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2020

Acetylcholine Muscarinic M4 Receptors as a Therapeutic Target for Alcohol Use Disorder: Converging Evidence From Humans and Rodents

Walker, L. C., Berizzi, A. E., Chen, N. A., Rueda, P., Perreau, V. M., Huckstep, K., Srisontiyakul, J., Govitrapong, P., Xiaojian, J., Lindsley, C. W., Jones, C. K., Riddy, D. M., Christopoulos, A., Langmead, C. J. & Lawrence, A. J., 28 Feb 2020, (Accepted/In press) In : Biological Psychiatry. 12 p.

Research output: Contribution to journalArticleResearchpeer-review

1 Citation (Scopus)

Activation of canonical BMP4-Smad7 signaling suppresses breast cancer metastasis

Eckhardt, B. L., Cao, Y., Redfern, A. D., Chi, L. H., Burrows, A. D., Roslan, S., Sloan, E. K., Parker, B. S., Loi, S., Ueno, N. T., Lau, P. K. H., Latham, B. & Anderson, R. L., 15 Mar 2020, In : Cancer Research. 80, 6, p. 1304-1315 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Activation of the GLP-1 receptor by a non-peptidic agonist

Zhao, P., Liang, Y. L., Belousoff, M. J., Deganutti, G., Fletcher, M. M., Willard, F. S., Bell, M. G., Christe, M. E., Sloop, K. W., Inoue, A., Truong, T. T., Clydesdale, L., Furness, S. G. B., Christopoulos, A., Wang, M. W., Miller, L. J., Reynolds, C. A., Danev, R., Sexton, P. M. & Wootten, D., 8 Jan 2020, In : Nature. 577, 7790, p. 432-436 5 p.

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11 Citations (Scopus)

A CX3CR1 Reporter hESC Line Facilitates Integrative Analysis of In-Vitro-Derived Microglia and Improved Microglia Identity upon Neuron-Glia Co-culture

Grubman, A., Vandekolk, T. H., Schröder, J., Sun, G., Hatwell-Humble, J., Chan, J., Oksanen, M., Lehtonen, S., Hunt, C., Koistinaho, J. E., Nilsson, S. K., Haynes, J. M., Pouton, C. W. & Polo, J. M., 9 Jun 2020, In : Stem Cell Reports. 14, 6, p. 1018-1032 15 p.

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Application of a Sulfoxonium Ylide Electrophile to Generate Cathepsin X-Selective Activity-Based Probes

Mountford, S. J., Anderson, B. M., Xu, B., Tay, E. S. V., Szabo, M., Hoang, M-L., Diao, J., Aurelio, L., Campden, R. I., Lindström, E., Sloan, E. K., Yates, R. M., Bunnett, N. W., Thompson, P. E. & Edgington-Mitchell, L. E., 20 Mar 2020, In : ACS Chemical Biology. 15, 3, p. 718-727 10 p.

Research output: Contribution to journalArticleResearchpeer-review

Automatic local resolution-based sharpening of cryo-EM maps

Ramírez-Aportela, E., Vilas, J. L., Glukhova, A., Melero, R., Conesa, P., Martínez, M., Maluenda, D., Mota, J., Jiménez, A., Vargas, J., Marabini, R., Sexton, P. M., Carazo, J. M. & Sorzano, C. O. S., 1 Feb 2020, In : Bioinformatics. 36, 3, p. 765-772 8 p.

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7 Citations (Scopus)

Basic Mechanisms of Diabetic Heart Disease

Ritchie, R. H. & Dale Abel, E., 22 May 2020, In : Circulation Research. 126, 11, p. 1501-1525 25 p.

Research output: Contribution to journalArticleResearchpeer-review

4 Citations (Scopus)

Biased M1-muscarinic-receptor-mutant mice inform the design of next-generation drugs

Bradley, S. J., Molloy, C., Valuskova, P., Dwomoh, L., Scarpa, M., Rossi, M., Finlayson, L., Svensson, K. A., Chernet, E., Barth, V. N., Gherbi, K., Sykes, D. A., Wilson, C. A., Mistry, R., Sexton, P. M., Christopoulos, A., Mogg, A. J., Rosethorne, E. M., Sakata, S., John Challiss, R. A. & 2 others, Broad, L. M. & Tobin, A. B., 20 Feb 2020, In : Nature Chemical Biology. 16, 3, p. 240-249 10 p.

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2 Citations (Scopus)

Cellular Interactions of Liposomes and PISA Nanoparticles during Human Blood Flow in a Microvascular Network

Vu, M. N., Kelly, H. G., Wheatley, A. K., Peng, S., Pilkington, E. H., Veldhuis, N. A., Davis, T. P., Kent, S. J. & Truong, N. P., 25 Jun 2020, (Accepted/In press) In : Small. 12 p.

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Characterization of the Core Ribosomal Binding Region for the Oxazolidone Family of Antibiotics Using Cryo-EM

Wright, A., Deane-Alder, K., Marschall, E., Bamert, R., Venugopal, H., Lithgow, T., Lupton, D. W. & Belousoff, M. J., 12 Jun 2020, In : ACS Pharmacology & Translational Science. 3, 3, p. 425-432 8 p.

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Detailed In Vitro Pharmacological Characterization of Clinically Tested Negative Allosteric Modulators of the Metabotropic Glutamate Receptor 5

Arsova, A., Møller, T. C., Vedel, L., Hansen, J. L., Foster, S. R., Gregory, K. J. & Bräuner-Osborne, H., 1 Jul 2020, In : Molecular Pharmacology. 98, 1, p. 49-60 12 p.

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Development of Clickable Photoaffinity Ligands for Metabotropic Glutamate Receptor 2 Based on Two Positive Allosteric Modulator Chemotypes

Hellyer, S. D., Aggarwal, S., Chen, A. N. Y., Leach, K., Lapinsky, D. J. & Gregory, K. J., 3 Jun 2020, In : ACS Chemical Neuroscience. 11, 11, p. 1597-1609 13 p.

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Differential contribution of metabotropic glutamate receptor 5 common allosteric binding site residues to biased allosteric agonism

Sengmany, K., Hellyer, S. D., Christopoulos, A., Lapinsky, D. J., Leach, K. & Gregory, K. J., 5 May 2020, (Accepted/In press) In : Biochemical Pharmacology. 15 p., 114011.

Research output: Contribution to journalArticleResearchpeer-review

1 Citation (Scopus)

Effects of chronic silencing of relaxin-3 production in nucleus incertus neurons on food intake, body weight, anxiety-like behaviour and limbic brain activity in female rats

de Ávila, C., Chometton, S., Ma, S., Pedersen, L. T., Timofeeva, E., Cifani, C. & Gundlach, A. L., Apr 2020, In : Psychopharmacology. 237, 4, p. 1091-1106 16 p.

Research output: Contribution to journalArticleResearchpeer-review

1 Citation (Scopus)

Endosomal Signaling of Delta Opioid Receptors Is an Endogenous Mechanism and Therapeutic Target for Relief From Inflammatory Pain

Jiménez-Vargas, N. N., Gong, J., Wisdom, M. J., Jensen, D. D., Latorre, R., Hegron, A., Teng, S. L., Di Cello, J., Rajasekhar, P., Veldhuis, N. A., Carbone, S., Yu, Y., Lopez, C. L., Polanco, J. J., Canals, M., Reed, D., Lomax, A. E., Schmidt, B. L., Leong, K. W., Vanner, S. & 3 others, Halls, M. L., Bunnett, N. & Poole, D. P., Jun 2020, (Accepted/In press) In : Proceedings of the National Academy of Sciences of the United States of America. 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Engaging older people as university-based instructors: A model to improve the empathy and attitudes of pharmacists in training

Abeyaratne, C., Bell, J. S., Dean, L., White, P. & Maher-Sturgess, S., 1 Jan 2020, In : Currents in Pharmacy Teaching and Learning. 12, 1, p. 58-64 7 p.

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Evaluation of Operational Models of Agonism and Allosterism at Receptors with Multiple Orthosteric Binding Sites

Gregory, K., Giraldo, J., Diao, J., Christopoulos, A. & Leach, K., 2020, In : Molecular Pharmacology. 97, 1, p. 35-45 11 p.

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2 Citations (Scopus)

Granulocyte-macrophage colony stimulating factor as an indirect mediator of nociceptor activation and pain

Tewari, D., Cook, A., Lee, M. C., Christensen, A. D., Croxford, A. L., Becher, B., Poole, D. P., Rajasekhar, P., Bunnett, N., Smith, J. E., Hamilton, J. A. & McMahon, S. B., 11 Mar 2020, In : Journal of Neuroscience. 40, 11, p. 2189-2199 11 p.

Research output: Contribution to journalArticleResearchpeer-review

1 Citation (Scopus)

Granzyme A in Chikungunya and Other Arboviral Infections

Schanoski, A. S., Le, T. T., Kaiserman, D., Rowe, C., Prow, N. A., Barboza, D. D., Santos, C. A., Zanotto, P. M. A., Magalhães, K. G., Aurelio, L., Muller, D., Young, P., Zhao, P., Bird, P. I. & Suhrbier, A., 14 Jan 2020, In : Frontiers in Immunology. 10, 14 p., 3083.

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2 Citations (Scopus)

Identification of monellin as the first naturally derived proteinaceous allosteric agonist of metabotropic glutamate receptor 5

Chen, A. N. Y., Hellyer, S. D., Trinh, P. N. H., Leach, K. & Gregory, K. J., Jun 2020, In : Basic & Clinical Pharmacology & Toxicology. 126, S6, p. 104-115 12 p.

Research output: Contribution to journalArticleResearchpeer-review

1 Citation (Scopus)

Inflammation without pain: Immune-derived opioids hold the key

Carbone, S. & Poole, D. P., 1 Feb 2020, In : Neurogastroenterology and Motility. 32, 2, 5 p., e13787.

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Intravascular Follistatin gene delivery improves glycemic control in a mouse model of type 2 diabetes

Davey, J. R., Estevez, E., Thomson, R. E., Whitham, M., Watt, K. I., Hagg, A., Qian, H., Henstridge, D. C., Ludlow, H., Hedger, M. P., McGee, S. L., Coughlan, M. T., Febbraio, M. A. & Gregorevic, P., Apr 2020, In : The FASEB Journal. 34, 4, p. 5697-5714 18 p.

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1 Citation (Scopus)

Low intrinsic efficacy for G protein activation can explain the improved side effect profiles of new opioid agonists

Gillis, A., Gondin, A. B., Kliewer, A., Sanchez, J., Lim, H. D., Alamein, C., Manandhar, P., Santiago, M., Fritzwanker, S., Schmiedel, F., Katte, T. A., Reekie, T. A., Grimsey, N. L., Kassiou, M., Kellam, B., Krasel, C., Halls, M. L., Connor, M., Lane, J. R., Schulz, S. & 2 others, Christie, M. J. & Canals, M., 31 Mar 2020, In : Science Signaling. 13, 625, 18 p., eaaz3140.

Research output: Contribution to journalArticleResearchpeer-review

4 Citations (Scopus)

Modelling lyssavirus infections in human stem cell-derived neural cultures

Sundaramoorthy, V., Godde, N., Farr, R. J., Green, D., Haynes, J. M., Bingham, J., O’Brien, C. M. & Dearnley, M., 25 Mar 2020, In : Viruses. 12, 4, 24 p., 359.

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Molecular Basis for Hormone Recognition and Activation of Corticotropin-Releasing Factor Receptors

Ma, S., Shen, Q., Zhao, L. H., Mao, C., Zhou, X. E., Shen, D. D., de Waal, P. W., Bi, P., Li, C., Jiang, Y., Wang, M. W., Sexton, P. M., Wootten, D., Melcher, K., Zhang, Y. & Xu, H. E., 6 Feb 2020, In : Molecular Cell. 77, 3, p. 669-680.e4 16 p.

Research output: Contribution to journalArticleResearchpeer-review

5 Citations (Scopus)

Mu and Delta Opioid Receptors Are Coexpressed and Functionally Interact in the Enteric Nervous System of the Mouse Colon

DiCello, J. J., Carbone, S. E., Saito, A., Rajasekhar, P., Ceredig, R. A., Pham, V., Valant, C., Christopoulos, A., Veldhuis, N. A., Canals, M., Massotte, D. & Poole, D. P., Mar 2020, In : Cellular and Molecular Gastroenterology and Hepatology. 9, 3, p. 465-483 19 p.

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1 Citation (Scopus)

Negative allosteric modulators of the human calcium-sensing receptor bind to overlapping and distinct sites within the 7-transmembrane domain

Josephs, T. M., Keller, A. N., Khajehali, E., DeBono, A., Langmead, C. J., Conigrave, A. D., Capuano, B., Kufareva, I., Gregory, K. J. & Leach, K., Apr 2020, In : British Journal of Pharmacology. 177, 8, p. 1917-1930 14 p.

Research output: Contribution to journalArticleResearchpeer-review

1 Citation (Scopus)

Nitric Oxide Resistance, Induced in the Myocardium by Diabetes, Is Circumvented by the Nitric Oxide Redox Sibling, Nitroxyl

Qin, C. X., Anthonisz, J., Leo, C. H., Kahlberg, N., Velagic, A., Li, M., Jap, E., Woodman, O. L., Parry, L. J., Horowitz, J. D., Kemp-Harper, B. K. & Ritchie, R. H., 1 Jan 2020, In : Antioxidants and Redox Signaling. 32, 1, p. 60-78 19 p.

Research output: Contribution to journalArticleResearchpeer-review

3 Citations (Scopus)

Pharmacological characterization of mono-, dual- and tri-peptidic agonists at GIP and GLP-1 receptors

Yuliantie, E., Darbalaei, S., Dai, A., Zhao, P., Yang, D., Sexton, P. M., Wang, M-W. & Wootten, D., Jul 2020, In : Biochemical Pharmacology. 177, 13 p., 114001.

Research output: Contribution to journalArticleResearchpeer-review

1 Citation (Scopus)

Polymers with Dithiobenzoate End Groups Constitutively Release Hydrogen Sulfide upon Exposure to Cysteine and Homocysteine

Urquhart, M. C., Dao, N. V., Ercole, F., Boyd, B. J., Davis, T. P., Whittaker, M. R. & Quinn, J. F., 21 Apr 2020, In : ACS Macro Letters. 9, 4, p. 553-557 5 p.

Research output: Contribution to journalArticleResearchpeer-review

Ptpn6 inhibits caspase-8- and Ripk3/Mlkl-dependent inflammation

Speir, M., Nowell, C. J., Chen, A. A., O’Donnell, J. A., Shamie, I. S., Lakin, P. R., D’Cruz, A. A., Braun, R. O., Babon, J. J., Lewis, R. S., Bliss-Moreau, M., Shlomovitz, I., Wang, S., Cengia, L. H., Stoica, A. I., Hakem, R., Kelliher, M. A., O’Reilly, L. A., Patsiouras, H., Lawlor, K. E. & 5 others, Weller, E., Lewis, N. E., Roberts, A. W., Gerlic, M. & Croker, B. A., 1 Jan 2020, In : Nature Immunology. 21, 1, p. 54-64 11 p.

Research output: Contribution to journalArticleResearchpeer-review

2 Citations (Scopus)

Qualitative evaluation of how a virtual dementia experience impacts medical and pharmacy students’ self-reported knowledge and attitudes towards people with dementia

Gilmartin-Thomas, J. F-M., McNeil, J., Powell, A., Malone, D. T., Larson, I. C., O’Reilly, C. L., Kirkpatrick, C. M., Kipen, E., Petrovich, T., Ryan-Atwood, T. E. & Bell, J. S., Feb 2020, In : Dementia. 19, 2, p. 205-220 16 p.

Research output: Contribution to journalArticleResearchpeer-review

2 Citations (Scopus)

Rational development of a high-affinity secretin receptor antagonist

Dong, M., Harikumar, K. G., Raval, S. R., Milburn, J. E., Clark, C., Alcala-Torano, R., Mobarec, J. C., Reynolds, C. A., Ghirlanda, G., Christopoulos, A., Wootten, D., Sexton, P. M. & Miller, L. J., Jul 2020, In : Biochemical Pharmacology. 177, 13 p., 113929.

Research output: Contribution to journalArticleResearchpeer-review

Roadmap for the Emerging Field of Cancer Neuroscience

Monje, M., Borniger, J. C., D'Silva, N. J., Deneen, B., Dirks, P. B., Fattahi, F., Frenette, P. S., Garzia, L., Gutmann, D. H., Hanahan, D., Hervey-Jumper, S. L., Hondermarck, H., Hurov, J. B., Kepecs, A., Knox, S. M., Lloyd, A. C., Magnon, C., Saloman, J. L., Segal, R. A., Sloan, E. K. & 8 others, Sun, X., Taylor, M. D., Tracey, K. J., Trotman, L. C., Tuveson, D. A., Wang, T. C., White, R. A. & Winkler, F., 16 Apr 2020, In : Cell. 181, 2, p. 219-222 4 p.

Research output: Contribution to journalArticleOtherpeer-review

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1 Citation (Scopus)

Sex-specific adipose tissue imprinting of regulatory T cells

Vasanthakumar, A., Chisanga, D., Blume, J., Gloury, R., Britt, K., Henstridge, D. C., Zhan, Y., Torres, S. V., Liene, S., Collins, N., Cao, E., Sidwell, T., Li, C., Spallanzani, R. G., Liao, Y., Beavis, P. A., Gebhardt, T., Trevaskis, N., Nutt, S. L., Zajac, J. D. & 5 others, Davey, R. A., Febbraio, M. A., Mathis, D., Shi, W. & Kallies, A., 26 Mar 2020, In : Nature. 579, 7800, p. 581–585+ 29 p.

Research output: Contribution to journalArticleResearchpeer-review

5 Citations (Scopus)

Structural basis of Gs and Gi recognition by the human glucagon receptor

Qiao, A., Han, S., Li, X., Li, Z., Zhao, P., Dai, A., Chang, R., Tai, L., Tan, Q., Chu, X., Ma, L., Thorsen, T. S., Reedtz-Runge, S., Yang, D., Wang, M-W., Sexton, P. M., Wootten, D., Sun, F., Zhao, Q. & Wu, B., 20 Mar 2020, In : Science. 367, 6484, p. 1346-1352 7 p.

Research output: Contribution to journalArticleResearchpeer-review

2 Citations (Scopus)

Sulfoxide-Containing Polymer-Coated Nanoparticles Demonstrate Minimal Protein Fouling and Improved Blood Circulation

Qiao, R., Fu, C., Li, Y., Qi, X., Ni, D., Nandakumar, A., Siddiqui, G., Wang, H., Zhang, Z., Wu, T., Zhong, J., Tang, S-Y., Pan, S., Zhang, C., Whittaker, M. R., Engle, J. W., Creek, D. J., Caruso, F., Ke, P. C., Cai, W. & 2 others, Whittaker, A. K. & Davis, T. P., May 2020, In : Advanced Science. 7, 13, 13 p., 2000406.

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2 Citations (Scopus)

The novel small-molecule annexin-a1 mimetic, compound 17b, elicits vasoprotective actions in streptozotocin-induced diabetic mice

Marshall, S. A., Qin, C. X., Jelinic, M., O’sullivan, K., Deo, M., Walsh, J., Li, M., Parry, L. J., Ritchie, R. H. & Leo, C. H., 2 Feb 2020, In : International Journal of Molecular Sciences. 21, 4, 21 p., 1384.

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The transient receptor potential vanilloid 4 (TRPV4) ion channel mediates protease activated receptor 1 (PAR1)-induced vascular hyperpermeability

Peng, S., Grace, M., Gondin, AB., Retamal, J. S., Dill, L., Darby, W. G., Bunnett, N., Abogadie, F. C., Carbone, S., Tigani, T., Davis, T. P., Poole, D. P., Veldhuis, N. & McIntyre, P., 2 Apr 2020, (Accepted/In press) In : Laboratory Investigation. 11 p.

Research output: Contribution to journalArticleResearchpeer-review

Three-dimensional differentiation of human pluripotent stem cell-derived neural precursor cells using tailored porous polymer scaffolds

Murphy, A. R., Haynes, J. M., Laslett, A. L., Cameron, N. R. & O'Brien, C. M., 1 Jan 2020, In : Acta Biomaterialia. 101, p. 102-116 15 p.

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4 Citations (Scopus)

Toward a Structural Understanding of Class B GPCR Peptide Binding and Activation

Liang, Y. L., Belousoff, M. J., Zhao, P., Koole, C., Fletcher, M. M., Truong, T. T., Julita, V., Christopoulos, G., Xu, H. E., Zhang, Y., Khoshouei, M., Christopoulos, A., Danev, R., Sexton, P. M. & Wootten, D., 6 Feb 2020, In : Molecular Cell. 77, 3, p. 656-668.e5 18 p.

Research output: Contribution to journalArticleResearchpeer-review

7 Citations (Scopus)
2019

6-Phenylpyrimidin-4-ones as Positive Allosteric Modulators at the M1 mAChR: The Determinants of Allosteric Activity

Jorg, M. T., van der Westhuizen, E. T., Khajehali, E., Burger, W. A. C., White, J., Choy, K. H. C., Tobin, A. B., Sexton, P. M., Valant, C., Capuano, B., Christopoulos, A. & Scammells, P. J., 20 Mar 2019, In : ACS Chemical Neuroscience. 10, 3, p. 1099-1114 16 p.

Research output: Contribution to journalArticleResearchpeer-review

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Acquisition of analgesic properties by the cholecystokinin (CCK)/CCK2 receptor system within the amygdala in a persistent inflammatory pain condition

Roca-Lapirot, O., Fossat, P., Ma, S., Egron, K., Trigilio, G., López-González, M. J., Covita, J., Bouali-Benazzouz, R., Favereaux, A., Gundlach, A. L. & Landry, M., 1 Feb 2019, In : Pain. 160, 2, p. 345-357 13 p.

Research output: Contribution to journalArticleResearchpeer-review

3 Citations (Scopus)

Activated platelets in the tumor microenvironment for targeting of antibody-drug conjugates to tumors and metastases

Yap, M. L., McFadyen, J. D., Wang, X., Ziegler, M., Chen, Y. C., Willcox, A., Nowell, C. J., Scott, A. M., Sloan, E. K., Hogarth, P. M., Pietersz, G. A. & Peter, K., 1 Jan 2019, In : Theranostics. 9, 4, p. 1154-1169 16 p.

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3 Citations (Scopus)

Activation of pruritogenic TGR5, MRGPRA3, and MRGPRC11 on colon-innervating afferents induces visceral hypersensitivity

Castro, J., Harrington, A. M., Lieu, T. M., Garcia-Caraballo, S., Maddern, J., Schober, G., O'Donnell, T., Grundy, L., Lumsden, A. L., Miller, P., Ghetti, A., Steinhoff, M. S., Poole, D. P., Dong, X., Chang, L., Bunnett, N. W. & Brierley, S. M., 17 Oct 2019, In : JCI Insight. 4, 20, 42 p., e131712.

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1 Citation (Scopus)

Acute β-adrenoceptor mediated glucose clearance in brown adipose tissue; a distinct pathway independent of functional insulin signaling

Olsen, J. M., Åslund, A., Bokhari, M. H., Hutchinson, D. S. & Bengtsson, T., Dec 2019, In : Molecular Metabolism. 30, p. 240-249 10 p.

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Adipocyte-specific deletion of IL-6 does not attenuate obesity-induced weight gain or glucose intolerance in mice

Whitham, M., Pal, M., Petzold, T., Hjorth, M., Egan, C. L., Brunner, J. S., Estevez, E., Iliades, P., Zivanovic, B., Reibe, S., Hughes, W. E., Findeisen, M., Hidalgo, J. & Febbraio, M. A., 30 Sep 2019, In : American Journal of Physiology - Endocrinology and Metabolism. 317, 4, p. E597-E604 8 p.

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1 Citation (Scopus)

Agonist-dependent development of delta opioid receptor tolerance in the colon

DiCello, J. J., Saito, A., Rajasekhar, P., Sebastian, B. W., McQuade, R. M., Gondin, A. B., Veldhuis, N. A., Canals, M., Carbone, S. E. & Poole, D. P., Aug 2019, In : Cellular and Molecular Life Sciences. 76, 15, p. 3033–3050 18 p.

Research output: Contribution to journalArticleResearchpeer-review

2 Citations (Scopus)