Name & title Donatella Taramelli, PhD Date and Place Brief chronology 1976 PhD in Biological Sciences (110/110 cum laude ) University of Perugia(Italy) of employment 1978-81 Visiting Fellow , NCI, NIH, Bethesda, MD, USA 1982-85 Research Associate, National Cancer Institute, Milan, Italy 1985-87 Research Associate, Dept. Exp. Medicine University of Rome "La Sapienza" 1987-89 Visiting Scientist, Div. of Rheum Clinical Immunol. Univ. of Maryland at
Baltimore,USA 1987-99 AssociateProfessor of Pathology,School of Pharmacy,University of Milan. 2000-present Full Professor of Pathology, School of Pharmacy,University of Milan. Affiliation/
School of Pharmacy, Dipartimento Sanità Pubblica-Microbiologia-Virologia, Università di
Milano, Via Pascal 36, 20133 Milano. Italy Phone +39 02 5031 5071, Fax +39 02 5031
Research Grants 1992-93– P.I. project “Pathogenesis of opportunistic mycosis in neutropenic patients
treated with anti-tumor chemotherapy” from Italian Cancer Res. Ass.
1996-99 – Associated Partner EU with JRC, Environment and Climate DGXII-ESCY for research on "Early indicators of contact sensitisation to haevy metals” 1996 - P.I. -WHO/ TDR grant entitled "Anti -malarial activity of Fe2+-porphyrins: pilot
study for the development of a screening method for new drugs"
1997 – 98 P.I. WHO/TDR grant entitled "Oxidation of Fe(II) protoporphyrin IX and
depolymerisation of plasmodia haemozoin: new targets for antimalarial drugs"
1997-99-00 P.I. Nat Res Progr on AIDS, ISS "New in vitro human models for studies
on the pathogenicity of P. marneffei, an opportunistic fungus in AIDS 1997 - P.I. PRIN MURST Cofinanziamento 1997-99 on malaria 2001 - P.I. National Projects PRIN 2000 "Molecular, immunological and pharmacological
analysis of the interactions between parasites, hosts and vectors.” with prof M.Coluzzi. 2001 – Int. Coop. Italy- South Africa, Project on “Identification of new molecular
targets for the synthesis and screening of new drugs active during the intraerythrocytic
stage of malaria parasites” with Prof. T. J. Egan , University of Cape Town, South Africa. 2003- P.I. National Projects PRIN 2003 " 2003-07 Italian representative in the EU COST Action B22-Drug development for 2005-2011 WP manager- EU IP Project 18834- ANTIMAL- 2006-2008 Cluster head-Italian Malaria Network, financed by Compagnia di San 2008-2011 Italian representative in the EU COST Action BM0802 Life or death of protozoan parasites 2009-2011 WP manager- EU Project CRIMALDDI- Coordination rationalization
intergration of antimalarial drug discovery initiatives
2009-2014- PI NIH-RO1 Research Grant with Univ. Massachussets on Innate Immunity Research 1-Drug screening (in vitro chemosensitivity assays against P. falciparum strains subjects/ platforms
using the pLDH method) for the identification of new compounds with antimalarial activity and SAR studies. Development of novel screening assays with fluorescent probes (Picogreen)
2-Studies on the mechanism of action of antimalarials active during the intraerythrocytic stage of malaria parasites
Identification of inhibitors of the haem detoxification process and the formation
of haemozoin using a spectrophotometric microassay (BHIA, beta-haematin inhibitory activity ) developed for medium /low throughput screening, recently adapted for robotic platforms
Identification of inhibitors of haemoglobin proteases (plasmepsin II and IV)
using in vitro spectrophotometric assays of enzyme activity
3-Studies on the mechanism of toxicity of quinoline and artemisinin antimalarials (Role or oxygen and iron on drug action). 4-Pathophysiology of parasite-host relationships (effects of parasite products on the host immune response, mechanisms of accelerated senescence of RBC in relationship to anemia) 5- Effects of artemisinin derivatives on angiogenesis and erythroid differentiation ( K562, CD34+, human precursors) Products
Italian patent application N MI 2003A002044 for novel quinoline derivatives with
antimalarial activity, under PCT extension
Bibliography: 118 papers in international journals, 270 congress presentations,
List of Publications from the last 3 years
1. Gemma S, Campiani G, Butini S, Kukreja G, Joshi BP, Persico M, Catalanotti B, Novellino E, Fattorusso E, Nacci
V, Savini L, Taramelli D, Basilico N, Morace, G, Yardley V, Fattorusso C. Design and synthesis of potent antimalarial agents based on clotrimazole scaffold: exploring an innovative pharmacophore. J Med Chem. 2007 Feb 22;50(4):595-8. IF 4.9
2. Gemma S, Kukreja G, Campiani G, Butini S, Bernetti M, Joshi BP, Savini L,Basilico N, Taramelli D, Yardley V,
Bertamino A, Novellino E, Persico M,Catalanotti B, Fattorusso C. Development of piperazine-tethered heterodimers as potent antimalarials against chloroquine-resistant P. falciparum strains. Synthesis and molecular modeling. Bioorg Med Chem Lett. 2007 Jul 1;17(13):3535-9. Epub 2007 Apr 29.
3. Omodeo-Sale F, Cortelezzi L, Riva E, Vanzulli E, Taramelli D. Modulation of glyceraldehyde 3 phosphate
dehydrogenase activity and tyr-phosphorylation of Band 3 in human erythrocytes treated with ferriprotoporphyrin IX. Biochem Pharmacol. 2007 Nov 1;74(9):1383-9.
4. Haynes RK, Chan WC, Lung CM, Uhlemann AC, Eckstein U, Taramelli D, Parapini S, Monti D, Krishna S. The
Fe(2+)-Mediated Decomposition, PfATP6 Binding, and Antimalarial Activities of Artemisone and Other Artemisinins: The Unlikelihood of C-Centered Radicals as Bioactive Intermediates. ChemMedChem. 2007 Oct 8;2(10):1480-1497
5. D'Alessandro S, Gelati M, Basilico N, Parati EA, Haynes RK, Taramelli D. Differential effects on angiogenesis of
two antimalarial compounds,dihydroartemisinin and artemisone: Implications for embryotoxicity.Toxicology. 2007 Nov 20;241(1-2):66-74.
6. Nuchsongsin F, Chotivanich K, Charunwatthana P, Omodeo-Salè F, Taramelli D, Day NP, White NJ, Dondorp
AM.Effects of malaria heme products on red blood cell deformability.Am J Trop Med Hyg. 2007 Oct;77(4):617-22.
7. Dell’Agli mario,Germana V. Galli, Silvia Parapini, Nicoletta Basilico,Donatella Taramelli, Ataa Said , Khaled
Rashed, Enrica Bosisio. Antiplasmodial activity of Ailanthus excelsa. Phytotherapy Fitoterapia. 2008 Feb;79(2):112-6.
8. Romeo Sergio, Silvia Parapini, Mario Dell’Agli,Nadia Vaiana, Pietro Magrone, Germana Galli, Anna Sparatore,
Donatella Taramelli, Enrica Bosisio Atovaquone-Statine “Double-Drugs” with High Antiplasmodial Activity Chem.Med.Chem ChemMedChem. 2008 Mar 14;3(3):418-420.
9. Gemma S, Campiani G, Butini S, Kukreja G, Coccone SS, Joshi BP, Persico M,Nacci V, Fiorini I, Novellino E,
Fattorusso E, Taglialatela-Scafati O, Savini L, Taramelli D, Basilico N, Parapini S, Morace G, Yardley V, Croft S,
Coletta M,Marini S, Fattorusso C.Clotrimazole scaffold as an innovative pharmacophore towards potent antimalarial agents: design, synthesis, and biological and structure-activity relationship studies. J Med Chem. 2008 Mar 13;51(5):1278-94.
10. Fattorusso C, Campiani G, Kukreja G, Persico M, Butini S, Romano MP, Altarelli M, Ros S, Brindisi M, Savini L,
Novellino E, Nacci V, Fattorusso E, Parapini S, Basilico N, Taramelli D, Yardley V, Croft S, Borriello M, Gemma S.Design, synthesis, and structure-activity relationship studies of 4-quinolinyl-and 9-acrydinylhydrazones as potent antimalarial agents.J Med Chem. 2008 Mar 13;51(5):1333-43.
11. Costi MP, Taramelli D, González-Pacanowska D.Opening Opportunities for New Drugs Against Neglected
Diseases.ChemMedChem. 2008 Mar 14;3(3):371-373.
12. Sparatore A, Basilico N, Casagrande M, Parapini S, Taramelli D, Brun R,Wittlin S, Sparatore F. Antimalarial
activity of novel pyrrolizidinyl derivatives of 4-aminoquinoline. Bioorg Med Chem Lett. 2008 Jul 1;18(13):3737-40. Epub 2008 May 16.
13. Basilico N, Bosisio E, Buelli F, Campiani G, Casagrande M, Castelli F, CoghiP, Corbett Y, Cortelezzi L,
D'Alessandro S, Dell'Agli M, Esposito F, FattorussoC, Fattorusso E, Finaurini S, Galli GV, Gemma S, Habluetzel A, Lucantoni L,Melato S, Monti D, Olliaro P, Omodeo-Salè F, Parapini S, Persico M, Rizzi M,Romeo S, Rossi F, Rusconi C, Sparatore A, Scafati OT, van den Bogaart E,Taramelli D, Vaiana N, Yerbanga S. Old and new targets for innovativeantimalarial compounds: the different strategies of the Italian Malaria Network. Parassitologia. 2008 Jun;50(1-2):133-6. PubMed PMID: 18693579.
14. Bonifacio A, Finaurini S, Krafft C, Parapini S, Taramelli D, Sergo V. Spatial distribution of heme species in
erythrocytes infected with Plasmodium falciparum by use of resonance Raman imaging and multivariate analysis. Anal Bioanal Chem.2008 Dec;392(7-8):1277-82. Epub 2008 Oct 5. PubMed PMID: 18836854.
15. Gemma S, Campiani G, Butini S, Joshi BP, Kukreja G, Coccone SS, Bernetti M,Persico M, Nacci V, Fiorini I,
Novellino E, Taramelli D, Basilico N, Parapini S, Yardley V, Croft S, Keller-Maerki S, Rottmann M, Brun R, Coletta M, Marini S,Guiso G, Caccia S, Fattorusso C. Combining 4-aminoquinoline- and clotrimazole-based pharmacophores toward innovative and potent hybrid antimalarials. J Med Chem. 2009 Jan 22;52(2):502-13. PubMed PMID: 19113955.
16. Basilico N, Cortelezzi L, Serpellini C, Taramelli D, Omodeo-Salè F. Two complementary fluorimetric assays for
the determination of aminoquinoline binding and uptake by human erythrocytes in vitro. Anal Biochem. 2009 Feb15;385(2):371-3. Epub 2008 Nov 13.
17. O'Neill PM, Shone AE, Stanford D, Nixon G, Asadollahy E, Park BK, Maggs JL,Roberts P, Stocks PA, Biagini G,
Bray PG, Davies J, Berry N, Hall C, Rimmer K,Winstanley PA, Hindley S, Bambal RB, Davis CB, Bates M, Gresham SL, Brigandi RA, Gomez-de-Las-Heras FM, Gargallo DV, Parapini S, Vivas L, Lander H, Taramelli D,Ward SA. Synthesis, antimalarial activity, and preclinical pharmacology of anovel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine. J Med Chem. 2009 Apr 9;52(7):1828-44. PubMed PMID: 19284751.
18. Dell'Agli M, Galli GV, Corbett Y, Taramelli D, Lucantoni L, Habluetzel A,Maschi O, Caruso D, Giavarini F,
Romeo S, Bhattacharya D, Bosisio E. Antiplasmodial activity of Punica granatum L. fruit rind. J. Ethnopharmacol. 2009 Jul 3. [Epub ahead of print] PubMed PMID:19577622.
19. Omodeo-Salè F, Cortelezzi L, Basilico N, Casagrande M, Sparatore A, Taramelli D. Novel antimalarial
aminoquinolines: heme binding and effects on normal or Plasmodium falciparum parasitized human erythrocytes. Antimicrob Agents Chemother. 2009 Oct;53(10):4339-44. Epub 2009 Aug 3.
20. Coghi P, Basilico N, Taramelli D, Chan WC, Haynes RK, Monti D. Interaction of Artemisinins with
Oxyhemoglobin Hb-Fe(II), Hb-Fe(II), CarboxyHb-Fe(II), Heme-Fe(II), and Carboxyheme Fe(II): Significance for Mode of Action and Implications for Therapy of Cerebral Malaria. ChemMedChem. 2009 Oct 20. [Epub ahead of print] PubMed PMID: 19844934. ChemMedChem. 2009 Dec;4(12):2045-53.IF 3.15
21. Basilico N, Parapini S, Sisto F, Omodeo-Salè F, Coghi P, Ravagnani F, Olliaro P, Taramelli D. The lipid moiety of
haemozoin (Malaria Pigment) and P. falciparum parasitised red blood cells bind synthetic and native endothelin-1. J Biomed Biotechnol. 2010; 2010:854927. Epub 2010 Feb 24
22. Fattorusso C, Persico M, Calcinai B, Cerrano C, Parapini S, Taramelli D,Novellino E, Romano A, Scala F,
Fattorusso E, Taglialatela-Scafati O. Manadoperoxides A-D from the Indonesian sponge Plakortis cfr. simplex. Further insights on the structure-activity relationships of simple 1,2-dioxane antimalarials. J Nat Prod. 2010 Jun 25;73(6):1138-45. PubMed PMID: 20521782.
23. Boulton IC, Nwaka S, Bathurst I, Lanzer M, Taramelli D, Vial H, Doerig C, Chibale K, Ward SA. CRIMALDDI:
a co-ordinated, rational, and integrated effort to set logical priorities in anti-malarial drug discovery initiatives. Malar J. 2010 Jul 13;9(1):202. [Epub ahead of print] PubMed PMID: 20626844.
24. Dell'agli M, Galli GV, Bulgari M, Basilico N, Romeo S, Bhattacharya D, Taramelli D, Bosisio E. Ellagitannins of
the fruit rind of pomegranate (Punica granatum) antagonize in vitro the host inflammatory response mechanisms involved in the onset of malaria. Malar J. 2010 Jul 19;9(1):208. [Epub ahead of print] PubMed PMID: 20642847.
25. Chianese G, Yerbanga SR, Lucantoni L, Habluetzel A, Basilico N, Taramelli D, Fattorusso E, Taglialatela-Scafati
O. Antiplasmodial triterpenoids from the fruits of neem, Azadirachta indica. J Nat Prod. 2010 Aug 27;73(8):1448-52.
26. Casagrande M, Basilico N, Rusconi C, Taramelli D, Sparatore A. Synthesis, antimalarial activity, and cellular
toxicity of new arylpyrrolylaminoquinolines. Bioorg Med Chem. 2010 Sep 15;18(18):6625-33.
27. Finaurini S, Ronzoni L, Colancecco A, Cattaneo A, Cappellini MD, Ward SA, Taramelli D. Selective toxicity of
dihydroartemisinin on human CD34+ erythroid cell differentiation. Toxicology. 2010 Oct 9;276(2):128-34.
ALSO IN THIS ISSUE: Canada Red Cross Used HIV Blood Charcoal is an amazing substance. It adsorbs moreWar I; and it effectively counteracted poison gas. poisons than any other substance known to mankind. Bad odors, caused by skin ulcers, have been elimi-It can adsorb lead acetate, strychnine, DDT, manynated by placing charcoal-filled cloth over plastic casts. drugs (including cocaine, iodi
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