi: 10.1097/WNR.0b013e3282fb7898.


The PPARgamma agonist pioglitazone is effective in the MPTP mouse model of Parkinson's disease through inhibition of monoamine oxidase B.

Quinn LP, Crook B, Hows ME, Vidgeon-Hart M, Chapman H, Upton N, Medhurst AD, Virley DJ.

Br J Pharmacol. 2008 May;154(1):226-33. doi: 10.1038/bjp.2008.78. Epub 2008 Mar 10.


Novel histamine H3 receptor antagonists GSK189254 and GSK334429 are efficacious in surgically-induced and virally-induced rat models of neuropathic pain.

Medhurst SJ, Collins SD, Billinton A, Bingham S, Dalziel RG, Brass A, Roberts JC, Medhurst AD, Chessell IP.

Pain. 2008 Aug 15;138(1):61-9. doi: 10.1016/j.pain.2007.11.006. Epub 2007 Dec 31.


GSK189254, a novel H3 receptor antagonist that binds to histamine H3 receptors in Alzheimer's disease brain and improves cognitive performance in preclinical models.

Medhurst AD, Atkins AR, Beresford IJ, Brackenborough K, Briggs MA, Calver AR, Cilia J, Cluderay JE, Crook B, Davis JB, Davis RK, Davis RP, Dawson LA, Foley AG, Gartlon J, Gonzalez MI, Heslop T, Hirst WD, Jennings C, Jones DN, Lacroix LP, Martyn A, Ociepka S, Ray A, Regan CM, Roberts JC, Schogger J, Southam E, Stean TO, Trail BK, Upton N, Wadsworth G, Wald JA, White T, Witherington J, Woolley ML, Worby A, Wilson DM.

J Pharmacol Exp Ther. 2007 Jun;321(3):1032-45. Epub 2007 Feb 27.


Structurally novel histamine H3 receptor antagonists GSK207040 and GSK334429 improve scopolamine-induced memory impairment and capsaicin-induced secondary allodynia in rats.

Medhurst AD, Briggs MA, Bruton G, Calver AR, Chessell I, Crook B, Davis JB, Davis RP, Foley AG, Heslop T, Hirst WD, Medhurst SJ, Ociepka S, Ray A, Regan CM, Sargent B, Schogger J, Stean TO, Trail BK, Upton N, White T, Orlek B, Wilson DM.

Biochem Pharmacol. 2007 Apr 15;73(8):1182-94. Epub 2007 Jan 7.


MPTP treatment of common marmosets impairs proteasomal enzyme activity and decreases expression of structural and regulatory elements of the 26S proteasome.

Zeng BY, Iravani MM, Lin ST, Irifune M, Kuoppamäki M, Al-Barghouthy G, Smith L, Jackson MJ, Rose S, Medhurst AD, Jenner P.

Eur J Neurosci. 2006 Apr;23(7):1766-74.


Bicyclic heteroarylpiperazines as selective brain penetrant 5-HT6 receptor antagonists.

Ahmed M, Briggs MA, Bromidge SM, Buck T, Campbell L, Deeks NJ, Garner A, Gordon L, Hamprecht DW, Holland V, Johnson CN, Medhurst AD, Mitchell DJ, Moss SF, Powles J, Seal JT, Stean TO, Stemp G, Thompson M, Trail B, Upton N, Winborn K, Witty DR.

Bioorg Med Chem Lett. 2005 Nov 1;15(21):4867-71.


Proteasomal activity in brain differs between species and brain regions and changes with age.

Zeng BY, Medhurst AD, Jackson M, Rose S, Jenner P.

Mech Ageing Dev. 2005 Jun-Jul;126(6-7):760-6. Epub 2005 Mar 5.


Protection but maintained dysfunction of nigral dopaminergic nerve cell bodies and striatal dopaminergic terminals in MPTP-lesioned mice after acute treatment with the mGluR5 antagonist MPEP.

Aguirre JA, Kehr J, Yoshitake T, Liu FL, Rivera A, Fernandez-Espinola S, Andbjer B, Leo G, Medhurst AD, Agnati LF, Fuxe K.

Brain Res. 2005 Feb 8;1033(2):216-20.


Modulation of hippocampal excitability by 5-HT4 receptor agonists persists in a transgenic model of Alzheimer's disease.

Spencer JP, Brown JT, Richardson JC, Medhurst AD, Sehmi SS, Calver AR, Randall AD.

Neuroscience. 2004;129(1):49-54.


The GABA(B2) subunit is critical for the trafficking and function of native GABA(B) receptors.

Thuault SJ, Brown JT, Sheardown SA, Jourdain S, Fairfax B, Spencer JP, Restituito S, Nation JH, Topps S, Medhurst AD, Randall AD, Couve A, Moss SJ, Collingridge GL, Pangalos MN, Davies CH, Calver AR.

Biochem Pharmacol. 2004 Oct 15;68(8):1655-66.


Pharmacological and immunohistochemical characterization of the APJ receptor and its endogenous ligand apelin.

Medhurst AD, Jennings CA, Robbins MJ, Davis RP, Ellis C, Winborn KY, Lawrie KW, Hervieu G, Riley G, Bolaky JE, Herrity NC, Murdock P, Darker JG.

J Neurochem. 2003 Mar;84(5):1162-72.


Molecular cloning and characterisation of a novel GABAB-related G-protein coupled receptor.

Calver AR, Michalovich D, Testa TT, Robbins MJ, Jaillard C, Hill J, Szekeres PG, Charles KJ, Jourdain S, Holbrook JD, Boyfield I, Patel N, Medhurst AD, Pangalos MN.

Brain Res Mol Brain Res. 2003 Feb 20;110(2):305-17.


mRNA distribution analysis of human TRPC family in CNS and peripheral tissues.

Riccio A, Medhurst AD, Mattei C, Kelsell RE, Calver AR, Randall AD, Benham CD, Pangalos MN.

Brain Res Mol Brain Res. 2002 Dec 30;109(1-2):95-104.


Application of TaqMan RT-PCR for real-time semiquantitative analysis of gene expression in the striatum.

Medhurst AD, Pangalos MN.

Methods Mol Med. 2003;79:229-41. No abstract available.


Cloning and functional expression of human short TRP7, a candidate protein for store-operated Ca2+ influx.

Riccio A, Mattei C, Kelsell RE, Medhurst AD, Calver AR, Randall AD, Davis JB, Benham CD, Pangalos MN.

J Biol Chem. 2002 Apr 5;277(14):12302-9. Epub 2002 Jan 22.


Up-regulation of secretoneurin immunoreactivity and secretogranin II mRNA in rat striatum following 6-hydroxydopamine lesioning and chronic L-DOPA treatment.

Medhurst AD, Zeng BY, Charles KJ, Gray J, Reavill C, Hunter AJ, Shale JA, Jenner P.

Neuroscience. 2001;105(2):353-64.


Quantitative mRNA analysis of five C-terminal splice variants of the human 5-HT4 receptor in the central nervous system by TaqMan real time RT-PCR.

Medhurst AD, Lezoualc'h F, Fischmeister R, Middlemiss DN, Sanger GJ.

Brain Res Mol Brain Res. 2001 Jun 20;90(2):125-34.


Kinetic modification of the alpha(1I) subunit-mediated T-type Ca(2+) channel by a human neuronal Ca(2+) channel gamma subunit.

Green PJ, Warre R, Hayes PD, McNaughton NC, Medhurst AD, Pangalos M, Duckworth DM, Randall AD.

J Physiol. 2001 Jun 1;533(Pt 2):467-78.


Distribution analysis of human two pore domain potassium channels in tissues of the central nervous system and periphery.

Medhurst AD, Rennie G, Chapman CG, Meadows H, Duckworth MD, Kelsell RE, Gloger II, Pangalos MN.

Brain Res Mol Brain Res. 2001 Jan 31;86(1-2):101-14.


Cloning and characterization of human NTT5 and v7-3: two orphan transporters of the Na+/Cl- -dependent neurotransmitter transporter gene family.

Farmer MK, Robbins MJ, Medhurst AD, Campbell DA, Ellington K, Duckworth M, Brown AM, Middlemiss DN, Price GW, Pangalos MN.

Genomics. 2000 Dec 1;70(2):241-52.


Cloning and functional expression of a human orthologue of rat vanilloid receptor-1.

Hayes P, Meadows HJ, Gunthorpe MJ, Harries MH, Duckworth DM, Cairns W, Harrison DC, Clarke CE, Ellington K, Prinjha RK, Barton AJ, Medhurst AD, Smith GD, Topp S, Murdock P, Sanger GJ, Terrett J, Jenkins O, Benham CD, Randall AD, Gloger IS, Davis JB.

Pain. 2000 Nov;88(2):205-15.


The expression of GABA(B1) and GABA(B2) receptor subunits in the cNS differs from that in peripheral tissues.

Calver AR, Medhurst AD, Robbins MJ, Charles KJ, Evans ML, Harrison DC, Stammers M, Hughes SA, Hervieu G, Couve A, Moss SJ, Middlemiss DN, Pangalos MN.

Neuroscience. 2000;100(1):155-70.


Nonpeptide tachykinin receptor antagonists. II. Pharmacological and pharmacokinetic profile of SB-222200, a central nervous system penetrant, potent and selective NK-3 receptor antagonist.

Sarau HM, Griswold DE, Bush B, Potts W, Sandhu P, Lundberg D, Foley JJ, Schmidt DB, Webb EF, Martin LD, Legos JJ, Whitmore RG, Barone FC, Medhurst AD, Luttmann MA, Giardina GA, Hay DW.

J Pharmacol Exp Ther. 2000 Oct;295(1):373-81.


Pharmacological actions of a novel, high-affinity, and selective human dopamine D(3) receptor antagonist, SB-277011-A.

Reavill C, Taylor SG, Wood MD, Ashmeade T, Austin NE, Avenell KY, Boyfield I, Branch CL, Cilia J, Coldwell MC, Hadley MS, Hunter AJ, Jeffrey P, Jewitt F, Johnson CN, Jones DN, Medhurst AD, Middlemiss DN, Nash DJ, Riley GJ, Routledge C, Stemp G, Thewlis KM, Trail B, Vong AK, Hagan JJ.

J Pharmacol Exp Ther. 2000 Sep;294(3):1154-65.


Molecular cloning and characterization of two novel retinoic acid-inducible orphan G-protein-coupled receptors (GPRC5B and GPRC5C).

Robbins MJ, Michalovich D, Hill J, Calver AR, Medhurst AD, Gloger I, Sims M, Middlemiss DN, Pangalos MN.

Genomics. 2000 Jul 1;67(1):8-18.


The use of TaqMan RT-PCR assays for semiquantitative analysis of gene expression in CNS tissues and disease models.

Medhurst AD, Harrison DC, Read SJ, Campbell CA, Robbins MJ, Pangalos MN.

J Neurosci Methods. 2000 May 15;98(1):9-20.


Characterization of SB-269970-A, a selective 5-HT(7) receptor antagonist.

Hagan JJ, Price GW, Jeffrey P, Deeks NJ, Stean T, Piper D, Smith MI, Upton N, Medhurst AD, Middlemiss DN, Riley GJ, Lovell PJ, Bromidge SM, Thomas DR.

Br J Pharmacol. 2000 Jun;130(3):539-48.


Cloning, localisation and functional expression of the human orthologue of the TREK-1 potassium channel.

Meadows HJ, Benham CD, Cairns W, Gloger I, Jennings C, Medhurst AD, Murdock P, Chapman CG.

Pflugers Arch. 2000 Apr;439(6):714-22.


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