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Items: 1 to 50 of 134

1.

The effect of two selective A1 -receptor agonists and the bitopic ligand VCP746 on heart rate and regional vascular conductance in conscious rats.

Cooper SL, March J, Sabbatini AR, Hill SJ, Jörg M, Scammells PJ, Woolard J.

Br J Pharmacol. 2019 Oct 9. doi: 10.1111/bph.14870. [Epub ahead of print]

PMID:
31596949
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 Oct 23. doi: 10.1021/acs.jmedchem.9b00864. [Epub ahead of print]

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.

Cryptic pocket formation underlies allosteric modulator selectivity at muscarinic GPCRs.

Hollingsworth SA, Kelly B, Valant C, Michaelis JA, Mastromihalis O, Thompson G, Venkatakrishnan AJ, Hertig S, Scammells PJ, Sexton PM, Felder CC, Christopoulos A, Dror RO.

Nat Commun. 2019 Jul 23;10(1):3289. doi: 10.1038/s41467-019-11062-7.

5.

Novel Human Aminopeptidase N Inhibitors: Discovery and Optimization of Subsite Binding Interactions.

Lee J, Vinh NB, Drinkwater N, Yang W, Kannan Sivaraman K, Schembri LS, Gazdik M, Grin PM, Butler GS, Overall CM, Charman SA, McGowan S, Scammells PJ.

J Med Chem. 2019 Aug 8;62(15):7185-7209. doi: 10.1021/acs.jmedchem.9b00757. Epub 2019 Jul 18.

PMID:
31251594
6.

Unlocking the full potential of lipid-based formulations using lipophilic salt/ionic liquid forms.

Williams HD, Ford L, Igonin A, Shan Z, Botti P, Morgen MM, Hu G, Pouton CW, Scammells PJ, Porter CJH, Benameur H.

Adv Drug Deliv Rev. 2019 Mar 1;142:75-90. doi: 10.1016/j.addr.2019.05.008. Epub 2019 May 29. Review.

PMID:
31150666
7.

Effects of VCP979 Novel p38 Mitogen Activated Protein Kinase Inhibitor on Progression of Pancreatic Cancer in Mouse Model with Diabetic Conditions.

Xu T, Ding J, Ge H, Xu X, Scammells P, Wang B, Ju S.

J Biomed Nanotechnol. 2019 Jun 1;15(6):1325-1333. doi: 10.1166/jbn.2019.2775.

PMID:
31072439
8.

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
9.

Identification of the Binding Site of Apical Membrane Antigen 1 (AMA1) Inhibitors Using a Paramagnetic Probe.

Akter M, Drinkwater N, Devine SM, Drew SC, Krishnarjuna B, Debono CO, Wang G, Scanlon MJ, Scammells PJ, McGowan S, MacRaild CA, Norton RS.

ChemMedChem. 2019 Mar 5;14(5):603-612. doi: 10.1002/cmdc.201800802. Epub 2019 Feb 13.

PMID:
30653832
10.

Probe dependence of allosteric enhancers on the binding affinity of adenosine A1 -receptor agonists at rat and human A1 -receptors measured using NanoBRET.

Cooper SL, Soave M, Jörg M, Scammells PJ, Woolard J, Hill SJ.

Br J Pharmacol. 2019 Apr;176(7):864-878. doi: 10.1111/bph.14575. Epub 2019 Mar 6.

11.

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
12.

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
13.

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
14.

Enhancing the Oral Absorption of Kinase Inhibitors Using Lipophilic Salts and Lipid-Based Formulations.

Williams HD, Ford L, Han S, Tangso KJ, Lim S, Shackleford DM, Vodak DT, Benameur H, Pouton CW, Scammells PJ, Porter CJH.

Mol Pharm. 2018 Dec 3;15(12):5678-5696. doi: 10.1021/acs.molpharmaceut.8b00858. Epub 2018 Nov 13.

15.

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
16.
17.

Probing the binding site of novel selective positive allosteric modulators at the M1 muscarinic acetylcholine receptor.

Khajehali E, Valant C, Jörg M, Tobin AB, Conn PJ, Lindsley CW, Sexton PM, Scammells PJ, Christopoulos A.

Biochem Pharmacol. 2018 Aug;154:243-254. doi: 10.1016/j.bcp.2018.05.009. Epub 2018 May 17.

18.

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
19.

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
20.

Diffusion Tensor Imaging Evaluation of Axonal/White Matter Remodeling in a Mouse Model of Diabetic Stroke Treated with Novel p38 MAPK Inhibitor, VCP979.

Cai Y, Lu C, Xu T, Ma Y, Min S, Scammells P, Wang B, Ju S.

J Biomed Nanotechnol. 2018 Mar 1;14(3):585-593. doi: 10.1166/jbn.2018.2522.

PMID:
29663930
21.

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
22.

A Structure-Activity Relationship Study of Bitopic N6-Substituted Adenosine Derivatives as Biased Adenosine A1 Receptor Agonists.

Aurelio L, Baltos JA, Ford L, Nguyen ATN, Jörg M, Devine SM, Valant C, White PJ, Christopoulos A, May LT, Scammells PJ.

J Med Chem. 2018 Mar 8;61(5):2087-2103. doi: 10.1021/acs.jmedchem.8b00047. Epub 2018 Feb 23.

PMID:
29446948
23.

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.

24.

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.

25.

Fluorescently Labeled Morphine Derivatives for Bioimaging Studies.

Lam R, Gondin AB, Canals M, Kellam B, Briddon SJ, Graham B, Scammells PJ.

J Med Chem. 2018 Feb 8;61(3):1316-1329. doi: 10.1021/acs.jmedchem.7b01811. Epub 2018 Jan 10.

PMID:
29291353
26.

Ionic Liquid Forms of Weakly Acidic Drugs in Oral Lipid Formulations: Preparation, Characterization, in Vitro Digestion, and in Vivo Absorption Studies.

Sahbaz Y, Nguyen TH, Ford L, McEvoy CL, Williams HD, Scammells PJ, Porter CJH.

Mol Pharm. 2017 Nov 6;14(11):3669-3683. doi: 10.1021/acs.molpharmaceut.7b00442. Epub 2017 Oct 10.

PMID:
28954512
27.

Transformation of Biopharmaceutical Classification System Class I and III Drugs Into Ionic Liquids and Lipophilic Salts for Enhanced Developability Using Lipid Formulations.

Williams HD, Ford L, Lim S, Han S, Baumann J, Sullivan H, Vodak D, Igonin A, Benameur H, Pouton CW, Scammells PJ, Porter CJH.

J Pharm Sci. 2018 Jan;107(1):203-216. doi: 10.1016/j.xphs.2017.05.019. Epub 2017 May 23.

PMID:
28549907
28.

Structure of the Adenosine A1 Receptor Reveals the Basis for Subtype Selectivity.

Glukhova A, Thal DM, Nguyen AT, Vecchio EA, Jörg M, Scammells PJ, May LT, Sexton PM, Christopoulos A.

Cell. 2017 Feb 23;168(5):867-877.e13. doi: 10.1016/j.cell.2017.01.042.

29.

Novel Irreversible Agonists Acting at the A1 Adenosine Receptor.

Jörg M, Glukhova A, Abdul-Ridha A, Vecchio EA, Nguyen AT, Sexton PM, White PJ, May LT, Christopoulos A, Scammells PJ.

J Med Chem. 2016 Dec 22;59(24):11182-11194. doi: 10.1021/acs.jmedchem.6b01561. Epub 2016 Dec 13.

PMID:
27958734
30.

Antimalarial drug discovery targeting apical membrane antigen 1.

Devine SM, MacRaild CA, Norton RS, Scammells PJ.

Medchemcomm. 2016 Nov 4;8(1):13-20. doi: 10.1039/c6md00495d. eCollection 2017 Jan 1. Review.

31.

Role of the Second Extracellular Loop of the Adenosine A1 Receptor on Allosteric Modulator Binding, Signaling, and Cooperativity.

Nguyen AT, Vecchio EA, Thomas T, Nguyen TD, Aurelio L, Scammells PJ, White PJ, Sexton PM, Gregory KJ, May LT, Christopoulos A.

Mol Pharmacol. 2016 Dec;90(6):715-725. Epub 2016 Sep 28.

PMID:
27683013
32.

Positive Allosteric Modulation of the Muscarinic M1 Receptor Improves Efficacy of Antipsychotics in Mouse Glutamatergic Deficit Models of Behavior.

Choy KH, Shackleford DM, Malone DT, Mistry SN, Patil RT, Scammells PJ, Langmead CJ, Pantelis C, Sexton PM, Lane JR, Christopoulos A.

J Pharmacol Exp Ther. 2016 Nov;359(2):354-365. Epub 2016 Sep 14.

PMID:
27630144
33.

The hybrid molecule, VCP746, is a potent adenosine A2B receptor agonist that stimulates anti-fibrotic signalling.

Vecchio EA, Chuo CH, Baltos JA, Ford L, Scammells PJ, Wang BH, Christopoulos A, White PJ, May LT.

Biochem Pharmacol. 2016 Oct 1;117:46-56. doi: 10.1016/j.bcp.2016.08.007. Epub 2016 Aug 9.

PMID:
27520486
34.

Structure and substrate fingerprint of aminopeptidase P from Plasmodium falciparum.

Drinkwater N, Sivaraman KK, Bamert RS, Rut W, Mohamed K, Vinh NB, Scammells PJ, Drag M, McGowan S.

Biochem J. 2016 Oct 1;473(19):3189-204. doi: 10.1042/BCJ20160550. Epub 2016 Jul 26.

PMID:
27462122
35.

VCP746, a novel A1 adenosine receptor biased agonist, reduces hypertrophy in a rat neonatal cardiac myocyte model.

Chuo CH, Devine SM, Scammells PJ, Krum H, Christopoulos A, May LT, White PJ, Wang BH.

Clin Exp Pharmacol Physiol. 2016 Oct;43(10):976-82. doi: 10.1111/1440-1681.12616.

PMID:
27377874
36.

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
37.

Guidelines for the Synthesis of Small-Molecule Irreversible Probes Targeting G Protein-Coupled Receptors.

Jörg M, Scammells PJ.

ChemMedChem. 2016 Jul 19;11(14):1488-98. doi: 10.1002/cmdc.201600066. Epub 2016 Jun 27. Review.

PMID:
27347648
38.

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.

39.

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
40.

Potent dual inhibitors of Plasmodium falciparum M1 and M17 aminopeptidases through optimization of S1 pocket interactions.

Drinkwater N, Vinh NB, Mistry SN, Bamert RS, Ruggeri C, Holleran JP, Loganathan S, Paiardini A, Charman SA, Powell AK, Avery VM, McGowan S, Scammells PJ.

Eur J Med Chem. 2016 Mar 3;110:43-64. doi: 10.1016/j.ejmech.2016.01.015. Epub 2016 Jan 13.

PMID:
26807544
41.

Solution NMR characterization of apical membrane antigen 1 and small molecule interactions as a basis for designing new antimalarials.

Krishnarjuna B, Lim SS, Devine SM, Debono CO, Lam R, Chandrashekaran IR, Jaipuria G, Yagi H, Atreya HS, Scanlon MJ, MacRaild CA, Scammells PJ, Norton RS.

J Mol Recognit. 2016 Jun;29(6):281-91. doi: 10.1002/jmr.2529. Epub 2016 Jan 24.

PMID:
26804042
42.

Synthesis, Biological Evaluation, and Utility of Fluorescent Ligands Targeting the μ-Opioid Receptor.

Schembri LS, Stoddart LA, Briddon SJ, Kellam B, Canals M, Graham B, Scammells PJ.

J Med Chem. 2015 Dec 24;58(24):9754-67. doi: 10.1021/acs.jmedchem.5b01664. Epub 2015 Dec 16.

PMID:
26632862
43.

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
44.

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
45.

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
46.

Transformation of poorly water-soluble drugs into lipophilic ionic liquids enhances oral drug exposure from lipid based formulations.

Sahbaz Y, Williams HD, Nguyen TH, Saunders J, Ford L, Charman SA, Scammells PJ, Porter CJ.

Mol Pharm. 2015 Jun 1;12(6):1980-91. doi: 10.1021/mp500790t. Epub 2015 May 5.

PMID:
25905624
47.

Design, Synthesis, and Biological Evaluation of Tetra-Substituted Thiophenes as Inhibitors of p38α MAPK.

Vinh NB, Devine SM, Munoz L, Ryan RM, Wang BH, Krum H, Chalmers DK, Simpson JS, Scammells PJ.

ChemistryOpen. 2015 Feb;4(1):56-64. doi: 10.1002/open.201402076. Epub 2014 Nov 11.

48.

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
49.

Screening the Medicines for Malaria Venture "Malaria Box" against the Plasmodium falciparum aminopeptidases, M1, M17 and M18.

Paiardini A, Bamert RS, Kannan-Sivaraman K, Drinkwater N, Mistry SN, Scammells PJ, McGowan S.

PLoS One. 2015 Feb 20;10(2):e0115859. doi: 10.1371/journal.pone.0115859. eCollection 2015.

50.

Promiscuous 2-aminothiazoles (PrATs): a frequent hitting scaffold.

Devine SM, Mulcair MD, Debono CO, Leung EW, Nissink JW, Lim SS, Chandrashekaran IR, Vazirani M, Mohanty B, Simpson JS, Baell JB, Scammells PJ, Norton RS, Scanlon MJ.

J Med Chem. 2015 Feb 12;58(3):1205-14. doi: 10.1021/jm501402x. Epub 2015 Jan 16.

PMID:
25559643

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