Biography

ResearcherID profilehttp://www.researcherid.com/rid/F-6698-2011

PhD Positions

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Ganesan obtained a BSc (Hons) in Chemistry at the National University of Singapore (1986). He completed his PhD in synthetic methodology and total synthesis under the supervision of Clayton Heathcock at the Department of Chemistry, University of California-Berkeley (1992) and was subsequently a postdoctoral fellow with Gregory Verdine at the Department of Chemistry at Harvard University. In 1993, he joined the Institute of Molecular and Cell Biology in Singapore as a Senior Research Chemist at the Centre for Natural Product Research and in 1996 became Principal Investigator of the Institute’s Medicinal and Combinatorial Chemistry group. In 1999 he joined the University of Southampton as a Reader in the Combinatorial Chemistry Centre for Excellence. In 2011 he became the Chair of Chemical Biology at UEA’s School of Pharmacy. He is Director of Postgraduate Research and Head of the Healthy Ageing research theme within the School. 

Ganesan is co-founder of the biotech company Karus Therapeutics and Chair of the EU COST Action CM1406, 'Epigenetic Chemical Biology'. He sits on the IUPAC Subcommittee for Medicinal Chemistry and Drug Development and the Royal Society of Chemistry's Bioorganic & Medicinal Chemistry Sector committee.

Ganesan's research centres around chemical biology, medicinal chemistry and organic synthesis with an emphasis on biologically active natural products and epigenetics.

Selected publications

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.
Cardiovasc. Res. 2015, 108, 357–366.
DOI: 10.1093/cvr/cvv226

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. 
ACS Chem. Biol. 2013, 8, 1677–1682.
DOI: 10.1021//cb4001926

Total Synthesis and Stereochemical Assignment of Burkholdac B, a Depsipeptide HDAC Inhibitor
Benelkebir, H.; Donlevy, A. M.; Packham, G.; Ganesan, A
Org. Lett. 2011, 13, 6334–6337.
DOI: 10.1021/ol202197q

Determination of Molecular Torsion Angles Using Nuclear Singlet Relaxation
Tayler, M. C. D.; Marie, S.; Ganesan, A.; Levitt, M. H.
J. Am. Chem. Soc. 2010, 132, 8225–8227.
DOI: 10.1021/ja1012917

Identification of a Chemical Probe for NAADP by Virtual Screening
Naylor, E.; Arredouani, A.; Vasudevan, S. R.; Lewis, A. M.; Parkesh, R.; Mizote, A.; Rosen, D.; Thomas, J. M.; Izumi, M.; Ganesan, A.; Galione, A.; Churchill, G. C.
Nat. Chem. Biol. 2009, 5, 220-226.
DOI: 10.1038/nchembio.150
 

Highlighted Publications

See All

Hamon, M., Dickinson, N., Devineau, A., Bolien, D., Tranchant, M., Taillier, C., Jabin, I., Harrowven, D. C., Whitby, R. J., Ganesan, A., Dalla, V.

(2014)

Intra- and Intermolecular Alkylation of N , O -Acetals and π-Activated Alcohols Catalyzed by in Situ Generated Acid,

in Journal of Organic Chemistry

79.

pp. 1900-1912

Full Text UEA Repository

(Article)

(Published)


Li, M., Luo, B., Liu, Q., Hu, Y., Ganesan, A., Huang, P., Wen, S.

(2014)

Synthesis of N -Acyl- N , O -acetals Mediated by Titanium Ethoxide,

in Organic Letters

16.

pp. 10-13

Full Text UEA Repository

(Article)

(Published)


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.

(2013)

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

in ACS Chemical Biology

8.

pp. 1677-1682

Full Text UEA Repository

(Article)

(Published)


All Publications

See Highlights
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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.

(2017)

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

in Bioorganic & Medicinal Chemistry Letters

27

(10)

pp. 2099–2101

Full Text UEA Repository

(Article)

(Published)


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., O’reilly, K. M., Davies, D. E.

(2017)

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

in Oncotarget

8

pp. 48737-48754

Full Text UEA Repository

(Article)

(Published)


Hau, M., Zenk, F., Ganesan, A., Iovino, N., Jung, M.

(2017)

Cellular analysis of the action of epigenetics drugs and probes,

in Clinical Epigenetics

12

(5)

pp. 308-322

Full Text UEA Repository

(Article)

(Published)


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.

(2016)

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,

in Cardiovascular Research

108

(3)

pp. 357-366

Full Text UEA Repository

(Article)

(Published)


Santos, G. B., Ganesan, A., Emery, F. S.

(2016)

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

in ChemMedChem

11

(20)

pp. 2245–2251

Full Text

(Literature review)

(Published)


de Lera, A. R., Ganesan, A.

(2016)

Epigenetic polypharmacology: from combination therapy to multitargeted drugs,

in Clinical Epigenetics

8

article no. 105

Full Text UEA Repository

(Article)

(Published)


Shaheen, F., Jabeen, A., Ashraf, S., Nadeem-ul-Haque, M., Ali Shah, Z., Asad Ziaee, M., Dastagir, N., Ganesan, A.

(2016)

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

in Journal of Peptide Science

22

(9)

pp. 607-617

Full Text UEA Repository

(Article)

(Published)


Ganesan, A.

(2016)

Multitarget Drugs: an Epigenetic Epiphany,

in ChemMedChem

11

(12)

pp. 1227-1241

Full Text UEA Repository

(Article)

(Published)


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.

(2016)

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

in RSC Advances

6

(27)

pp. 22777-22780

Full Text UEA Repository

(Article)

(Published)


Zhu, D., Wu, Y., Wu, B., Luo, B., Ganesan, A., Wu, F., Pi, R., Huang, P., Wen, S.

(2014)

Three-Component Pd/Cu-Catalyzed Cascade Reactions of Cyclic Iodoniums, Alkynes, and Boronic Acids: An Approach to Methylidenefluorenes,

in Organic Letters

16

(9)

pp. 2350-2353

Full Text UEA Repository

(Article)

(Published)


Hamon, M., Dickinson, N., Devineau, A., Bolien, D., Tranchant, M., Taillier, C., Jabin, I., Harrowven, D. C., Whitby, R. J., Ganesan, A., Dalla, V.

(2014)

Intra- and Intermolecular Alkylation of N , O -Acetals and π-Activated Alcohols Catalyzed by in Situ Generated Acid,

in Journal of Organic Chemistry

79

(5)

pp. 1900-1912

Full Text UEA Repository

(Article)

(Published)


Li, M., Luo, B., Liu, Q., Hu, Y., Ganesan, A., Huang, P., Wen, S.

(2014)

Synthesis of N -Acyl- N , O -acetals Mediated by Titanium Ethoxide,

in Organic Letters

16

(1)

pp. 10-13

Full Text UEA Repository

(Article)

(Published)


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.

(2013)

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

in ACS Chemical Biology

8

(8)

pp. 1677-1682

Full Text UEA Repository

(Article)

(Published)


Robertson, J. C., Hurley, N. C., Tortorici, M., Ciossani, G., Borrello, M. T., Vellore, N. A., Ganesan, A., Mattevi, A., Baron, R., Briggs, J. M. (ed.)

(2013)

Expanding the Druggable Space of the LSD1/CoREST Epigenetic Target: New Potential Binding Regions for Drug-Like Molecules, Peptides, Protein Partners, and Chromatin,

in PLoS Computational Biology

9

(7)

article no. e1003158

Full Text UEA Repository

(Article)

(Published)


Shaheen, F., Rizvi, T. S., Musharraf, S. G., Ganesan, A., Xiao, K., Townsend, J. B., Lam, K. S., Choudhary, M. I.

(2012)

Solid-Phase Total Synthesis of Cherimolacyclopeptide E and Discovery of More Potent Analogues by Alanine Screening,

in Journal of Natural Products

75

(11)

pp. 1882-1887

Full Text UEA Repository

(Article)

(Published)


Bonnet, D., Margathe, J., Radford, S., Pflimlin, E., Riche, S., Doman, P., Hibert, M., Ganesan, A.

(2012)

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

in ACS Combinatorial Science

14

pp. 323-334

Full Text UEA Repository

(Article)

(Published)


Davies, E., Haitchi, H., Thatcher, T., Sime, P., Kottmann, R., Ganesan, A., Packham, G., O'Reilly, K., Davies, D.

(2012)

Spiruchostatin A Inhibits Proliferation and Differentiation of Fibroblasts from Patients with Pulmonary Fibrosis,

in American Journal of Respiratory Cell and Molecular Biology

46

(5)

pp. 687-694

Full Text UEA Repository

(Article)

(Published)


Benelkebir, H., Hodgkinson, C., Duriez, P., Hayden, A., Bulleid, R., Crabb, S., Packham, G., Ganesan, A.

(2011)

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

in Bioorganic & Medicinal Chemistry

19

(12)

pp. 3709-3716

Full Text UEA Repository

(Article)

(Published)


Benelkebir, H., Marie, S., Hayden, A., Lyle, J., Loadman, P., Crabb, S., Packham, G., Ganesan, A.

(2011)

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

in Bioorganic & Medicinal Chemistry

19

(12)

pp. 3650-3658

Full Text UEA Repository

(Article)

(Published)


Tiffon, C., Adams, J., van der Fits, L., Wen, S., Townsend, P., Ganesan, A., Hodges, E., Vermeer, M., Packham, G.

(2011)

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

in British Journal of Pharmacology

162

(7)

pp. 1590-1602

Full Text UEA Repository

(Article)

(Published)


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Key Research Interests

Cancer Research UK
Histone Methylation Inhibitors
G. Packham (U. Southampton) and A. Ganesan
2007-2011
£91,000

BBSRC
NAADP Receptor Antagonists
A. Gansan
2009-2012
£351,000

External Activities and Indicators of Esteem

  • 2010 - Chairman, EU COST Action ‘Epigenetics: Bench to Bedside’
  • 2007-2011 - Member, Organic Division Executive, Royal Society of Chemistry
  • 2006 - Committee Member, IUPAC Subcommitee for Medicinal Chemistry and Drug Development
  • 2006 - Treasurer, High-throughput Chemistry and New Technologies Subject Group, Royal Society of Chemistry
  • 2004 - Visiting professorship at Tokyo Institute of Technology, Japan Society for the Promotion of Science

Professional Activities

Patents

  • Packham, G. K.; Ganesan, A.; Mann, D. A.; Oakley, F.; Srinivasan, N. Sulfasalazine Analogues as NF- Inhibitors. WO2006072783.
  • Packham, G. K.; Ganesan, A.; Yurek-George, A.; Cecil, A. R. L. FK228 Derivates as HDAC Inhibitors. WO2006129105.
  • Packham, G. K.; Ganesan, A.; Cecil, A. R. L. Depsipeptides and their Therapeutic Use. WO2008062201.
  • Packham, G. K.; Ganesan, A.; Cecil, A. R. L. Depsipeptides and their Therapeutic Use. WO2008062232.
  • Rahman, Atta-ur; Choudhary, M. I.; Shaheen, F.; Ganesan, A.; Simjee, S. U.; Raza, A. M. New Anticonvulsant Compounds. US2008004353.