Researchers

Erika Bourguet

Title: Ass. Professor

First name: Erika

Surname: Bourguet

Web Site:

E-mail: e.bourguet@imb.uq.edu.au

Background:

I received my Ph.D. in Organic Chemistry from the University of Montpellier II in France in 2000, after which I completed a two-year postdoctoral appointment with Pr. D. Schinzer at the Chemisches Institut of the University of Magdeburg (Germany). I then worked for two years with Pr. J. D. Brion in the BioCIS laboratory (UMR-CNRS-8076) at the University of Châtenay-Malabry (France). In 2004, I was appointed Associate Professor of Organic Chemistry at the Reims Institute of Molecular Chemistry (UMR-CNRS-7312) at the University of Reims-Champagne-Ardenne (France), and I obtained the habilitation in 2011.

 

My research interests:

My first research topics were the synthesis of peptide mimetics (RGD, beta-strand/sheet) and total synthesis of natural compounds (Epothilone, Trungapeptin). Then, I shifted my research interests to the development of metalloenzyme inhibitors (MMPI, HDACI).

 

In 2018, I join Professor Fairlie’s group at the Institute for Molecular Bioscience in a visting position with an expectation to utilize IMB’s world-class infrastructure and expertise in both HDAC field and its application. It is a very interesting laboratory where you can work with a team of chemists, molecular modellers, biologists and pharmacologists in one place.

Publications:

HDACs

E. Bourguet*, K. Ozdarska, G. Moroy, J. Jeanblanc, M. Naassila*, “Class I HDAC Inhibitors: Potential New Epigenetic Therapy for Alcohol Use Disorder (AUD)”, J. Med. Chem. Perspective, 2017, DOI: 10.1021/acs.jmedchem.7b00115

 

R. Legastelois, J. Jeanblanc, C. Vilpoux, E. Bourguet, M. Naassila*, ”Mécanismes  épigénétiques et troubles de l’usage d’alcool : une cible thérapeutique intéressante ?”, Biologie Aujourd’hui, 2017, 211(1), 83-91.

 

MMPs

E. Bourguet*, K. Brazhnik, A. Sukhanova, G. Moroy, S. Brassart-Pasco, A-P. Martin, I. Villena, G. Bellon, J. Sapi, I. Nabiev, “Design, synthesis and use of MMP-2 inhibitor-conjugated quantum dots in functional biochemical assays”, Bio. Conj. Chem., 2016, 27(4), 1067-1081.

 

G. Moroy, E. Bourguet, M. Decarme, J. Sapi, A. J. P. Alix, W. Hornebeck, S. Lorimier*, “Inhibition of Human Neutrophil Elastase, Plasmin and Matrix Metalloproteinases
by Oleic acid and Oleoyl-Galardin derivative(s)”, Biochem. Pharmacol., 2011, 81, 626–635.

 

M. Rouffet, C. Denhez, E. Bourguet, F. Bohr, D. Guillaume*, “In silico study of new inhibitors of MMPs”, Org. Biomol. Chem., 2009, 7(18), 3817-3825.

 

G. LeDour, G. Moroy, M. Rouffet, E. Bourguet, D. Guillaume, M. Decarme, H. ElMourabit, F. Augé, A. J. P. Alix, J-Y. Laronze, G. Bellon, W. Hornebeck, J. Sapi*, “Introduction of the 4-(4-bromophenyl)benzenesulfonyl group to hydrazide analogs of Ilomastat leads to potent gelatinase-B (MMP-9) inhibitors with improved selectivity”, Bioorg. Med. Chem., 2008, 16(18), 8745-8759.

 

G. Moroy, H. El Mourabit, A. Toribio, C. Denhez, A. Dassonville, M. Decarme, J. H. Renault, C. Mirand, G. Bellon, J. Sapi, A. J. P. Alix, W. Hornebeck, E. Bourguet*, “Simultaneous presence of unsaturation and long alkyl chain at P1’ of Ilomastat confers selectivity for gelatinase A (MMP-2) over gelatinase B (MMP-9) inhibition as shown by molecular modelling studies”, Bioorg. Med. Chem., 2007, 15(14), 4753-4766.

 

Total synthesis

F. Fécourt, J. Sapi, E. Bourguet* , “The Total Synthesis of Trungapeptin A”, Synlett, 2010, 3, 399-402.

 

D. Schinzer,* E. Bourguet, S. Ducki, “Synthesis of Furano-Epothilone D”, Chem. Eur. J., 2004, 10(13), 3217-3224.

 

RGD peptidomimetics

E. Bourguet, J-L. Banères, J. Parello, X. Lusinchi, J-P. Girard,* J-P. Vidal, “Nonpeptide RGD antagonists. A novel class of mimetics, the 5,8-disubstituted 1-azabicyclo[5.2.0]nonan-2-one lactam”, Bioorg. Med. Chem. Lett., 2003, 13(9), 1561-1564.

 

E. Bourguet, J-L. Baneres, J-P. Girard,* J. Parello, J-P. Vidal, X. Lusinchi, J-P. Declercq, ”Photochemical Rearrangement of Oxaziridines and Nitrones in the Hexahydroindole Series: A Convenient Synthetic Route to 1-Azabicyclo[5.2.0]nonan-2-ones as Novel RGD Mimetics”, Org. Lett., 2001, 3(20), 3067-3070.

 

 

Former Group Members