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Items: 1 to 50 of 56

1.

A Novel Class of N-Sulfonyl and N-Sulfamoyl Noscapine Derivatives that Promote Mitotic Arrest in Cancer Cells.

Yong C, Devine SM, Gao X, Yan A, Callaghan R, Capuano B, Scammells PJ.

ChemMedChem. 2019 Nov 12. doi: 10.1002/cmdc.201900477. [Epub ahead of print]

PMID:
31714012
2.

Structure-Kinetic Profiling of Haloperidol Analogues at the Human Dopamine D2 Receptor.

Fyfe TJ, Kellam B, Sykes DA, Capuano B, Scammells PJ, Lane JR, Charlton SJ, Mistry SN.

J Med Chem. 2019 Nov 14;62(21):9488-9520. doi: 10.1021/acs.jmedchem.9b00864. Epub 2019 Oct 23.

PMID:
31580666
3.

Molecular Determinants of the Intrinsic Efficacy of the Antipsychotic Aripiprazole.

Klein Herenbrink C, Verma R, Lim HD, Kopinathan A, Keen A, Shonberg J, Draper-Joyce CJ, Scammells PJ, Christopoulos A, Javitch JA, Capuano B, Shi L, Lane JR.

ACS Chem Biol. 2019 Aug 16;14(8):1780-1792. doi: 10.1021/acschembio.9b00342. Epub 2019 Aug 5.

PMID:
31339684
4.

Subtle modifications to a thieno[2,3-d]pyrimidine scaffold yield negative allosteric modulators and agonists of the dopamine D2 receptor.

Fyfe TJ, Kellam B, Mistry SN, Scammells PJ, Lane JR, Capuano B.

Eur J Med Chem. 2019 Apr 15;168:474-490. doi: 10.1016/j.ejmech.2019.01.061. Epub 2019 Feb 11.

PMID:
30849613
5.

6-Phenylpyrimidin-4-ones as Positive Allosteric Modulators at the M1 mAChR: The Determinants of Allosteric Activity.

Jörg M, van der Westhuizen ET, Khajehali E, Burger WAC, White JM, Choy KHC, Tobin AB, Sexton PM, Valant C, Capuano B, Christopoulos A, Scammells PJ.

ACS Chem Neurosci. 2019 Mar 20;10(3):1099-1114. doi: 10.1021/acschemneuro.8b00613. Epub 2018 Dec 28.

PMID:
30547573
6.

Overcoming P-Glycoprotein-Mediated Drug Resistance with Noscapine Derivatives.

Muthiah D, Henshaw GK, DeBono AJ, Capuano B, Scammells PJ, Callaghan R.

Drug Metab Dispos. 2019 Feb;47(2):164-172. doi: 10.1124/dmd.118.083188. Epub 2018 Nov 26.

PMID:
30478158
7.

Reply to 'Antipsychotics with similar association kinetics at dopamine D2 receptors differ in extrapyramidal side-effects'.

Sykes DA, Lane JR, Szabo M, Capuano B, Javitch JA, Charlton SJ.

Nat Commun. 2018 Sep 3;9(1):3568. doi: 10.1038/s41467-018-05678-4. No abstract available.

8.

Synthesis and Pharmacological Evaluation of Noscapine-Inspired 5-Substituted Tetrahydroisoquinolines as Cytotoxic Agents.

Devine SM, Yong C, Amenuvegbe D, Aurelio L, Muthiah D, Pouton C, Callaghan R, Capuano B, Scammells PJ.

J Med Chem. 2018 Sep 27;61(18):8444-8456. doi: 10.1021/acs.jmedchem.8b00986. Epub 2018 Sep 14.

PMID:
30156410
9.
10.

Assessment of the Molecular Mechanisms of Action of Novel 4-Phenylpyridine-2-One and 6-Phenylpyrimidin-4-One Allosteric Modulators at the M1 Muscarinic Acetylcholine Receptors.

van der Westhuizen ET, Spathis A, Khajehali E, Jörg M, Mistry SN, Capuano B, Tobin AB, Sexton PM, Scammells PJ, Valant C, Christopoulos A.

Mol Pharmacol. 2018 Jul;94(1):770-783. doi: 10.1124/mol.118.111633. Epub 2018 Apr 24.

PMID:
29691279
11.

A Thieno[2,3- d]pyrimidine Scaffold Is a Novel Negative Allosteric Modulator of the Dopamine D2 Receptor.

Fyfe TJ, Zarzycka B, Lim HD, Kellam B, Mistry SN, Katrich V, Scammells PJ, Lane JR, Capuano B.

J Med Chem. 2019 Jan 10;62(1):174-206. doi: 10.1021/acs.jmedchem.7b01565. Epub 2018 May 15.

PMID:
29683325
12.

Synthesis and Pharmacological Evaluation of Heterocyclic Carboxamides: Positive Allosteric Modulators of the M1 Muscarinic Acetylcholine Receptor with Weak Agonist Activity and Diverse Modulatory Profiles.

Dallagnol JCC, Khajehali E, van der Westhuizen ET, Jörg M, Valant C, Gonçalves AG, Capuano B, Christopoulos A, Scammells PJ.

J Med Chem. 2018 Apr 12;61(7):2875-2894. doi: 10.1021/acs.jmedchem.7b01812. Epub 2018 Mar 23.

PMID:
29544056
13.

The action of a negative allosteric modulator at the dopamine D2 receptor is dependent upon sodium ions.

Draper-Joyce CJ, Verma RK, Michino M, Shonberg J, Kopinathan A, Klein Herenbrink C, Scammells PJ, Capuano B, Abramyan AM, Thal DM, Javitch JA, Christopoulos A, Shi L, Lane JR.

Sci Rep. 2018 Jan 19;8(1):1208. doi: 10.1038/s41598-018-19642-1.

14.

The structural determinants of the bitopic binding mode of a negative allosteric modulator of the dopamine D2 receptor.

Draper-Joyce CJ, Michino M, Verma RK, Klein Herenbrink C, Shonberg J, Kopinathan A, Scammells PJ, Capuano B, Thal DM, Javitch JA, Christopoulos A, Shi L, Lane JR.

Biochem Pharmacol. 2018 Feb;148:315-328. doi: 10.1016/j.bcp.2018.01.002. Epub 2018 Jan 9.

15.

The cationic small molecule GW4869 is cytotoxic to high phosphatidylserine-expressing myeloma cells.

Vuckovic S, Vandyke K, Rickards DA, McCauley Winter P, Brown SHJ, Mitchell TW, Liu J, Lu J, Askenase PW, Yuriev E, Capuano B, Ramsland PA, Hill GR, Zannettino ACW, Hutchinson AT.

Br J Haematol. 2017 May;177(3):423-440. doi: 10.1111/bjh.14561. Epub 2017 Feb 17.

PMID:
28211573
16.

Testing of direct acting antiviral agents purchased overseas: a necessary precaution to protect patients?

Lubel J, Chivers S, Taylor D, Capuano B.

Intern Med J. 2016 Sep;46(9):1111-3. doi: 10.1111/imj.13182. No abstract available.

PMID:
27633473
17.

The dopamine D2 receptor dimer and its interaction with homobivalent antagonists: homology modeling, docking and molecular dynamics.

Kaczor AA, Jörg M, Capuano B.

J Mol Model. 2016 Sep;22(9):203. doi: 10.1007/s00894-016-3065-2. Epub 2016 Aug 4.

18.

Multivalent approaches and beyond: novel tools for the investigation of dopamine D2 receptor pharmacology.

Kopinathan A, Scammells PJ, Lane JR, Capuano B.

Future Med Chem. 2016 Jul;8(11):1349-72. doi: 10.4155/fmc-2016-0010. Epub 2016 Jun 30. Review.

PMID:
27357619
19.

The role of kinetic context in apparent biased agonism at GPCRs.

Klein Herenbrink C, Sykes DA, Donthamsetti P, Canals M, Coudrat T, Shonberg J, Scammells PJ, Capuano B, Sexton PM, Charlton SJ, Javitch JA, Christopoulos A, Lane JR.

Nat Commun. 2016 Feb 24;7:10842. doi: 10.1038/ncomms10842.

20.

Novel Fused Arylpyrimidinone Based Allosteric Modulators of the M1 Muscarinic Acetylcholine Receptor.

Mistry SN, Lim H, Jörg M, Capuano B, Christopoulos A, Lane JR, Scammells PJ.

ACS Chem Neurosci. 2016 May 18;7(5):647-61. doi: 10.1021/acschemneuro.6b00018. Epub 2016 Mar 3.

PMID:
26891194
21.

4-Phenylpyridin-2-one Derivatives: A Novel Class of Positive Allosteric Modulator of the M1 Muscarinic Acetylcholine Receptor.

Mistry SN, Jörg M, Lim H, Vinh NB, Sexton PM, Capuano B, Christopoulos A, Lane JR, Scammells PJ.

J Med Chem. 2016 Jan 14;59(1):388-409. doi: 10.1021/acs.jmedchem.5b01562. Epub 2015 Dec 31.

PMID:
26624844
22.

Discovery of a Novel Class of Negative Allosteric Modulator of the Dopamine D2 Receptor Through Fragmentation of a Bitopic Ligand.

Mistry SN, Shonberg J, Draper-Joyce CJ, Klein Herenbrink C, Michino M, Shi L, Christopoulos A, Capuano B, Scammells PJ, Lane JR.

J Med Chem. 2015 Sep 10;58(17):6819-43. doi: 10.1021/acs.jmedchem.5b00585. Epub 2015 Aug 28.

PMID:
26258690
23.

Structure-activity study of N-((trans)-4-(2-(7-cyano-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)cyclohexyl)-1H-indole-2-carboxamide (SB269652), a bitopic ligand that acts as a negative allosteric modulator of the dopamine D2 receptor.

Shonberg J, Draper-Joyce C, Mistry SN, Christopoulos A, Scammells PJ, Lane JR, Capuano B.

J Med Chem. 2015 Jul 9;58(13):5287-307. doi: 10.1021/acs.jmedchem.5b00581. Epub 2015 Jun 24.

PMID:
26052807
24.

Synthesis and pharmacological evaluation of M4 muscarinic receptor positive allosteric modulators derived from VU10004.

Huynh T, Valant C, Crosby IT, Sexton PM, Christopoulos A, Capuano B.

ACS Chem Neurosci. 2015 Jun 17;6(6):838-44. doi: 10.1021/acschemneuro.5b00035. Epub 2015 Apr 17.

PMID:
25857219
25.

Progress Toward the Development of Noscapine and Derivatives as Anticancer Agents.

DeBono A, Capuano B, Scammells PJ.

J Med Chem. 2015 Aug 13;58(15):5699-727. doi: 10.1021/jm501180v. Epub 2015 Apr 16.

PMID:
25811651
26.

Proof of concept study for designed multiple ligands targeting the dopamine D2, serotonin 5-HT2A, and muscarinic M1 acetylcholine receptors.

Szabo M, Lim HD, Herenbrink CK, Christopoulos A, Lane JR, Capuano B.

J Med Chem. 2015 Feb 12;58(3):1550-5. doi: 10.1021/jm5013243. Epub 2015 Jan 30.

PMID:
25590655
27.

Synthesis and pharmacological evaluation of dual acting ligands targeting the adenosine A2A and dopamine D2 receptors for the potential treatment of Parkinson's disease.

Jörg M, May LT, Mak FS, Lee KC, Miller ND, Scammells PJ, Capuano B.

J Med Chem. 2015 Jan 22;58(2):718-38. doi: 10.1021/jm501254d. Epub 2014 Dec 24.

PMID:
25490054
28.

Development of a photoactivatable allosteric ligand for the m1 muscarinic acetylcholine receptor.

Davie BJ, Sexton PM, Capuano B, Christopoulos A, Scammells PJ.

ACS Chem Neurosci. 2014 Oct 15;5(10):902-7. doi: 10.1021/cn500173x. Epub 2014 Sep 9.

PMID:
25188871
29.

A new mechanism of allostery in a G protein-coupled receptor dimer.

Lane JR, Donthamsetti P, Shonberg J, Draper-Joyce CJ, Dentry S, Michino M, Shi L, López L, Scammells PJ, Capuano B, Sexton PM, Javitch JA, Christopoulos A.

Nat Chem Biol. 2014 Sep;10(9):745-52. doi: 10.1038/nchembio.1593. Epub 2014 Aug 10.

30.

NMR case study of ropinirole: concentration-dependent effects of nonexchangeable proton resonances.

Jörg M, Headey S, Scammells PJ, Capuano B.

Magn Reson Chem. 2014 Nov;52(11):715-8. doi: 10.1002/mrc.4114. Epub 2014 Aug 7. No abstract available.

PMID:
25104507
31.

Synthesis and pharmacological evaluation of analogues of benzyl quinolone carboxylic acid (BQCA) designed to bind irreversibly to an allosteric site of the M ₁ muscarinic acetylcholine receptor.

Davie BJ, Valant C, White JM, Sexton PM, Capuano B, Christopoulos A, Scammells PJ.

J Med Chem. 2014 Jun 26;57(12):5405-18. doi: 10.1021/jm500556a. Epub 2014 Jun 5.

PMID:
24856614
32.

Structure-activity relationships of privileged structures lead to the discovery of novel biased ligands at the dopamine D₂ receptor.

Szabo M, Klein Herenbrink C, Christopoulos A, Lane JR, Capuano B.

J Med Chem. 2014 Jun 12;57(11):4924-39. doi: 10.1021/jm500457x. Epub 2014 May 30.

PMID:
24827597
33.

Biased agonism at G protein-coupled receptors: the promise and the challenges--a medicinal chemistry perspective.

Shonberg J, Lopez L, Scammells PJ, Christopoulos A, Capuano B, Lane JR.

Med Res Rev. 2014 Nov;34(6):1286-330. doi: 10.1002/med.21318. Epub 2014 May 5. Review.

PMID:
24796277
34.

The dopamine D2 and adenosine A2A receptors: past, present and future trends for the treatment of Parkinson's disease.

Jorg M, Scammells PJ, Capuano B.

Curr Med Chem. 2014;21(27):3188-210. Review.

PMID:
24533801
35.

The synthesis and biological evaluation of multifunctionalised derivatives of noscapine as cytotoxic agents.

Debono AJ, Mistry SJ, Xie J, Muthiah D, Phillips J, Ventura S, Callaghan R, Pouton CW, Capuano B, Scammells PJ.

ChemMedChem. 2014 Feb;9(2):399-410. doi: 10.1002/cmdc.201300395. Epub 2013 Dec 11.

PMID:
24339417
36.

A structure-activity analysis of biased agonism at the dopamine D2 receptor.

Shonberg J, Herenbrink CK, López L, Christopoulos A, Scammells PJ, Capuano B, Lane JR.

J Med Chem. 2013 Nov 27;56(22):9199-221. doi: 10.1021/jm401318w. Epub 2013 Nov 8.

PMID:
24138311
37.

Probing structural requirements of positive allosteric modulators of the M4 muscarinic receptor.

Huynh T, Valant C, Crosby IT, Sexton PM, Christopoulos A, Capuano B.

J Med Chem. 2013 Oct 24;56(20):8196-200. doi: 10.1021/jm401032k. Epub 2013 Oct 11.

PMID:
24074052
38.

Synthesis and pharmacological profiling of analogues of benzyl quinolone carboxylic acid (BQCA) as allosteric modulators of the M1 muscarinic receptor.

Mistry SN, Valant C, Sexton PM, Capuano B, Christopoulos A, Scammells PJ.

J Med Chem. 2013 Jun 27;56(12):5151-72. doi: 10.1021/jm400540b. Epub 2013 Jun 17.

PMID:
23718562
39.

Novel adenosine A(2A) receptor ligands: a synthetic, functional and computational investigation of selected literature adenosine A(2A) receptor antagonists for extending into extracellular space.

Jörg M, Shonberg J, Mak FS, Miller ND, Yuriev E, Scammells PJ, Capuano B.

Bioorg Med Chem Lett. 2013 Jun 1;23(11):3427-33. doi: 10.1016/j.bmcl.2013.03.070. Epub 2013 Apr 2.

PMID:
23602401
40.

Synthesis and biological evaluation of N-substituted noscapine analogues.

DeBono AJ, Xie JH, Ventura S, Pouton CW, Capuano B, Scammells PJ.

ChemMedChem. 2012 Dec;7(12):2122-33. doi: 10.1002/cmdc.201200365. Epub 2012 Oct 10.

PMID:
23055449
41.

Synthesis and SAR study of 4-arylpiperidines and 4-aryl-1,2,3,6-tetrahydropyridines as 5-HT₂C agonists.

Conway RJ, Valant C, Christopoulos A, Robertson AD, Capuano B, Crosby IT.

Bioorg Med Chem Lett. 2012 Apr 1;22(7):2560-4. doi: 10.1016/j.bmcl.2012.01.122. Epub 2012 Feb 9.

PMID:
22381048
42.

Homobivalent ligands of the atypical antipsychotic clozapine: design, synthesis, and pharmacological evaluation.

McRobb FM, Crosby IT, Yuriev E, Lane JR, Capuano B.

J Med Chem. 2012 Feb 23;55(4):1622-34. doi: 10.1021/jm201420s. Epub 2012 Feb 2.

PMID:
22243698
43.

The design, synthesis and biological evaluation of novel URB602 analogues as potential monoacylglycerol lipase inhibitors.

Szabo M, Agostino M, Malone DT, Yuriev E, Capuano B.

Bioorg Med Chem Lett. 2011 Nov 15;21(22):6782-7. doi: 10.1016/j.bmcl.2011.09.038. Epub 2011 Sep 18.

PMID:
21982493
44.

Design strategies for bivalent ligands targeting GPCRs.

Shonberg J, Scammells PJ, Capuano B.

ChemMedChem. 2011 Jun 6;6(6):963-74. doi: 10.1002/cmdc.201100101. Epub 2011 Apr 21. Review.

PMID:
21520422
45.

Characterization of the N-methyltransferase activities of the multifunctional polypeptide cyclosporin synthetase.

Velkov T, Horne J, Scanlon MJ, Capuano B, Yuriev E, Lawen A.

Chem Biol. 2011 Apr 22;18(4):464-75. doi: 10.1016/j.chembiol.2011.01.017.

46.

Schizophrenia: a systematic review of the disease state, current therapeutics and their molecular mechanisms of action.

Shin JK, Malone DT, Crosby IT, Capuano B.

Curr Med Chem. 2011;18(9):1380-404. Review.

PMID:
21366526
47.

Homology modeling and docking evaluation of aminergic G protein-coupled receptors.

McRobb FM, Capuano B, Crosby IT, Chalmers DK, Yuriev E.

J Chem Inf Model. 2010 Apr 26;50(4):626-37. doi: 10.1021/ci900444q.

PMID:
20187660
48.

JL13 has clozapine-like actions on thermoregulatory cutaneous blood flow in rats: Involvement of serotonin 5-HT1A and 5-HT2A receptor mechanisms.

Capuano B, Crosby IT, McRobb FM, Taylor DA, Vom A, Blessing WW.

Prog Neuropsychopharmacol Biol Psychiatry. 2010 Feb 1;34(1):136-42. doi: 10.1016/j.pnpbp.2009.10.014. Epub 2009 Oct 29.

PMID:
19878703
49.

Di-tert-butyl N-[2,6-bis-(methoxy-meth-oxy)phen-yl]imino-diacetate.

Capuano B, Crosby IT, Forsyth CM, Khakham Y, Manallack DT.

Acta Crystallogr Sect E Struct Rep Online. 2009 Mar 25;65(Pt 4):o819. doi: 10.1107/S1600536809009246.

50.

2,2,7-Trichloro-3,4-dihydro-naphthalen-1(2H)-one.

Capuano B, Crosby IT, Forsyth CM, Shin JK.

Acta Crystallogr Sect E Struct Rep Online. 2009 Aug 26;65(Pt 9):o2254. doi: 10.1107/S1600536809032772.

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