Philip Thompson

2020

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 journal › Article › Research › peer-review

Heterodimeric Analogues of the Potent Y1R Antagonist 1229U91, Lacking One of the Pharmacophoric C-Terminal Structures, Retain Potent Y1R Affinity and Show Improved Selectivity over Y4R

Richardson, R. R., Groenen, M., Liu, M., Mountford, S. J., Briddon, S. J., Holliday, N. D. & Thompson, P. E., 28 May 2020, In : Journal of Medicinal Chemistry. 63, 10, p. 5274-5286 13 p.

Research output: Contribution to journal › Article › Research › peer-review

Macrocyclic peptidomimetics as inhibitors of insulin-regulated aminopeptidase (IRAP)

Barlow, N., Vanga, S. R., Sävmarker, J., Sandström, A., Burns, P., Hallberg, A., Åqvist, J., Gutiérrez-De-Terán, H., Hallberg, M., Larhed, M., Chai, S. Y. & Thompson, P. E., Feb 2020, In : RSC Medicinal Chemistry. 11, 2, p. 234-244 11 p.

Research output: Contribution to journal › Article › Research › peer-review

1 Citation (Scopus)

Substituted 1-methyl-4-phenylpyrrolidin-2-ones – Fragment-based design of N-methylpyrrolidone-derived bromodomain inhibitors

Hilton-Proctor, J. P., Ilyichova, O., Zheng, Z., Jennings, I. G., Johnstone, R. W., Shortt, J., Mountford, S. J., Scanlon, M. J. & Thompson, P. E., 1 Apr 2020, In : European Journal of Medicinal Chemistry. 191, 112120.

Research output: Contribution to journal › Article › Research › peer-review

Synthesis and biological evaluation of a novel photo-activated histone deacetylase inhibitor

Sama, G. R., Liu, H., Mountford, S., Thompson, P., Robinson, A. & Dear, A. E., 15 Aug 2020, In : Bioorganic and Medicinal Chemistry Letters. 30, 16, 5 p., 127291.

Research output: Contribution to journal › Article › Research › peer-review

2019

(S)-(−)-Fluorenylethylchloroformate (FLEC); preparation using asymmetric transfer hydrogenation and application to the analysis and resolution of amines

Al Amin, M., Camerino, M. A., Mountford, S. J., Ma, X., Manallack, D. T., Chalmers, D. K., Wills, M. & Thompson, P. E., 1 Jan 2019, In : Tetrahedron. 75, 43, p. 1-7 7 p., 130591.

Research output: Contribution to journal › Article › Research › peer-review

1 Citation (Scopus)

An apically located hybrid guanylate cyclase-ATPase is critical for the initiation of Ca²⁺ signaling and motility in Toxoplasma gondii

Yang, L., Uboldi, A. D., Seizova, S., Wilde, M. L., Coffey, M. J., Katris, N. J., Yamaryo-Botté, Y., Kocan, M., Bathgate, R. A. D., Stewart, R. J., McConville, M. J., Thompson, P. E., Botté, C. Y. & Tonkin, C. J., 31 May 2019, In : The Journal of Biological Chemistry. 294, 22, p. 8959-8972 14 p.

Research output: Contribution to journal › Article › Research › peer-review

5 Citations (Scopus)

Controlled Construction of Cyclic d / l Peptide Nanorods

Silk, M. R., Mohanty, B., Sampson, J. B., Scanlon, M. J., Thompson, P. E. & Chalmers, D. K., 8 Jan 2019, In : Angewandte Chemie - International Edition. 58, 2, p. 596-601 6 p.

Research output: Contribution to journal › Article › Research › peer-review

4 Citations (Scopus)

History, Chemistry and Antibacterial Spectrum

Velkov, T., Thompson, P. E., Azad, M. A. K., Roberts, K. D. & Bergen, P. J., 2019, Polymyxin Antibiotics: From Laboratory Bench to Bedside. Li, J., Nation, R. L. & Kaye, K. S. (eds.). 1st ed. Switzerland: Springer, p. 15-36 22 p. (Advances in Experimental Medicine and Biology; vol. 1145).

Research output: Chapter in Book/Report/Conference proceeding › Chapter (Book) › Other › peer-review

1 Citation (Scopus)

Structural Determinants of Isoform Selectivity in PI3K Inhibitors

Miller, M. S., Thompson, P. E. & Gabelli, S. B., 26 Feb 2019, In : Biomolecules. 9, 3, 35 p., 82.

Research output: Contribution to journal › Review Article › Research › peer-review

Open Access

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7 Citations (Scopus)

Synthesis and elaboration of N-methylpyrrolidone as an acetamide fragment substitute in bromodomain inhibition

Hilton-Proctor, J. P., Ilyichova, O., Zheng, Z., Jennings, I. G., Johnstone, R. W., Shortt, J., Mountford, S. J., Scanlon, M. J. & Thompson, P. E., 15 Dec 2019, In : Bioorganic & Medicinal Chemistry. 27, 24, 9 p., 115157.

Research output: Contribution to journal › Article › Research › peer-review

1 Citation (Scopus)

2018

A Cyclic Peptide Inhibitor of the iNOS-SPSB Protein-Protein Interaction as a Potential Anti-Infective Agent

Sadek, M. M., Barlow, N., Leung, E. W. W., Williams-Noonan, B. J., Yap, B. K., Shariff, F. M., Caradoc-Davies, T. T., Nicholson, S. E., Chalmers, D. K., Thompson, P. E., Law, R. H. P. & Norton, R. S., 19 Oct 2018, In : ACS Chemical Biology. 13, 10, p. 2930-2938 9 p.

Research output: Contribution to journal › Article › Research › peer-review

4 Citations (Scopus)

Cyclic Hexapeptide Mimics of the LEDGF Integrase Recognition Loop in Complex with HIV-1 Integrase

Northfield, S. E., Wielens, J., Headey, S. J., Williams-Noonan, B. J., Mulcair, M., Scanlon, M., Parker, M. W., Thompson, P. E. & Chalmers, D. K., 10 Aug 2018, In : ChemMedChem. 13, 15, p. 1555-1565 11 p.

Research output: Contribution to journal › Article › Research › peer-review

2 Citations (Scopus)

Methionine ameliorates polymyxin-induced nephrotoxicity by attenuating cellular oxidative stress

Azad, M. A. K., Sivanesan, S., Wang, J., Chen, K., Nation, R. L., Thompson, P. E., Roberts, K. D., Velkov, T. & Li, J., 1 Jan 2018, In : Antimicrobial Agents and Chemotherapy. 62, 1, 9 p., e01254.

Research output: Contribution to journal › Article › Research › peer-review

Open Access

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11 Citations (Scopus)

Structure, Function, and Biosynthetic Origin of Octapeptin Antibiotics Active against Extensively Drug-Resistant Gram-Negative Bacteria

Velkov, T., Gallardo-Godoy, A., Swarbrick, J. D., Blaskovich, M. A. T., Elliott, A. G., Han, M., Thompson, P. E., Roberts, K. D., Huang, J. X., Becker, B., Butler, M. S., Lash, L. H., Henriques, S. T., Nation, R. L., Sivanesan, S., Sani, M. A., Separovic, F., Mertens, H., Bulach, D., Seemann, T. & 3 others, Owen, J., Li, J. & Cooper, M. A., 19 Apr 2018, In : Cell Chemical Biology. 25, 4, p. 380-391 12 p.

Research output: Contribution to journal › Article › Research › peer-review

Open Access

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22 Citations (Scopus)

2017

Characterization of the Polymyxin D Synthetase Biosynthetic Cluster and Product Profile of Paenibacillus polymyxa ATCC 10401

Galea, C. A., Han, M., Zhu, Y., Roberts, K., Wang, J., Thompson, P. E., Li, J. & Velkov, T., 26 May 2017, In : Journal of Natural Products. 80, 5, p. 1264-1274 11 p.

Research output: Contribution to journal › Article › Research › peer-review

4 Citations (Scopus)

Class II phosphoinositide 3-kinases as novel drug targets

Falasca, M., Hamilton, J. R., Selvadurai, M. V., Sundaram, K., Adamska, A. & Thompson, P., 12 Jan 2017, In : Journal of Medicinal Chemistry. 60, 1, p. 47-65 19 p.

Research output: Contribution to journal › Article › Research › peer-review

18 Citations (Scopus)

Design and evaluation of novel polymyxin fluorescent probes

Yun, B., Roberts, K. D., Thompson, P. E., Nation, R. L., Velkov, T. & Li, J., 11 Nov 2017, In : Sensors. 17, 11, 8 p., 2598.

Research output: Contribution to journal › Article › Research › peer-review

Open Access

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2 Citations (Scopus)

Functional characterization of the unique terminal thioesterase domain from polymyxin synthetase

Galea, C., Roberts, K. D., Zhu, Y., Thompson, P. E., Li, J. & Velkov, T., 31 Jan 2017, In : Biochemistry. 56, 4, p. 657-668 12 p.

Research output: Contribution to journal › Article › Research › peer-review

2 Citations (Scopus)

Investigating the Interaction of Octapeptin A3 with Model Bacterial Membranes

Han, M. L., Shen, H. H., Hansford, K. A., Schneider, E. K., Sivanesan, S., Roberts, K. D., Thompson, P. E., Le Brun, A. P., Zhu, Y., Sani, M-A., Separovic, F., Blaskovich, M. A. T., Baker, M. A., Moskowitz, S. M., Cooper, M. A., Li, J. & Velkov, T., 11 Aug 2017, In : ACS Infectious Diseases. 3, 8, p. 606-619 14 p.

Research output: Contribution to journal › Article › Research › peer-review

9 Citations (Scopus)

Parallel and antiparallel cyclic d/l peptide nanotubes

Silk, M. R., Newman, J., Ratcliffe, J. C., White, J. F., Caradoc-Davies, T., Price, J. R., Perrier, S., Thompson, P. E. & Chalmers, D. K., 2017, In : Chemical Communications. 53, 49, p. 6613-6616 4 p.

Research output: Contribution to journal › Article › Research › peer-review

14 Citations (Scopus)

Pharmacokinetics of the individual major components of polymyxin B and colistin in rats

Sivanesan, S., Roberts, K., Wang, J., Cheah, S-E., Thompson, P. E., Li, J., Nation, R. & Velkov, T., 27 Jan 2017, In : Journal of Natural Products. 80, 1, p. 225-229 5 p.

Research output: Contribution to journal › Article › Research › peer-review

13 Citations (Scopus)

Synthesis and biological evaluation of 8-aryl-2-morpholino-7-O-substituted benzo[e][1,3]oxazin-4-ones against DNA-PK, PI3K, PDE3A enzymes and platelet aggregation

Saifuzzaman, M., Morrison, R., Zheng, Z., Orive, S., Hamilton, J., Thompson, P. E. & Al-Rawi, J. M. A., 15 Oct 2017, In : Bioorganic & Medicinal Chemistry. 25, 20, p. 5531-5536 6 p.

Research output: Contribution to journal › Article › Research › peer-review

2 Citations (Scopus)

2016

A novel chemical biology approach for mapping of polymyxin lipopeptide antibody binding epitopes

Velkov, T., Yun, B., Schneider, E. K., Azad, M. A. K., Dolezal, O., Morris, F. C., Nation, R. L., Wang, J., Chen, K., Yu, H., Wang, L., Thompson, P. E., Roberts, K. D. & Li, J., 2016, In : ACS Infectious Diseases. 2, 5, p. 341-351 11 p.

Research output: Contribution to journal › Article › Research › peer-review

9 Citations (Scopus)

A novel serpin regulatory mechanism: SERPINB9 is reversibly inhibited by vicinal disulfide bond formation in the reactive center loop

Mangan, M. S. J., Bird, C. H., Kaiserman, D., Matthews, A. Y., Hitchen, C., Steer, D. L., Thompson, P. E. & Bird, P. I., 12 Feb 2016, In : The Journal of Biological Chemistry. 291, 7, p. 3626-3638 13 p.

Research output: Contribution to journal › Article › Research › peer-review

7 Citations (Scopus)

Beta amino acid-modified and fluorescently labelled kisspeptin analogues with potent KISS1R activity

Camerino, M., Liu, M., Moriya, S., Kitahashi, T., Mahgoub, A., Mountford, S., Chalmers, D. K., Soga, T., Parhar, I. & Thompson, P., 1 Jun 2016, In : Journal of Peptide Science. 22, 6, p. 406-414 9 p.

Research output: Contribution to journal › Article › Research › peer-review

6 Citations (Scopus)

Design, synthesis, and characterization of cyclic peptidomimetics of the inducible nitric oxide synthase binding epitope that disrupt the protein-protein interaction involving SPRY domain-containing suppressor of cytokine signaling box protein (SPSB) 2 and inducible nitric oxide synthase

Harjani, J. R., Yap, B. K., Leung, E. W. W., Lucke, A., Nicholson, S. E., Scanlon, M. J., Chalmers, D. K., Thompson, P. E., Norton, R. S. & Baell, J. B., 23 Jun 2016, In : Journal of Medicinal Chemistry. 59, 12, p. 5799-5809 11 p.

Research output: Contribution to journal › Article › Research › peer-review

10 Citations (Scopus)

Development of single and mixed isoform selectivity PI3Kδ inhibitors by targeting Asn836 of PI3Kδ

Miller, M. S., Mountford, S. J., Pinson, J-A., Zheng, Z., Künzli, M., Patel, V., Hogg, S. J., Shortt, J., Jennings, I. G. & Thompson, P. E., 1 Oct 2016, In : Bioorganic and Medicinal Chemistry Letters. 26, 19, p. 4790-4794 5 p.

Research output: Contribution to journal › Article › Research › peer-review

7 Citations (Scopus)

Discovery and antiplatelet activity of a selective PI3Kβ inhibitor (MIPS-9922)

Zheng, Z., Pinson, J. A., Mountford, S. J., Orive, S., Schoenwaelder, S. M., Shackleford, D., Powell, A., Nelson, E. M., Hamilton, J. R., Jackson, S., Jennings, I. G. & Thompson, P. E., 21 Oct 2016, In : European Journal of Medicinal Chemistry. 122, p. 339-351 13 p.

Research output: Contribution to journal › Article › Research › peer-review

16 Citations (Scopus)

Identification of a cyanine-dye labeled peptidic ligand for Y₁R and Y₄R, based upon the neuropeptide y C-terminal analogue, BVD-15

Liu, M., Richardson, R. R., Mountford, S. J., Zhang, L., Tempone, M. H., Herzog, H., Holliday, N. D. & Thompson, P. E., 21 Sep 2016, In : Bioconjugate Chemistry. 27, 9, p. 2166-2175 10 p.

Research output: Contribution to journal › Article › Research › peer-review

5 Citations (Scopus)

Optically pure, structural, and fluorescent analogues of a dimeric Y₄ receptor agonist derived by an olefin metathesis approach

Liu, M., Mountford, S. J., Richardson, R. R., Groenen, M., Holliday, N. D. & Thompson, P. E., 14 Jul 2016, In : Journal of Medicinal Chemistry. 59, 13, p. 6059-6069 11 p.

Research output: Contribution to journal › Article › Research › peer-review

9 Citations (Scopus)

Polymyxins: a new hope in combating Gram-negative superbugs?

Velkov, T., Roberts, K. D., Thompson, P. E. & Li, J., 1 Jun 2016, In : Future Medicinal Chemistry. 8, 10, p. 1017-1025 9 p.

Research output: Contribution to journal › Review Article › Research › peer-review

35 Citations (Scopus)

Quantitation of polymyxin-lipopolysaccharide interactions using an image-based fluorescent probe

McInerney, M. P., Roberts, K. D., Thompson, P. E., Li, J., Nation, R. L., Velkov, T. & Nicolazzo, J. A., 2016, In : Journal of Pharmaceutical Sciences. 105, 2, p. 1006-1010 5 p.

Research output: Contribution to journal › Article › Research › peer-review

5 Citations (Scopus)

Redox-stable cyclic peptide inhibitors of the SPSB2-iNOS interaction

Yap, B. K., Harjani, J. R., Leung, E. W. W., Nicholson, S. E., Scanlon, M. J., Chalmers, D. K., Thompson, P. E., Baell, J. B. & Norton, R. S., 1 Mar 2016, In : FEBS Letters. 590, 6, p. 696-704 9 p.

Research output: Contribution to journal › Article › Research › peer-review

11 Citations (Scopus)

Structure–activity studies of β-hairpin peptide inhibitors of the Plasmodium falciparum AMA1–RON2 interaction

Wang, G., Drinkwater, N., Drew, D. R., MacRaild, C. A., Chalmers, D. K., Mohanty, B., Lim, S. S., Anders, R. F., Beeson, J. G., Thompson, P. E., McGowan, S., Simpson, J. S., Norton, R. S. & Scanlon, M. J., 9 Oct 2016, In : Journal of Molecular Biology. 428, 20, p. 3986-3998 13 p.

Research output: Contribution to journal › Article › Research › peer-review

9 Citations (Scopus)

Synthesis, structure elucidation, DNA-PK and PI3K and anti-cancer activity of 8- and 6-aryl-substituted-1-3-benzoxazines

Morrison, R., Al-Rawi, J. M. A., Jennings, I. G., Thompson, P. E. & Angove, M. J., 3 Mar 2016, In : European Journal of Medicinal Chemistry. 110, p. 326-339 14 p.

Research output: Contribution to journal › Article › Research › peer-review

21 Citations (Scopus)

Synthesis of linear and angular aryl-morpholino-naphth-oxazines, their DNA-PK, PI3K, PDE3A and antiplatelet activity

Morrison, R., Zheng, Z., Jennings, I. G., Thompson, P. E. & Al-Rawi, J. M. A., 2016, In : Bioorganic and Medicinal Chemistry Letters. 26, 22, p. 5534-5538 5 p.

Research output: Contribution to journal › Article › Research › peer-review

5 Citations (Scopus)

The extracellular surface of the GLP-1 receptor is a molecular trigger for biased agonism

Wootten, D., Reynolds, C. A., Smith, K. J., Mobarec, J. C., Koole, C., Savage, E. E., Pabreja, K., Simms, J., Sridhar, R., Furness, S. G. B., Liu, M., Thompson, P. E., Miller, L. J., Christopoulos, A. & Sexton, P. M., 16 Jun 2016, In : Cell. 165, 7, p. 1632-1643 12 p.

Research output: Contribution to journal › Article › Research › peer-review

64 Citations (Scopus)

Transcriptomic analysis of the activity of a novel polymyxin against Staphylococcus aureus

Zhao, J., Cheah, S-E., Roberts, K. D., Nation, R. L., Thompson, P. E., Velkov, T., Du, Z., Johnson, M. D. & Li, J., 2016, In : mSphere. 1, 4, 13 p., e00119-16.

Research output: Contribution to journal › Article › Research › peer-review

Open Access

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5 Citations (Scopus)

2015

Antimicrobial activity and toxicity of the major lipopeptide components of polymyxin B and colistin: last-line antibiotics against multidrug-resistant gram-negative bacteria

Roberts, K. D., Azad, M. A. K., Wang, J., Horne, A. S., Thompson, P. E., Nation, R. L., Velkov, T. & Li, J., 2015, In : ACS Infectious Diseases. 1, 11, p. 568-575 8 p.

Research output: Contribution to journal › Article › Research › peer-review

58 Citations (Scopus)

Cellular uptake and localization of polymyxins in renal tubular cells using rationally designed fluorescent probes

Yun, B., Azad, M. A. K., Nowell, C. J., Nation, R. L., Thompson, P. E., Roberts, K. D., Velkov, T. & Li, J., 2015, In : Antimicrobial Agents and Chemotherapy. 59, 12, p. 7489-7496 8 p.

Research output: Contribution to journal › Article › Research › peer-review

Open Access

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15 Citations (Scopus)

Class II but not second class - prospects for the development of class II PI3K inhibitors

Mountford, S. J., Zheng, Z., Sundaram, K., Jennings, I., Hamilton, J. R. & Thompson, P., 2015, In : ACS Medicinal Chemistry Letters. 6, 1, p. 3 - 6 4 p.

Research output: Contribution to journal › Editorial › Research › peer-review

4 Citations (Scopus)

Identification of potent phosphodiesterase inhibitors that demonstrate cyclic nucleotide-dependent functions in apicomplexan parasites

Howard, B. L., Harvey, K. L., Stewart, R. J., Azevedo, M. F., Crabb, B. S., Jennings, I., Sanders, P. R., Manallack, D. T., Thompson, P., Tonkin, C. J. & Gilson, P. R., 2015, In : ACS Chemical Biology. 10, 4, p. 1145 - 1154 10 p.

Research output: Contribution to journal › Article › Research › peer-review

36 Citations (Scopus)

Imaging the distribution of polymyxins in the kidney

Yun, B., Azad, M. A. K., Wang, J., Nation, R. L., Thompson, P., Roberts, K. D., Velkov, T. & Li, J., 2015, In : Journal of Antimicrobial Chemotherapy. 70, 3, p. 827 - 829 3 p.

Research output: Contribution to journal › Article › Research › peer-review

Open Access

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29 Citations (Scopus)

Propargyloxyproline regio- and stereoisomers for click-conjugation of peptides: synthesis and application in linear and cyclic peptides

Northfield, S. E., Mountford, S. J., Wielens, J., Liu, M., Zhang, L., Herzog, H., Holliday, N. D., Scanlon, M., Parker, M. W., Chalmers, D. K. & Thompson, P., 2015, In : Australian Journal of Chemistry. 68, 9, p. 1365-1372 8 p.

Research output: Contribution to journal › Article › Research › peer-review

8 Citations (Scopus)

Significant accumulation of polymyxin in single renal tubular cells: a medicinal chemistry and triple correlative microscopy approach

Azad, M. A. K., Roberts, K. D., Yu, H., Liu, B., Schofield, A. V., James, S. A., Howard, D. L., Nation, R. L., Rogers, K. L., de Jonge, M. D., Thompson, P., Fu, J., Velkov, T. & Li, J., 2015, In : Analytical Chemistry. 87, 3, p. 1590 - 1595 6 p.

Research output: Contribution to journal › Article › Research › peer-review

Open Access

23 Citations (Scopus)

2014

A potent cyclic peptide targeting SPSB2 protein as a potential anti-infective agent

Yap, B. K., Leung, E. W. W., Yagi, H., Galea, C., Chhabra, S., Chalmers, D. K., Nicholson, S. E., Thompson, P. & Norton, R. S., 2014, In : Journal of Medicinal Chemistry. 57, 16, p. 7006 - 7015 10 p.

Research output: Contribution to journal › Article › Research › peer-review

15 Citations (Scopus)

A secondary mode of action of polymyxins against Gram-negative bacteria involves the inhibition of NADH-quinone oxidoreductase activity

Deris, Z. Z., Akter, J., Sivanesan, S., Roberts, K. D., Thompson, P., Nation, R. L., Li, J. & Velkov, T., 2014, In : Journal of Antibiotics. 67, 2, p. 147 - 151 5 p.

Research output: Contribution to journal › Article › Research › peer-review

63 Citations (Scopus)

Discovery of phosphodiesterase-4 inhibitors: Serendipity and rational drug design

Feil, S. C., Holien, J. K., Morton, C. J., Hancock, N. C., Thompson, P. & Parker, M. W., 2014, In : Australian Journal of Chemistry. 67, 12, p. 1780 - 1785 6 p.

Research output: Contribution to journal › Article › Research › peer-review

2 Citations (Scopus)

Measuring polymyxin uptake by renal tubular cells: Is bodipy-polymyxin B an appropriate probe?

Azad, M. A. K., Yun, B., Roberts, K. D., Nation, R. L., Thompson, P., Velkov, T. & Li, J., 1 Oct 2014, In : Antimicrobial Agents and Chemotherapy. 58, 10, p. 6337-6338 2 p.

Research output: Contribution to journal › Letter › Other › peer-review

Open Access

9 Citations (Scopus)