Items where Author is "Ganesan, A."

Article

Tammam, Mohamed A., Pereira, Florbela, Skellam, Elizabeth, Bidula, Stefan, Ganesan, A. and El-Demerdash, Amr (2025) The cytochalasans: Potent fungal natural products with application from bench to bedside. Natural Product Reports, 42 (5). pp. 788-841. ISSN 0265-0568

Le, Meiling, Lu, Wenhua, Tan, Xiaozhuo, Luo, Bingling, Yu, Tiantian, Sun, Yameng, Guo, Zhirong, Huang, Peng, Zhu, Daqian, Wu, Qiang, Ganesan, A. and Wen, Shijun (2024) Design, synthesis, and biological evaluation of potent EZH2/LSD1 dual inhibitors for prostate cancer. Journal of Medicinal Chemistry, 67 (17). pp. 15586-15605. ISSN 0022-2623

Bulut, Ipek, Lee, Adam, Cevatemre, Buse, Ruzic, Dusan, Belle, Roman, Kawamura, Akane, Gul, Sheraz, Nikolic, Katarina, Ganesan, A. and Acilan, Ceyda (2022) Dual LSD1 and HDAC6 inhibition induces doxorubicin sensitivity in acute myeloid leukemia cells. Cancers, 14 (23). ISSN 2072-6694

Ruzic, Dusan, Ellinger, Bernhard, Djokovic, Nemanja, Santibanez, Juan F., Gul, Sheraz, Beljkas, Milan, Djuric, Ana, Ganesan, Arasu, Pavic, Aleksandar, Srdic-Rajic, Tatjana, Petkovic, Milos and Nikolic, Katarina (2022) Discovery of 1-benzhydryl-piperazine-based HDAC inhibitors with anti-breast cancer activity: Synthesis, molecular modeling, in vitro and in vivo biological evaluation. Pharmaceutics, 14 (12). ISSN 1999-4923

Eliandro da Silva Júnior, Paulo, de Melo, Shaiani Maria Gil, de Paula, Murilo Helder, Vessecchi, Ricardo, Opatz, Till, Day, James E. H., Ganesan, A. and da Silva Emery, Flavio (2022) Growth vector elaboration of fragments: Regioselective functionalization of 5-hydroxy-6-azaindazole and 3-hydroxy-2,6-naphthyridine. Organic and Biomolecular Chemistry, 20 (37). pp. 7483-7490. ISSN 1477-0520

Nadeem-ul-Haque, Muhammad, Bashir, Anila, Karim, Humira, Khan, Sadiq Noor, Shah, Zafar Ali, Jabeen, Almas, Qayyum, Shaista, Ganesan, A., Choudhary, M. Iqbal and Shaheen, Farzana (2022) Synthesis of [1-8-NαC]-zanriorb A1, alanine-containing analogues, and their cytotoxic and anti-inflammatory activity. Journal of Peptide Science, 28 (8). ISSN 1075-2617

Ganesan, A., Aldholmi, Mohammed, Ahmad, Rizwan, Carretero-Molina, Daniel, Pérez-Victoria, Ignacio, Martín, Jesús, Reyes, Fernando, Genilloud, Olga, Gourbeyre, Léa, Gefflaut, Thierry, Carlsson, Hanne, Maklakov, Alexei, Field, Robert A., O'Neill, Ellis, Wilkinson, Barrie and O'Connell, Maria (2022) Euglenatides, potent antiproliferative cyclic peptides isolated from the freshwater photosynthetic microalga Euglena gracilis. Angewandte Chemie-International Edition, 61 (23). ISSN 1433-7851

Vaidergorn, Miguel M., da Silva Emery, Flavio and Ganesan, A. (2021) From hit seeking to magic bullets: The successful union of epigenetic and fragment based drug discovery (EPIDD + FBDD). Journal of Medicinal Chemistry, 64 (19). pp. 13980-14010. ISSN 0022-2623

Piyasirananda, Waraporn, Beekman, Andrew, Ganesan, A., Bidula, Stefan and Stokes, Leanne (2021) Insights into the structure-activity relationship of glycosides as positive allosteric modulators acting on P2X7 receptors. Molecular Pharmacology, 99 (2). pp. 163-174. ISSN 0026-895X

De Lera, Angel R. and Ganesan, A. (2020) Two-hit wonders: The expanding universe of multitargeting epigenetic agents. Current Opinion in Chemical Biology, 57. pp. 135-154. ISSN 1367-5931

Kawamura, Akane and Ganesan, A. (2020) Editorial overview: Epigenetics equals chemical biology. Current Opinion in Chemical Biology, 57. A1-A4. ISSN 1367-5931

Coutinho Carneiro, Vitor, de Abreu da Silva, Isabel Caetano, Amaral, Murilo Sena, Pereira, Adriana S.A., Silveira, Gilbert Oliveira, Pires, David da Silva, Verjovski-Almeida, Sergio, Dekker, Frank J., Rotili, Dante, Mai, Antonello, Lopes-Torres, Eduardo José, Robaa, Dina, Sippl, Wolfgang, Pierce, Raymond J., Borrello, M. Teresa, Ganesan, A., Lancelot, Julien, Thiengo, Silvana, Fernandez, Monica Ammon, Vicentino, Amanda Roberta Revoredo, Mourão, Marina Moraes, Coelho, Fernanda Sales and Fantappié, Marcelo Rosado (2020) Pharmacological inhibition of lysine-specific demethylase 1 (LSD1) induces global transcriptional deregulation and ultrastructural alterations that impair viability in Schistosoma mansoni. PLoS Neglected Tropical Diseases, 14 (7). ISSN 1935-2727

Aldholmi, Mohammed, Wilkinson, Barrie and Ganesan, A (2020) Epigenetic modulation of secondary metabolite profiles in Aspergillus calidoustus and Aspergillus westerdijkiae through histone deacetylase (HDAC) inhibition by vorinostat. Journal of Antibiotics, 73 (6). 410–413. ISSN 0021-8820

Liang, Liyun, Wang, Haiwen, Du, Yongliang, Luo, Bingling, Meng, Ning, Cen, Meifeng, Huang, Peng, Ganesan, A. and Wen, Shijun (2020) New tranylcypromine derivatives containing sulfonamide motif as potent LSD1 inhibitors to target acute myeloid leukemia: Design, synthesis and biological evaluation. Bioorganic Chemistry, 99. ISSN 0045-2068

Ohsawa, Kosuke, Zhao, Hongbin, Tokunaga, Takuya, Thomas, Carys, Ganesan, A., Masuda, Yuichi and Doi, Takayuki (2020) Stereoselective synthesis of protected l-allo-Enduracididine and l-Enduracididine via asymmetric nitroaldol reaction. Synthesis, 52 (6). pp. 942-948. ISSN 0039-7881

Maujean, Timothé, Girard, Nicolas, Ganesan, A., Gulea, Mihaela and Bonnet, Dominique (2020) Three cheers for nitrogen: aza-DKPs, the aza analogues of 2,5-diketopiperazines. RSC Advances, 10 (71). pp. 43358-43370. ISSN 2046-2069

Aldholmi, Mohammed, Marchand, Pascal, Ourliac-Garnier, Isabelle, Le Pape, Patrice and Ganesan, A. (2019) A decade of antifungal leads from natural products: 2010-2019. Pharmaceuticals, 12 (4). ISSN 1424-8247

Ganesan, A., Arimondo, Paola B., Rots, Marianne G., Jeronimo, Carmen and Berdasco, Mariá (2019) The timeline of epigenetic drug discovery:From reality to dreams. Clinical Epigenetics, 11 (1). ISSN 1868-7075

Ruzic, Dusan, Petkovic, Milos, Agbaba, Danica, Ganesan, A. and Nikolic, Katarina (2019) Combined ligand and fragment-based drug design of selective histone deacetylase – 6 inhibitors. Molecular Informatics, 38 (5). ISSN 1868-1743

Vaidergorn, Miguel M., Carneiro, Zumira A., Lopes, Carla D., de Albuquerque, Sérgio, Reis, Felipe C.C., Nikolaou, Sofia, Mello, Juliana F.R., Genesi, Giovani L., Trossini, Gustavo H.G., Ganesan, A. and Emery, Flavio S. (2018) β-amino alcohols and their respective 2-phenyl-N-alkyl aziridines as potential DNA minor groove binders. European Journal of Medicinal Chemistry, 157. pp. 657-664. ISSN 0223-5234

Shaheen, Farzana, Nadeem-ul-Haque, Muhammad, Ahmed, Aqeel, Simjee, Shabana U., Ganesan, A., Jabeen, Almas, Shah, Zafar Ali and Choudhary, M. Iqbal (2018) Synthesis of breast cancer targeting conjugate of temporin-SHa analog and its effect on pro- and anti-apoptotic protein expression in MCF-7 cells. Peptides, 106. pp. 68-82. ISSN 0196-9781

Regufe da Mota, Sergio, Bailey, Sarah, Strivens, Rosemary A., Hayden, Annette L., Douglas, Leon R., Duriez, Patrick J., Borrello, M. Teresa, Benelkebir, Hanae, Ganesan, A., Packham, Graham and Crabb, Simon J. (2018) LSD1 inhibition attenuates androgen receptor V7 splice variant activation in castration resistant prostate cancer models. Cancer Cell International, 18. ISSN 1475-2867

Silva, Anna C., Benelkebir, Hanae, Lopes, Rosangela S. C., Lopes, Claudio C. and Ganesan, A. (2018) Total synthesis of altissimacoumarin D, a small molecule sirtuin1 activator. Journal of the Brazilian Chemical Society, 29 (5). pp. 1157-1161. ISSN 0103-5053

Borrello, Maria Teresa, Schinor, Benjamin, Bartels, Katharina, Benelkebir, Hanae, Pereira, Sara, Al-Jamal, Wafa T., Douglas, Leon, Duriez, Patrick J., Packham, Graham, Haufe, Günter and Ganesan, A. (2017) Fluorinated tranylcypromine analogues as inhibitors of lysine-specific demethylase 1 (LSD1, KDM1A). Bioorganic & Medicinal Chemistry Letters, 27 (10). 2099–2101. ISSN 0960-894X

Conforti, Franco, Davies, Elizabeth R., Calderwood, Claire J., Thatcher, Thomas H., Jones, Mark G., Smart, David E., Mahajan, Sumeet, Alzetani, Aiman, Havelock, Tom, Maher, Toby M., Molyneaux, Philip L., Thorley, Andrew J., Tetley, Teresa D., Warner, Jane A.­, Packham, Graham, Ganesan, A., Skipp, Paul J., Marshall, Benjamin J., Richeldi, Luca, Sime, Patricia J., O’reilly, Katherine M.a. and Davies, Donna E. (2017) The histone deacetylase inhibitor, romidepsin, as a potential treatment for pulmonary fibrosis. Oncotarget, 8. pp. 48737-48754. ISSN 1949-2553

Hau, Mirjam, Zenk, Fides, Ganesan, A., Iovino, Nicola and Jung, Manfred (2017) Cellular analysis of the action of epigenetics drugs and probes. Epigenetics, 12 (5). pp. 308-322. ISSN 1559-2294

Davidson, Sean M., Foote, Kirsty, Kunuthur, Suma, Gosain, Raj, Tan, Noah, Tyser, Richard, Zhao, Yong Juan, Graeff, Richard, Ganesan, A., Duchen, Michael R., Patel, Sandip and Yellon, Derek 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. Cardiovascular Research, 108 (3). pp. 357-366. ISSN 0008-6363

Santos, Gabriela B., Ganesan, A. and Emery, Flavio S. (2016) Oral administration of peptide-based drugs: Beyond Lipinski's rule. ChemMedChem, 11 (20). 2245–2251. ISSN 1860-7179

de Lera, Angel R. and Ganesan, A. (2016) Epigenetic polypharmacology: from combination therapy to multitargeted drugs. Clinical Epigenetics, 8. ISSN 1868-7075

Shaheen, Farzana, Jabeen, Almas, Ashraf, Samreen, Nadeem-ul-Haque, Muhammad, Ali Shah, Zafar, Asad Ziaee, Muhammad, Dastagir, Nida and Ganesan, A. (2016) Total synthesis, structural, and biological evaluation of stylissatin A and related analogs. Journal of Peptide Science, 22 (9). pp. 607-617. ISSN 1075-2617

Ganesan, A. (2016) Multitarget drugs: an epigenetic epiphany. ChemMedChem, 11 (12). pp. 1227-1241. ISSN 1860-7179

Silva Júnior, P. E., Rezende, L. C D, Gimenes, Julia Possamai, Maltarollo, Vinícius Goncąlves, Dale, James, Trossini, G. H G, Emery, F. S. and Ganesan, A. (2016) Synthesis of two 'heteroaromatic rings of the future' for applications in medicinal chemistry. RSC Advances, 6 (27). pp. 22777-22780. ISSN 2046-2069

Zhu, Daqian, Wu, Yongcheng, Wu, Baojian, Luo, Bingling, Ganesan, A., Wu, Fu-hai, Pi, Rongbiao, Huang, Peng and Wen, Shijun (2014) Three-component Pd/Cu-catalyzed cascade reactions of cyclic iodoniums, alkynes, and boronic acids: An approach to methylidenefluorenes. Organic Letters, 16 (9). pp. 2350-2353. ISSN 1523-7060

Hamon, Mélanie, Dickinson, Niall, Devineau, Alice, Bolien, David, Tranchant, Marie-José, Taillier, Catherine, Jabin, Ivan, Harrowven, David C., Whitby, Richard J., Ganesan, A. and Dalla, Vincent (2014) Intra- and intermolecular alkylation of N,O-acetals and π-activated alcohols catalyzed by in situ generated acid. Journal of Organic Chemistry, 79 (5). pp. 1900-1912. ISSN 0022-3263

Li, Min, Luo, Bingling, Liu, Qi, Hu, Yumin, Ganesan, A., Huang, Peng and Wen, Shijun (2014) Synthesis of N-acyl-N,O-acetals mediated by titanium ethoxide. Organic Letters, 16 (1). pp. 10-13. ISSN 1523-7060

Tortorici, Marcello, Borrello, Maria Teresa, Tardugno, Maria, Chiarelli, Laurent R, Pilotto, Simona, Ciossani, Giuseppe, Vellore, Nadeem A, Bailey, Sarah G, Cowan, Jonathan, O'Connell, Maria, Crabb, Simon J, Packham, Graham, Mai, Antonello, Baron, Riccardo, Ganesan, A and Mattevi, Andrea (2013) Protein recognition by short peptide reversible inhibitors of the chromatin-modifying LSD1/CoREST lysine demethylase. ACS Chemical Biology, 8 (8). pp. 1677-1682. ISSN 1554-8937

Robertson, James C., Hurley, Nate C., Tortorici, Marcello, Ciossani, Giuseppe, Borrello, Maria Teresa, Vellore, Nadeem A., Ganesan, A., Mattevi, Andrea and Baron, Riccardo (2013) Expanding the druggable space of the LSD1/CoREST epigenetic target: New potential binding regions for drug-like molecules, peptides, protein partners, and chromatin. PLoS Computational Biology, 9 (7). ISSN 1553-7358

Shaheen, Farzana, Rizvi, Tania S., Musharraf, Syed G., Ganesan, A., Xiao, Kai, Townsend, Jared B., Lam, Kit S. and Choudhary, M. Iqbal (2012) Solid-phase total synthesis of cherimolacyclopeptide E and discovery of more potent analogues by alanine screening. Journal of Natural Products, 75 (11). pp. 1882-1887. ISSN 0163-3864

Davies, Elizabeth R., Haitchi, Hans Michael, Thatcher, Thomas H., Sime, Patricia J., Kottmann, R. Matthew, Ganesan, A, Packham, Graham, O'Reilly, Katherine M. A. and Davies, Donna E. (2012) Spiruchostatin A inhibits proliferation and differentiation of fibroblasts from patients with pulmonary fibrosis. American Journal of Respiratory Cell and Molecular Biology, 46 (5). pp. 687-694. ISSN 1044-1549

Bonnet, Dominique, Margathe, Jean-François, Radford, Sally, Pflimlin, Elsa, Riche, Stéphanie, Doman, Pete, Hibert, Marcel and 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). ACS Combinatorial Science, 14 (5). pp. 323-334. ISSN 2156-8952

Benelkebir, Hanae, Hodgkinson, Christopher, Duriez, Patrick J., Hayden, Annette L., Bulleid, Rosemary A., Crabb, Simon J., Packham, Graham and Ganesan, A (2011) Enantioselective synthesis of tranylcypromine analogues as lysine demethylase (LSD1) inhibitors. Bioorganic & Medicinal Chemistry, 19 (12). pp. 3709-3716.

Benelkebir, Hanae, Marie, Sabrina, Hayden, Annette L., Lyle, Jason, Loadman, Paul M., Crabb, Simon J., Packham, Graham and Ganesan, A (2011) Total synthesis of largazole and analogues: HDAC inhibition, antiproliferative activity and metabolic stability. Bioorganic & Medicinal Chemistry, 19 (12). pp. 3650-3658.

Tiffon, C. E., Adams, J. E., van der Fits, L., Wen, S., Townsend, P. A., Ganesan, A., Hodges, E., Vermeer, M. H. and Packham, G. (2011) The histone deacetylase inhibitors vorinostat and romidepsin downmodulate IL-10 expression in cutaneous T-cell lymphoma cells. British Journal of Pharmacology, 162 (7). pp. 1590-1602. ISSN 1476-5381

Benelkebir, Hanae, Donlevy, Alison M., Packham, Graham and Ganesan, A. (2011) Total synthesis and stereochemical assignment of burkholdac B, a depsipeptide HDAC inhibitor. Organic Letters, 13 (24). pp. 6334-6337. ISSN 1523-7060

Izumi, Minoru, Kido, Takeshi, Murakami, Miyu, Nakajima, Shuhei and Ganesan, A (2011) Pictet-Spengler reaction using ion-exchange resin as a catalyst and support for ‘catch and release’ purification. Bioscience, Biotechnology, and Biochemistry, 75 (2). pp. 391-392. ISSN 0916-8451

Pitt, Samantha J., Funnell, Tim M., Sitsapesan, Mano, Venturi, Elisa, Rietdorf, Katja, Ruas, Margarida, Ganesan, A, Gosain, Rajendra, Churchill, Grant C., Zhu, Michael X., Parrington, John, Galione, Antony and Sitsapesan, Rebecca (2010) TPC2 is a novel NAADP-sensitive Ca2+ release channel, operating as a dual sensor of luminal pH and Ca2+. Journal of Biological Chemistry, 285 (45). pp. 35039-35046. ISSN 0021-9258

Tayler, Michael C. D., Marie, Sabrina, Ganesan, A. and Levitt, Malcolm H. (2010) Determination of molecular torsion angles using nuclear singlet relaxation. Journal of the American Chemical Society, 132 (24). pp. 8225-8227. ISSN 0002-7863

Rosen, Daniel, Lewis, Alexander M., Mizote, Akiko, Thomas, Justyn M., Aley, Parvinder K., Vasudevan, Sridhar R., Parkesh, Raman, Galione, Antony, Izumi, Minoru, Ganesan, A. and Churchill, Grant C. (2009) Analogues of the nicotinic acid adenine dinucleotide phosphate (NAADP) antagonist Ned-19 indicate two binding sites on the NAADP receptor. Journal of Biological Chemistry, 284 (50). pp. 34930-34934. ISSN 0021-9258

Ganesan, A., Nolan, L., Crabb, S. J. and Packham, G. (2009) Epigenetic therapy: Histone acetylation, DNA methylation and anti-cancer drug discovery. Current Cancer Drug Targets, 9 (8). pp. 963-981. ISSN 1568-0096

Sharp, Adam, Crabb, Simon J., Johnson, Peter W. M., Hague, Angela, Cutress, Ramsey, Townsend, Paul A., Ganesan, A. and Packham, Graham (2009) Thioflavin S (NSC71948) interferes with Bcl-2-associated athanogene (BAG-1)-mediated protein-protein interactions. Journal of Pharmacology and Experimental Therapeutics, 331 (2). pp. 680-689. ISSN 0022-3565

Iijima, Yusuke, Munakata, Asami, Shin-ya, Kazuo, Ganesan, A., Doi, Takayuki and Takahashi, Takashi (2009) A solid-phase total synthesis of the cyclic depsipeptide HDAC inhibitor spiruchostatin A. Tetrahedron Letters, 50 (24). pp. 2970-2972.

Naylor, Edmund, Arredouani, Abdelilah, Vasudevan, Sridhar R., Lewis, Alexander M., Parkesh, Raman, Mizote, Akiko, Rosen, Daniel, Thomas, Justyn M., Izumi, Minoru, Ganesan, A., Galione, Antony and Churchill, Grant C. (2009) Identification of a chemical probe for NAADP by virtual screening. Nature Chemical Biology, 5 (4). pp. 220-226. ISSN 1552-4450

Wen, Shijun, Packham, Graham and Ganesan, A. (2008) Macrolactamization versus macrolactonization: Total synthesis of FK228, the depsipeptide histone deacetylase inhibitor. The Journal of Organic Chemistry, 73 (23). pp. 9353-9361. ISSN 0022-3263

Nolan, L, Johnson, P W M, Ganesan, A, Packham, G and Crabb, S J (2008) Will histone deacetylase inhibitors require combination with other agents to fulfil their therapeutic potential? British Journal of Cancer, 99 (5). pp. 689-694. ISSN 0007-0920

Ganesan, A (2008) The impact of natural products upon modern drug discovery. Current Opinion in Chemical Biology, 12 (3). pp. 306-317. ISSN 1879-0402

Yurek-George, Alexander, Cecil, Alexander Richard Liam, Mo, Alex Hon Kit, Wen, Shijun, Rogers, Helen, Habens, Fay, Maeda, Satoko, Yoshida, Minoru, Packham, Graham and Ganesan, A. (2007) The first biologically active synthetic analogues of FK228, the depsipeptide histone deacetylase inhibitor. Journal of Medicinal Chemistry, 50 (23). pp. 5720-5726. ISSN 0022-2623

Wen, Shijun, Carey, Krystle L., Nakao, Yoichi, Fusetani, Nobuhiro, Packham, Graham and Ganesan, A. (2007) Total synthesis of azumamide A and azumamide E, evaluation as histone deacetylase inhibitors, and design of a more potent analogue. Organic Letters, 9 (6). pp. 1105-1108. ISSN 1523-7060

Book Section

Ganesan, A. (2020) Targeting the Zinc-Dependent Histone Deacetylases (HDACs) for Drug Discovery. In: Topics in Medicinal Chemistry. Topics in Medicinal Chemistry . Springer, pp. 1-27. ISBN 978-3-030-42981-2

Ganesan, A. (2020) HDAC inhibitors in cancer therapy. In: Histone Modifications in Therapy. Elsevier, pp. 19-49. ISBN 9780128164228

Patent

Shuttleworth, Steven Joseph (2009) Depsipeptide Derivatives and their Therapeutic Use. WO/2009/022182.

Packham, Graham (2008) Depsipeptides and their Therapeutic Use. WO2008062232.

Ganesan, A. (2006) Sulfasalazine analogues as nf-kb inhibitors. WO2006072783.

Ganesan, A. (2005) Fk 228 derivates as hdac inhibitors. WO-2006129105-A1.