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Items: 1 to 50 of 102

1.

On-target and off-target effects of novel orthosteric and allosteric activators of GPR84.

Mancini SJ, Mahmud ZA, Jenkins L, Bolognini D, Newman R, Barnes M, Edye ME, McMahon SB, Tobin AB, Milligan G.

Sci Rep. 2019 Feb 12;9(1):1861. doi: 10.1038/s41598-019-38539-1.

2.

Receptor selectivity between the G proteins Gα12 and Gα13 is defined by a single leucine-to-isoleucine variation.

Mackenzie AE, Quon T, Lin LC, Hauser AS, Jenkins L, Inoue A, Tobin AB, Gloriam DE, Hudson BD, Milligan G.

FASEB J. 2019 Jan 2:fj201801956R. doi: 10.1096/fj.201801956R. [Epub ahead of print]

3.

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. 2018 Dec 14. doi: 10.1021/acschemneuro.8b00613. [Epub ahead of print]

PMID:
30547573
4.

Design, Synthesis, and Evaluation of a Diazirine Photoaffinity Probe for Ligand-Based Receptor Capture Targeting G Protein-Coupled Receptors.

Müskens FM, Ward RJ, Herkt D, van de Langemheen H, Tobin AB, Liskamp RMJ, Milligan G.

Mol Pharmacol. 2019 Feb;95(2):196-209. doi: 10.1124/mol.118.114249. Epub 2018 Dec 4.

5.

Alterations in neuronal metabolism contribute to the pathogenesis of prion disease.

Bourgognon JM, Spiers JG, Scheiblich H, Antonov A, Bradley SJ, Tobin AB, Steinert JR.

Cell Death Differ. 2018 Aug;25(8):1408-1425. doi: 10.1038/s41418-018-0148-x. Epub 2018 Jun 18.

6.

Muscarinic acetylcholine receptors in the central nervous system.

Bradley SJ, Tobin AB, Prihandoko R.

Neuropharmacology. 2018 Jul 1;136(Pt C):361. doi: 10.1016/j.neuropharm.2018.06.012. Epub 2018 Jun 9. No abstract available.

PMID:
29894772
7.

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.

8.

Bitopic Binding Mode of an M1 Muscarinic Acetylcholine Receptor Agonist Associated with Adverse Clinical Trial Outcomes.

Bradley SJ, Molloy C, Bundgaard C, Mogg AJ, Thompson KJ, Dwomoh L, Sanger HE, Crabtree MD, Brooke SM, Sexton PM, Felder CC, Christopoulos A, Broad LM, Tobin AB, Langmead CJ.

Mol Pharmacol. 2018 Jun;93(6):645-656. doi: 10.1124/mol.118.111872. Epub 2018 Apr 25.

9.

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
10.

The use of chemogenetic approaches to study the physiological roles of muscarinic acetylcholine receptors in the central nervous system.

Bradley SJ, Tobin AB, Prihandoko R.

Neuropharmacology. 2018 Jul 1;136(Pt C):421-426. doi: 10.1016/j.neuropharm.2017.11.043. Epub 2017 Nov 27. Review.

PMID:
29191752
11.

Cohesiveness and flowability of particulated solid and semi-solid food systems.

Tobin AB, Heunemann P, Wemmer J, Stokes JR, Nicholson T, Windhab EJ, Fischer P.

Food Funct. 2017 Oct 18;8(10):3647-3653. doi: 10.1039/c7fo00715a.

PMID:
28914313
12.

FFA4/GPR120: Pharmacology and Therapeutic Opportunities.

Milligan G, Alvarez-Curto E, Hudson BD, Prihandoko R, Tobin AB.

Trends Pharmacol Sci. 2017 Sep;38(9):809-821. doi: 10.1016/j.tips.2017.06.006. Epub 2017 Jul 19. Review.

13.

M1 muscarinic allosteric modulators slow prion neurodegeneration and restore memory loss.

Bradley SJ, Bourgognon JM, Sanger HE, Verity N, Mogg AJ, White DJ, Butcher AJ, Moreno JA, Molloy C, Macedo-Hatch T, Edwards JM, Wess J, Pawlak R, Read DJ, Sexton PM, Broad LM, Steinert JR, Mallucci GR, Christopoulos A, Felder CC, Tobin AB.

J Clin Invest. 2017 Feb 1;127(2):487-499. doi: 10.1172/JCI87526. Epub 2016 Dec 19.

14.

Targeted Elimination of G Proteins and Arrestins Defines Their Specific Contributions to Both Intensity and Duration of G Protein-coupled Receptor Signaling.

Alvarez-Curto E, Inoue A, Jenkins L, Raihan SZ, Prihandoko R, Tobin AB, Milligan G.

J Biol Chem. 2016 Dec 30;291(53):27147-27159. doi: 10.1074/jbc.M116.754887. Epub 2016 Nov 16.

15.

A new tool for the chemical genetic investigation of the Plasmodium falciparum Pfnek-2 NIMA-related kinase.

Mitcheson DF, Bottrill AR, Carr K, Coxon CR, Cano C, Golding BT, Griffin RJ, Fry AM, Doerig C, Bayliss R, Tobin AB.

Malar J. 2016 Nov 7;15(1):535.

16.

Identification of key phosphorylation sites in PTH1R that determine arrestin3 binding and fine-tune receptor signaling.

Zindel D, Engel S, Bottrill AR, Pin JP, Prézeau L, Tobin AB, Bünemann M, Krasel C, Butcher AJ.

Biochem J. 2016 Nov 15;473(22):4173-4192. Epub 2016 Sep 13.

17.

A Novel Allosteric Activator of Free Fatty Acid 2 Receptor Displays Unique Gi-functional Bias.

Bolognini D, Moss CE, Nilsson K, Petersson AU, Donnelly I, Sergeev E, König GM, Kostenis E, Kurowska-Stolarska M, Miller A, Dekker N, Tobin AB, Milligan G.

J Biol Chem. 2016 Sep 2;291(36):18915-31. doi: 10.1074/jbc.M116.736157. Epub 2016 Jul 5.

18.

Mapping physiological G protein-coupled receptor signaling pathways reveals a role for receptor phosphorylation in airway contraction.

Bradley SJ, Wiegman CH, Iglesias MM, Kong KC, Butcher AJ, Plouffe B, Goupil E, Bourgognon JM, Macedo-Hatch T, LeGouill C, Russell K, Laporte SA, König GM, Kostenis E, Bouvier M, Chung KF, Amrani Y, Tobin AB.

Proc Natl Acad Sci U S A. 2016 Apr 19;113(16):4524-9. doi: 10.1073/pnas.1521706113. Epub 2016 Apr 8.

19.

β-Arrestin biosensors reveal a rapid, receptor-dependent activation/deactivation cycle.

Nuber S, Zabel U, Lorenz K, Nuber A, Milligan G, Tobin AB, Lohse MJ, Hoffmann C.

Nature. 2016 Mar 31;531(7596):661-4. doi: 10.1038/nature17198. Epub 2016 Mar 23.

20.

Distinct phosphorylation sites on the ghrelin receptor, GHSR1a, establish a code that determines the functions of ß-arrestins.

Bouzo-Lorenzo M, Santo-Zas I, Lodeiro M, Nogueiras R, Casanueva FF, Castro M, Pazos Y, Tobin AB, Butcher AJ, Camiña JP.

Sci Rep. 2016 Mar 3;6:22495. doi: 10.1038/srep22495.

21.

Distinct Phosphorylation Clusters Determine the Signaling Outcome of Free Fatty Acid Receptor 4/G Protein-Coupled Receptor 120.

Prihandoko R, Alvarez-Curto E, Hudson BD, Butcher AJ, Ulven T, Miller AM, Tobin AB, Milligan G.

Mol Pharmacol. 2016 May;89(5):505-20. doi: 10.1124/mol.115.101949. Epub 2016 Feb 12.

PMID:
26873857
22.

An Antibody Biosensor Establishes the Activation of the M1 Muscarinic Acetylcholine Receptor during Learning and Memory.

Butcher AJ, Bradley SJ, Prihandoko R, Brooke SM, Mogg A, Bourgognon JM, Macedo-Hatch T, Edwards JM, Bottrill AR, Challiss RA, Broad LM, Felder CC, Tobin AB.

J Biol Chem. 2016 Apr 22;291(17):8862-75. doi: 10.1074/jbc.M115.681726. Epub 2016 Jan 29.

23.

Design of Next-Generation G Protein-Coupled Receptor Drugs: Linking Novel Pharmacology and In Vivo Animal Models.

Bradley SJ, Tobin AB.

Annu Rev Pharmacol Toxicol. 2016;56:535-59. doi: 10.1146/annurev-pharmtox-011613-140012. Review.

PMID:
26738479
24.

The Pharmacology and Function of Receptors for Short-Chain Fatty Acids.

Bolognini D, Tobin AB, Milligan G, Moss CE.

Mol Pharmacol. 2016 Mar;89(3):388-98. doi: 10.1124/mol.115.102301. Epub 2015 Dec 30. Review.

PMID:
26719580
25.

The experimental power of FR900359 to study Gq-regulated biological processes.

Schrage R, Schmitz AL, Gaffal E, Annala S, Kehraus S, Wenzel D, Büllesbach KM, Bald T, Inoue A, Shinjo Y, Galandrin S, Shridhar N, Hesse M, Grundmann M, Merten N, Charpentier TH, Martz M, Butcher AJ, Slodczyk T, Armando S, Effern M, Namkung Y, Jenkins L, Horn V, Stößel A, Dargatz H, Tietze D, Imhof D, Galés C, Drewke C, Müller CE, Hölzel M, Milligan G, Tobin AB, Gomeza J, Dohlman HG, Sondek J, Harden TK, Bouvier M, Laporte SA, Aoki J, Fleischmann BK, Mohr K, König GM, Tüting T, Kostenis E.

Nat Commun. 2015 Dec 14;6:10156. doi: 10.1038/ncomms10156.

26.

CK2 acts as a potent negative regulator of receptor-mediated insulin release in vitro and in vivo.

Rossi M, Ruiz de Azua I, Barella LF, Sakamoto W, Zhu L, Cui Y, Lu H, Rebholz H, Matschinsky FM, Doliba NM, Butcher AJ, Tobin AB, Wess J.

Proc Natl Acad Sci U S A. 2015 Dec 8;112(49):E6818-24. doi: 10.1073/pnas.1519430112. Epub 2015 Nov 23.

27.

Determination of GPCR Phosphorylation Status: Establishing a Phosphorylation Barcode.

Prihandoko R, Bradley SJ, Tobin AB, Butcher AJ.

Curr Protoc Pharmacol. 2015 Jun 1;69:2.13.1-26. doi: 10.1002/0471141755.ph0213s69. Review.

PMID:
26344213
28.

Phosphoproteomics reveals malaria parasite Protein Kinase G as a signalling hub regulating egress and invasion.

Alam MM, Solyakov L, Bottrill AR, Flueck C, Siddiqui FA, Singh S, Mistry S, Viskaduraki M, Lee K, Hopp CS, Chitnis CE, Doerig C, Moon RW, Green JL, Holder AA, Baker DA, Tobin AB.

Nat Commun. 2015 Jul 7;6:7285. doi: 10.1038/ncomms8285.

29.

Applying chemical genetic tools to the study of phospho-signalling pathways in malaria parasites.

Mitcheson DF, Tobin AB, Alam MM.

Biochim Biophys Acta. 2015 Oct;1854(10 Pt B):1650-6. doi: 10.1016/j.bbapap.2015.06.014. Epub 2015 Jul 2. Review.

PMID:
26143498
30.

British Pharmacological Society, 5th Focused Meeting on Cell Signalling: Matters arising ….

Willars GB, Tobin AB, Challiss RA.

Br J Pharmacol. 2015 Jul;172(13):3194-5. doi: 10.1111/bph.13171. No abstract available.

31.

Post-translational protein modifications in malaria parasites.

Doerig C, Rayner JC, Scherf A, Tobin AB.

Nat Rev Microbiol. 2015 Mar;13(3):160-72. doi: 10.1038/nrmicro3402. Epub 2015 Feb 9. Review.

PMID:
25659318
32.

Engineered hyperphosphorylation of the β2-adrenoceptor prolongs arrestin-3 binding and induces arrestin internalization.

Zindel D, Butcher AJ, Al-Sabah S, Lanzerstorfer P, Weghuber J, Tobin AB, Bünemann M, Krasel C.

Mol Pharmacol. 2015 Feb;87(2):349-62. doi: 10.1124/mol.114.095422. Epub 2014 Nov 25.

33.

Inhibition of the SR protein-phosphorylating CLK kinases of Plasmodium falciparum impairs blood stage replication and malaria transmission.

Kern S, Agarwal S, Huber K, Gehring AP, Strödke B, Wirth CC, Brügl T, Abodo LO, Dandekar T, Doerig C, Fischer R, Tobin AB, Alam MM, Bracher F, Pradel G.

PLoS One. 2014 Sep 4;9(9):e105732. doi: 10.1371/journal.pone.0105732. eCollection 2014.

34.

Reply to "Letter to the editor: 'Systems biology versus reductionism in cell physiology'".

Tobin AB, Prihandoko R.

Am J Physiol Cell Physiol. 2014 Aug 1;307(3):C310. doi: 10.1152/ajpcell.00192.2014. No abstract available.

35.

Challenges of assigning protein kinases to in vivo phosphorylation events. Focus on "Use of LC-MS/MS and Bayes' theorem to identify protein kinases that phosphorylate aquaporin-2 at Ser256".

Prihandoko R, Tobin AB.

Am J Physiol Cell Physiol. 2014 Jul 15;307(2):C121-2. doi: 10.1152/ajpcell.00136.2014. Epub 2014 May 14. No abstract available.

36.

Concomitant action of structural elements and receptor phosphorylation determines arrestin-3 interaction with the free fatty acid receptor FFA4.

Butcher AJ, Hudson BD, Shimpukade B, Alvarez-Curto E, Prihandoko R, Ulven T, Milligan G, Tobin AB.

J Biol Chem. 2014 Jun 27;289(26):18451-65. doi: 10.1074/jbc.M114.568816. Epub 2014 May 9.

37.

Employing novel animal models in the design of clinically efficacious GPCR ligands.

Bradley SJ, Riaz SA, Tobin AB.

Curr Opin Cell Biol. 2014 Apr;27:117-25. doi: 10.1016/j.ceb.2013.12.002. Epub 2013 Dec 31. Review.

38.

Malaria protein kinase CK2 (PfCK2) shows novel mechanisms of regulation.

Graciotti M, Alam M, Solyakov L, Schmid R, Burley G, Bottrill AR, Doerig C, Cullis P, Tobin AB.

PLoS One. 2014 Mar 21;9(3):e85391. doi: 10.1371/journal.pone.0085391. eCollection 2014.

39.

ERK5 activation by Gq-coupled muscarinic receptors is independent of receptor internalization and β-arrestin recruitment.

Sánchez-Fernández G, Cabezudo S, García-Hoz C, Tobin AB, Mayor F Jr, Ribas C.

PLoS One. 2013 Dec 17;8(12):e84174. doi: 10.1371/journal.pone.0084174. eCollection 2013.

40.

The pharmacology of TUG-891, a potent and selective agonist of the free fatty acid receptor 4 (FFA4/GPR120), demonstrates both potential opportunity and possible challenges to therapeutic agonism.

Hudson BD, Shimpukade B, Mackenzie AE, Butcher AJ, Pediani JD, Christiansen E, Heathcote H, Tobin AB, Ulven T, Milligan G.

Mol Pharmacol. 2013 Nov;84(5):710-25. doi: 10.1124/mol.113.087783. Epub 2013 Aug 26.

41.

Identification of phosphorylation sites in the COOH-terminal tail of the μ-opioid receptor.

Chen YJ, Oldfield S, Butcher AJ, Tobin AB, Saxena K, Gurevich VV, Benovic JL, Henderson G, Kelly E.

J Neurochem. 2013 Jan;124(2):189-99. doi: 10.1111/jnc.12071. Epub 2012 Nov 30.

42.

A unique protein phosphatase with kelch-like domains (PPKL) in Plasmodium modulates ookinete differentiation, motility and invasion.

Guttery DS, Poulin B, Ferguson DJ, Szöőr B, Wickstead B, Carroll PL, Ramakrishnan C, Brady D, Patzewitz EM, Straschil U, Solyakov L, Green JL, Sinden RE, Tobin AB, Holder AA, Tewari R.

PLoS Pathog. 2012 Sep;8(9):e1002948. doi: 10.1371/journal.ppat.1002948. Epub 2012 Sep 20.

43.

Stimulus bias provides evidence for conformational constraints in the structure of a G protein-coupled receptor.

Gregory KJ, Sexton PM, Tobin AB, Christopoulos A.

J Biol Chem. 2012 Oct 26;287(44):37066-77. doi: 10.1074/jbc.M112.408534. Epub 2012 Sep 10.

44.

An evolutionary perspective on the kinome of malaria parasites.

Talevich E, Tobin AB, Kannan N, Doerig C.

Philos Trans R Soc Lond B Biol Sci. 2012 Sep 19;367(1602):2607-18. doi: 10.1098/rstb.2012.0014. Review.

45.

Insights into the Plasmodium falciparum schizont phospho-proteome.

Lasonder E, Treeck M, Alam M, Tobin AB.

Microbes Infect. 2012 Aug;14(10):811-9. doi: 10.1016/j.micinf.2012.04.008. Epub 2012 May 5. Review.

PMID:
22569589
46.

Influence of the accessory protein SET on M3 muscarinic receptor phosphorylation and G protein coupling.

Simon V, Oner SS, Cohen-Tannoudji J, Tobin AB, Lanier SM.

Mol Pharmacol. 2012 Jul;82(1):17-26. doi: 10.1124/mol.111.075523. Epub 2012 Mar 30.

47.

A putative homologue of CDC20/CDH1 in the malaria parasite is essential for male gamete development.

Guttery DS, Ferguson DJ, Poulin B, Xu Z, Straschil U, Klop O, Solyakov L, Sandrini SM, Brady D, Nieduszynski CA, Janse CJ, Holder AA, Tobin AB, Tewari R.

PLoS Pathog. 2012 Feb;8(2):e1002554. doi: 10.1371/journal.ppat.1002554. Epub 2012 Feb 23. Erratum in: PLoS Pathog. 2012 Mar;8(3). doi: 10.1371/annotation/ef70d427-0816-4a63-aeaf-874b734793b0.

48.

Physiological role of G-protein coupled receptor phosphorylation.

Butcher AJ, Kong KC, Prihandoko R, Tobin AB.

Handb Exp Pharmacol. 2012;(208):79-94. doi: 10.1007/978-3-642-23274-9_5. Review.

PMID:
22222696
49.

Global kinomic and phospho-proteomic analyses of the human malaria parasite Plasmodium falciparum.

Solyakov L, Halbert J, Alam MM, Semblat JP, Dorin-Semblat D, Reininger L, Bottrill AR, Mistry S, Abdi A, Fennell C, Holland Z, Demarta C, Bouza Y, Sicard A, Nivez MP, Eschenlauer S, Lama T, Thomas DC, Sharma P, Agarwal S, Kern S, Pradel G, Graciotti M, Tobin AB, Doerig C.

Nat Commun. 2011 Nov 29;2:565. doi: 10.1038/ncomms1558.

PMID:
22127061
50.

The role of M(3)-muscarinic receptor signaling in insulin secretion.

Kong KC, Tobin AB.

Commun Integr Biol. 2011 Jul;4(4):489-91. doi: 10.4161/cib.4.4.15716. Epub 2011 Jul 1.

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