A. Ganesan

Search results

• 2022

  Euglenatides, potent antiproliferative cyclic peptides isolated from the freshwater photosynthetic microalga Euglena gracilis

  Ganesan, A., Aldholmi, M., Ahmad, R., Carretero-Molina, D., Pérez-Victoria, I., Martín, J., Reyes, F., Genilloud, O., Gourbeyre, L., Gefflaut, T., Carlsson, H., Maklakov, A., Field, R. A., O'Neill, E., Wilkinson, B. & O'Connell, M., 7 Jun 2022, In: Angewandte Chemie-International Edition. 61, 23, e202203175.

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

  Open Access

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  11 Citations (Scopus)

  15 Downloads (Pure)
• 2021

  From hit seeking to magic bullets: The successful union of epigenetic and fragment based drug discovery (EPIDD + FBDD)

  Vaidergorn, M. M., da Silva Emery, F. & Ganesan, A., 14 Oct 2021, In: Journal of Medicinal Chemistry. 64, 19, p. 13980-14010 31 p.

  Research output: Contribution to journal › Article › peer-review
  14 Citations (Scopus)

• Insights into the structure-activity relationship of glycosides as positive allosteric modulators acting on P2X7 receptors

  Piyasirananda, W., Beekman, A., Ganesan, A., Bidula, S. & Stokes, L., 1 Feb 2021, In: Molecular Pharmacology. 99, 2, p. 163-174 12 p.

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

  Open Access

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  9 Citations (Scopus)

  24 Downloads (Pure)

• Synthesis of carboxamide-containing tranylcypromine analogues as LSD1 (KDM1A) inhibitors targeting acute myeloid leukemia

  Teresa Borrello, M., Benelkebir, H., Lee, A., Hin Tam, C., Shafat, M., Rushworth, S. A., Bowles, K. M., Douglas, L., Duriez, P. J., Bailey, S., Crabb, S. J., Packham, G. & Ganesan, A., 20 Apr 2021, In: ChemMedChem. 16, 8, p. 1316-1324 9 p.

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

  Open Access

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  7 Citations (Scopus)

  13 Downloads (Pure)

• The clinical landscape of HDAC inhibitors

  Ganesan, A., 3 Sep 2021, Medical Epigenetics. Elsevier, p. 885-899 15 p.

  Research output: Chapter in Book/Report/Conference proceeding › Chapter
• 2020

  Editorial overview: Epigenetics equals chemical biology

  Kawamura, A. & Ganesan, A., Aug 2020, In: Current Opinion in Chemical Biology. 57, p. A1-A4 4 p.

  Research output: Contribution to journal › Editorial › peer-review
  1 Citation (Scopus)

• Epigenetic modulation of secondary metabolite profiles in Aspergillus calidoustus and Aspergillus westerdijkiae through histone deacetylase (HDAC) inhibition by vorinostat

  Aldholmi, M., Wilkinson, B. & Ganesan, A., Jun 2020, In: Journal of Antibiotics. 73, 6, p. 410–413 4 p.

  Research output: Contribution to journal › Article › peer-review
  19 Citations (Scopus)

• HDAC inhibitors in cancer therapy

  Ganesan, A., 2020, Histone Modifications in Therapy. Elsevier, p. 19-49 31 p.

  Research output: Chapter in Book/Report/Conference proceeding › Chapter
  3 Citations (Scopus)

• New tranylcypromine derivatives containing sulfonamide motif as potent LSD1 inhibitors to target acute myeloid leukemia: design, synthesis and biological evaluation

  Liang, L., Wang, H., Du, Y., Luo, B., Meng, N., Cen, M., Huang, P., Ganesan, A. & Wen, S., Jun 2020, In: Bioorganic Chemistry. 99, 103808.

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

  Open Access

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  19 Citations (Scopus)

  13 Downloads (Pure)

• Pharmacological inhibition of lysine-specific demethylase 1 (LSD1) induces global transcriptional deregulation and ultrastructural alterations that impair viability in Schistosoma mansoni

  Coutinho Carneiro, V., de Abreu da Silva, I. C., Amaral, M. S., Pereira, A. S. A., Silveira, G. O., Pires, D. D. S., Verjovski-Almeida, S., Dekker, F. J., Rotili, D., Mai, A., Lopes-Torres, E. J., Robaa, D., Sippl, W., Pierce, R. J., Borrello, M. T., Ganesan, A., Lancelot, J., Thiengo, S., Fernandez, M. A., Vicentino, A. R. R., & 3 othersMourão, M. M., Coelho, F. S. & Fantappié, M. R., 1 Jul 2020, In: PLoS Neglected Tropical Diseases. 14, 7, e0008332.

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

  Open Access

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  7 Citations (Scopus)

  31 Downloads (Pure)

• QSAR studies on the human sirtuin 2 inhibition by non-covalent 7,5,2-anilinobenzamide derivatives

  Ferreira, G. M., de Magalhães, J. G., Maltarollo, V. G., Kronenberger, T., Ganesan, A., Emery, F. D. S. & Trossini, G. H. G., 22 Jan 2020, In: Journal of Biomolecular Structure and Dynamics. 38, 2, p. 354-363 10 p.

  Research output: Contribution to journal › Article › peer-review
  5 Citations (Scopus)

• Stereoselective synthesis of protected l-allo-Enduracididine and l-Enduracididine via asymmetric nitroaldol reaction

  Ohsawa, K., Zhao, H., Tokunaga, T., Thomas, C., Ganesan, A., Masuda, Y. & Doi, T., 17 Mar 2020, In: Synthesis-Stuttgart. 52, 6, p. 942-948 7 p.

  Research output: Contribution to journal › Article › peer-review
  1 Citation (Scopus)

• Targeting the Zinc-Dependent Histone Deacetylases (HDACs) for Drug Discovery

  Ganesan, A., 2020, Topics in Medicinal Chemistry. Springer, p. 1-27 27 p. (Topics in Medicinal Chemistry; vol. 33).

  Research output: Chapter in Book/Report/Conference proceeding › Chapter
  6 Citations (Scopus)

• Thirty years of HDAC inhibitors: 2020 hindsight

  Ho, T. C. S., Chan, A. H. Y. & Ganesan, A., 12 Nov 2020, In: Journal of Medicinal Chemistry. 63, 21, p. 12460–12484 25 p.

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

  Open Access

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  428 Citations (Scopus)

  18 Downloads (Pure)

• Three cheers for nitrogen: aza-DKPs, the aza analogues of 2,5-diketopiperazines

  Maujean, T., Girard, N., Ganesan, A., Gulea, M. & Bonnet, D., 2020, In: RSC Advances. 10, 71, p. 43358-43370 13 p.

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

  Open Access

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  4 Citations (Scopus)

  30 Downloads (Pure)

• Two-hit wonders: The expanding universe of multitargeting epigenetic agents

  De Lera, A. R. & Ganesan, A., Aug 2020, In: Current Opinion in Chemical Biology. 57, p. 135-154 20 p.

  Research output: Contribution to journal › Article › peer-review
  33 Citations (Scopus)
• 2019

  A decade of antifungal leads from natural products: 2010-2019

  Aldholmi, M., Marchand, P., Ourliac-Garnier, I., Le Pape, P. & Ganesan, A., 12 Dec 2019, In: Pharmaceuticals. 12, 4, 182.

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

  Open Access

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  59 Citations (Scopus)

  31 Downloads (Pure)

• Combined ligand and fragment-based drug design of selective histone deacetylase – 6 inhibitors

  Ruzic, D., Petkovic, M., Agbaba, D., Ganesan, A. & Nikolic, K., May 2019, In: Molecular Informatics. 38, 5, 1800083.

  Research output: Contribution to journal › Article › peer-review
  16 Citations (Scopus)

• The timeline of epigenetic drug discovery: From reality to dreams

  Ganesan, A., Arimondo, P. B., Rots, M. G., Jeronimo, C. & Berdasco, M., 2 Dec 2019, In: Clinical Epigenetics. 11, 1, 174.

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

  Open Access

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  252 Citations (Scopus)

  38 Downloads (Pure)
• 2018

  LSD1 inhibition attenuates androgen receptor V7 splice variant activation in castration resistant prostate cancer models

  Regufe da Mota, S., Bailey, S., Strivens, R. A., Hayden, A. L., Douglas, L. R., Duriez, P. J., Borrello, M. T., Benelkebir, H., Ganesan, A., Packham, G. & Crabb, S. J., 9 May 2018, In: Cancer Cell International. 18, 71.

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

  Open Access

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  19 Citations (Scopus)

  20 Downloads (Pure)

• Synthesis of breast cancer targeting conjugate of temporin-SHa analog and its effect on pro- and anti-apoptotic protein expression in MCF-7 cells

  Shaheen, F., Nadeem-ul-Haque, M., Ahmed, A., Simjee, S. U., Ganesan, A., Jabeen, A., Shah, Z. A. & Choudhary, M. I., Aug 2018, In: Peptides. 106, p. 68-82 15 p.

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

  Open Access

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  16 Citations (Scopus)

  33 Downloads (Pure)

• Total synthesis of altissimacoumarin D, a small molecule sirtuin1 activator

  Silva, A. C., Benelkebir, H., Lopes, R. S. C., Lopes, C. C. & Ganesan, A., 9 Feb 2018, In: Journal of the Brazilian Chemical Society. 29, 5, p. 1157-1161 5 p.

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

  Open Access

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  5 Citations (Scopus)

  22 Downloads (Pure)

• β-amino alcohols and their respective 2-phenyl-N-alkyl aziridines as potential DNA minor groove binders

  Vaidergorn, M. M., Carneiro, Z. A., Lopes, C. D., de Albuquerque, S., Reis, F. C. C., Nikolaou, S., Mello, J. F. R., Genesi, G. L., Trossini, G. H. G., Ganesan, A. & Emery, F. S., 5 Sep 2018, In: European Journal of Medicinal Chemistry. 157, p. 657-664 8 p.

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

  Open Access

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  17 Citations (Scopus)

  17 Downloads (Pure)
• 2017

  Cellular analysis of the action of epigenetics drugs and probes

  Hau, M., Zenk, F., Ganesan, A., Iovino, N. & Jung, M., Jan 2017, In: Epigenetics. 12, 5, p. 308-322 15 p.

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

  Open Access

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  6 Citations (Scopus)

  16 Downloads (Pure)

• Fluorinated tranylcypromine analogues as inhibitors of lysine-specific demethylase 1 (LSD1, KDM1A)

  Borrello, M. T., Schinor, B., Bartels, K., Benelkebir, H., Pereira, S., Al-Jamal, W. T., Douglas, L., Duriez, P. J., Packham, G., Haufe, G. & Ganesan, A., 15 May 2017, In: Bioorganic & Medicinal Chemistry Letters. 27, 10, p. 2099–2101

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

  Open Access

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  19 Citations (Scopus)

  19 Downloads (Pure)

• The histone deacetylase inhibitor, romidepsin, as a potential treatment for pulmonary fibrosis

  Conforti, F., Davies, E. R., Calderwood, C. J., Thatcher, T. H., Jones, M. G., Smart, D. E., Mahajan, S., Alzetani, A., Havelock, T., Maher, T. M., Molyneaux, P. L., Thorley, A. J., Tetley, T. D., Warner, J. A. ., Packham, G., Ganesan, A., Skipp, P. J., Marshall, B. J., Richeldi, L., Sime, P. J., & 2 othersO’reilly, K. M. A. & Davies, D. E., 14 Apr 2017, In: Oncotarget. 8, p. 48737-48754 18 p.

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

  Open Access

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  42 Citations (Scopus)

  20 Downloads (Pure)
• 2016

  Epigenetic polypharmacology: from combination therapy to multitargeted drugs

  de Lera, A. R. & Ganesan, A., 12 Oct 2016, In: Clinical Epigenetics. 8, 105.

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

  Open Access

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  115 Citations (Scopus)

  31 Downloads (Pure)

• Inhibition of NAADP signalling on reperfusion protects the heart by preventing lethal calcium oscillations via two-pore channel 1 and opening of the mitochondrial permeability transition pore

  Davidson, S. M., Foote, K., Kunuthur, S., Gosain, R., Tan, N., Tyser, R., Zhao, Y. J., Graeff, R., Ganesan, A., Duchen, M. R., Patel, S. & Yellon, D. M., 1 Dec 2016, In: Cardiovascular Research. 108, 3, p. 357-366 10 p.

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

  Open Access

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  39 Citations (Scopus)

  17 Downloads (Pure)

• Multitarget drugs: an epigenetic epiphany

  Ganesan, A., 20 Jun 2016, In: ChemMedChem. 11, 12, p. 1227-1241 15 p.

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

  Open Access

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  74 Citations (Scopus)

  9 Downloads (Pure)

• Oral administration of peptide-based drugs: Beyond Lipinski's rule

  Santos, G. B., Ganesan, A. & Emery, F. S., 19 Oct 2016, In: ChemMedChem. 11, 20, p. 2245–2251 7 p.

  Research output: Contribution to journal › Literature review
  107 Citations (Scopus)

• Synthesis of two 'heteroaromatic rings of the future' for applications in medicinal chemistry

  Silva Júnior, P. E., Rezende, L. C. D., Gimenes, J. P., Maltarollo, V. G., Dale, J., Trossini, G. H. G., Emery, F. S. & Ganesan, A., 22 Feb 2016, In: RSC Advances. 6, 27, p. 22777-22780 4 p.

  Research output: Contribution to journal › Article › peer-review
  8 Citations (Scopus)

• Total synthesis, structural, and biological evaluation of stylissatin A and related analogs

  Shaheen, F., Jabeen, A., Ashraf, S., Nadeem-ul-Haque, M., Ali Shah, Z., Asad Ziaee, M., Dastagir, N. & Ganesan, A., Sep 2016, In: Journal of Peptide Science. 22, 9, p. 607-617 11 p.

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

  Open Access

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  14 Citations (Scopus)

  22 Downloads (Pure)
• 2014

  Intra- and intermolecular alkylation of N,O-acetals and π-activated alcohols catalyzed by in situ generated acid

  Hamon, M., Dickinson, N., Devineau, A., Bolien, D., Tranchant, M-J., Taillier, C., Jabin, I., Harrowven, D. C., Whitby, R. J., Ganesan, A. & Dalla, V., 7 Mar 2014, In: Journal of Organic Chemistry. 79, 5, p. 1900-1912 13 p.

  Research output: Contribution to journal › Article › peer-review
  34 Citations (Scopus)

• Synthesis of N-acyl-N,O-acetals mediated by titanium ethoxide

  Li, M., Luo, B., Liu, Q., Hu, Y., Ganesan, A., Huang, P. & Wen, S., 3 Jan 2014, In: Organic Letters. 16, 1, p. 10-13 4 p.

  Research output: Contribution to journal › Article › peer-review
  34 Citations (Scopus)

• Three-component Pd/Cu-catalyzed cascade reactions of cyclic iodoniums, alkynes, and boronic acids: An approach to methylidenefluorenes

  Zhu, D., Wu, Y., Wu, B., Luo, B., Ganesan, A., Wu, F., Pi, R., Huang, P. & Wen, S., 2 May 2014, In: Organic Letters. 16, 9, p. 2350-2353 4 p.

  Research output: Contribution to journal › Article › peer-review
  73 Citations (Scopus)
• 2013

  Expanding the druggable space of the LSD1/CoREST epigenetic target: New potential binding regions for drug-like molecules, peptides, protein partners, and chromatin

  Robertson, J. C., Hurley, N. C., Tortorici, M., Ciossani, G., Borrello, M. T., Vellore, N. A., Ganesan, A., Mattevi, A. & Baron, R., 18 Jul 2013, In: PLoS Computational Biology. 9, 7, e1003158.

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

  Open Access
  27 Citations (Scopus)

• Protein recognition by short peptide reversible inhibitors of the chromatin-modifying LSD1/CoREST lysine demethylase

  Tortorici, M., Borrello, M. T., Tardugno, M., Chiarelli, L. R., Pilotto, S., Ciossani, G., Vellore, N. A., Bailey, S. G., Cowan, J., O'Connell, M., Crabb, S. J., Packham, G., Mai, A., Baron, R., Ganesan, A. & Mattevi, A., 16 Aug 2013, In: ACS Chemical Biology. 8, 8, p. 1677-1682 6 p.

  Research output: Contribution to journal › Article › peer-review
  60 Citations (Scopus)
• 2012

  Combinational aid for underprivileged scaffolds: solution and solid-phase strategies for a rapid and efficient access to novel aza-diketopiperazines (Aza-DKP)

  Bonnet, D., Margathe, J-F., Radford, S., Pflimlin, E., Riche, S., Doman, P., Hibert, M. & Ganesan, A., 2012, In: ACS Combinatorial Science. 14, 5, p. 323-334 12 p.

  Research output: Contribution to journal › Article › peer-review
  27 Citations (Scopus)

• Solid-phase total synthesis of cherimolacyclopeptide E and discovery of more potent analogues by alanine screening

  Shaheen, F., Rizvi, T. S., Musharraf, S. G., Ganesan, A., Xiao, K., Townsend, J. B., Lam, K. S. & Choudhary, M. I., 26 Nov 2012, In: Journal of Natural Products. 75, 11, p. 1882-1887 6 p.

  Research output: Contribution to journal › Article › peer-review
  18 Citations (Scopus)

• Spiruchostatin A inhibits proliferation and differentiation of fibroblasts from patients with pulmonary fibrosis

  Davies, E. R., Haitchi, H. M., Thatcher, T. H., Sime, P. J., Kottmann, R. M., Ganesan, A., Packham, G., O'Reilly, K. M. A. & Davies, D. E., May 2012, In: American Journal of Respiratory Cell and Molecular Biology. 46, 5, p. 687-694 8 p.

  Research output: Contribution to journal › Article › peer-review
  55 Citations (Scopus)
• 2011

  Enantioselective synthesis of tranylcypromine analogues as lysine demethylase (LSD1) inhibitors

  Benelkebir, H., Hodgkinson, C., Duriez, P. J., Hayden, A. L., Bulleid, R. A., Crabb, S. J., Packham, G. & Ganesan, A., 15 Jun 2011, In: Bioorganic & Medicinal Chemistry. 19, 12, p. 3709-3716 8 p.

  Research output: Contribution to journal › Article › peer-review
  83 Citations (Scopus)

• Pictet-Spengler reaction using ion-exchange resin as a catalyst and support for ‘catch and release’ purification

  Izumi, M., Kido, T., Murakami, M., Nakajima, S. & Ganesan, A., 2011, In: Bioscience, Biotechnology, and Biochemistry. 75, 2, p. 391-392 2 p.

  Research output: Contribution to journal › Article › peer-review
  3 Citations (Scopus)

• The histone deacetylase inhibitors vorinostat and romidepsin downmodulate IL-10 expression in cutaneous T-cell lymphoma cells

  Tiffon, C. E., Adams, J. E., van der Fits, L., Wen, S., Townsend, P. A., Ganesan, A., Hodges, E., Vermeer, M. H. & Packham, G., Apr 2011, In: British Journal of Pharmacology. 162, 7, p. 1590-1602 13 p.

  Research output: Contribution to journal › Article › peer-review
  76 Citations (Scopus)

• Total synthesis and stereochemical assignment of burkholdac B, a depsipeptide HDAC inhibitor

  Benelkebir, H., Donlevy, A. M., Packham, G. & Ganesan, A., 2011, In: Organic Letters. 13, 24, p. 6334-6337 4 p.

  Research output: Contribution to journal › Article › peer-review
  36 Citations (Scopus)

• Total synthesis of largazole and analogues: HDAC inhibition, antiproliferative activity and metabolic stability

  Benelkebir, H., Marie, S., Hayden, A. L., Lyle, J., Loadman, P. M., Crabb, S. J., Packham, G. & Ganesan, A., 15 Jun 2011, In: Bioorganic & Medicinal Chemistry. 19, 12, p. 3650-3658 9 p.

  Research output: Contribution to journal › Article › peer-review
  54 Citations (Scopus)
• 2010

  Determination of molecular torsion angles using nuclear singlet relaxation

  Tayler, M. C. D., Marie, S., Ganesan, A. & Levitt, M. H., 27 May 2010, In: Journal of the American Chemical Society. 132, 24, p. 8225-8227 3 p.

  Research output: Contribution to journal › Article › peer-review
  42 Citations (Scopus)

• TPC2 is a novel NAADP-sensitive Ca²⁺ release channel, operating as a dual sensor of luminal pH and Ca²⁺

  Pitt, S. J., Funnell, T. M., Sitsapesan, M., Venturi, E., Rietdorf, K., Ruas, M., Ganesan, A., Gosain, R., Churchill, G. C., Zhu, M. X., Parrington, J., Galione, A. & Sitsapesan, R., 5 Nov 2010, In: Journal of Biological Chemistry. 285, 45, p. 35039-35046 8 p.

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

  Open Access
  184 Citations (Scopus)
• 2009

  Analogues of the nicotinic acid adenine dinucleotide phosphate (NAADP) antagonist Ned-19 indicate two binding sites on the NAADP receptor

  Rosen, D., Lewis, A. M., Mizote, A., Thomas, J. M., Aley, P. K., Vasudevan, S. R., Parkesh, R., Galione, A., Izumi, M., Ganesan, A. & Churchill, G. C., 11 Dec 2009, In: Journal of Biological Chemistry. 284, 50, p. 34930-34934 5 p.

  Research output: Contribution to journal › Article › peer-review
  38 Citations (Scopus)

• A solid-phase total synthesis of the cyclic depsipeptide HDAC inhibitor spiruchostatin A

  Iijima, Y., Munakata, A., Shin-ya, K., Ganesan, A., Doi, T. & Takahashi, T., 17 Jun 2009, In: Tetrahedron Letters. 50, 24, p. 2970-2972 3 p.

  Research output: Contribution to journal › Article › peer-review
  25 Citations (Scopus)

• Depsipeptide Derivatives and their Therapeutic Use

  Shuttleworth, S. J., Ganesan, A., Cecil, A. R. L., Hill, T., Tomassi, C. & Silva, F. A., 2009, Patent No. WO/2009/022182

  Research output: Patent