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1

Mechanisms of signalling and biased agonism in G protein-coupled receptors

Wootten, Denise, Christopoulos, Arthur, Marti-Solano, Maria, Babu, M. Madan, Sexton, Patrick M.

Journal:

Nature Reviews Molecular Cell Biology

Year:

2018

Language:

english

File:

PDF, 6.08 MB

english, 2018

2

Allosteric Modulation of G Protein–Coupled Receptors

May, Lauren T., Leach, Katie, Sexton, Patrick M., Christopoulos, Arthur

Journal:

Annual Review of Pharmacology

Year:

2007

Language:

english

File:

PDF, 643 KB

english, 2007

3

The Best of Both Worlds? Bitopic Orthosteric/Allosteric Ligands of G Protein–Coupled Receptors

Valant, Celine, Robert Lane, J., Sexton, Patrick M., Christopoulos, Arthur

Journal:

Annual Review of Pharmacology

Year:

2012

Language:

english

File:

PDF, 1.15 MB

english, 2012

4

Synthesis and cannabinoid activity of 1-substituted-indole-3-oxadiazole derivatives: Novel agonists for the CB1 receptor

Gerard P. Moloney, James A. Angus, Alan D. Robertson, Martin J. Stoermer, Michael Robinson, Christine E. Wright, Ken McRae, Arthur Christopoulos

Journal:

European Journal of Medicinal Chemistry

Year:

2008

Language:

english

File:

PDF, 1.44 MB

english, 2008

5

Scheme, based on travelling-waves, for the protection of major transmission lines

Christopoulos, Christos, Thomas, D.W.P., Wright, Arthur

Journal:

IEE Proceedings C Generation Transmission and Distribution

Year:

1988

Language:

english

File:

PDF, 974 KB

english, 1988

6

Allosteric modulation of G protein-coupled receptors: A pharmacological perspective

Peter Keov, Patrick M. Sexton, Arthur Christopoulos

Journal:

Neuropharmacology

Year:

2011

Language:

english

File:

PDF, 1.00 MB

english, 2011

7

A Simple Method for Quantifying Functional Selectivity and Agonist Bias

Kenakin, Terry, Watson, Christian, Muniz-Medina, Vanessa, Christopoulos, Arthur, Novick, Steven

Journal:

ACS Chemical Neuroscience

Year:

2012

Language:

english

File:

PDF, 3.92 MB

english, 2012

8

Kinetic and system bias as drivers of metabotropic glutamate receptor 5 allosteric modulator pharmacology

Sengmany, Kathy, Hellyer, Shane D., Albold, Sabine, Wang, Taide, Conn, P. Jeffrey, May, Lauren T., Christopoulos, Arthur, Leach, Katie, Gregory, Karen J.

Journal:

Neuropharmacology

Year:

2019

Language:

english

File:

PDF, 2.23 MB

english, 2019

9

[Handbook of Experimental Pharmacology] Muscarinic Receptors Volume 208 || Muscarinic Modulation of Striatal Function and Circuitry

Fryer, Allison D., Christopoulos, Arthur, Nathanson, Neil M.

Year:

2012

Language:

english

File:

PDF, 179 KB

english, 2012

10

Extracellular loops 2 and 3 of the calcitonin receptor selectively modify agonist binding and efficacy

Dal Maso, Emma, Zhu, Yue, Pham, Vi, Reynolds, Christopher A., Deganutti, Giuseppe, Hick, Caroline A., Yang, Dehua, Christopoulos, Arthur, Hay, Debbie L., Wang, Ming-Wei, Sexton, Patrick M., Furness, S

Journal:

Biochemical Pharmacology

Year:

2018

Language:

english

File:

PDF, 5.59 MB

english, 2018

11

Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders

Jeffrey Conn, P., Christopoulos, Arthur, Lindsley, Craig W.

Journal:

Nature Reviews Drug Discovery

Year:

2009

Language:

english

File:

PDF, 553 KB

english, 2009

12

[Handbook of Experimental Pharmacology] Muscarinic Receptors Volume 208 ||

Fryer, Allison D., Christopoulos, Arthur, Nathanson, Neil M.

Year:

2012

Language:

english

File:

PDF, 6.00 MB

english, 2012

13

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

Glukhova, Alisa, Thal, David M., Nguyen, Anh T., Vecchio, Elizabeth A., Jörg, Manuela, Scammells, Peter J., May, Lauren T., Sexton, Patrick M., Christopoulos, Arthur

Journal:

Year:

2017

Language:

english

File:

PDF, 7.46 MB

english, 2017

14

Muscarinic M5 receptors modulate ethanol seeking in rats

Berizzi, Alice E., Perry, Christina J., Shackleford, David M., Lindsley, Craig W., Jones, Carrie K., Chen, Nicola A., Sexton, Patrick M., Christopoulos, Arthur, Langmead, Christopher J., Lawrence, And

Journal:

Neuropsychopharmacology

Year:

2018

Language:

english

File:

PDF, 1.31 MB

english, 2018

15

To Bind or Not to Bind: Unravelling GPCR Polypharmacology

Sexton, Patrick M., Christopoulos, Arthur

Journal:

Year:

2018

Language:

english

File:

PDF, 473 KB

english, 2018

16

Allosteric Modulation as a Unifying Mechanism for Receptor Function and Regulation

Changeux, Jean-Pierre, Christopoulos, Arthur

Journal:

Year:

2016

Language:

english

File:

PDF, 2.77 MB

english, 2016

17

Overview of Receptor Allosterism

Christopoulos, Arthur

Journal:

Current Protocols in Pharmacology

Year:

2000

Language:

english

File:

PDF, 458 KB

english, 2000

18

THE CONCISE GUIDE TO PHARMACOLOGY 2017/18: G protein-coupled receptors

Alexander, Stephen PH, Christopoulos, Arthur, Davenport, Anthony P, Kelly, Eamonn, Marrion, Neil V, Peters, John A, Faccenda, Elena, Harding, Simon D, Pawson, Adam J, Sharman, Joanna L, Southan, Chris

Journal:

British Journal of Pharmacology

Year:

2017

Language:

english

File:

PDF, 3.71 MB

english, 2017

19

Emerging paradigms in GPCR allostery: implications for drug discovery

Wootten, Denise, Christopoulos, Arthur, Sexton, Patrick M.

Journal:

Nature Reviews Drug Discovery

Year:

2013

Language:

english

File:

PDF, 1.14 MB

english, 2013

20

ALLOSTERIC BINDING SITES ON CELL-SURFACE RECEPTORS: NOVEL TARGETS FOR DRUG DISCOVERY

Christopoulos, Arthur

Journal:

Nature Reviews Drug Discovery

Year:

2002

Language:

english

File:

PDF, 2.00 MB

english, 2002

21

Signalling bias in new drug discovery: detection, quantification and therapeutic impact

Kenakin, Terry, Christopoulos, Arthur

Journal:

Nature Reviews Drug Discovery

Year:

2012

Language:

english

File:

PDF, 1.02 MB

english, 2012

22

Structural insights into G-protein-coupled receptor allostery

Thal, David M., Glukhova, Alisa, Sexton, Patrick M., Christopoulos, Arthur

Journal:

Year:

2018

Language:

english

File:

PDF, 3.25 MB

english, 2018

23

ALLOSTERIC INTERACTIONS AT MUSCARINIC CHOLINOCEPTORS

Arthur Christopoulos, Alfred Lanzafame, Fred Mitchelson

Journal:

Clinical and Experimental Pharmacology and Physiology

Year:

1998

Language:

english

File:

PDF, 300 KB

english, 1998

24

Pharmacological analysis of cannabinoid receptor activity in the rat vas deferens

Arthur Christopoulos, Peter Coles, Lucy Lay, Michael J Lew, James A Angus

Journal:

British Journal of Pharmacology

Year:

2001

Language:

english

File:

PDF, 215 KB

english, 2001

25

Application of an Allosteric Ternary Complex Model to the Technique of Pharmacological Resultant Analysis

ARTHUR CHRISTOPOULOS, FRED MITCHELSON

Journal:

Journal of Pharmacy and Pharmacology

Year:

1997

Language:

english

File:

PDF, 545 KB

english, 1997

26

2-Aminothienopyridazines as Novel Adenosine A 1 Receptor Allosteric Modulators and Antagonists

Ferguson, Gemma N., Valant, Celine, Horne, James, Figler, Heidi, Flynn, Bernard L., Linden, Joel, Chalmers, David K., Sexton, Patrick M., Christopoulos, Arthur, Scammells, Peter J.

Journal:

Journal of Medicinal Chemistry

Year:

2008

Language:

english

File:

PDF, 147 KB

english, 2008

27

Synthesis and Pharmacological Evaluation of M 4 Muscarinic Receptor Positive Allosteric Modulators Derived from VU10004

Huynh, Tracey, Valant, Celine, Crosby, Ian T., Sexton, Patrick M., Christopoulos, Arthur, Capuano, Ben

Journal:

ACS Chemical Neuroscience

Year:

2015

Language:

english

File:

PDF, 975 KB

english, 2015

28

Editorial [Hot Topic: G Protein-Coupled Receptor Drug Targets (Executive Editors: P.M. Sexton and A. Christopoulos)]

Sexton, Patrick, Christopoulos, Arthur

Journal:

Current Pharmaceutical Design

Year:

2006

Language:

english

File:

PDF, 18 KB

english, 2006

29

The allosteric interaction of otenzepad (AF-DX 116) at muscarinic M2 receptors in guinea pig atria

Alfred Lanzafame, Arthur Christopoulos, Fred Mitchelson

Journal:

European Journal of Pharmacology

Year:

2001

Language:

english

File:

PDF, 100 KB

english, 2001

30

Impact of chronic congestive heart failure on pharmacokinetics and vasomotor effects of infused nitrite

Maher, Abdul R, Arif, Sayqa, Madhani, Melanie, Abozguia, Khalid, Ahmed, Ibrar, Fernandez, Bernadette O, Feelisch, Martin, O'Sullivan, AG, Christopoulos, Arthur, Sverdlov, Aaron L, Ngo, Doan, Dautov, R

Journal:

British Journal of Pharmacology

Year:

2013

Language:

english

File:

PDF, 1.16 MB

english, 2013

31

Minireview: Signal Bias, Allosterism, and Polymorphic Variation at the GLP-1R: Implications for Drug Discovery

Koole, Cassandra, Savage, Emilia E., Christopoulos, Arthur, Miller, Laurence J., Sexton, Patrick M., Wootten, Denise

Journal:

Molecular Endocrinology

Year:

2013

Language:

english

File:

PDF, 782 KB

english, 2013

32

Use of Cysteine Trapping to Map Spatial Approximations between Residues Contributing to the Helix N-capping Motif of Secretin and Distinct Residues within Each of the Extracellular Loops of Its Receptor

Dong, Maoqing, Lam, Polo C.-H., Orry, Andrew, Sexton, Patrick M., Christopoulos, Arthur, Abagyan, Ruben, Miller, Laurence J.

Journal:

Journal of Biological Chemistry

Year:

2016

Language:

english

File:

PDF, 4.30 MB

english, 2016

33

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, Emma T, Spathis, Arthur, Khajehali, Elham, Jorg, Maneula, Mistry, Shailesh N, Capuano, Ben, Tobin, Andrew B, Sexton, Patrick M., Scammells, Peter J, Valant, Celine, Christopoulos,

Journal:

Molecular Pharmacology

Year:

2018

Language:

english

File:

PDF, 2.59 MB

english, 2018

34

Regulation of serotonin 5-HT2C receptors by chronic ligand exposure

Mark G. Devlin, Nicola J. Smith, Olivia M. Ryan, Elizabeth Guida, Patrick M. Sexton, Arthur Christopoulos

Journal:

European Journal of Pharmacology

Year:

2004

Language:

english

File:

PDF, 305 KB

english, 2004

35

[Handbook of Experimental Pharmacology] Muscarinic Receptors Volume 208 || Structure–Function Studies of Muscarinic Acetylcholine Receptors

Fryer, Allison D., Christopoulos, Arthur, Nathanson, Neil M.

Year:

2012

Language:

english

File:

PDF, 452 KB

english, 2012

36

[Handbook of Experimental Pharmacology] Muscarinic Receptors Volume 208 || Muscarinic Receptor Agonists and Antagonists: Effects on Ocular Function

Fryer, Allison D., Christopoulos, Arthur, Nathanson, Neil M.

Year:

2012

Language:

english

File:

PDF, 293 KB

english, 2012

37

[Handbook of Experimental Pharmacology] Muscarinic Receptors Volume 208 || Activation of Muscarinic Receptors by Non-neuronal Acetylcholine

Fryer, Allison D., Christopoulos, Arthur, Nathanson, Neil M.

Year:

2012

Language:

english

File:

PDF, 457 KB

english, 2012

38

Assessing the distribution of parameters in models of ligand–receptor interaction: to log or not to log

Arthur Christopoulos

Journal:

Trends in Pharmacological Sciences

Year:

1998

Language:

english

File:

PDF, 168 KB

english, 1998

39

Insurmountable AT1 receptor antagonism: message in a model?

Michael Lew, Arthur Christopoulos, James Ziogas

Journal:

Trends in Pharmacological Sciences

Year:

2001

Language:

english

File:

PDF, 41 KB

english, 2001

40

Pharmacological analysis of the mode of interaction of McN-A-343 at atrial muscarinic M2 receptors

Arthur Christopoulos, Fred Mitchelson

Journal:

European Journal of Pharmacology

Year:

1997

Language:

english

File:

PDF, 93 KB

english, 1997

41

Positive and Negative Allosteric Modulators Promote Biased Signaling at the Calcium-Sensing Receptor

Davey, Anna E., Leach, Katie, Valant, Celine, Conigrave, Arthur D., Sexton, Patrick M., Christopoulos, Arthur

Journal:

Year:

2012

Language:

english

File:

PDF, 1.75 MB

english, 2012

42

Discovery of a Novel Class of Negative Allosteric Modulator of the Dopamine D 2 Receptor Through Fragmentation of a Bitopic Ligand

Mistry, Shailesh N, Shonberg, Jeremy, Draper-Joyce, Christopher J., Klein Herenbrink, Carmen, Michino, Mayako, Shi, Lei, Christopoulos, Arthur, Capuano, Ben, Scammells, Peter J., Lane, J. Robert

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 1.61 MB

english, 2015

43

Recent advances in the determination of G protein-coupled receptor structures

Thal, David M, Vuckovic, Ziva, Draper-Joyce, Christopher J, Liang, Yi-Lynn, Glukhova, Alisa, Christopoulos, Arthur, Sexton, Patrick M

Journal:

Current Opinion in Structural Biology

Year:

2018

Language:

english

File:

PDF, 876 KB

english, 2018

44

Benzodiazepine ligands can act as allosteric modulators of the Type 1 cholecystokinin receptor

Fan Gao, Patrick M. Sexton, Arthur Christopoulos, Laurence J. Miller

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2008

Language:

english

File:

PDF, 455 KB

english, 2008

45

[3H]N-methylscopolamine dissociation from muscarine receptors affected by low concentrations of allosteric modulators

Arthur Christopoulos, Fred Mitchelson

Journal:

European Journal of Pharmacology: Molecular Pharmacology

Year:

1995

Language:

english

File:

PDF, 301 KB

english, 1995

46

Spatiotemporal neural interactions underlying continuous drawing movements as revealed by magnetoencephalography

Vassilios N. Christopoulos, Arthur C. Leuthold…

Journal:

Experimental Brain Research

Year:

2012

Language:

english

File:

PDF, 917 KB

english, 2012

47

Functional and structural perspectives on allosteric modulation of GPCRs

Langmead, Christopher J, Christopoulos, Arthur

Journal:

Current Opinion in Cell Biology

Year:

2014

Language:

english

File:

PDF, 1.59 MB

english, 2014

48

Allostery in GPCRs: ‘MWC’ revisited

Meritxell Canals, Patrick M. Sexton, Arthur Christopoulos

Journal:

Trends in Biochemical Sciences

Year:

2011

Language:

english

File:

PDF, 1.09 MB

english, 2011

49

Consequences of splice variation on Secretin family G protein-coupled receptor function

Sebastian GB Furness, Denise Wootten, Arthur Christopoulos, Patrick M Sexton

Journal:

British Journal of Pharmacology

Year:

2012

Language:

english

File:

PDF, 2.46 MB

english, 2012

50

[Handbook of Experimental Pharmacology] Muscarinic Receptors Volume 208 || Muscarinic Pain Pharmacology: Realizing the Promise of Novel Analgesics by Overcoming Old Challenges

Fryer, Allison D., Christopoulos, Arthur, Nathanson, Neil M.

Year:

2012

Language:

english

File:

PDF, 297 KB

english, 2012

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