Mu.Ta.Lig - COST ACTION CA15135

Prof. Maria Laura BOLOGNESI

14 June 2016

bolo

General information

Name: Maria Laura
Surname: Bolognesi
E-mail: marialaura.bolognesi@unibo.it
Cell phone number with international prefix: +39 349 1678389
Country: Italy
Affiliation: Department of Pharmacy and Biotechnology, Alma Mater Studiorum – University of Bologna, Via Belmeloro, 6, 40126 Bologna, Italy
Gender: F þ M
Year of the PhD title: 1996
Personal web page: http://www.unibo.it/sitoweb/marialaura.bolognesi/
Previous COST participation: No □ Yes þ

 

List of 10 selected publications within last 5 years

1. Lemes, L.F.N.; De Andrade Ramos, G.; De Oliveira, A.S.; Da Silva, F.M.R.; De Castro Couto, G.; Da Silva Boni, M.; Guimarães, M.J.R.; Souza, I.N.O.; Bartolini, M.; Andrisano, V.; Do Nascimento Nogueira, P.C.; Silveira, E.R.; Brand, G.D.; Soukup, O.;  Korábečný, J.; Romeiro, N.C.; Castro, N.G.; Bolognesi, M.L.*; Romeiro, L.A.S. Cardanol-derived AChE inhibitors: Towards the development of dual binding derivatives for Alzheimer’s disease. Eur J Med Chem 2016, DOI: 10.1016/j.ejmech.2015.12.024
2. Bolognesi, M. L.*; Bongarzone, S.; Aulic, S.; Tran, H. N.; Prati, F.; Carloni, P.; Legname, G.; Rational approach to an antiprion compound with a multiple mechanism of action. Future Med Chem 2015, 7, 2113-2120
3. Prati, F.; Bergamini, C.; Molina, M. T.; Falchi, F.; Cavalli, A.; Kaiser, M.; Brun, R.; Fato, R.; Bolognesi, M. L.* 2-Phenoxy-1,4-naphthoquinones: From a Multitarget Antitrypanosomal to a Potential Antitumor Profile. J Med Chem 2015, 58, 6422-6434.
4. Prati, F.; De Simone, A.; Armirotti, A.; Summa, M.; Pizzirani, D.; Scarpelli, R.; Bertozzi, S. M.; Perez, D. I.; Andrisano, V.; Perez-Castillo, A.; Monti, B.; Massenzio, F.; Polito, L.; Racchi, M.; Sabatino, P.; Bottegoni, G.; Martinez, A.; Cavalli, A.; Bolognesi, M. L.* 3,4-Dihydro-1,3,5-triazin-2(1H)-ones as the first dual BACE-1/GSK-3β fragment hits against Alzheimer’s disease. ACS Chem Neurosci 2015, 6, 1665-1682
5. Prati, F.; De Simone, A.; Bisignano, P.; Armirotti, A.; Summa, M.; Pizzirani, D.; Scarpelli, R.; Perez, D. I.; Andrisano, V.; Perez-Castillo, A.; Monti, B.; Massenzio, F.; Polito, L.; Racchi, M.; Favia, A. D.; Bottegoni, G.; Martinez, A.; Bolognesi, M. L.*; Cavalli, A. Multitarget drug discovery for Alzheimer’s disease: triazinones as BACE-1 and GSK-3β inhibitors. Angew Chem Int Ed Engl 2015, 54, 1578-1582.
6. Nepovimova, E.; Uliassi, E.; Korabecny, J.; Pena-Altamira, L. E.; Samez, S.; Pesaresi, A.; Garcia, G. E.; Bartolini, M.; Andrisano, V.; Bergamini, C.; Fato, R.; Lamba, D.; Roberti, M.; Kuca, K.; Monti, B.; Bolognesi, M. L.* Multitarget Drug Design Strategy: Quinone-Tacrine Hybrids Designed To Block Amyloid-beta Aggregation and To Exert Anticholinesterase and Antioxidant Effects. J Med Chem 2014, 57, 8576-89.
7. Belluti, F.; Uliassi, E.; Veronesi, G.; Bergamini, C.; Kaiser, M.; Brun, R.; Viola, A.; Fato, R.; Michels, P. A.; Krauth-Siegel, R. L.; Cavalli, A.; Bolognesi, M. L.* Toward the development of dual-targeted glyceraldehyde-3-phosphate dehydrogenase/trypanothione reductase inhibitors against Trypanosoma brucei and Trypanosoma cruzi. ChemMedChem 2014, 9, 371-82.
8. Pieretti, S.; Haanstra, J.R.; Mazet, M.; Perozzo, R.; Bergamini, C.; Prati, F.; Fato, R.; Lenaz, G.; Capranico, G.; Brun, R.; Bakker, B.M.; Michels, P.A.; Scapozza, L.; Bolognesi, M. L.*; Cavalli, A. Naphthoquinone derivatives exert their antitrypanosomal activity via a multi-target mechanism. PLoS Negl Trop Dis 2013, e2012.
9. Bolognesi, M. L.* Polypharmacology in a single drug: multitarget drugs. Curr Med Chem 2013, 20, 639-45.
10. Lizzi, F.; Veronesi, G.; Belluti, F.; Bergamini C.; López-Sánchez, A.; Kaiser, M.; Brun, R., Hall, D; Rivas, L., Bolognesi, M. L.* Conjugation of quinones with natural polyamines: Toward an expanded antitrypanosomatid profile. J Med Chem 2012, 55, 10490-10500.

 

Main skills and expertise (up to 5)

1. Polypharmacology
2.Multitarget drug discovery
3.Medicinal Chemistry
4.Chemical biology
5.Synthesis of biologically active molecules

 

Main equipment/facilities available in the participants’ lab (up to 5)

1. State-of-the-art dedicated laboratories for synthetic chemistry
2. Parallel synthesizers, H-Cube Mini™ reactor
3. MW instrumentation
4. Varian 400 and 600 MHz NMR instruments
5. HPLC

 


 

Short personal activity proposal for the COST Action CA15135 (max 1000 characters)

The ‘one target, one drug’ paradigm has dominated drug discovery, inspiring the development of innovative and reasonably selective small molecules. However, they have proven inadequate for addressing the immense complexity of currently incurable diseases, or the growing problem of antimicrobial drug resistance. In this respect, neurodegenerative and neglected tropical diseases represent two groups of maladies where the failures of the reductionist approach are particularly evident. Our lab developed the concept that single chemical entities capable to modulate more than one target (the so-called multitarget-directed ligands, MTDLs) in neurodegenerative and neglected tropical diseases may demonstrate more efficacious, tolerable and sustainable than the currently available drugs. Building on this knowledge, in this project our activities will be focused on the application of rational strategies for the identification of high-quality MTDLs hit against the above-mentioned medical needs.

 

Work Group preference: score from 1 (preferred) to 4 (not preferred)

Work Group of the CA15135 COST Action Score
WG1: Development of new chemical entities 1
WG2: Selection of biological targets and assessment of biological data 2
WG3: Development of chemical databases 3
WG4: Development of Computational methods for multiple ligand design and discovery 4