Raphaël Rodriguez, PhD, DR2 CNRS

Curriculum Vitae

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Raphaël Rodriguez was born in 1978 in Avignon. He performed his PhD studies under the supervision of Prof Sir Jack E. Baldwin and Prof Maurice Santelli at the University of Oxford and in Marseille, where he completed the synthesis of structurally complex natural products by means of pericyclic processes. He joined The University of Cambridge in November 2005 as a postdoctoral fellow, working under the mentorship of Prof. Sir Shankar Balasubramanian, where his work led to the invention of the potent G-quadruplex targeting small molecule pyridostatin. Together with Prof. Steve Jackson (Gurdon Institute, UK), they firmly established a link between G-quadruplex DNA structures and genomic instability. Raphaël joined the CNRS as a group leader in 2012 and was promoted Director of Research at Institut Curie in 2017. His recent achievements include the development of the anti-aging small molecule remodelin, the first chemical synthesis of the complex natural product marmycin and the iron metabolism targeting drug ironomycin. His group has recently elucidated the mechanism of action of salinomycin against cancer stem cells and identified a role of iron in the maintenance of these cells. The group has also provided evidence for a role of chromatin in regulating genome targeting with cisplatin.

2015-2017 Group Leader at Institut Curie, Paris, France

2012-2014 Group Leader at ICSN, Gif-sur-Yvette, France

2012 Habilitation à Diriger des Recherches (HDR), University Paris 11, France

2009-2012 Senior Research Associate (tenure), Department of Chemistry, Cambridge, UK

2005-2009 Postdoctoral Research Associate, Department of Chemistry, Cambridge, UK

2002-2005 European Doctorate (PhD), organic chemistry (very honorable distinction)

2000-2002 MSc, organic chemistry (very good distinction, ranked 1st), Montpellier, France

1997-2000 BSc, organic chemistry (good distinction, ranked 1st), Avignon, France

1994-1999 Fireman/Paramedic

Awards and Nominations

• 2019 Tetrahedron Young Investigator Award
• 2019 i-Lab Award for the company SideROS
• 2019 Grand Prix de l’Institut de France ‘Charles Defforey’
• 2019 SUNRISE Cancer Stem Cell Award
• 2017 Fellow of the Royal Society of Chemistry
• Franco-British Young Leaders
• K2 Trophy in oncology
• Pierre Fabre Award for Therapeutic Innovation
• ERC Consolidator Award
• Emergence Ville de Paris Award
• Junior Scientists Participation Program 48^th Bürgenstock Conference
• Fournier-SFC Prize

Full publication list

Articles

Visualizing biologically active small molecules in cells using click chemistry. Tatiana Cañeque, Sebastian Müller, Raphaël Rodriguez*. Nature Rev. Chem. (2018), in press

Targeting NAT10 enhances healthspan and lifespan in a mouse model of human accelerated aging syndrome. Gabriel Balmus, Delphine Larrieu, Ana C. Barros, Casey Collins, Monica Abrudan, Mukerrem Demir, Nicola Geisler, Christopher J. Lelliott, Jacqui White, Natasha A. Karp, James Atkinson, Andrea Kirton, Matt Jacobsen, Dean Clift, Sanger Mouse Genetics Project, Raphaël Rodriguez, David J. Adams, Stephen P. Jackson. Nature Comm. 9, (2018) 

An iron hand over cancer stem cells. A. Hamaï, T. Cañeque, S. Müller, T. T. Mai,A. Hienzsch, C. Ginestier, E. Charafe-Jauffret, P. Codogno, M. Mehrpour, R. Rodriguez. Autophagy, 2017, DOI:10.1080/15548627.2017.1327104

Click chemistry enables preclinical evaluation of targeted epigenetic therapies. Dean S. Tyler, Johanna Vappiani, Tatiana Cañeque, Enid Y. N. Lam, Aoife Ward, Omer Gilan, Yih-Chih Chan, Antje Hienzsch, Anna Rutkowska, Thilo Werner, Anne J. Wagner, Dave Lugo, Richard Gregory, Cesar Ramirez Molina, Neil Garton, Christopher R. Wellaway, Susan Jackson, Laura MacPherson, Margarida Figueiredo, Sabine Stolzenburg, Charles C. Bell, Colin House, Sarah-Jane Dawson, Edwin D. Hawkins, Gerard Drewes, Rab K. Prinjha, Raphaël Rodriguez, Paola Grandi, Mark A. Dawson. Science, 356, 1397-1401 (2017)

Salinomycin kills cancer stem cells by sequestering iron in lysosomes. Trang Thi Mai, Ahmed Hamaï, Antje Hienzsch, Tatiana Cañeque, Sebastian Müller, Julien Wicinski, Olivier Cabaud, Christine Leroy, Amandine David, Verónica Acevedo, Akihide Ryo, Christophe Ginestier, Daniel Birnbaum, Emmanuelle Charafe-Jauffret, Patrice Codogno, Maryam Mehrpour*, Raphaël Rodriguez* Nature Chem. 9,1025–1033 (2017), Highlighted in chemical & engineering news

Chromatin regulates genome targeting with cisplatin. Emmanouil Zacharioudakis, Poonam Agarwal, Alexandra Bartoli, Nathan Abell, Lavaniya Kunalingam, Valérie Bergoglio, Blerta Xhemalce, Kyle M. Miller*, Raphaël Rodriguez* Angew. Chem. Int. Ed. DOI: 10.1002/anie.201701144R1

PSL chemical biology symposia first 2016 edition: when chemistry and biology share the language of discovery. Arnaud Gautier, Raphaël Rodriguez* ChemBioChem DOI: 10.1002/cbic.201700117 (2017)

HNF1a acts as a tumor suppressor in steatosis-associated liver cancer by repressing PPAR g Cecilia Patitucci, Gabrielle Couchy, Alessia Bagattin, Tatiana Cañeque, Aurélien de Reynies, Jean-Yves Scoazec, Raphaël Rodriguez, Marco Pontoglio, Jessica Zucman-Rossi, Mario Pende, Ganna Panasyuk J. Clin. Invest. In Press (2017)

Click quantitative mass spectrometry identifies PIWIL3 as a mechanistic target of RNA interference activator enoxacin in cancer cells. Nathan S. Abell, Marvin Mercado, Tatiana Cañeque, Raphaël Rodriguez*, Blerta Xhemalce* J. Am. Chem. Soc. 139, 1400-1403 (2017)

Targeting cancer stem cells with small molecules. Sebastian Müller, Tatiana Cañeque, Verónica Acevedo, Raphaël Rodriguez* Isr. J. Chem. DOI: 10.1002/ijch.201600109. Special Stuart L. Schreiber & Kyriacos C. Nicolaou Wolf Prize special issue

Quinolizinium as a new fluorescent lysosomotropic probe. Emmanouil Zacharioudakis, Tatiana Cañeque, Raúl Custodio, Sebastian Müller, Ana M. Cuadro, Juan J. Vaquero, Raphaël Rodriguez Bioorg. & Med. Chem. Lett. 27, 203-207 (2017)

A synthetic study towards the marmycins and analogues. Tatiana Cañeque, Gomes Filipe, Trang Thi Mai, Florent Blanchard, Pascal Retailleau, Jean-François Gallard, Giovanni Maestri, Max Malacria, Raphaël Rodriguez Synthesis 48, A-F (2016)

Iron-dependent lysosomal dysfunction mediated by a natural products hybrid. Angelica Mariani, Trang Thi Mai, Emmanouil Zacharioudakis, Antje Hienzsch, Alexandra Bartoli, Tatiana Cañeque, Raphaël Rodriguez* Chem. Commun. 52, 1358-1360 (2016)

Synthesis of marmycin A and investigation into its cellular activity. Tatiana Cañeque, Filipe Gomes, Trang Thi Mai, Giovanni Maestri, Max Malacria, Raphaël Rodriguez* Nature Chem. 7, 744-751 (2015)

Differential targeting of human topoisomerase isoforms with small molecules. Angelica Mariani, Alexandra Bartoli, Mandeep Atwal, Ka C. Lee, Caroline A. Austin, Raphaël Rodriguez* J. Med. Chem. 58, 4851-4856 (2015)

Synthesis of unnatural steroids using the BISTRO strategy. Philippe Maurin, Delphine Moraleda, Raphaël Rodriguez, Maurice Santelli Synlett 26, 725-736 (2015)

Unravelling the genomic targets of small molecules using high-throughput sequencing. Raphaël Rodriguez*, Kyle M. Miller Nature Rev. Genet. 15, 783-796 (2014)

Chemical inhibition of NAT10 corrects defects of laminopathic cells. Delphine Larrieu, Sébastien Britton, Mukerrem Demir, Raphaël Rodriguez*, Stephen P. Jackson* Science 344, 527-532 (2014). Highlight in CEN

Modular construction of dynamic nucleodendrimers. Valentina Abet, Robert Evans, Florian Guibbal, Stefano Caldarelli, Raphaël Rodriguez* Angew. Chem. Int. Ed. 53, 4862-4866 (2014)

L’inhibition chimique de NAT10 corrige les défauts des cellules laminopathiques. Delphine Larrieu, Raphaël Rodriguez, Sébastien Britton Médecine & Science 30, 745-747 (2014)

Conference report: The 49^th EUCHEM conference on stereochemistry (Bürgenstock Conference 2014). Jan Cvengros, Raphaël Rodriguez* Chimia 68, 742-745 (2014)

G-quadruplex interacting small molecules and drug: from bench to bedside. Sebastian Müller, Raphaël Rodriguez Expert Rev. Clin. Pharmacol. 7, 663-679 (2014)

Guanosine and isoguanosine derivatives for supramolecular devices. Valentina Abet, Raphaël Rodriguez New J. Chem. 38, 5122-5128 (2014)

Biased and unbiased strategies to identify biologically active small molecules. Valentina Abet, Angelica Mariani, Fiona Truscott, Sébastien Britton, Raphaël Rodriguez* Bioorg. & Med. Chem. 22, 4474-4489 (2014). Special Shankar Balasubramanian Tetrahedron Prize special issue.

Electrophilic activation of allenenes and allenynes: analogies and differences between Brønsted and Lewis acid activation. Tatiana Cañeque, Fiona. M. Truscott, Raphaël Rodriguez, Giovanni Maestri, Max Malacria Chem. Soc. Rev. 43, 2916-2926 (2014)

Targeting G-quadruplexes with helical small molecules. Sebastian Müller, Katta Laxmi-Reddy, Prakrit V. Jena, Benoît Baptiste, Zeyuan Dong, Frédéric Godde, Taekjip Ha, Raphaël Rodriguez, Shankar Balasubramanian, Ivan Huc ChemBioChem 15, 2563-2570 (2014)

Nucleotide contributions to the structural integrity and DNA replication initiation activity of noncoding y RNA. Iren Wang, Madzia P. Kowalski, Alexander R. Langley, Raphaël Rodriguez, Shankar Balasubramanian, Shang-Te Danny Hsu, Torsten Krude Biochemistry 53, 5848-5863 (2014)

Selective RNA versus DNA G-quadruplex targeting by in situ click chemistry. Marco Di Antonio, Giulia Biffi, Angelica Mariani, Eun-Ang Raiber, Raphaël Rodriguez*, Shankar Balasubramanian* Angew. Chem. Int. Ed. 51, 11073-11078 (2012) Very Important Paper; Highlight in CEN; Cover Picture

Pyridostatin analogues promote telomere dysfunction and long-term growth inhibition in human cancer cells. Sebastian Müller, Deborah A. Sanders, Marco Di Antonio, Stephanos Matsis, Jean-François Riou, Raphaël Rodriguez*, Shankar Balasubramanian Org. Biomol. Chem. 10, 6537-6546 (2012)

Experimental approaches to identify cellular G-quadruplex structures and functions. Marco Di Antonio, Raphaël Rodriguez, Shankar Balasubramanian Methods 57, 84-92 (2012)

Small molecule-induced DNA damage identifies alternative DNA structures in human genes. Raphaël Rodriguez, Kyle M. Miller, Josep V. Forment, Charles R. Bradshaw, Sébastien Britton, Tobias Oelschlaegel, Mehran Nikan, Blerta Xhemalce, Shankar Balasubramanian, Stephen P. Jackson Nature Chem. Biol. 8, 301-310 (2012). Highlights in Nature Chem. Biol. and F1000; Most Accessed Article

A single-molecule platform for investigation of interactions between G-quadruplexes and small-molecule ligands. Deepak Koirala, Soma Dhakal, Beth Ashbridge, Yuta Sannohe, Raphaël Rodriguez, Hiroshi Sugiyama, Shankar Balasubramanian, Hanbin Mao Nature Chem. 3, 782-787 (2011)

The transcription factor FOXM1 is a cellular target of the natural product thiostrepton. Nagaratna S. Hegde, Deborah A. Sanders, Raphaël Rodriguez, Shankar Balasubramanian Nature Chem. 3, 725-731 (2011)

G-quadruplex-binding benzo[a]phenoxazines down-regulate c-KIT expression in human gastric carcinoma cells. Keith I. E. McLuckie, Zoë A. E. Waller, Deborah A. Sanders, David Alves, Raphaël Rodriguez, Jyotirmayee Dash, Grahame J. McKenzie, Ashok R. Venkitaraman, Shankar Balasubramanian J. Am. Chem. Soc. 133, 2658-2663 (2011)

G-quadruplexes: selective DNA targeting for cancer therapeutics? Kyle M. Miller, Raphaël Rodriguez* Expert Rev. Clin. Pharmacol. 4, 139-142 (2011)

Small-molecule-mediated G-quadruplex isolation from human cells. Sebastian Müller, Sunita Kumari, Raphaël Rodriguez*, Shankar Balasubramanian* Nature Chem. 2, 1095-1098 (2010). Highlight in F1000

Small molecule-mediated inhibition of translation by targeting a native RNA G-quadruplex. Anthony Bugaut, Raphaël Rodriguez, Sunita Kumari, Shang-Te Danny Hsu, Shankar Balasubramanian Org. Biomol. Chem. 8, 2771-2776 (2010)

Controlled-folding of a small molecule modulates DNA G-quadruplex recognition. Sebastian Müller, G. Dan Pantoş, Raphaël Rodriguez, Shankar Balasubramanian Chem. Commun. 80-82 (2009)

A novel small molecule that alters shelterin integrity and triggers a DNA-damage response at telomeres. Raphaël Rodriguez, Sebastian Müller, Justin A. Yeoman, Chantal Trentesaux, Jean-François Riou, Shankar Balasubramanian J. Am. Chem. Soc. 130, 15758-15759 (2008)

Selective recognition of a DNA G-quadruplex by an engineered antibody. Himesh Fernando, Raphaël Rodriguez, Shankar Balasubramanian Biochemistry 47, 9365-9371 (2008)

Exploring the differential recognition of DNA G-quadruplex targets by small molecules using dynamic combinatorial chemistry. Anthony Bugaut, Katja Jantos, Jean-Luc Wietor, Raphaël Rodriguez, Jeremy K. M. Sanders, Shankar Balasubramanian Angew. Chem. Int. Ed. 47, 2677-2680 (2008)

Triarylpyridines: a versatile small molecule scaffold for G-quadruplex recognition. Zoë A. E. Waller, Pravin S. Shirude, Raphaël Rodriguez, Shankar Balasubramanian Chem. Commun. 1467-1469 (2008)

Tri-substituted isoalloxazines as a new class of G-quadruplex binding ligands: small molecule regulation of c-kit oncogene expression. Mallesham Bejugam, Sven Sewitz, Pravin S. Shirude, Raphaël Rodriguez, Ramla Shahid, Shankar Balasubramanian J. Am. Chem. Soc. 129, 12926-12927 (2007)

Ligand-driven G-quadruplex conformational switching by using an unusual mode of interaction. Raphaël Rodriguez, G. Dan Pantoş, Diana P. N. Gonçalves, Jeremy K. M. Sanders, Shankar Balasubramanian Angew. Chem. Int. Ed. 46, 5405-5407 (2007)

Oxazole-based peptide macrocycles: a new class of G-quadruplex binding ligands. Katja Jantos, Raphaël Rodriguez, Sylvain Ladame, Pravin S. Shirude, Shankar Balasubramanian J. Am. Chem. Soc. 128, 13662-13663 (2006)

Tetramethylpyridiniumporphyrazines-a new class of G-quadruplex inducing and stabilising ligands. Diana P. N. Gonçalves, Raphaël Rodriguez, Shankar Balasubramanian, Jeremy K. M. Sanders Chem. Commun. 4685-4687 (2006)

Stereoselective synthesis of CD-ring precursors of vitamin D derivatives. Raphaël Rodriguez, Anne-Sophie Chapelon, Cyril Ollivier, Maurice Santelli Tetrahedron 65, 7001-7015 (2009)

Biomimetic synthesis of pyrone-derived natural products: exploring chemical pathways from a unique polyketide precursor. Serena J. Eade, Magnus W. Walter, Colin Byrne, Barbara Odell, Raphaël Rodriguez, Jack E. Baldwin, Robert M. Adlington, John E. Moses J. Org. Chem. 73, 4830-4839 (2008)

Enantioselective synthesis of steroids. Anne-Sophie Chapelon, Delphine Moraleda, Raphaël Rodriguez, Cyril Ollivier, Maurice Santelli Tetrahedron 63, 11511-11616 (2007)

Total synthesis of cyercene A and the biomimetic synthesis of (±)-9,10-deoxytridachione and (±)-ocellapyrone A. Raphaël Rodriguez, Robert M. Adlington, Serena J. Eade, Magnus W. Walter, Jack E. Baldwin, John E. Moses Tetrahedron 63, 4500-4509 (2007)

Desymmetrization of the anti-meso-acetylmethyldivinylcyclopentane by directed epoxidation and its application to the synthesis of a polyfunctionalized trans-hydrindane unit. Raphaël Rodriguez, Cyril Ollivier, Maurice Santelli Synlett 312-314 (2006)

A new and efficient method for o-quinone methide intermediate generation: application to the biomimetic synthesis of the benzopyran derived natural products (±)-lucidene and (±)-alboatrin. Raphaël Rodriguez, John E. Moses, Robert M. Adlington, Jack E. Baldwin Org. Biomol. Chem. 3, 3488-3495 (2005). Hot Paper; Cover Picture

Biomimetic synthesis of the (±)-9,10-deoxytridachione. John E. Moses, Robert M. Adlington, Raphaël Rodriguez, Serena J. Eade, Jack E. Baldwin Chem. Commun. 1687-1689 (2005)

A new and efficient method for o-quinone methide intermediate generation: application to the biomimetic synthesis of (±)-alboatrin. Raphaël Rodriguez, Robert M. Adlington, John E. Moses, Andrew Cowley, Jack E. Baldwin Org. Lett. 6, 3617-3619 (2004)

Vitamin D: a concise synthesis of the C₁₉ hydroxylated enyne A-ring, an interesting precursor for the preparation of C₁₉ substituted vitamin D analogues. Raphaël Rodriguez, Cyril Ollivier, Maurice Santelli Tetrahedron Lett. 45, 2289-2292 (2004)

 

Book chapters

Evidence of G-quadruplexes in cells. Sébastien Britton, Alexandra Bartoli, Raphaël Rodriguez* Future Science DOI: 10.4155/FSEB2013.13.110, eISBN number 978-1-910419-68-7

Catalytic cycloaddition reactions. Fiona R. Truscott, Giovanni Maestri, Raphaël Rodriguez, Max Malacria in Modern Alkyne Chemistry: Catalytic and Atom-Economic Transformations: (Eds.: Barry M. Trost & Chao-Jun Li), John Wiley & Sons, Inc. 143-167 (2014)

Target-oriented and diversity-oriented organic synthesis. Raphaël Rodriguez* in Modern Tools for the Synthesis of Complex Bioactive Molecules: (Eds.: J. Cossy & S. Arseniyadis), John Wiley & Sons, Inc. 513-538 (2012)

Commentaries

Voices of chemical biology. Raphaël Rodriguez Nature Chem. Biol. 11, 826-827 (2015)

Voices of chemical biology. Raphaël Rodriguez Nature Chem. Biol. 11, 546-547 (2015)

Patents

Visual detection of platinated DNA lesions from a clickable cisplatin probe used as diagnostic tool or to identify synergistic treatments. Emmanouil Zacharioudakis, Lavaniya Kunalingam, Poonam Agarwal, Alexandra Bartoli, Kyle M. Miller, Raphaël Rodriguez. PCT/EP2016/081166

Total cellular iron as a marker of cancer stem cells and uses thereof. Trang Mai, Ahmed Hamaï, Maryam Mehrpour, Raphaël Rodriguez. EP16305266.5

Nitrogen-containing analogs of Salinomycin, synthesis and use against cancer stem cells and malaria. Trang Mai, Antje Hienzsch, Ahmed Hamaï, Maryam Mehrpour, Raphaël Rodriguez. PCT/EP2015/070975

Method for preparing marmycin a and analogues thereof, and also uses thereof. Tatiana Cañeque, Filipe Gomes, Trang Thi Mai, Giovanni Maestri, Max Malacria, Raphaël Rodriguez. WO2016034559 A1

KAT inhibitors for the treatment of laminopathies, ageing and cancer. Delphine Larrieu, Sébastien Britton, Raphaël Rodriguez, Stephen P. Jackson. PCT/GB2015/051040