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Department of Pharmacology




Preti B, Suchankova A, Deganutti G, Leuenberger M, Barkan K, Manulak I, Huang X, Carvalho S, Ladds G, Lochner M. (2022) Discovery and Structure-Activity Relationship Studies of Novel Adenosine A1 Receptor-Selective Agonists J Med Chem. 2022 Nov 10;65(21):14864-14890. doi: 10.1021/acs.jmedchem.2c01414.

Stampelou M, Suchankova A, Tzortzini E, Dhingra L, Barkan K, Lougiakis N, Marakos P, Pouli N, Ladds G, Kolocouris A. (2022) Dual A1/A3 Adenosine Receptor Antagonists: Binding Kinetics and Structure-Activity Relationship Studies Using Mutagenesis and Alchemical Binding Free Energy Calculations. J Med Chem. 2022 Oct 13;65(19):13305-13327. doi: 10.1021/acs.jmedchem.2c01123.

Shaw WM, Zhang Y, Lu X, Khalil AS, Ladds G, Luo X, Ellis T. (2022) Screening microbially produced Δ9-tetrahydrocannabinol using a yeast biosensor workflow Nat Commun. 2022 Jul 18;13(1):4150. doi: 10.1038/s41467-022-31652-2

Wall MJ, Hill E, Huckstepp R, Barkan K, Deganutti G, Leuenberger M, Preti B, Winfield I, Carvalho S, Suchankova A, Wei H, Safitri D, Huang X, Imlach W, La Mache C, Dean E, Hume C, Hayward S, Oliver J, Zhao FY, Spanswick D, Reynolds CA, Lochner M, Ladds G, Frenguelli BG. (2022) Nat Commun. 2022 Jul 18;13(1):4150. doi: 10.1038/s41467-022-31652-2.

Suchankova A, Stampelou M, Koutsouki K, Pousias A, Dhingra L, Barkan K, Pouli N, Marakos P, Tenta R, Kolocouris A, Lougiakis N, Ladds G. (2022) Discovery of a High Affinity Adenosine A1/A3 Receptor Antagonist with a Novel 7-Amino-pyrazolo[3,4- d]pyridazine Scaffold ACS Med Chem Lett. 2022 May 31;13(6):923-934. doi: 10.1021/acsmedchemlett.2c00052.

Pearce A, Redfern-Nichols T, Harris M, Poyner DR, Wigglesworth M, Ladds G. (2022).  Determining the Effects of Differential Expression of GRKs and β-arrestins on CLR-RAMP Agonist Bias. Front Physiol. 13: 840763. doi: 10.3389/fphys.2022.840763

Winfield, I. Ladds, G. (2022) The Role of ICL1 and H8 in Class B1 GPCRs; Implications for Receptor Activation. Front Endocrinol 12:792912. doi: 10.3389/fendo.2021.792912


Clark, A.J., Mullooly, N., Safitri, D., Harris, M., de Vries, T., MassenVanDenBrink, A., Poyner, D.R., Gianni, D., Wigglesworth, M. & Ladds. G. (2021) CGRP, adrenomedullin and adrenomedullin 2 display endogenous GPCR agonist bias in primary human cardiovascular cells. Commun. Biol. 4:776.

Deganutti, G., Barkan, K., Preti, B., Leuenberger, M., Wall, M., Frenguelli, B.G., Lochner, M., Ladds, G.* & Reynolds C. A.* (2021) Deciphering the Agonist Binding Mechanism to the Adenosine A1 Receptor. ACS Pharmacol. Transl. Sci.  DOI: acsptsci.0c00195. (* co-corresponding authors)

Suchankova, A., Harris, M., & Ladds, G. (2021) Measuring the rapid kinetics of receptor-ligand interactions in live cells using NanoBRET. Methods Cell Bio. DOI: 10.1016/bs.mcb.2021.06.013

Deganutti, G., Barkan, K., Ladds, G. & Reynolds C. A. (2021) Multisite Model of allosterism for the Adenosine A1 Receptor. J. Chem. Inf. Model 61: 2001.

Kopanitsa, L., Kopanitsa, M.V., Safitri, D., Ladds, G & Bailey, D.S. (2021) Suppression of Proliferation of Human Glioblastoma Cells by Combined Phosphodiesterase and Multidrug Resistance-Associated Protein 1 Inhibition. Int. J. Mol. Sci. 22: 9665.

Kalash, L., Winfiled, I., Safitri., …Ladds, G.* & Bender A.* (2021) Structure-based identification of dual ligands at the A2AR and PDE10A with anti-proliferative effects in lung cancer cell-lines. J. Cheminform. 13: 17. (* co-corresponding authors)

Carvalho, S., Pearce, A. & Ladds, G. (2021) Novel mathematical and computational models of G protein-coupled receptor signalling. Curr Opin. Endocrin. Metab. Res. 16: 28.

Rosa, M., Noel, T., Harris, M. & Ladds, G. (2021) Emerging roles of adhesion G protein-coupled receptors. Biochem. Soc. Trans. 20:BST20201144.

Dolezalova, N …Ladds, G., … Saeb-Parsy, K. (2021) Accelerating cryoprotectant diffusion kinetics improves cryopreservation of pancreatic islets. Sci. Rep. 11:10418.

Shapovalov, V., Kopanitsa, L., Pruteanu, L.-L., Ladds, G. & Bailey, D.S. (2021) Transcriptomics-Based Phenotypic Screening Supports Drug Discovery in Human Glioblastoma Cells. Cancers 13:3780.



Marti-Solano, M., Crilly, S.E., Malinverni, D., …Ladds, G. …. Babu, M.M. (2020) Combinatorial expression of functionally distinct GPCR isoforms can diversify receptor signalling response. Nature 588(7838):E24. doi: 10.1038/s41586-020-2999-9.

Barkan K, …Ladds G. (2020) Pharmacological characterisation of novel adenosine A 3 receptor antagonists. Sci Rep. 10:20781. 

Clark, A.J., & Ladds. G. (2020). “Adrenomedullin/Intermedin” Encyclopedia of Molecular Pharmacology 67383_0_En, (Chapter 5055-1).

Greenhalgh, J.C., Chandram, A., Harper, M.T., Ladds, G. & Rahman, T. (2020) Proposed model of the Dictyostelium cAMP receptors bound cAMP. J. Mol. Graph. Model. 100: 107662.

Safitri, D., Harris, M., …… Ladds, G. (2020) Elevated intracellular cAMP concentration mediates growth suppression in glioma cells. Biochem Pharmacol. 174:113823. doi: 10.1016/

Routledge, SJ, …… Ladds, G.* & Poyner, D.R.* (2020) Receptor component protein, an endogenous allosteric modulator of family B G protein coupled receptors. Biochim Biophys Acta Biomembr. 1862: 183174. (* co-corresponding authors).

Lagarias, P., Barkan, K., … Ladds, G.* and Kolocouoris, A.* (2020) Insights to the Binding of a Selective Adenosine A3 Receptor Antagonist Using Molecular Dynamic Simulations, MM-PBSA and MM-GBSA Free Energy Calculations, and Mutagenesis. J Chem Info Model 59: 5183-5197. (* co-corresponding authors).



MacKie, D.I., Nielsen, N.R., Harris, M., Singh. S., Davis, R.B., Dy, D., Ladds, G., and Caron, K.M. (2019) RAMP3 determines rapid recycling of atypical chemokine receptor-3 for guided angiogenesis. Proc. Natl. Acad. Sci. In Press (accepted 21.10.19).

Stamatis, D., Lagarias, P., Barkan, K., Vrontake, E., Ladds, G.* and Kolocouoris, A.* (2019) Structural Characterization of Agonist Binding to A3Adenosine Receptor through Biomolecular Simulations and Mutagenesis Experiments. J. Med. Chem. doi: 10.1021/acs.jmedchem.9b01164. (* co-corresponding authors).

Shaw, W.M., Yamauchi, H., Mead, J., Gowers, G.F., Oling, D., Larsson, N., Wigglesworth, M.*, Ladds, G.* and Ellis, T.* (2019) Engineering a model cell for rational tuning of GPCR signalling Cell. 177: 782-796. (* co-corresponding authors). (F1000Prime recommended).

Bailey, S., Harris, M……..Ladds, G.*, Poyner, D.* and Wheatley, M.* (2019) Interactions Between RAMP2 And CRF Receptors: The Effect Of Receptor Subtypes, Splice Variants And Cell Context. BBA – Biomembranes 1861: 997-1003. (* co-corresponding authors).

Neganova, I., Cotts, L., Gassner, K., Armstrong, L., Ladds, G. and Lako, M. (2019) EDG5 plays an important role in induction and maintenance of pluripotency. Stem Cell 37:318-331.

Bridge, L., Mead, J., Frattini, E., Winfield, I., and Ladds, G. (2018) Modelling and simulation of biased agonism dynamics at a G protein-coupled receptor. J. Theor. Biol. 7: 44-65.



Harris, M., Svensson, F., Kopanitsa, L., Ladds, G., and Bailey D. (2018) Emerging patents in the therapeutic areas of glioma and glioblastoma. Expert Opin. Ther. Pat. 28: 573-590.

Lazarus, K.A., …… Ladds, G., Liu, P., Evan, G., McCaughan, F., Le Quesne, J., Lee, J.H., Calado, D., and Khaled, W.T. (2018) BCL11A interacts with SOX2 to control the expression of epigenetic regulators in lung squamous cell carcinoma. Nat Commun. 20: 3327.



Kalash, L., Val., C., Azuaje, J., Loza, M.I., Svensson, F., Zoufir, A., Mervin, L., Ladds, G., Brea, J., Sotelo, E. and Bender, A. (2017) Computer-Aided Design of Multi-target Ligands at A1R, A2AR and PDE10A, Key Proteins in Neurodegenerative Diseases. J. Cheminform. 9(1):67.

Recino, A., Barkan ,K., Ladds, G., Cooke, A., Wong, F.S. and Wallberg, M. (2017) Hyperglycemia does not affect antigen specific activation and cytolytic killing by CD8+ T cells in vivo. Biosci Rep. 37(4): pii: BSR20171079.

Routledge, S.J., Ladds, G. and Poyner, D.R. (2017) The effects of RAMPs upon cell signalling. Mol Cell Endocrinol.  pii: S0303-7207(17)30198-3.



Weston, C., Winfield, I., Harris, M., Hodgson, R., Shah, A., Dowell, S.J., Moarec, J-C, Woodlock, D.A., Reynolds, C.A., Poyner, D.R., Watkins, H.A. and Ladds, G. (2016) Receptor activity modifying protein-directed G protein signaling specificity for the calcitonin gene-related peptide family of receptors. J. Biol. Chem. 91: 21925.

Hay, D.L., Walker, C.S., Gingell, J.J., Ladds, G., Reynolds, C.A. and Poyner, D.R. (2016) Receptor activity-modifying proteins; multifunctional G protein-coupled receptor accessory proteins. Biochem Soc Trans. 44: 568.

Knight, A., Hemmings, J.L., Frenguelli, B.G., Dowell, S.J., Lochner, M. and Ladds, G. (2016) Discovery of Novel Adenosine Receptor Agonists that Exhibit Subtype Selectivity. J. Med Chem. 59: 947.

Hennig, A., Markwart, R., Wolff, K., Schubert, K., Cui, Y., Prior, I.A., Esparza-Franco, M.A., Ladds, G. and Rubio I. (2016) Feedback activation of neurofibromin terminates growth factor-induced Ras activation. Cell Commun Signal.14: 5.



Weston, C., Li, J., Li, N., Barkan, G., Richards, G.O., Roberts, D., Skerry, T.M., Poyner, D., Pardamwar, M., Reynolds, C.A., Dowell, S., Willars, G. and Ladds, G. (2015) Erratum: Modulation of glucagon receptor pharmacology by RAMP2. J. Biol. Chem. 290: 23009.

Shigeto, M., Ramracheya, R., Cha, C-Y., Chibalina, M., Tarasov, A., Philippaert, K., Reinbothe, T., Rorsman, N., Salehi. A., Sones, W., Vergari, E., Weston, C., Gorelik, J., Katsura, M., Nikolaev, O., Vennekens, R., Zaccolo, M., Gallione, A., Johnson, P.R.V., Kaku, K., Ladds, G. and Rorsman, P. (2015) Physiological concentrations of GLP-1 increases insulin secretion in mouse and human pancreatic b-cells by PKC-dependent activation of TRPM4 channels. J Clin Invest. 125: 4714.

Prokic, E., Weston, C., Yamawaki, N., Hall, S., Stanford, I., Ladds, G. and Woodhall, G. (2015) Benzodiazepine-site modulation of tonic inhibition in fast spiking interneurons alters cortical oscillatory dynamics. Neuropharmacology. 95: 192.

Weston, C., Li, J., Li, N., Barkan, G., Richards, G.O., Roberts, D., Skerry, T.M., Poyner, D., Pardamwar, M., Reynolds, C.A., Dowell, S., Willars, G. and Ladds, G. (2015) Modulation of glucagon receptor pharmacology by RAMP2. J. Biol. Chem. 290: 23009.

Hennig, A., Markwart, R., Esparza-Franco, M.A., Ladds, G. and Rubio I. (2015) Ras activation revisited: role of GEF and GAP systems. Biol. Chem. 396: 831.

Croft, W., Elliott, C.M., Ladds, G., Stinner, B., Venkataraman, C., and Weston, C. (2015) Parameter identification problems in the modelling of cell motility. J. Math Biol. 71: 399-436. Note – authors in alphabetical order.

Lockley, R., Ladds, G. and Bretschneider, T. (2015) Image based validation of dynamical models for cell reorientation. Cytometry A. 87: 471.



Weston, C., Poyner, D., Patel, V., Dowell, S. and Ladds, G. (2014) Investigating G protein signaling bias at the glucagon-like peptide-1 receptor in yeast. Brit. J. Pharmacol. 171(15):3651-65.

Lock, A., Forfar, R., Weston, C., Bowsher, L., Reynolds, C., Ladds, G., Dixon, A.M. (2014) One Motif to Bind Them: A Transmembrane Motif of Two Small Residues Affects Oligomerization, Function, Localization, and Cross-talk Between Two Yeast GPCRs. Biochim. Biophys. Acta. 1838: 3036-51.

Croft, W. Hill, C., McCann, E., Bond, M., Esparza-Franco, A., Bennett, J., Rand, D., Davey, J., Ladds, G. (2013) A Physiologically Required GPCR - RGS Interaction that Compartmentalizes RGS Activity J. Biol. Chem. 288: 27327-42.



Weston, C., Bond, M., Croft, W., and Ladds, G. (2013) Oncogenic Ras mutations inhibits Cdc42-directed cell growth. – PLOS ONE 16;8(10):e77487. doi: 10.1371/journal.pone.0077487.

Mos, M., Esparza-Franco, A., Godfrey, E.L., Richardson, K. and Ladds, G. (2013) The Role of the RACK1 Orthologue Cpc2 in Modulating Cell Cycle Arrest in Fission Yeast. PLOS ONE doi/10.1371/journal.pone.0065927.

Bond, M., Croft, W., Tyson, R., Bretschneider, T., Davey, J. and Ladds G. (2013) Quantitative analysis of human ras localization and function in the fission yeast Schizosaccharomyces pombe. Yeast 30(4):145-56. doi: 10.1002/yea.2949.



Davey, J. and Ladds, G. (2011) Heterologous expression of GPCRs in fission yeast Methods Mol Biol. 746: 113-131.

A full list of publications before 2011 can be found on pubmed


Publications available on pre-print servers

Harris, M., Mackie, D., Pawlak, J.B., Carvalho, S.,  …Ladds, G* (2021) RAMPs regulate signalling bias and internalisation of the GIPR. bioRxiv 2021.04.08.436756; doi:

Wall, M.J. …Deganutti, G., …Reynolds, C. A., …Ladds, G.*, & Frenguelli, B. G.* (2020) A biased adenosine A1R agonist elicits analgesia without cardiorespiratory depression. bioRxiv 2020.04.04.023945; doi: Under revision Nat Comms. (* co-corresponding authors)

Recino, A., Barkan, K., Schmidt-Christensen, A. S., ….Ladds, G. & Wallberg, M. (2019) GLP-1R is downregulated in bet cells of NOD mice and T1D patients DOI: bioRxiv 845776; doi:

Guida, C., Miranda, C., Asterholm, I. W., Basco, D., Benrick, A., Chanclón, B., Chibalina, M., Harris, M., Kellard, J., McCulloch, L., Real, J. I., Rorsman, N., Yeung, H. Y., Reimann, F., Shigeto, M., Clark, A., Thornes, B., Rorsman, P., Ladds, G. and Ramracheya, R. (2019) Promiscuous receptor activation mediates glucagonostatic effects of GLP-1(9-36) and GLP-1(7-36). Available on BioRxiv -