Past and Future Perspectives of Synthetic Peptide Libraries (562 views)
Curr Protein Pept Sci (ISSN: 1389-2037, 1389-2037linking), 2008 Oct; 9(5): 447-467.
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Paper type: Journal Article,
Impact factor: 3.011, 5-year impact factor: 3.549
Url: http://www.scopus.com/inward/record.url?eid=2-s2.0-55949103501&partnerID=40&md5=15ce760cecfb8ea8831e37c94aeca539
Keywords: Combinatorial Chemistry, High Throughput Screening, Molecular Complexity, Peptide Libraries, Simplified Libraries, Amino Acid, Cell Penetrating Peptide, Dendrimer, Galectin, Glycoprotein, Heparin, Hepatitis Vaccine, Human Immunodeficiency Virus Vaccine, Liposome, Nanoparticle, Peptide Deformylase, Peptide Deformylase Inhibitor, Peptide Derivative, Peptide Inhibitor, Phosphotransferase Inhibitor, Proprotein Convertase 1, Proprotein Convertase 1 Inhibitor, Proprotein Convertase 2 Inhibitor, Protein Inhibitor, Proteinase Inhibitor, Resin, Serine Proteinase, Synthetic Peptide, Tetrapeptide, Tyrosinase Inhibitor, Unclassified Drug, Affinity Chromatography, Antigenicity, Automation, Binding Affinity, Capillary Electrophoresis, Catalyst, Chemoluminescence, Drug Delivery System, Drug Design, Drug Half Life, Drug Mechanism, Drug Potency, Drug Screening, Drug Specificity, Enzyme Inhibition, Enzyme Linked Immunosorbent Assay, Fluorescence Resonance Energy Transfer, High Performance Liquid Chromatography, Ligand Binding, Lipophilicity, Mass Spectrometry, Matrix Assisted Laser Desorption Ionization Time Of Flight Mass Spectrometry, Molecular Weight, Nonhuman, Nuclear Magnetic Resonance, Peptide Synthesis, Protein Assembly, Protein Conformation, Protein Denaturation, Protein Microarray, Protein Protein Interaction, Protein Stability, Protein Structure, Protein Targeting, Review, Rna Translation, Robotics, Thermodynamics, Amino Acid Sequence, Methodology, Molecular Genetics, Combinatorial Chemistry Techniques, Molecular Sequence Data,
Affiliations:
*** IBB - CNR ***
Istituto di Biostrutture e Bioimmagini, CNR, via Mezzocannone 16, 80134 Napoli, Italy
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Curr Protein Pept Sci (ISSN: 1389-2037, 1389-2037linking), 2008 Oct; 9(5): 447-467.
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Paper type: Journal Article,
Impact factor: 3.011, 5-year impact factor: 3.549
Url: http://www.scopus.com/inward/record.url?eid=2-s2.0-55949103501&partnerID=40&md5=15ce760cecfb8ea8831e37c94aeca539
Keywords: Combinatorial Chemistry, High Throughput Screening, Molecular Complexity, Peptide Libraries, Simplified Libraries, Amino Acid, Cell Penetrating Peptide, Dendrimer, Galectin, Glycoprotein, Heparin, Hepatitis Vaccine, Human Immunodeficiency Virus Vaccine, Liposome, Nanoparticle, Peptide Deformylase, Peptide Deformylase Inhibitor, Peptide Derivative, Peptide Inhibitor, Phosphotransferase Inhibitor, Proprotein Convertase 1, Proprotein Convertase 1 Inhibitor, Proprotein Convertase 2 Inhibitor, Protein Inhibitor, Proteinase Inhibitor, Resin, Serine Proteinase, Synthetic Peptide, Tetrapeptide, Tyrosinase Inhibitor, Unclassified Drug, Affinity Chromatography, Antigenicity, Automation, Binding Affinity, Capillary Electrophoresis, Catalyst, Chemoluminescence, Drug Delivery System, Drug Design, Drug Half Life, Drug Mechanism, Drug Potency, Drug Screening, Drug Specificity, Enzyme Inhibition, Enzyme Linked Immunosorbent Assay, Fluorescence Resonance Energy Transfer, High Performance Liquid Chromatography, Ligand Binding, Lipophilicity, Mass Spectrometry, Matrix Assisted Laser Desorption Ionization Time Of Flight Mass Spectrometry, Molecular Weight, Nonhuman, Nuclear Magnetic Resonance, Peptide Synthesis, Protein Assembly, Protein Conformation, Protein Denaturation, Protein Microarray, Protein Protein Interaction, Protein Stability, Protein Structure, Protein Targeting, Review, Rna Translation, Robotics, Thermodynamics, Amino Acid Sequence, Methodology, Molecular Genetics, Combinatorial Chemistry Techniques, Molecular Sequence Data,
Affiliations:
*** IBB - CNR ***
Istituto di Biostrutture e Bioimmagini, CNR, via Mezzocannone 16, 80134 Napoli, Italy
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Past and Future Perspectives of Synthetic Peptide Libraries
Combinatorial preparation and HTS of arrays of compounds have increased the speed of drug discovery. A strong impulse in this field has come by the introduction of the solid phase synthesis method that, through automation and miniaturization, has paved the way to the preparation of large collections of compounds in compact and trackable formats. Due to the well established synthetic procedures, peptides have been largely used to develop the basic concepts of combinatorial chemistry and peptide libraries are still successfully employed in screening programs. However, peptides generally do not fulfil the requirements of low conformational flexibility, stability and bioavailability needed for good drug candidates and peptide leads with high potency and selectivity are often made "druggable" by conversion to more stable structures with improved pharmacological profiles. Such an approach makes the screening of peptide libraries still a valuable tool for drug discovery. We propose here a panoramic review of the most common methods for the preparation and screening of peptide libraries and the most interesting findings of the last decade. We also report on a new approach we follow in our laboratory that is based on the use of "simplified" libraries composed by a minimum number of non-redundant amino acids for the assembly of short peptides. The choice of amino acids is dictated by diversity in lipophilicity, MW, charge and polarity. Newly identified active sequences are then modified by preparing new variants containing analogous amino acids, so that the chemical space occupied by the excluded residues can be explored. This approach offers the advantage of simplifying the synthesis and deconvolution of libraries and provides new active compounds with a molecular size similar to that of small molecules, to which they can be easily converted.
Combinatorial preparation and HTS of arrays of compounds have increased the speed of drug discovery. A strong impulse in this field has come by the introduction of the solid phase synthesis method that, through automation and miniaturization, has paved the way to the preparation of large collections of compounds in compact and trackable formats. Due to the well established synthetic procedures, peptides have been largely used to develop the basic concepts of combinatorial chemistry and peptide libraries are still successfully employed in screening programs. However, peptides generally do not fulfil the requirements of low conformational flexibility, stability and bioavailability needed for good drug candidates and peptide leads with high potency and selectivity are often made "druggable" by conversion to more stable structures with improved pharmacological profiles. Such an approach makes the screening of peptide libraries still a valuable tool for drug discovery. We propose here a panoramic review of the most common methods for the preparation and screening of peptide libraries and the most interesting findings of the last decade. We also report on a new approach we follow in our laboratory that is based on the use of "simplified" libraries composed by a minimum number of non-redundant amino acids for the assembly of short peptides. The choice of amino acids is dictated by diversity in lipophilicity, MW, charge and polarity. Newly identified active sequences are then modified by preparing new variants containing analogous amino acids, so that the chemical space occupied by the excluded residues can be explored. This approach offers the advantage of simplifying the synthesis and deconvolution of libraries and provides new active compounds with a molecular size similar to that of small molecules, to which they can be easily converted.
Past and Future Perspectives of Synthetic Peptide Libraries
Past and Future Perspectives of Synthetic Peptide Libraries
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Impact Factor: 2.851
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Sandomenico A, Focà A, Sanguigno L, Caporale A, Focà G, Pignalosa A, Corvino G, Caragnano A, Beltrami AP, Antoniali G, Tell G, Leonardi A, Ruvo M
* Monoclonal antibodies against pools of mono- and polyacetylated peptides selectively recognize acetylated lysines within the context of the original antigen (391 views) (PDF 219 views)
Mabs-Austin (ISSN: 1942-0862), 2016 Aug; 8: 1575-1589.
Impact Factor: 4.881
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Caporale A, Selis F, Pain D, Sandomenico A, Jotti S, Tonon G, Ruvo M
* The LQSP tetrapeptide is a new highly efficient substrate of microbial transglutaminase for the site-specific derivatization of peptides and proteins (683 views)
Biotechnol J (ISSN: 1860-6768), 2015 Jan; 10(1): 154-161.
Impact Factor: 3.781
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Pappalardo M, Shachaf N, Basile L, Milardi D, Zeidan M, Raiyn J, Guccione S, Rayan A
* Sequential Application of Ligand and Structure Based Modeling Approaches to Index Chemicals for Their hH(4)R Antagonism (394 views)
Plosone (ISSN: 1932-6203, 1932-6203electronic, 1932-6203linking), 2014 Oct 16; 9(10): e109340-e109340.
Impact Factor: 3.234
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Zanoli LM, Spoto G
* Isothermal amplification methods for the detection of nucleic acids in microfluidic devices (368 views)
Biosensors (ISSN: 2079-6374), 2013 Mar; 3(1): 18-43.
Impact Factor: 0
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Merolla F, Luise C, Muller MT, Pacelli R, Fusco A, Celetti A
* Loss of CCDC6, the First Identified RET Partner Gene, Affects pH2AX S139 Levels and Accelerates Mitotic Entry upon DNA Damage (364 views)
Plosone (ISSN: 1932-6203, 1932-6203electronic, 1932-6203linking), 2012 May 24; 7(5): N/D-N/D.
Impact Factor: 3.73
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Doti N, Scognamiglio PL, Madonna S, Scarponi C, Ruvo M, Perretta G, Albanesi C, Marasco D
* New mimetic peptides of the kinase-inhibitory region (KIR) of SOCS1 through focused peptide libraries (1334 views)
Biochemical Journal, 2012 Apr 1; 443: 231-240.
Impact Factor: 4.779
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Zaccaro L, Garcia-lopez Mt Gonzalez-muniz RG
* TRPV1 modulators: Structure-activity relationships using a rational combinatorial approach (461 views)
Bioorganic & Medicinal Chemistry Letters (ISSN: 0960-894x), 2011 Jun 15; 21(12): 3541-3545.
Impact Factor: 2.554
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Ruvo M, Sandomenico A, Tudisco L, De Falco S
* Branched peptides for the modulation of protein-protein interactions: More arms are better than one? (532 views)
Curr Med Chem (ISSN: 0929-8673, 1875-533x, 1875-533xelectronic), 2011 Jun; 18(16): 2429-2437.
Impact Factor: 4.859
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Scognamiglio PL, Doti N, Grieco P, Pedone C, Ruvo M, Marasco D
* Discovery Of Small Peptide Antagonists Of Ped/Pea15-D4alpha Interaction From Simplified Combinatorial Libraries (504 views)
Chem Biol Drug Des (ISSN: 1747-0277, 1747-0285), 2011 May; 77(5): 319-327.
Impact Factor: 2.282
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Doti N, Marasco D, Pedone C, Sabatella M, Ruvo M
* Optimizing A Kinase Assay For Ikkbeta On An Hts Station (478 views)
J Biomol Screen (ISSN: 1087-0571, 1552-454x, 1552-454xelectronic), 2009 Dec; 14(10): 1263-1268.
Impact Factor: 2.395
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Ponticelli S, Marasco D, Tarallo V, Albuquerque RJC, Mitola S, Takeda A, Stassen J, Presta M, Ambati J, Ruvo M, De Falco S
* Modulation of Angiogenesis by a Tetrameric Tripeptide That Antagonizes Vascular Endothelial Growth Factor Receptor (615 views)
Jbc Papers (ISSN: 0021-9258, 1083-351x, 0021-9258linking), 2008 Dec 5; 283(49): 34250-34259.
Impact Factor: 5.52
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Bernini E De Nuccio R, Brescia F, Minardo A, Zeni L, Sarro PM, Palumbo R, Scarf MR
* Development and characterization of an integrated silicon micro flow cytometer (366 views)
Anal Bioanal Chem (ISSN: 1618-2642), 2006; 386(5): 1267-1272.
Impact Factor: 2.591
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Marino M, Rossi M, Ruvo M, Fassina G
* Novel molecular targets for systemic lupus erythematosus (399 views)
Curr Drug Targets (ISSN: 1389-4501), 2002 Jun; 3(3): 223-228.
Impact Factor: 3.597
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Fassina G, Ruvo M, Palombo G, Verdoliva A, Marino M
* Novel ligands for the affinity-chromatographic purification of antibodies (1313 views)
J Biochem Biophys Methods (ISSN: 0165-022x, 0165-022xlinking), 2001 Oct 30; 49(1-3): 481-490.
Impact Factor: 1.218
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* The Screening of Combinatorial Peptide Libraries for Targeting Key Molecules or Protein-Protein Interactions in the NF-κB Pathway (9 views)
Methods Mol Biol (ISSN: 1064-3745linking, 1940-6029electronic), 2021; 2366: 343-356.
Impact Factor: 1.17
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Sandomenico A, Caporale A, Doti N, Cross S, Cruciani G, Chambery A, De Falco S, Ruvo M
* Synthetic Peptide Libraries: From Random Mixtures to In Vivo Testing (283 views)
Curr Med Chem (ISSN: 1875-533xelectronic, 0929-8673linking), 2018 Jul 15; 27(6): 997-1016.
Impact Factor: 4.63
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Sandomenico A, Severino V, Apone F, De Lucia A, Caporale A, Doti N, Russo A, Russo R, Rega C, Del Giacco T, Falcigno L, Ruvo M, Chambery A
* Trifluoroacetylated tyrosine-rich D-tetrapeptides have potent antioxidant activity (401 views)
Peptides (ISSN: 0196-9781, 1873-5169electronic, 0196-9781linking), 2017 Mar; 89: 50-59.
Impact Factor: 2.851
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Sandomenico A, Focà A, Sanguigno L, Caporale A, Focà G, Pignalosa A, Corvino G, Caragnano A, Beltrami AP, Antoniali G, Tell G, Leonardi A, Ruvo M
* Monoclonal antibodies against pools of mono- and polyacetylated peptides selectively recognize acetylated lysines within the context of the original antigen (391 views) (PDF 219 views)
Mabs-Austin (ISSN: 1942-0862), 2016 Aug; 8: 1575-1589.
Impact Factor: 4.881
View Export to BibTeX Export to EndNote
Caporale A, Selis F, Pain D, Sandomenico A, Jotti S, Tonon G, Ruvo M
* The LQSP tetrapeptide is a new highly efficient substrate of microbial transglutaminase for the site-specific derivatization of peptides and proteins (683 views)
Biotechnol J (ISSN: 1860-6768), 2015 Jan; 10(1): 154-161.
Impact Factor: 3.781
View Export to BibTeX Export to EndNote
Pappalardo M, Shachaf N, Basile L, Milardi D, Zeidan M, Raiyn J, Guccione S, Rayan A
* Sequential Application of Ligand and Structure Based Modeling Approaches to Index Chemicals for Their hH(4)R Antagonism (394 views)
Plosone (ISSN: 1932-6203, 1932-6203electronic, 1932-6203linking), 2014 Oct 16; 9(10): e109340-e109340.
Impact Factor: 3.234
View Export to BibTeX Export to EndNote
Zanoli LM, Spoto G
* Isothermal amplification methods for the detection of nucleic acids in microfluidic devices (368 views)
Biosensors (ISSN: 2079-6374), 2013 Mar; 3(1): 18-43.
Impact Factor: 0
View Export to BibTeX Export to EndNote
Merolla F, Luise C, Muller MT, Pacelli R, Fusco A, Celetti A
* Loss of CCDC6, the First Identified RET Partner Gene, Affects pH2AX S139 Levels and Accelerates Mitotic Entry upon DNA Damage (364 views)
Plosone (ISSN: 1932-6203, 1932-6203electronic, 1932-6203linking), 2012 May 24; 7(5): N/D-N/D.
Impact Factor: 3.73
View Export to BibTeX Export to EndNote
Doti N, Scognamiglio PL, Madonna S, Scarponi C, Ruvo M, Perretta G, Albanesi C, Marasco D
* New mimetic peptides of the kinase-inhibitory region (KIR) of SOCS1 through focused peptide libraries (1334 views)
Biochemical Journal, 2012 Apr 1; 443: 231-240.
Impact Factor: 4.779
View Export to BibTeX Export to EndNote
Zaccaro L, Garcia-lopez Mt Gonzalez-muniz RG
* TRPV1 modulators: Structure-activity relationships using a rational combinatorial approach (461 views)
Bioorganic & Medicinal Chemistry Letters (ISSN: 0960-894x), 2011 Jun 15; 21(12): 3541-3545.
Impact Factor: 2.554
View Export to BibTeX Export to EndNote
Ruvo M, Sandomenico A, Tudisco L, De Falco S
* Branched peptides for the modulation of protein-protein interactions: More arms are better than one? (532 views)
Curr Med Chem (ISSN: 0929-8673, 1875-533x, 1875-533xelectronic), 2011 Jun; 18(16): 2429-2437.
Impact Factor: 4.859
View Export to BibTeX Export to EndNote
Scognamiglio PL, Doti N, Grieco P, Pedone C, Ruvo M, Marasco D
* Discovery Of Small Peptide Antagonists Of Ped/Pea15-D4alpha Interaction From Simplified Combinatorial Libraries (504 views)
Chem Biol Drug Des (ISSN: 1747-0277, 1747-0285), 2011 May; 77(5): 319-327.
Impact Factor: 2.282
View Export to BibTeX Export to EndNote
Doti N, Marasco D, Pedone C, Sabatella M, Ruvo M
* Optimizing A Kinase Assay For Ikkbeta On An Hts Station (478 views)
J Biomol Screen (ISSN: 1087-0571, 1552-454x, 1552-454xelectronic), 2009 Dec; 14(10): 1263-1268.
Impact Factor: 2.395
View Export to BibTeX Export to EndNote
Ponticelli S, Marasco D, Tarallo V, Albuquerque RJC, Mitola S, Takeda A, Stassen J, Presta M, Ambati J, Ruvo M, De Falco S
* Modulation of Angiogenesis by a Tetrameric Tripeptide That Antagonizes Vascular Endothelial Growth Factor Receptor (615 views)
Jbc Papers (ISSN: 0021-9258, 1083-351x, 0021-9258linking), 2008 Dec 5; 283(49): 34250-34259.
Impact Factor: 5.52
View Export to BibTeX Export to EndNote
Bernini E De Nuccio R, Brescia F, Minardo A, Zeni L, Sarro PM, Palumbo R, Scarf MR
* Development and characterization of an integrated silicon micro flow cytometer (366 views)
Anal Bioanal Chem (ISSN: 1618-2642), 2006; 386(5): 1267-1272.
Impact Factor: 2.591
View Export to BibTeX Export to EndNote
Marino M, Rossi M, Ruvo M, Fassina G
* Novel molecular targets for systemic lupus erythematosus (399 views)
Curr Drug Targets (ISSN: 1389-4501), 2002 Jun; 3(3): 223-228.
Impact Factor: 3.597
View Export to BibTeX Export to EndNote
Fassina G, Ruvo M, Palombo G, Verdoliva A, Marino M
* Novel ligands for the affinity-chromatographic purification of antibodies (1313 views)
J Biochem Biophys Methods (ISSN: 0165-022x, 0165-022xlinking), 2001 Oct 30; 49(1-3): 481-490.
Impact Factor: 1.218
View Export to BibTeX Export to EndNote
17 Records (15 excluding Abstracts).
Total impact factor: 54.072 (47.108 excluding Abstracts).
Total 5 year impact factor: 63.784 (55.838 excluding Abstracts).
Total impact factor: 54.072 (47.108 excluding Abstracts).
Total 5 year impact factor: 63.784 (55.838 excluding Abstracts).
562 views. Last view on Tuesday 06 June 2023, 1:41:36
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