Number of items: 58.
2021
Milligan, G. , Barki, N. and Tobin, A.
(2021)
Chemogenetic approaches to explore the functions of Free Fatty Acid Receptor 2.
Trends in Pharmacological Sciences,
(doi: 10.1016/j.tips.2020.12.003)
(PMID:33495026)
(In Press)
Morgan, D. C. et al.
(2021)
Stapled ACE2 peptidomimetics designed to target the SARS-CoV-2 spike protein do not prevent virus internalisation.
Peptide Science,
(doi: 10.1002/pep2.24217)
(Early Online Publication)
Scammells, P. J. et al.
(2021)
Development of novel 4‐arylpyridin‐2‐one and 6‐arylpyrimidin‐4‐one positive allosteric modulators of the M1 muscarinic acetylcholine receptor.
ChemMedChem, 16(1),
pp. 216-233.
(doi: 10.1002/cmdc.202000540)
(PMID:32851779)
2020
Marti-Solano, M. et al.
(2020)
Combinatorial expression of GPCR isoforms affects signalling and drug responses.
Nature, 587,
pp. 650-656.
(doi: 10.1038/s41586-020-2888-2)
(PMID:33149304)
Mahindra, A., Janha, O., Mapesa, K., Sanchez Azqueta, A., Alam, M. M. , Amambua-Ngwa, A., Nwakanma, D. C., Tobin, A. B. and Jamieson, A. G.
(2020)
Development of potent PfCLK3 inhibitors based on TCMDC-135051 as a new class of antimalarials.
Journal of Medicinal Chemistry, 63(17),
pp. 9300-9315.
(doi: 10.1021/acs.jmedchem.0c00451)
(PMID:32787140)
(PMCID:PMC7497403)
Marsango, S., Barki, N., Jenkins, L. , Tobin, A. B. and Milligan, G.
(2020)
Therapeutic validation of an orphan G protein-coupled receptor: the case of GPR84.
British Journal of Pharmacology,
(doi: 10.1111/bph.15248)
(PMID:32869860)
(Early Online Publication)
Prihandoko, R. et al.
(2020)
Pathophysiological regulation of lung function by the free fatty acid receptor FFA4.
Science Translational Medicine, 12(557),
eaaw9009.
(doi: 10.1126/scitranslmed.aaw9009)
(PMID:32817367)
Quon, T., Lin, L.-C., Ganguly, A., Tobin, A. B. and Milligan, G.
(2020)
Therapeutic opportunities and challenges in targeting the orphan G protein-coupled receptor GPR35.
ACS Pharmacology and Translational Science, 3(5),
pp. 801-812.
(doi: 10.1021/acsptsci.0c00079)
(PMID:33073184)
Vanaerschot, M. et al.
(2020)
Inhibition of resistance-refractory P. falciparum kinase PKG delivers prophylactic, blood stage, and transmission-blocking antiplasmodial activity.
Cell Chemical Biology, 27(7),
806-816.e8.
(doi: 10.1016/j.chembiol.2020.04.001)
(PMID:32359426)
(PMCID:PMC7369637)
Thompson, K. J. and Tobin, A. B.
(2020)
Crosstalk between the M1 muscarinic acetylcholine receptor and the endocannabinoid system: A relevance for Alzheimer's disease?
Cellular Signalling, 70,
109545.
(doi: 10.1016/j.cellsig.2020.109545)
(PMID:31978506)
(PMCID:PMC7184673)
Tobin, A. B. and Bradley, S. J.
(2020)
Editorial for Advances in G Protein-Coupled Receptor Signal Transduction Special Issue.
ACS Pharmacology and Translational Science, 3(2),
pp. 169-170.
(doi: 10.1021/acsptsci.0c00029)
(PMID:32296759)
Rexen Ulven, E. et al.
(2020)
Structure-activity relationship studies of tetrahydroquinolone free fatty acid receptor 3 modulators.
Journal of Medicinal Chemistry, 63(7),
pp. 3577-3595.
(doi: 10.1021/acs.jmedchem.9b02036)
(PMID:32141297)
(PMCID:PMC7307922)
Bradley, S. J. et al.
(2020)
Biased M1-muscarinic-receptor-mutant mice inform the design of next-generation drugs.
Nature Chemical Biology, 16(3),
pp. 240-249.
(doi: 10.1038/s41589-019-0453-9)
(PMID:32080630)
2019
Vuckovic, Z. et al.
(2019)
Crystal structure of the M5 muscarinic acetylcholine receptor.
Proceedings of the National Academy of Sciences of the United States of America, 116(51),
pp. 26001-26007.
(doi: 10.1073/pnas.1914446116)
(PMID:31772027)
(PMCID:PMC6926013)
Alam, M. M. et al.
(2019)
Validation of the protein kinase PfCLK3 as a multistage cross-species malarial drug target.
Science, 365(6456),
eaau1682.
(doi: 10.1126/science.aau1682)
(PMID:31467193)
Thompson, K.J., Khajehali, E., Molloy, C. , Valant, C., Bradley, S.J. , Sexton, P.M., Christopoulos, A. and Tobin, A.B.
(2019)
The In Vitro Characterisation of DREADD Agonist 21, a Novel Ligand for Muscarinic DREADD Receptors.
British Journal of Pharmacology 176(16): 3002-3003. Selected Abstract from Pharmacology 2018, London, UK, 18-20 Dec 2018.
(doi:10.1111/bph.14681)
Bolognini, D. et al.
(2019)
Chemogenetics defines receptor-mediated functions of short chain free fatty acids.
Nature Chemical Biology, 15(5),
pp. 489-498.
(doi: 10.1038/s41589-019-0270-1)
(PMID:30992568)
Mackenzie, A. E., Quon, T., Lin, L.-C., Hauser, A. S., Jenkins, L. , Inoue, A., Tobin, A. B. , Gloriam, D. E., Hudson, B. D. and Milligan, G.
(2019)
Receptor selectivity between the G proteins Gα12 and Gα13 is defined by a single leucine-to-isoleucine variation.
FASEB Journal, 33(4),
pp. 5005-5017.
(doi: 10.1096/fj.201801956R)
(PMID:30601679)
(PMCID:PMC6436656)
Jörg, M. et al.
(2019)
6-Phenylpyrimidin-4-ones as positive allosteric modulators at the M1 mAChR: the determinants of allosteric activity.
ACS Chemical Neuroscience, 10(3),
pp. 1099-1114.
(doi: 10.1021/acschemneuro.8b00613)
(PMID:30547573)
Mancini, S., Mahmud, Z. A., Jenkins, L. , Bolognini, D., Newman, R., Barnes, M., Edye, M. E., McMahon, S. B., Tobin, A. B. and Milligan, G.
(2019)
On-target and off-target effects of novel orthosteric and allosteric activators of GPR84.
Scientific Reports, 9,
1861.
(doi: 10.1038/s41598-019-38539-1)
(PMID:30755705)
(PMCID:PMC6372602)
Müskens, F. M., Ward, R. J., Herkt, D., van de Langemheen, H., Tobin, A. B. , Liskamp, R. M.J. and Milligan, G.
(2019)
Design, synthesis and evaluation of a diazirine photoaffinity probe for ligand-based receptor capture targeting G protein-coupled receptors.
Molecular Pharmacology, 95(2),
pp. 196-209.
(doi: 10.1124/mol.118.114249)
(PMID:30514721)
(PMCID:PMC6324650)
2018
Thompson, K. J. et al.
(2018)
DREADD agonist 21 is an effective agonist for muscarinic-based DREADDs in vitro and in vivo.
ACS Pharmacology and Translational Science, 1(1),
pp. 61-72.
(doi: 10.1021/acsptsci.8b00012)
(PMID:30868140)
(PMCID:PMC6407913)
Bourgognon, J.-M. , Spiers, J. G., Scheiblich, H., Antonov, A., Bradley, S. J. , Tobin, A. B. and Steinert, J. R.
(2018)
Alterations in neuronal metabolism contribute to the pathogenesis of prion disease.
Cell Death and Differentiation, 25(8),
pp. 1408-1425.
(doi: 10.1038/s41418-018-0148-x)
(PMID:29915278)
(PMCID:PMC6113283)
Khajehali, E., Valant, C., Jörg, M., Tobin, A. B. , Conn, P. J., Lindsley, C. W., Sexton, P. M., Scammells, P. J. and Christopoulos, A.
(2018)
Probing the binding site of novel selective positive allosteric modulators at the M1 muscarinic acetylcholine receptor.
Biochemical Pharmacology, 154,
pp. 243-254.
(doi: 10.1016/j.bcp.2018.05.009)
(PMID:29777683)
(PMCID:PMC6066355)
Bradley, S. J. , Tobin, A. B. and Prihandoko, R.
(2018)
Muscarinic acetylcholine receptors in the central nervous system.
Neuropharmacology, 136(Part C),
p. 361.
(doi: 10.1016/j.neuropharm.2018.06.012)
(PMID:29894772)
van der Westhuizen, E. T. et al.
(2018)
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.
Molecular Pharmacology, 94(1),
pp. 770-783.
(doi: 10.1124/mol.118.111633)
(PMID:29691279)
Bradley, S. J. , Tobin, A. B. and Prihandoko, R.
(2018)
The use of chemogenetic approaches to study the physiological roles of muscarinic acetylcholine receptors in the central nervous system.
Neuropharmacology, 136(Part C),
pp. 421-426.
(doi: 10.1016/j.neuropharm.2017.11.043)
(PMID:29191752)
Bradley, S. J. et al.
(2018)
Bitopic binding mode of an M1 muscarinic acetylcholine receptor agonist associated with adverse clinical trial outcomes.
Molecular Pharmacology, 93(6),
pp. 645-656.
(doi: 10.1124/mol.118.111872)
(PMID:29695609)
(PMCID:PMC5963591)
2017
Milligan, G. , Alvarez-Curto, E. , Hudson, B. D. , Prihandoko, R. and Tobin, A. B.
(2017)
FFA4/GPR120: pharmacology and therapeutic opportunities.
Trends in Pharmacological Sciences, 38(9),
pp. 809-821.
(doi: 10.1016/j.tips.2017.06.006)
(PMID:28734639)
(PMCID:PMC5582618)
Bradley, S. J. et al.
(2017)
M1 muscarinic allosteric modulators slow prion neurodegeneration and restore memory loss.
Journal of Clinical Investigation, 127(2),
pp. 487-499.
(doi: 10.1172/JCI87526)
(PMID:27991860)
(PMCID:PMC5272187)
2016
Alvarez-Curto, E. , Inoue, A., Jenkins, L. , Raihan, S. Z., Prihandoko, R., Tobin, A. B. and Milligan, G.
(2016)
Targeted elimination of G proteins and arrestins defines their specific contributions to both intensity and duration of G protein-coupled receptor signalling.
Journal of Biological Chemistry, 291(53),
pp. 27147-27159.
(doi: 10.1074/jbc.M116.754887)
(PMID:27852822)
(PMCID:PMC5207144)
Mitcheson, D. F. et al.
(2016)
A new tool for the chemical genetic investigation of the Plasmodium falciparum Pfnek-2 NIMA-related kinase.
Malaria Journal, 15(1),
535.
(doi: 10.1186/s12936-016-1580-3)
(PMID:27821169)
(PMCID:PMC510031)
Zindel, D., Engel, S., Bottrill, A. R., Pin, J.-P., Prézeau, L., Tobin, A. B. , Bünemann, M., Krasel, C. and Butcher, A. J.
(2016)
Identification of key phosphorylation sites in PTH1R that determine arrestin3 binding and fine-tune receptor signaling.
Biochemical Journal, 473(22),
pp. 4173-4192.
(doi: 10.1042/bcj20160740)
(PMID:27623777)
(PMCID:PMC5103873)
Bolognini, D. et al.
(2016)
A novel allosteric activator of free fatty acid 2 receptor displays unique Gi-functional bias.
Journal of Biological Chemistry, 291,
pp. 18915-18931.
(doi: 10.1074/jbc.M116.736157)
(PMID:27385588)
(PMCID:PMC5009265)
Butcher, A. J. et al.
(2016)
An antibody biosensor establishes the activation of the M1 muscarinic acetylcholine receptor during learning and memory.
Journal of Biological Chemistry, 291(17),
pp. 8862-8875.
(doi: 10.1074/jbc.M115.681726)
(PMID:26826123)
(PMCID:PMC4861454)
Bradley, S. J. et al.
(2016)
Mapping physiological G protein-coupled receptor signaling pathways reveals a role for receptor phosphorylation in airway contraction.
Proceedings of the National Academy of Sciences of the United States of America, 113(16),
pp. 4524-4529.
(doi: 10.1073/pnas.1521706113)
(PMID:27071102)
(PMCID:PMC4843461)
Nuber, S., Zabel, U., Lorenz, K., Nuber, A., Milligan, G. , Tobin, A. B. , Lohse, M. J. and Hoffmann, C.
(2016)
β-Arrestin biosensors reveal a rapid, receptor-dependent activation/deactivation cycle.
Nature, 531,
pp. 661-664.
(doi: 10.1038/nature17198)
(PMID:27007855)
Bouzo-Lorenzo, M., Santo-Zas, I., Lodeiro, M., Nogueiras, R., Casanueva, F. F., Castro, M., Pazos, Y., Tobin, A. B. , Butcher, A. J. and Camiña, J. P.
(2016)
Distinct phosphorylation sites on the ghrelin receptor, GHSR1a, establish a code that determines the functions of ß-arrestins.
Scientific Reports, 6,
p. 22495.
(doi: 10.1038/srep22495)
(PMID:26935831)
(PMCID:PMC4776146)
Bolognini, D., Tobin, A. B. , Milligan, G. and Moss, C. E.
(2016)
The pharmacology and function of receptors for short-chain fatty acids.
Molecular Pharmacology, 89(3),
pp. 388-398.
(doi: 10.1124/mol.115.102301)
(PMID:26719580)
Bradley, S. J. and Tobin, A. B.
(2016)
Design of next-generation G protein–coupled receptor drugs: linking novel pharmacology and in vivo animal models.
Annual Review of Pharmacology and Toxicology, 56(1),
pp. 535-559.
(doi: 10.1146/annurev-pharmtox-011613-140012)
(PMID:26738479)
Prihandoko, R., Alvarez-Curto, E. , Hudson, B. D. , Butcher, A. J., Ulven, T., Miller, A. M., Tobin, A. B. and Milligan, G.
(2016)
Distinct phosphorylation clusters determines the signalling outcome of the free fatty acid receptor FFA4/GPR120.
Molecular Pharmacology, 89(5),
pp. 505-520.
(doi: 10.1124/mol.115.101949)
(PMID:26873857)
2015
Rossi, M. et al.
(2015)
CK2 acts as a potent negative regulator of receptor-mediated insulin release in vitro and in vivo.
Proceedings of the National Academy of Sciences of the United States of America, 112(49),
E6818-E6824.
(doi: 10.1073/pnas.1519430112)
(PMID:26598688)
(PMCID:PMC4679045)
Schrage, R. et al.
(2015)
The experimental power of FR900359 to study Gq-regulated biological processes.
Nature Communications, 6,
p. 10156.
(doi: 10.1038/ncomms10156)
(PMID:26658454)
(PMCID:PMC4682109)
Brochet, M., Tobin, A. B. , Billker, O. and Doerig, C.
(2015)
The kinomics of malaria.
In: Kraatz, H.-B. and Martic, S. (eds.)
Kinomics: Approaches and applications.
Wiley-VCH: Weinheim, pp. 115-136.
ISBN 9783527337651
(doi:10.1002/9783527683031.ch5)
Mitcheson, D. F., Tobin, A. B. and Alam, M. M.
(2015)
Applying chemical genetic tools to the study of phospho-signalling pathways in malaria parasites.
Biochimica et Biophysica Acta: Proteins and Proteomics, 1854(10),
pp. 1650-1656.
(doi: 10.1016/j.bbapap.2015.06.014)
(PMID:26143498)
Willars, G. B., Tobin, A. B. and Challiss, R.A. J.
(2015)
British Pharmacological Society, 5th Focused Meeting on Cell Signalling: Matters arising ….
British Journal of Pharmacology, 172(13),
pp. 3194-3195.
(doi: 10.1111/bph.13171)
(PMID:26095874)
(PMCID:PMC4500359)
Prihandoko, R., Bradley, S. J. , Tobin, A. and Butcher, A. J.
(2015)
Determination of GPCR phosphorylation status: establishing a phosphorylation barcode.
Current Protocols in Pharmacology, 69,
2.13.1-2.13.26.
(doi: 10.1002/0471141755.ph0213s69)
(PMID:26344213)
Doerig, C., Rayner, J. C., Scherf, A. and Tobin, A. B.
(2015)
Post-translational protein modifications in malaria parasites.
Nature Reviews Microbiology, 13(3),
pp. 160-172.
(doi: 10.1038/nrmicro3402)
(PMID:25659318)
Zindel, D., Butcher, A. J., Al-Sabah, S., Lanzerstorfer, P., Weghuber, J., Tobin, A. B. , Bunemann, M. and Krasel, C.
(2015)
Engineered hyperphosphorylation of the 2-adrenoceptor prolongs arrestin-3 binding and induces arrestin internalization.
Molecular Pharmacology, 87(2),
pp. 349-362.
(doi: 10.1124/mol.114.095422)
(PMID:25425623)
(PMCID:PMC4293452)
Alam, M. M. et al.
(2015)
Phosphoproteomics reveals malaria parasite Protein Kinase G as a signalling hub regulating egress and invasion.
Nature Communications, 6,
7285.
(doi: 10.1038/ncomms8285)
(PMID:26149123)
(PMCID:PMC4507021)
2014
Kern, S. et al.
(2014)
Inhibition of the SR protein-phosphorylating CLK kinases of plasmodium falciparum impairs blood stage replication and malaria transmission.
PLoS ONE, 9(9),
e105732.
(doi: 10.1371/journal.pone.0105732)
(PMID:25188378)
(PMCID:PMC415485)
Tobin, A. and Prihandoko, R.
(2014)
Reply to "Letter to the editor: 'Systems biology versus reductionism in cell physiology'".
American Journal of Physiology: Cell Physiology, 307(3),
C310-C310.
(doi: 10.1152/ajpcell.00192.2014)
(PMID:25088763)
(PMCID:PMC4121582)
Prihandoko, R. and Tobin, A. B.
(2014)
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".
American Journal of Physiology: Cell Physiology, 307(2),
C121-C122.
(doi: 10.1152/ajpcell.00136.2014)
(PMID:24829494)
Butcher, A. J., Hudson, B. D. , Shimpukade, B., Alvarez-Curto, E. , Prihandoko, R., Ulven, T., Milligan, G. and Tobin, A. B.
(2014)
Concomitant action of structural elements and receptor phosphorylation determine arrestin-3 interaction with the free fatty acid receptor FFA4.
Journal of Biological Chemistry, 289,
pp. 18451-18465.
(doi: 10.1074/jbc.M114.568816)
(PMID:24817122)
(PMCID:PMC4140278)
Bradley, S. J. , Riaz, S. A. and Tobin, A.
(2014)
Employing novel animal models in the design of clinically efficacious GPCR ligands.
Current Opinion in Cell Biology, 27,
pp. 117-125.
(doi: 10.1016/j.ceb.2013.12.002)
(PMID:24680437)
(PMCID:PMC3989050)
Graciotti, M., Alam, M. , Solyakov, L., Schmid, R., Burley, G., Bottrill, A. R., Doerig, C., Cullis, P. and Tobin, A. B.
(2014)
Malaria protein kinase CK2 (PfCK2) shows novel mechanisms of regulation.
PLoS ONE, 9(3),
e85391.
(doi: 10.1371/journal.pone.0085391)
(PMID:24658579)
(PMCID:PMC3962329)
2012
Lasonder, E., Treeck, M., Alam, M. and Tobin, A. B.
(2012)
Insights into the Plasmodium falciparum schizont phospho-proteome.
Microbes and Infection, 14(10),
pp. 811-819.
(doi: 10.1016/j.micinf.2012.04.008)
(PMID:22569589)
2011
Solyakov, L. et al.
(2011)
Global kinomic and phospho-proteomic analyses of the human malaria parasite Plasmodium falciparum.
Nature Communications, 2,
565.
(doi: 10.1038/ncomms1558)
(PMID:22127061)
This list was generated on Tue Apr 20 07:31:16 2021 BST.