SAMUELE, ALBERTA
SAMUELE, ALBERTA
Istituto di Genetica Molecolare "Luigi Luca Cavalli Sforza"
The power of enzyme kinetics in the drug development process
2013 Samuele, A; Crespan, E; Garbelli, A; Bavagnoli, L; Maga, G
2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies
2012 Rotili, D; Samuele, A; Tarantino, D; Ragno, R; Musmuca, I; Ballante, F; Botta, G; Morera, L; Pierini, M; Cirilli, R; Nawrozkij, Mb; Gonzalez, E; Clotet, B; Artico, M; Esté, Ja; Maga, G; Mai, A
Discovery of the first small molecule inhibitor of human DDX3 specifically designed to target the RNA binding site: towards the next generation HIV-1 inhibitors
2012 Radi, M; Falchi, F; Garbelli, A; Samuele, A; Bernardo, V; Paolucci, S; Baldanti, F; Schenone, S; Manetti, F; Maga, G; Botta, M
New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors
2012 La Regina, G; Coluccia, A; Brancale, A; Piscitelli, F; Famiglini, V; Cosconati, S; Maga, G; Samuele, A; Gonzalez, E; Clotet, B; Schols, D; Esté, Ja; Novellino, E; Silvestri, R
Synthesis, biological activity, and ADME properties of novel S-DABOs/N-DABOs as HIV reverse transcriptase inhibitors
2012 Radi M; Pagano M; Franchi L; Castagnolo D; Schenone S; Casaluce G; ZamperiniC; Dreassi E; Maga G; Samuele A; Gonzalo E; Clotet B; Esté JA; Botta M
Diarylpyrimidine-Dihydrobenzyloxopyrimidine Hybrids: New, Wide-Spectrum Anti-HIV-1 Agents Active at (Sub)-Nanomolar Level.
2011 Rotili D; Tarantino D; Artico M; Nawrozkij MB; GonzalezOrtega E; Clotet B; Samuele A; Estee JA; Maga G; Mai A.
Enantioselective binding of second generation pyrrolobenzoxazepinones to the catalytic ternary complex of HIV-1 RT wild-type and L100I and K103N drug resistant mutants.
2011 Butini, S; Gemma, S; Brindisi, M; Borrelli, G; Fiorini, I; Samuele, A; Karytinos, A; Facchini, M; Lossani, A; Zanoli, S; Campiani, G; Novellino, E; Focher, F; Maga, G
Indolylarylsulfones as HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors: New Cyclic Substituents at Indole-2-carboxamide.
2011 La Regina, G; Coluccia, A; Brancale, A; Piscitelli, F; Gatti, V; Maga, G; Samuele, A; Pannecouque, C; Schols, D; Balzarini, J; Novellino, E; Silvestri, R
Mechanism of interaction of novel indolylarylsulfone derivatives with K103N and Y181I mutant HIV-1 reverse transcriptase in complex with its substrates.
2011 Samuele A; Bisi S; Kataropoulou A; La Regina G; Piscitelli F; Gatti V; Silvestri R; Maga G.
Toward the discovery of novel anti-HIV drugs. Second-generation inhibitors of the cellular ATPase DDX3 with improved anti-HIV activity: synthesis, structure-activity relationship analysis, cytotoxicity studies, and target validation.
2011 Maga, G; Falchi, F; Radi, M; Botta, L; Casaluce, G; Bernardini, M; Irannejad, H; Manetti, F; Garbelli, A; Samuele, A; Zanoli, S; Este', Ja; Gonzalez, E; Zucca, E; Paolucci, S; Baldanti, F; De Rijck, J; Debyser, Z; Botta, M
Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants.
2009 Radi, M; Maga, G; Alongi, M; Angeli, L; Samuele, A; Zanoli, S; Bellucci, L; Tafi, A; Casaluce, G; Giorgi, G; Armandugon, M; Gonzalez, E; Esté, Ja; Baltzinger, M; Bec, G; Dumas, P; Ennifar, E; Botta, M
Indolylarylsulfones Bearing Natural and Unnatural Amino Acids. Discovery of Potent Inhibitors of HIV-1 Non-Nucleoside Wild Type and Resistant Mutant Strains Reverse Transcriptase and Coxsackie B4 Virus
2009 Piscitelli F; Coluccia A; Brancale A; La Regina G; Sansone A; Giordano C; Balzarini J; Maga G; Zanoli S; Samuele A; Cirilli R; La Torre F; Lavecchia A; Novellino E; Silvestri R
Specific Targeting of Highly Conserved Residues in the HIV-1 Reverse Transcriptase Primer Grip Region. 2. Stereoselective Interaction to Overcome the Effects of Drug Resistant Mutations.
2009 Butini S; Brindisi M; Cosconati S; Marinelli L; Borrelli G; Coccone SS; Ramunno A; Campiani G; Novellino E; Zanoli S; Samuele A; Giorgi G; Bergamini A; Mattia MD; Lalli S; Galletti B; Gemma S; Maga G.
Substrate-Induced Stable Enzyme-Inhibitor Complex Formation Allows Tight Binding of Novel 2-Aminopyrimidin-4(3H)-ones to Drug-Resistant HIV-1 Reverse Transcriptase Mutants.
2008 Samuele, A; Facchini, M; Rotili, D; Mai, A; Artico, M; Armandugón, M; Este', Ja; Maga, G
Towards novel S-DABOC inhibitors: Synthesis, biological investigation, and molecular modeling studies.
2008 Radi, M; Angeli, L; Franchi, L; Contemori, L; Maga, G; Samuele, A; Zanoli, S; Armandugon, M; Gonzalez, E; Llano, A; Esté, Ja; Botta, M
Characterization of novel N,N-DABOs as effective tight binding non-nucleoside inhibitors of HIV-1 RT.
2007 Facchini, M; Samuele, A; Ferrigno, L; Karytinos, A; Rotili, D; Mai, A; Maga, G
Dihydro-alkylthio-benzyl-oxopyrimidines as inhibitors of reverse transcriptase: synthesis and rationalization of the biological data on both wild-type enzyme and relevant clinical mutants.
2007 Mugnaini, C; Alongi, M; Togninelli, A; Gevariya, H; Brizzi, A; Manetti, F; Bernardini, C; Angeli, L; Tafi, A; Bellucci, L; Corelli, F; Massa, S; Maga, G; Samuele, A; Facchini, M; Clotetcodina, I; Armandugón, M; Este', Ja; Botta, M
Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity.
2007 La Regina GL; Coluccia A; Piscitelli F; Bergamini A; Sinistro A; Cavazza A; Maga G; Samuele A; Zanoli S; Novellino E; Artico M; Silvestri R.
Second generation PBOs show enantioselective binding to the catalytic complex of HIV-1 RT wt and drug resistant mutants.
2007 Amoroso A; Samuele A; Karytinos A; Facchini M; Zanoli S; Campiani G; Maga G.
Synthesis and Biological Properties of Novel 2-Aminopyrimidin-4(3H)-ones Highly Potent against HIV-1 Mutant Strains.
2007 Mai, A; Artico, M; Rotili, D; Tarantino, D; Clotetcodina, I; Armandugon, M; Ragno, R; Simeoni, S; Sbardella, G; Nawrozkij, Mb; Samuele, A; Maga, G; Este, Ja
| Titolo | Data di pubblicazione | Autore(i) | File |
|---|---|---|---|
| The power of enzyme kinetics in the drug development process | 1-gen-2013 | Samuele, A; Crespan, E; Garbelli, A; Bavagnoli, L; Maga, G | |
| 2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies | 1-gen-2012 | Rotili, D; Samuele, A; Tarantino, D; Ragno, R; Musmuca, I; Ballante, F; Botta, G; Morera, L; Pierini, M; Cirilli, R; Nawrozkij, Mb; Gonzalez, E; Clotet, B; Artico, M; Esté, Ja; Maga, G; Mai, A | |
| Discovery of the first small molecule inhibitor of human DDX3 specifically designed to target the RNA binding site: towards the next generation HIV-1 inhibitors | 1-gen-2012 | Radi, M; Falchi, F; Garbelli, A; Samuele, A; Bernardo, V; Paolucci, S; Baldanti, F; Schenone, S; Manetti, F; Maga, G; Botta, M | |
| New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors | 1-gen-2012 | La Regina, G; Coluccia, A; Brancale, A; Piscitelli, F; Famiglini, V; Cosconati, S; Maga, G; Samuele, A; Gonzalez, E; Clotet, B; Schols, D; Esté, Ja; Novellino, E; Silvestri, R | |
| Synthesis, biological activity, and ADME properties of novel S-DABOs/N-DABOs as HIV reverse transcriptase inhibitors | 1-gen-2012 | Radi M; Pagano M; Franchi L; Castagnolo D; Schenone S; Casaluce G; ZamperiniC; Dreassi E; Maga G; Samuele A; Gonzalo E; Clotet B; Esté JA; Botta M | |
| Diarylpyrimidine-Dihydrobenzyloxopyrimidine Hybrids: New, Wide-Spectrum Anti-HIV-1 Agents Active at (Sub)-Nanomolar Level. | 1-gen-2011 | Rotili D; Tarantino D; Artico M; Nawrozkij MB; GonzalezOrtega E; Clotet B; Samuele A; Estee JA; Maga G; Mai A. | |
| Enantioselective binding of second generation pyrrolobenzoxazepinones to the catalytic ternary complex of HIV-1 RT wild-type and L100I and K103N drug resistant mutants. | 1-gen-2011 | Butini, S; Gemma, S; Brindisi, M; Borrelli, G; Fiorini, I; Samuele, A; Karytinos, A; Facchini, M; Lossani, A; Zanoli, S; Campiani, G; Novellino, E; Focher, F; Maga, G | |
| Indolylarylsulfones as HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors: New Cyclic Substituents at Indole-2-carboxamide. | 1-gen-2011 | La Regina, G; Coluccia, A; Brancale, A; Piscitelli, F; Gatti, V; Maga, G; Samuele, A; Pannecouque, C; Schols, D; Balzarini, J; Novellino, E; Silvestri, R | |
| Mechanism of interaction of novel indolylarylsulfone derivatives with K103N and Y181I mutant HIV-1 reverse transcriptase in complex with its substrates. | 1-gen-2011 | Samuele A; Bisi S; Kataropoulou A; La Regina G; Piscitelli F; Gatti V; Silvestri R; Maga G. | |
| Toward the discovery of novel anti-HIV drugs. Second-generation inhibitors of the cellular ATPase DDX3 with improved anti-HIV activity: synthesis, structure-activity relationship analysis, cytotoxicity studies, and target validation. | 1-gen-2011 | Maga, G; Falchi, F; Radi, M; Botta, L; Casaluce, G; Bernardini, M; Irannejad, H; Manetti, F; Garbelli, A; Samuele, A; Zanoli, S; Este', Ja; Gonzalez, E; Zucca, E; Paolucci, S; Baldanti, F; De Rijck, J; Debyser, Z; Botta, M | |
| Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants. | 1-gen-2009 | Radi, M; Maga, G; Alongi, M; Angeli, L; Samuele, A; Zanoli, S; Bellucci, L; Tafi, A; Casaluce, G; Giorgi, G; Armandugon, M; Gonzalez, E; Esté, Ja; Baltzinger, M; Bec, G; Dumas, P; Ennifar, E; Botta, M | |
| Indolylarylsulfones Bearing Natural and Unnatural Amino Acids. Discovery of Potent Inhibitors of HIV-1 Non-Nucleoside Wild Type and Resistant Mutant Strains Reverse Transcriptase and Coxsackie B4 Virus | 1-gen-2009 | Piscitelli F; Coluccia A; Brancale A; La Regina G; Sansone A; Giordano C; Balzarini J; Maga G; Zanoli S; Samuele A; Cirilli R; La Torre F; Lavecchia A; Novellino E; Silvestri R | |
| Specific Targeting of Highly Conserved Residues in the HIV-1 Reverse Transcriptase Primer Grip Region. 2. Stereoselective Interaction to Overcome the Effects of Drug Resistant Mutations. | 1-gen-2009 | Butini S; Brindisi M; Cosconati S; Marinelli L; Borrelli G; Coccone SS; Ramunno A; Campiani G; Novellino E; Zanoli S; Samuele A; Giorgi G; Bergamini A; Mattia MD; Lalli S; Galletti B; Gemma S; Maga G. | |
| Substrate-Induced Stable Enzyme-Inhibitor Complex Formation Allows Tight Binding of Novel 2-Aminopyrimidin-4(3H)-ones to Drug-Resistant HIV-1 Reverse Transcriptase Mutants. | 1-gen-2008 | Samuele, A; Facchini, M; Rotili, D; Mai, A; Artico, M; Armandugón, M; Este', Ja; Maga, G | |
| Towards novel S-DABOC inhibitors: Synthesis, biological investigation, and molecular modeling studies. | 1-gen-2008 | Radi, M; Angeli, L; Franchi, L; Contemori, L; Maga, G; Samuele, A; Zanoli, S; Armandugon, M; Gonzalez, E; Llano, A; Esté, Ja; Botta, M | |
| Characterization of novel N,N-DABOs as effective tight binding non-nucleoside inhibitors of HIV-1 RT. | 1-gen-2007 | Facchini, M; Samuele, A; Ferrigno, L; Karytinos, A; Rotili, D; Mai, A; Maga, G | |
| Dihydro-alkylthio-benzyl-oxopyrimidines as inhibitors of reverse transcriptase: synthesis and rationalization of the biological data on both wild-type enzyme and relevant clinical mutants. | 1-gen-2007 | Mugnaini, C; Alongi, M; Togninelli, A; Gevariya, H; Brizzi, A; Manetti, F; Bernardini, C; Angeli, L; Tafi, A; Bellucci, L; Corelli, F; Massa, S; Maga, G; Samuele, A; Facchini, M; Clotetcodina, I; Armandugón, M; Este', Ja; Botta, M | |
| Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity. | 1-gen-2007 | La Regina GL; Coluccia A; Piscitelli F; Bergamini A; Sinistro A; Cavazza A; Maga G; Samuele A; Zanoli S; Novellino E; Artico M; Silvestri R. | |
| Second generation PBOs show enantioselective binding to the catalytic complex of HIV-1 RT wt and drug resistant mutants. | 1-gen-2007 | Amoroso A; Samuele A; Karytinos A; Facchini M; Zanoli S; Campiani G; Maga G. | |
| Synthesis and Biological Properties of Novel 2-Aminopyrimidin-4(3H)-ones Highly Potent against HIV-1 Mutant Strains. | 1-gen-2007 | Mai, A; Artico, M; Rotili, D; Tarantino, D; Clotetcodina, I; Armandugon, M; Ragno, R; Simeoni, S; Sbardella, G; Nawrozkij, Mb; Samuele, A; Maga, G; Este, Ja |