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Items: 1 to 50 of 189

1.

Synthesis and in vitro evaluation of fluorine-18 benzimidazole sulfones as CB2 PET-radioligands.

Kallinen A, Boyd R, Lane S, Bhalla R, Mardon K, Stimson DHR, Werry EL, Fulton R, Connor M, Kassiou M.

Org Biomol Chem. 2019 May 28;17(20):5086-5098. doi: 10.1039/c9ob00656g. Epub 2019 May 9.

PMID:
31070218
2.

O-GlcNAc Modification Protects against Protein Misfolding and Aggregation in Neurodegenerative Disease.

Ryan P, Xu M, Davey AK, Danon JJ, Mellick GD, Kassiou M, Rudrawar S.

ACS Chem Neurosci. 2019 May 15;10(5):2209-2221. doi: 10.1021/acschemneuro.9b00143. Epub 2019 Apr 26.

PMID:
30985105
3.

Radiosynthesis of (R,S)-[18 F]GE387: A Potential PET Radiotracer for Imaging Translocator Protein 18 kDa (TSPO) with Low Binding Sensitivity to the Human Gene Polymorphism rs6971.

Qiao L, Fisher E, McMurray L, Milicevic Sephton S, Hird M, Kuzhuppilly-Ramakrishnan N, Williamson DJ, Zhou X, Werry E, Kassiou M, Luthra S, Trigg W, Aigbirhio FI.

ChemMedChem. 2019 May 6;14(9):982-993. doi: 10.1002/cmdc.201900023. Epub 2019 Apr 8.

PMID:
30900397
4.

Imaging glial activation in patients with post-treatment Lyme disease symptoms: a pilot study using [11C]DPA-713 PET.

Coughlin JM, Yang T, Rebman AW, Bechtold KT, Du Y, Mathews WB, Lesniak WG, Mihm EA, Frey SM, Marshall ES, Rosenthal HB, Reekie TA, Kassiou M, Dannals RF, Soloski MJ, Aucott JN, Pomper MG.

J Neuroinflammation. 2018 Dec 19;15(1):346. doi: 10.1186/s12974-018-1381-4.

5.

Hydroxamic Acid Inhibitors Provide Cross-Species Inhibition of Plasmodium M1 and M17 Aminopeptidases.

Vinh NB, Drinkwater N, Malcolm TR, Kassiou M, Lucantoni L, Grin PM, Butler GS, Duffy S, Overall CM, Avery VM, Scammells PJ, McGowan S.

J Med Chem. 2019 Jan 24;62(2):622-640. doi: 10.1021/acs.jmedchem.8b01310. Epub 2019 Jan 4.

PMID:
30537832
6.

Targeting the Oxytocin System: New Pharmacotherapeutic Approaches.

Gulliver D, Werry E, Reekie TA, Katte TA, Jorgensen W, Kassiou M.

Trends Pharmacol Sci. 2019 Jan;40(1):22-37. doi: 10.1016/j.tips.2018.11.001. Epub 2018 Nov 30. Review.

PMID:
30509888
7.

In vivo assessment of neuroinflammation in progressive multiple sclerosis: a proof of concept study with [18F]DPA714 PET.

Hagens MHJ, Golla SV, Wijburg MT, Yaqub M, Heijtel D, Steenwijk MD, Schober P, Brevé JJP, Schuit RC, Reekie TA, Kassiou M, van Dam AM, Windhorst AD, Killestein J, Barkhof F, van Berckel BNM, Lammertsma AA.

J Neuroinflammation. 2018 Nov 13;15(1):314. doi: 10.1186/s12974-018-1352-9.

8.

Synthesis and in vitro evaluation of diverse heterocyclic diphenolic compounds as inhibitors of DYRK1A.

Zhou Q, Reekie TA, Abbassi RH, Indurthi Venkata D, Font JS, Ryan RM, Munoz L, Kassiou M.

Bioorg Med Chem. 2018 Dec 1;26(22):5852-5869. doi: 10.1016/j.bmc.2018.10.034. Epub 2018 Oct 28.

PMID:
30401502
9.

Remarkable Enhancement in Boron Uptake Within Glioblastoma Cells With Carboranyl-Indole Carboxamides.

Narlawar R, Austin CJD, Kahlert J, Selleri S, Da Pozzo E, Martini C, Werry EL, Rendina LM, Kassiou M.

Chem Asian J. 2018 Nov 2;13(21):3321-3327. doi: 10.1002/asia.201801175. Epub 2018 Oct 17.

PMID:
30369074
10.

Cubanes in Medicinal Chemistry.

Reekie TA, Williams CM, Rendina LM, Kassiou M.

J Med Chem. 2019 Feb 14;62(3):1078-1095. doi: 10.1021/acs.jmedchem.8b00888. Epub 2018 Sep 6.

PMID:
30137982
11.

Changes in cell morphology guide identification of tubulin as the off-target for protein kinase inhibitors.

Hoque M, Abbassi RH, Froio D, Man J, Johns TG, Stringer BW, Day BW, Pajic M, Kassiou M, Munoz L.

Pharmacol Res. 2018 Aug;134:166-178. doi: 10.1016/j.phrs.2018.06.023. Epub 2018 Jun 23.

PMID:
29944980
12.

Peptides, Peptidomimetics, and Carbohydrate-Peptide Conjugates as Amyloidogenic Aggregation Inhibitors for Alzheimer's Disease.

Ryan P, Patel B, Makwana V, Jadhav HR, Kiefel M, Davey A, Reekie TA, Rudrawar S, Kassiou M.

ACS Chem Neurosci. 2018 Jul 18;9(7):1530-1551. doi: 10.1021/acschemneuro.8b00185. Epub 2018 Jun 26.

PMID:
29782794
13.

Identification of the allosteric P2X7 receptor antagonist [11C]SMW139 as a PET tracer of microglial activation.

Janssen B, Vugts DJ, Wilkinson SM, Ory D, Chalon S, Hoozemans JJM, Schuit RC, Beaino W, Kooijman EJM, van den Hoek J, Chishty M, Doméné A, Van der Perren A, Villa A, Maggi A, Molenaar GT, Funke U, Shevchenko RV, Baekelandt V, Bormans G, Lammertsma AA, Kassiou M, Windhorst AD.

Sci Rep. 2018 Apr 26;8(1):6580. doi: 10.1038/s41598-018-24814-0.

14.

Multi-modal imaging of long-term recovery post-stroke by positron emission tomography and matrix-assisted laser desorption/ionisation mass spectrometry.

Henderson F, Hart PJ, Pradillo JM, Kassiou M, Christie L, Williams KJ, Boutin H, McMahon A.

Rapid Commun Mass Spectrom. 2018 May 15;32(9):721-729. doi: 10.1002/rcm.8090.

PMID:
29484723
15.

The chemistry and pharmacology of synthetic cannabinoid SDB-006 and its regioisomeric fluorinated and methoxylated analogs.

Banister SD, Olson A, Winchester M, Stuart J, Edington AR, Kevin RC, Longworth M, Herrera M, Connor M, McGregor IS, Gerona RR, Kassiou M.

Drug Test Anal. 2018 Jan 19. doi: 10.1002/dta.2362. [Epub ahead of print]

PMID:
29350472
16.

Conformationally rigid derivatives of WAY-267,464: Synthesis and pharmacology at the human oxytocin and vasopressin-1a receptors.

Jorgensen WT, Gulliver DW, Katte TA, Werry EL, Reekie TA, Connor M, Kassiou M.

Eur J Med Chem. 2018 Jan 1;143:1644-1656. doi: 10.1016/j.ejmech.2017.10.059. Epub 2017 Oct 23.

PMID:
29126725
17.

Longitudinal investigation of neuroinflammation and metabolite profiles in the APPswe ×PS1Δe9 transgenic mouse model of Alzheimer's disease.

Chaney A, Bauer M, Bochicchio D, Smigova A, Kassiou M, Davies KE, Williams SR, Boutin H.

J Neurochem. 2018 Feb;144(3):318-335. doi: 10.1111/jnc.14251. Epub 2017 Dec 15.

18.

A patent review of oxytocin receptor antagonists 2013-2017.

Katte TA, Kassiou M.

Expert Opin Ther Pat. 2017 Dec;27(12):1287-1290. doi: 10.1080/13543776.2017.1379992. Epub 2017 Sep 18. No abstract available.

PMID:
28906174
19.

Pharmacological Evaluation of Novel Bioisosteres of an Adamantanyl Benzamide P2X7 Receptor Antagonist.

Wilkinson SM, Barron ML, O'Brien-Brown J, Janssen B, Stokes L, Werry EL, Chishty M, Skarratt KK, Ong JA, Hibbs DE, Vugts DJ, Fuller S, Windhorst AD, Kassiou M.

ACS Chem Neurosci. 2017 Nov 15;8(11):2374-2380. doi: 10.1021/acschemneuro.7b00272. Epub 2017 Aug 25.

PMID:
28841278
20.

Pharmacology of Cumyl-Carboxamide Synthetic Cannabinoid New Psychoactive Substances (NPS) CUMYL-BICA, CUMYL-PICA, CUMYL-5F-PICA, CUMYL-5F-PINACA, and Their Analogues.

Longworth M, Banister SD, Boyd R, Kevin RC, Connor M, McGregor IS, Kassiou M.

ACS Chem Neurosci. 2017 Oct 18;8(10):2159-2167. doi: 10.1021/acschemneuro.7b00267. Epub 2017 Aug 11.

PMID:
28792725
21.

Increased Expression of Translocator Protein (TSPO) Marks Pro-inflammatory Microglia but Does Not Predict Neurodegeneration.

Beckers L, Ory D, Geric I, Declercq L, Koole M, Kassiou M, Bormans G, Baes M.

Mol Imaging Biol. 2018 Feb;20(1):94-102. doi: 10.1007/s11307-017-1099-1.

PMID:
28695372
22.

Synthesis and Pharmacological Profiling of the Metabolites of Synthetic Cannabinoid Drugs APICA, STS-135, ADB-PINACA, and 5F-ADB-PINACA.

Longworth M, Connor M, Banister SD, Kassiou M.

ACS Chem Neurosci. 2017 Aug 16;8(8):1673-1680. doi: 10.1021/acschemneuro.7b00116. Epub 2017 Jun 8.

PMID:
28574245
23.

Investigation of pyrazolo-sulfonamides as putative small molecule oxytocin receptor agonists.

Katte TA, Reekie TA, Werry EL, Jorgensen WT, Boyd R, Wong ECN, Gulliver DW, Connor M, Kassiou M.

Eur J Med Chem. 2017 Aug 18;136:330-333. doi: 10.1016/j.ejmech.2017.05.013. Epub 2017 May 4.

PMID:
28505537
24.

Ring-opened aminothienopyridazines as novel tau aggregation inhibitors.

Moir M, Chua SW, Reekie T, Martin AD, Ittner A, Ittner LM, Kassiou M.

Medchemcomm. 2017 May 5;8(6):1275-1282. doi: 10.1039/c6md00306k. eCollection 2017 Jun 1.

25.

Pharmacological evaluation of a novel series of urea, thiourea and guanidine derivatives as P2X7 receptor antagonists.

Wong ECN, Reekie TA, Werry EL, O'Brien-Brown J, Bowyer SL, Kassiou M.

Bioorg Med Chem Lett. 2017 Jun 1;27(11):2439-2442. doi: 10.1016/j.bmcl.2017.04.005. Epub 2017 Apr 4.

PMID:
28408229
26.

Detection of the recently emerged synthetic cannabinoid 5F-MDMB-PICA in 'legal high' products and human urine samples.

Mogler L, Franz F, Rentsch D, Angerer V, Weinfurtner G, Longworth M, Banister SD, Kassiou M, Moosmann B, Auwärter V.

Drug Test Anal. 2018 Jan;10(1):196-205. doi: 10.1002/dta.2201. Epub 2017 May 24.

PMID:
28371476
27.

Discovery and pharmacological evaluation of a novel series of adamantyl cyanoguanidines as P2X7 receptor antagonists.

O'Brien-Brown J, Jackson A, Reekie TA, Barron ML, Werry EL, Schiavini P, McDonnell M, Munoz L, Wilkinson S, Noll B, Wang S, Kassiou M.

Eur J Med Chem. 2017 Apr 21;130:433-439. doi: 10.1016/j.ejmech.2017.02.060. Epub 2017 Mar 2.

PMID:
28279849
28.

Structural Optimization and Pharmacological Evaluation of Inhibitors Targeting Dual-Specificity Tyrosine Phosphorylation-Regulated Kinases (DYRK) and CDC-like kinases (CLK) in Glioblastoma.

Zhou Q, Phoa AF, Abbassi RH, Hoque M, Reekie TA, Font JS, Ryan RM, Stringer BW, Day BW, Johns TG, Munoz L, Kassiou M.

J Med Chem. 2017 Mar 9;60(5):2052-2070. doi: 10.1021/acs.jmedchem.6b01840. Epub 2017 Feb 28.

PMID:
28206758
29.

Kinase targets in CNS drug discovery.

Gunosewoyo H, Yu L, Munoz L, Kassiou M.

Future Med Chem. 2017 Mar;9(3):303-314. doi: 10.4155/fmc-2016-0214. Epub 2017 Feb 8.

PMID:
28176536
30.

Translational evaluation of translocator protein as a marker of neuroinflammation in schizophrenia.

Notter T, Coughlin JM, Gschwind T, Weber-Stadlbauer U, Wang Y, Kassiou M, Vernon AC, Benke D, Pomper MG, Sawa A, Meyer U.

Mol Psychiatry. 2018 Feb;23(2):323-334. doi: 10.1038/mp.2016.248. Epub 2017 Jan 17.

PMID:
28093569
31.

Acute and residual effects in adolescent rats resulting from exposure to the novel synthetic cannabinoids AB-PINACA and AB-FUBINACA.

Kevin RC, Wood KE, Stuart J, Mitchell AJ, Moir M, Banister SD, Kassiou M, McGregor IS.

J Psychopharmacol. 2017 Jun;31(6):757-769. doi: 10.1177/0269881116684336. Epub 2017 Jan 16.

PMID:
28093016
32.

Mouse models of frontotemporal dementia: A comparison of phenotypes with clinical symptomatology.

Ahmed RM, Irish M, van Eersel J, Ittner A, Ke YD, Volkerling A, van der Hoven J, Tanaka K, Karl T, Kassiou M, Kril JJ, Piguet O, Götz J, Kiernan MC, Halliday GM, Hodges JR, Ittner LM.

Neurosci Biobehav Rev. 2017 Mar;74(Pt A):126-138. doi: 10.1016/j.neubiorev.2017.01.004. Epub 2017 Jan 11. Review.

PMID:
28088537
33.

The Polyphenol Altenusin Inhibits in Vitro Fibrillization of Tau and Reduces Induced Tau Pathology in Primary Neurons.

Chua SW, Cornejo A, van Eersel J, Stevens CH, Vaca I, Cueto M, Kassiou M, Gladbach A, Macmillan A, Lewis L, Whan R, Ittner LM.

ACS Chem Neurosci. 2017 Apr 19;8(4):743-751. doi: 10.1021/acschemneuro.6b00433. Epub 2017 Jan 12.

PMID:
28067492
34.

Rapid access to N-(indol-2-yl)amides and N-(indol-3-yl)amides as unexplored pharmacophores.

Reekie TA, Wilkinson SM, Law V, Hibbs DE, Ong JA, Kassiou M.

Org Biomol Chem. 2017 Jan 18;15(3):576-580. doi: 10.1039/c6ob02622b.

PMID:
27991628
35.

Imaging of Glial Cell Activation and White Matter Integrity in Brains of Active and Recently Retired National Football League Players.

Coughlin JM, Wang Y, Minn I, Bienko N, Ambinder EB, Xu X, Peters ME, Dougherty JW, Vranesic M, Koo SM, Ahn HH, Lee M, Cottrell C, Sair HI, Sawa A, Munro CA, Nowinski CJ, Dannals RF, Lyketsos CG, Kassiou M, Smith G, Caffo B, Mori S, Guilarte TR, Pomper MG.

JAMA Neurol. 2017 Jan 1;74(1):67-74. doi: 10.1001/jamaneurol.2016.3764.

36.

Determination and reduction of translocator protein (TSPO) ligand rs6971 discrimination.

Sokias R, Werry EL, Chua SW, Reekie TA, Munoz L, Wong ECN, Ittner LM, Kassiou M.

Medchemcomm. 2016 Nov 15;8(1):202-210. doi: 10.1039/c6md00523c. eCollection 2017 Jan 1.

37.

Derivatives of the pyrazolo[1,5-a]pyrimidine acetamide DPA-713 as translocator protein (TSPO) ligands and pro-apoptotic agents in human glioblastoma.

Werry EL, King VA, Barron ML, Banister SD, Sokias R, Kassiou M.

Eur J Pharm Sci. 2017 Jan 1;96:186-192. doi: 10.1016/j.ejps.2016.09.026. Epub 2016 Sep 19.

PMID:
27658888
38.

MDMA ('Ecstasy'), oxytocin and vasopressin modulate social preference in rats: A role for handling and oxytocin receptors.

Ramos L, Hicks C, Caminer A, Couto K, Narlawar R, Kassiou M, McGregor IS.

Pharmacol Biochem Behav. 2016 Nov - Dec;150-151:115-123. doi: 10.1016/j.pbb.2016.10.002. Epub 2016 Oct 7.

PMID:
27725273
39.

A systematic exploration of the effects of flexibility and basicity on sigma (σ) receptor binding in a series of substituted diamines.

Conroy T, Manohar M, Gong Y, Wilkinson SM, Webster M, Lieberman BP, Banister SD, Reekie TA, Mach RH, Rendina LM, Kassiou M.

Org Biomol Chem. 2016 Oct 4;14(39):9388-9405.

PMID:
27714195
40.

The 2-alkyl-2H-indazole regioisomers of synthetic cannabinoids AB-CHMINACA, AB-FUBINACA, AB-PINACA, and 5F-AB-PINACA are possible manufacturing impurities with cannabimimetic activities.

Longworth M, Banister SD, Mack JBC, Glass M, Connor M, Kassiou M.

Forensic Toxicol. 2016;34:286-303. doi: 10.1007/s11419-016-0316-y. Epub 2016 Apr 27.

41.

Disinhibition-like behavior in a P301S mutant tau transgenic mouse model of frontotemporal dementia.

Przybyla M, Stevens CH, van der Hoven J, Harasta A, Bi M, Ittner A, van Hummel A, Hodges JR, Piguet O, Karl T, Kassiou M, Housley GD, Ke YD, Ittner LM, Eersel Jv.

Neurosci Lett. 2016 Sep 19;631:24-9. doi: 10.1016/j.neulet.2016.08.007. Epub 2016 Aug 10.

PMID:
27521751
42.

Comparative Evaluation of Three TSPO PET Radiotracers in a LPS-Induced Model of Mild Neuroinflammation in Rats.

Sridharan S, Lepelletier FX, Trigg W, Banister S, Reekie T, Kassiou M, Gerhard A, Hinz R, Boutin H.

Mol Imaging Biol. 2017 Feb;19(1):77-89. doi: 10.1007/s11307-016-0984-3.

43.

Pharmacology of Valinate and tert-Leucinate Synthetic Cannabinoids 5F-AMBICA, 5F-AMB, 5F-ADB, AMB-FUBINACA, MDMB-FUBINACA, MDMB-CHMICA, and Their Analogues.

Banister SD, Longworth M, Kevin R, Sachdev S, Santiago M, Stuart J, Mack JB, Glass M, McGregor IS, Connor M, Kassiou M.

ACS Chem Neurosci. 2016 Sep 21;7(9):1241-54. doi: 10.1021/acschemneuro.6b00137. Epub 2016 Jul 27.

PMID:
27421060
44.

Neuroimaging of translocator protein in patients with systemic lupus erythematosus: a pilot study using [11C]DPA-713 positron emission tomography.

Wang Y, Coughlin JM, Ma S, Endres CJ, Kassiou M, Sawa A, Dannals RF, Petri M, Pomper MG.

Lupus. 2017 Feb;26(2):170-178. doi: 10.1177/0961203316657432. Epub 2016 Jul 11.

45.

The Formation of Seven-Membered Heterocycles under Mild Pictet-Spengler Conditions: A Route to Pyrazolo[3,4]benzodiazepines.

Katte TA, Reekie TA, Jorgensen WT, Kassiou M.

J Org Chem. 2016 Jun 3;81(11):4883-9. doi: 10.1021/acs.joc.6b00710. Epub 2016 May 13.

PMID:
27159074
46.

Detection of Neuroinflammation in a Rat Model of Subarachnoid Hemorrhage Using [18F]DPA-714 PET Imaging.

Thomas C, Vercouillie J, Doméné A, Tauber C, Kassiou M, Guilloteau D, Destrieux C, Sérrière S, Chalon S.

Mol Imaging. 2016 Apr 26;15. pii: 1536012116639189. doi: 10.1177/1536012116639189. Print 2016.

47.

In vivo markers of inflammatory response in recent-onset schizophrenia: a combined study using [(11)C]DPA-713 PET and analysis of CSF and plasma.

Coughlin JM, Wang Y, Ambinder EB, Ward RE, Minn I, Vranesic M, Kim PK, Ford CN, Higgs C, Hayes LN, Schretlen DJ, Dannals RF, Kassiou M, Sawa A, Pomper MG.

Transl Psychiatry. 2016 Apr 12;6:e777. doi: 10.1038/tp.2016.40.

48.
49.

Flexible analogues of WAY-267,464: Synthesis and pharmacology at the human oxytocin and vasopressin 1a receptors.

Jorgensen WT, Gulliver DW, Werry EL, Reekie T, Connor M, Kassiou M.

Eur J Med Chem. 2016 Jan 27;108:730-740. doi: 10.1016/j.ejmech.2015.11.050. Epub 2015 Dec 13.

PMID:
26741855
50.

TSPO as a target for glioblastoma therapeutics.

Werry EL, Barron ML, Kassiou M.

Biochem Soc Trans. 2015 Aug;43(4):531-6. doi: 10.1042/BST20150015. Epub 2015 Aug 3. Review.

PMID:
26551689

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