Research Output

2018

Ionophore and Biometal Modulation of P-glycoprotein Expression and Function in Human Brain Microvascular Endothelial Cells

McInerney, M. P., Volitakis, I., Bush, A. I., Banks, W. A., Short, J. L. & Nicolazzo, J. A., 1 Apr 2018, In : Pharmaceutical Research. 35, 4, 12 p., 83.

Research output: Contribution to journalArticleResearchpeer-review

6 Citations (Scopus)

Linker chemistry dictates the delivery of a phototoxic organometallic rhenium(i) complex to human cervical cancer cells from core crosslinked star polymer nanoparticles

Yu, S. H., Patra, M., Ferrari, S., Ramirez Garcia, P., Veldhuis, N. A., Kaminskas, L. M., Graham, B., Quinn, J. F., Whittaker, M. R., Gasser, G. & Davis, T. P., 29 Oct 2018, In : Journal of Materials Chemistry B. 6, 47, p. 7805-7810 6 p.

Research output: Contribution to journalArticleResearchpeer-review

4 Citations (Scopus)

Liver and biliary tract physiology/pathophysiology: Phenotypical heterogeneity in responder and nonresponder male ApoE*3Leiden.CETP mice

Tarasco, E., Pellegrini, G., Whiting, L. & Lutz, T. A., 5 Oct 2018, In : American Journal of Physiology - Gastrointestinal and Liver Physiology. 315, 4, p. G602-G617 16 p.

Research output: Contribution to journalArticleResearchpeer-review

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2 Citations (Scopus)

LMP2 immunoproteasome promotes lymphocyte survival by degrading apoptotic BH3-only proteins

Zanker, D., Pang, K., Oveissi, S., Lu, C., Faou, P., Nowell, C., Mbogo, G. W., Carotta, S., Quillici, C., Karupiah, G., Hibbs, M. L., Nutt, S. L., Neeson, P., Puthalakath, H. & Chen, W., 1 Oct 2018, In : Immunology and Cell Biology. 96, 9, p. 981-993 13 p.

Research output: Contribution to journalArticleResearchpeer-review

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2 Citations (Scopus)

Low dose aspirin blocks breast cancer-induced cognitive impairment in mice

Walker, A. K., Chang, A., Ziegler, A. I., Dhillon, H. M., Vardy, J. L. & Sloan, E. K., 10 Dec 2018, In : PLoS ONE. 13, 12, 15 p., e0208593.

Research output: Contribution to journalArticleResearchpeer-review

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6 Citations (Scopus)

MACROD2 haploinsufficiency impairs catalytic activity of PARP1 and promotes chromosome instability and growth of intestinal tumors

Sakthianandeswaren, A., Parsons, M. J., Mouradov, D., Mackinnon, R. N., Catimel, B., Liu, S., Palmieri, M., Love, C., Jorissen, R. N., Li, S., Whitehead, L., Putoczki, T. L., Preaudet, A., Tsui, C., Nowell, C. J., Ward, R. L., Hawkins, N. J., Desai, J., Gibbs, P., Ernst, M. & 3 others, Street, I., Buchert, M. & Sieber, O. M., 1 Aug 2018, In : Cancer Discovery. 8, 8, p. 988-1005 18 p.

Research output: Contribution to journalArticleResearchpeer-review

13 Citations (Scopus)

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

Wootten, D. L., Christopoulos, A., Marti-Solano, M., Babu, M. M. & Sexton, P. M., Oct 2018, In : Nature Reviews Molecular Cell Biology. 19, 10, p. 638-653 16 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

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92 Citations (Scopus)

Mirabegron: potential off target effects and uses beyond the bladder

Dehvari, N., Dantas da Silva Junior, E., Bengtsson, T. & Hutchinson, D. S., 1 Nov 2018, In : British Journal of Pharmacology. 175, 21, p. 4072-4082 11 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

13 Citations (Scopus)

Molecular pharmacology of GPCRs

Langmead, C. J. & Summers, R. J., 1 Nov 2018, In : British Journal of Pharmacology. 175, 21, p. 4005-4008 4 p.

Research output: Contribution to journalEditorialOther

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3 Citations (Scopus)

Multisite phosphorylation is required for sustained interaction with GRKs and arrestins during rapid -opioid receptor desensitization

Miess, E., Gondin, A. B., Yousuf, A., Steinborn, R., Mösslein, N., Yang, Y., Göldner, M., Ruland, J. G., Bünemann, M., Krasel, C., Christie, M. J., Halls, M. L., Schulz, S. & Canals, M., 17 Jul 2018, In : Science Signaling. 11, 539, 15 p., eaas9609.

Research output: Contribution to journalArticleResearchpeer-review

24 Citations (Scopus)

Muscarinic M5 receptors modulate ethanol seeking in rats

Berizzi, A. E., Perry, C. J., Shackleford, D. M., Lindsley, C. W., Jones, C. K., Chen, N. A., Sexton, P. M., Christopoulos, A., Langmead, C. J. & Lawrence, A. J., 1 Jun 2018, In : Neuropsychopharmacology. 43, 7, p. 1510-1517 8 p.

Research output: Contribution to journalArticleResearchpeer-review

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13 Citations (Scopus)

New paradigms in adenosine receptor pharmacology: allostery, oligomerization and biased agonism

Vecchio, E. A., Baltos, J. A., Nguyen, A. T. N., Christopoulos, A., White, P. J. & May, L. T., 1 Nov 2018, In : British Journal of Pharmacology. 175, 21, p. 4036-4046 11 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

15 Citations (Scopus)

NKX2-5 regulates human cardiomyogenesis via a HEY2 dependent transcriptional network

Anderson, D. J., Kaplan, D. I., Bell, K. M., Koutsis, K., Haynes, J. M., Mills, R. J., Phelan, D. G., Qian, E. L., Leitoguinho, A. R., Arasaratnam, D., Labonne, T., Ng, E. S., Davis, R. P., Casini, S., Passier, R., Hudson, J. E., Porrello, E. R., Costa, M. W., Rafii, A., Curl, C. L. & 9 others, Delbridge, L. M., Harvey, R. P., Oshlack, A., Cheung, M. M., Mummery, C. L., Petrou, S., Elefanty, A. G., Stanley, E. G. & Elliott, D. A., 10 Apr 2018, In : Nature Communications. 9, 1, 13 p., 1373.

Research output: Contribution to journalArticleResearchpeer-review

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20 Citations (Scopus)

Novel imaging of the prostate reveals spontaneous gland contraction and excretory duct quiescence together with different drug effects

Kügler, R., Mietens, A., Seidensticker, M., Tasch, S., Wagenlehner, F. M., Kaschtanow, A., Tjahjono, Y., Tomczyk, C. U., Beyer, D., Risbridger, G. P., Exintaris, B., Ellem, S. J. & Middendorff, R., 1 Mar 2018, In : The FASEB Journal. 32, 3, p. 1130-1138 9 p.

Research output: Contribution to journalArticleResearchpeer-review

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Perioperative events influence cancer recurrence risk after surgery

Hiller, J. G., Perry, N. J., Poulogiannis, G., Riedel, B. & Sloan, E. K., 1 Apr 2018, In : Nature Reviews Clinical Oncology. 15, 4, p. 205-218 14 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

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79 Citations (Scopus)

Peripheral modulation of the endocannabinoid system in metabolic disease

Shrestha, N., Cuffe, J. S. M., Hutchinson, D. S., Headrick, J. P., Perkins, A. V., McAinch, A. J. & Hryciw, D. H., 1 Mar 2018, In : Drug Discovery Today. 23, 3, p. 592-604 13 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

12 Citations (Scopus)

Phase-plate cryo-EM structure of a biased agonistbound human GLP-1 receptor-Gs complex

Liang, Y. L., Khoshouei, M., Glukhova, A., Furness, S. G. B., Zhao, P., Clydesdale, L., Koole, C., Truong, T. T., Thal, D. M., Lei, S., Radjainia, M., Danev, R., Baumeister, W., Wang, M. W., Miller, L. J., Christopoulos, A., Sexton, P. M. & Wootten, D., 1 Mar 2018, In : Nature. 555, 7694, p. 121-125 5 p.

Research output: Contribution to journalArticleResearchpeer-review

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120 Citations (Scopus)

Polymyxin B causes DNA damage in HK-2 cells and mice

Yun, B., Zhang, T., Azad, M. A. K., Wang, J., Nowell, C. J., Kalitsis, P., Velkov, T., Hudson, D. F. & Li, J., Jul 2018, In : Archives of Toxicology. 92, 7, p. 2259-2271 13 p.

Research output: Contribution to journalArticleResearchpeer-review

3 Citations (Scopus)

Preassembled GPCR signaling complexes mediate distinct cellular responses to ultralow ligand concentrations

Civciristov, S., Ellisdon, A. M., Suderman, R., Pon, C. K., Evans, B. A., Kleifeld, O., Charlton, S. J., Hlavacek, W. S., Canals, M. & Halls, M. L., 9 Oct 2018, In : Science Signaling. 11, 551, 22 p., eaan1188.

Research output: Contribution to journalArticleResearchpeer-review

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7 Citations (Scopus)

Predicting cancer cell invasion by single-cell physical phenotyping

Nyberg, K. D., Bruce, S. L., Nguyen, A. V., Chan, C. K., Gill, N. K., Kim, T. H., Sloan, E. K. & Rowat, A. C., 1 Apr 2018, In : Integrative Biology: Quantitative Biosciences from Nano to Macro. 10, 4, p. 218-231 14 p.

Research output: Contribution to journalArticleResearchpeer-review

11 Citations (Scopus)

Probing the binding site of novel selective positive allosteric modulators at the M1 muscarinic acetylcholine receptor

Khajehali, E., Valant, C., Jörg, M., Tobin, A. B., Conn, P. J., Lindsley, C. W., Sexton, P. M., Scammells, P. J. & Christopoulos, A., 1 Aug 2018, In : Biochemical Pharmacology. 154, p. 243-254 12 p.

Research output: Contribution to journalArticleResearchpeer-review

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4 Citations (Scopus)

Protease-activated receptor-2 in endosomes signals persistent pain of irritable bowel syndrome

Jimenez-Vargas, N. N., Pattison, L. A., Zhao, P., Lieu, T., Latorre, R., Jensen, D. D., Castro, J., Aurelio, L., Le, G. T., Flynn, B., Herenbrink, C. K., Yeatman, H. R., Edgington-Mitchell, L., Porter, C. J. H., Halls, M. L., Canals, M., Veldhuis, N. A., Poole, D. P., McLean, P., Hicks, G. A. & 7 others, Scheff, N., Chen, E., Bhattacharya, A., Schmidt, B. L., Brierley, S. M., Vanner, S. J. & Bunnett, N. W., 31 Jul 2018, In : Proceedings of the National Academy of Sciences of the United States of America. 115, 31, p. E7438-E7447 10 p.

Research output: Contribution to journalArticleResearchpeer-review

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28 Citations (Scopus)

Proteomic Identification of Interferon-Induced Proteins with Tetratricopeptide Repeats as Markers of M1 Macrophage Polarization

Huang, C., Lewis, C., Borg, N. A., Canals, M., Diep, H., Drummond, G. R., Goode, R. J., Schittenhelm, R. B., Vinh, A., Zhu, M., Kemp-Harper, B., Kleifeld, O. & Stone, M. J., 6 Apr 2018, In : Journal of Proteome Research. 17, 4, p. 1485-1499 15 p.

Research output: Contribution to journalArticleResearchpeer-review

5 Citations (Scopus)

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

Thal, D. M., Vuckovic, Z., Draper-Joyce, C. J., Liang, Y-L., Glukhova, A., Christopoulos, A. & Sexton, P. M., 1 Aug 2018, In : Current Opinion in Structural Biology. 51, p. 28-34 7 p.

Research output: Contribution to journalArticleResearchpeer-review

23 Citations (Scopus)

Reply to ‘Antipsychotics with similar association kinetics at dopamine D2 receptors differ in extrapyramidal side-effects’

Sykes, D. A., Lane, J. R., Szabo, M., Capuano, B., Javitch, J. A. & Charlton, S. J., 1 Dec 2018, In : Nature Communications. 9, 1, 5 p., 3568.

Research output: Contribution to journalLetterResearchpeer-review

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1 Citation (Scopus)

Rosiglitazone and a β3-adrenoceptor agonist are both required for functional browning of white adipocytes in culture

Merlin, J., Sato, M., Chia, L. Y., Fahey, R., Pakzad, M., Nowell, C. J., Summers, R. J., Bengtsson, T., Evans, B. A. & Hutchinson, D. S., 30 May 2018, In : Frontiers in Endocrinology. 9, MAY, 17 p., 249.

Research output: Contribution to journalArticleResearchpeer-review

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10 Citations (Scopus)

Rules of Engagement: GPCRs and G Proteins

Glukhova, A., Draper-Joyce, C. J., Sunahara, R. K., Christopoulos, A., Wootten, D. L. & Sexton, P. M., 7 Sep 2018, In : ACS Pharmacology & Translational Science. 1, 2, p. 73-83 11 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

Secondary Self-Assembly of Supramolecular Nanotubes into Tubisomes and Their Activity on Cells

Brendel, J. C., Sanchis, J., Catrouillet, S., Czuba, E., Chen, M. Z., Long, B. M., Nowell, C., Johnston, A., Jolliffe, K. A. & Perrier, S., 17 Dec 2018, In : Angewandte Chemie - International Edition. 57, 51, p. 16678-16682 5 p.

Research output: Contribution to journalArticleResearchpeer-review

18 Citations (Scopus)

Self-Crosslinking Lipopeptide/DNA/PEGylated Particles: A New Platform for DNA Vaccination Designed for Assembly in Aqueous Solution

Ho, J. K., White, P. J. & Pouton, C. W., 7 Sep 2018, In : Molecular Therapy - Nucleic Acids. 12, p. 504-517 14 p.

Research output: Contribution to journalArticleResearchpeer-review

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4 Citations (Scopus)

Strength in numbers - An arrestin interaction code

Draper-Joyce, C. J. & Christopoulos, A., 1 Jun 2018, In : Nature Structural & Molecular Biology. 25, 6, p. 437-439 3 p.

Research output: Contribution to journalReview ArticleOtherpeer-review

Structural Basis for Binding of Allosteric Drug Leads in the Adenosine A1 Receptor

Miao, Y., Bhattarai, A., Nguyen, A. T. N., Christopoulos, A. & May, L. T., 1 Dec 2018, In : Scientific Reports. 8, 1, 13 p., 16836.

Research output: Contribution to journalArticleResearchpeer-review

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12 Citations (Scopus)

Structural insights into binding specificity, efficacy and bias of a β 2 AR partial agonist

Masureel, M., Zou, Y., Picard, L. P., van der Westhuizen, E., Mahoney, J. P., Rodrigues, J. P. G. L. M., Mildorf, T. J., Dror, R. O., Shaw, D. E., Bouvier, M., Pardon, E., Steyaert, J., Sunahara, R. K., Weis, W. I., Zhang, C. & Kobilka, B. K., 1 Nov 2018, In : Nature Chemical Biology. 14, 11, p. 1059-1066 8 p.

Research output: Contribution to journalArticleResearchpeer-review

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36 Citations (Scopus)

Structural insights into G-protein-coupled receptor allostery

Thal, D. M., Glukhova, A., Sexton, P. M. & Christopoulos, A., 5 Jul 2018, In : Nature. 559, 7712, p. 45-53 9 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

82 Citations (Scopus)

Structure-Activity Relationships of Pan-Gαq/11 Coupled Muscarinic Acetylcholine Receptor Positive Allosteric Modulators

Berizzi, A. E., Bender, A. M., Lindsley, C. W., Conn, P. J., Sexton, P. M., Langmead, C. J. & Christopoulos, A., 18 Jul 2018, In : ACS Chemical Neuroscience. 9, 7, p. 1818-1828 11 p.

Research output: Contribution to journalArticleResearchpeer-review

4 Citations (Scopus)

Structure-based discovery of selective positive allosteric modulators of antagonists for the M2 muscarinic acetylcholine receptor

Korczynska, M., Clark, M. J., Valant, C., Xu, J., Moo, E. V., Albold, S., Weiss, D. R., Torosyan, H., Huang, W., Kruse, A. C., Lyda, B. R., May, L. T., Baltos, J. A., Sexton, P. M., Kobilka, B. K., Christopoulos, A., Shoichet, B. K. & Sunahara, R. K., 6 Mar 2018, In : Proceedings of the National Academy of Sciences of the United States of America. 115, 10, p. E2419-E2428 10 p.

Research output: Contribution to journalArticleResearchpeer-review

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21 Citations (Scopus)

Structure of the adenosine-bound human adenosine A1 receptor-Gi complex

Draper-Joyce, C. J., Khoshouei, M., Thal, D. M., Liang, Y. L., Nguyen, A. T. N., Furness, S. G. B., Venugopal, H., Baltos, J. A., Plitzko, J. M., Danev, R., Baumeister, W., May, L. T., Wootten, D., Sexton, P. M., Glukhova, A. & Christopoulos, A., 20 Jun 2018, In : Nature. 558, 7711, p. 559-565 7 p.

Research output: Contribution to journalArticleResearchpeer-review

105 Citations (Scopus)
4 Citations (Scopus)

Targeting adenosine receptor signaling in cancer immunotherapy

Sek, K., Mølck, C., Stewart, G. D., Kats, L., Darcy, P. K. & Beavis, P. A., 1 Dec 2018, In : International Journal of Molecular Sciences. 19, 12, 23 p., 3837.

Research output: Contribution to journalReview ArticleResearchpeer-review

Open Access
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39 Citations (Scopus)

Targeting the M1 muscarinic acetylcholine receptor to increase symptom domain coverage in schizophrenia

Mckenzie-Nickson, S., 2018.

Research output: Contribution to conferencePoster

The action of a negative allosteric modulator at the dopamine D2 receptor is dependent upon sodium ions

Draper-Joyce, C. J., Verma, R. K., Michino, M., Shonberg, J., Kopinathan, A., Klein Herenbrink, C., Scammells, P. J., Capuano, B., Abramyan, A. M., Thal, D. M., Javitch, J. A., Christopoulos, A., Shi, L. & Lane, J. R., 1 Dec 2018, In : Scientific Reports. 8, 1, 12 p., 1208.

Research output: Contribution to journalArticleResearchpeer-review

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6 Citations (Scopus)

The C and E subunits of the serotonin 5-HT3 receptor subtly modulate electrical properties of the receptor

Yaakob, N. S., Nguyen, D. T., Exintaris, B. & Irving, H. R., 1 Jan 2018, In : Biomedicine & Pharmacotherapy. 97, p. 1701-1709 9 p.

Research output: Contribution to journalArticleResearchpeer-review

1 Citation (Scopus)

The potentially beneficial central nervous system activity profile of ivacaftor and its metabolites

Schneider, E. K., McQuade, R. M., Carbone, V. C., Reyes-Ortega, F., Wilson, J. W., Button, B., Saito, A., Poole, D. P., Hoyer, D. & Li, J., 1 Jan 2018, In : ERJ Open Research. 4, 1, 10 p., 00127-2017.

Research output: Contribution to journalArticleResearchpeer-review

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The PPARγ agonist rosiglitazone promotes the induction of brite adipocytes, increasing β-adrenoceptor-mediated mitochondrial function and glucose uptake

Merlin, J., Sato, M., Nowell, C., Pakzad, M., Fahey, R., Gao, J., Dehvari, N., Summers, R. J., Bengtsson, T., Evans, B. A. & Hutchinson, D. S., 1 Jan 2018, In : Cellular Signalling. 42, p. 54-66 13 p.

Research output: Contribution to journalArticleResearchpeer-review

18 Citations (Scopus)

The structural determinants of the bitopic binding mode of a negative allosteric modulator of the dopamine D2 receptor

Draper-Joyce, C. J., Michino, M., Verma, R. K., Klein Herenbrink, C., Shonberg, J., Kopinathan, A., Scammells, P. J., Capuano, B., Thal, D. M., Javitch, J. A., Christopoulos, A., Shi, L. & Lane, J. R., 1 Feb 2018, In : Biochemical Pharmacology. 148, p. 315-328 14 p.

Research output: Contribution to journalArticleResearchpeer-review

8 Citations (Scopus)

Tight junction protein claudin-2 promotes self-renewal of human colorectal cancer stem-like cells

Paquet-Fifield, S., Koh, S. L., Cheng, L., Beyit, L. M., Shembrey, C., Mølck, C., Behrenbruch, C., Papin, M., Gironella, M., Guelfi, S., Nasr, R., Grillet, F., Prudhomme, M., Bourgaux, J. F., Castells, A., Pascussi, J. M., Heriot, A. G., Puisieux, A., Davis, M. J., Pannequin, J. & 3 others, Hill, A. F., Sloan, E. K. & Hollande, F. E., 1 Jun 2018, In : Cancer Research. 78, 11, p. 2925-2938 14 p.

Research output: Contribution to journalArticleResearchpeer-review

20 Citations (Scopus)

To Bind or Not to Bind: Unravelling GPCR Polypharmacology

Sexton, P. M. & Christopoulos, A., 8 Feb 2018, In : Cell. 172, 4, p. 636-638 3 p.

Research output: Contribution to journalShort SurveyOtherpeer-review

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7 Citations (Scopus)

Toward an understanding of the structural basis of allostery in muscarinic acetylcholine receptors

Burger, W. A. C., Sexton, P. M., Christopoulos, A. & Thal, D. M., 1 Oct 2018, In : Journal of General Physiology. 150, 10, p. 1360-1372 13 p.

Research output: Contribution to journalArticleResearchpeer-review

15 Citations (Scopus)

Toward better treatment for lower urinary tract symptoms associated with benign prostatic hyperplasia?

Ventura, S., 1 Jul 2018, In : American Journal of Physiology-Renal Physiology. 315, 1, p. F138-F139 2 p.

Research output: Contribution to journalEditorialOtherpeer-review

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Two distinct domains of the glucagon-like peptide-1 receptor control peptide-mediated biased agonism

Lei, S., Clydesdale, L., Dai, A., Cai, X., Yang, F., Yang, D., Liang, Y-L., Koole, C., Zhao, P., Coudrat, T., Christopoulos, A., Wang, M-W., Wootten, D. & Sexton, P. M., 1 Jan 2018, In : The Journal of Biological Chemistry. 293, 24, p. 9370-9387 18 p.

Research output: Contribution to journalArticleResearchpeer-review

18 Citations (Scopus)