Design, synthesis and efficacy of novel G protein-coupled receptor kinase 2 inhibitors (527 views)
Eur J Med Chem (ISSN: 0223-5234, 1768-3254, 1768-3254electronic), 2013; 69: 384-392.
Export to BibTeX Export to EndNote
Paper type: Journal Article,
Impact factor: 3.432, 5-year impact factor: 4.071
Url: http://www.scopus.com/inward/record.url?eid=2-s2.0-84884612383&partnerID=40&md5=063cc3be44019c0b56a4b4f89b7435ab
Keywords: Cardiovascular System, Cyclic Peptides, Grk2 Inhibitors, Nmr Conformational Analysis, Cyclopeptide, G Protein Coupled Receptor Kinase 2, G Protein Coupled Receptor Kinase 2 Inhibitor, Lactam Derivative, Protein Serine Threonine Kinase Inhibitor, Unclassified Drug, Article, Controlled Study, Drug Conformation, Drug Design, Drug Efficacy, Drug Potency, Drug Selectivity, Drug Synthesis, Enzyme Inhibition, Enzyme Structure, Human, Human Cell, Nuclear Magnetic Resonance Spectroscopy, Nuclear Overhauser Effect, Peptide Library, Protein Structure, 7-Pentamethyldihydro Benzofuran-5-Sulfonyl, 2-(1h-Benzotriazole-1-Yl)-1, 3-Tetramethyluronium Hexafluoro-Phosphate, 9-Fluorenyl-Methoxycarbonyl, Adenosine Triphosphate, Cyclic Adenosine Monophosphate, Dichloromethane, Dipea, Dodecylphosphocholine, Egta, Electrospray Ionization, Ethylene Diamine Tetraacetic Acid, Ethylene Glycol Tetraacetic Acid, Fmoc, Hbtu, Liquid Chromatography Quadrupole Mass Spectrometry, N-Diisopropylethyl-Amine, N-Dimethylformamide, N-Hydroxy-Benzotriazole, Pr(3)sih Or Tis, Reversed-Phase High Performance Liquid Chromatography, Rp-Hplc, Structure-Activity Relationship, Trifluoroacetic Acid, Triisopropylsilane, Trityl, Dose-Response Relationship, G-Protein-Coupled Receptor Kinase 2, Models, Molecular, Protein Kinase Inhibitors,
Affiliations:
*** IBB - CNR ***
Dipartimento di Farmacia Federico II, University of Naples, Italy
Dipartimento di Scienze Biomediche Avanzate Federico II, University of Naples, Italy
Dipartimento di Medicina e Chirurgia, University of Salerno, Italy
IRCCS Multimedica, Milano, Italy
Pharmaceutical Science, University of Salerno, Salerno, Italy
References:
Pitcher, J.A., Freedman, N.J., Lefkowitz, R.J., G protein-coupled receptor kinases (1998) Annual Review of Biochemistry, 67, pp. 653-692. , DOI 10.1146/annurev.biochem.67.1.65
Ferguson, S.S.G., Evolving concepts in G protein-coupled receptor endocytosis: The role in receptor desensitization and signaling (2001) Pharmacological Reviews, 53 (1), pp. 1-24
Reiter, E., Lefkowitz, R.J., GRKs and beta-arrestins: Roles in receptor silencing, trafficking and signalling (2006) Trends Endocrinol. Metab., 17, pp. 159-165
Moore, C.A.C., Milano, S.K., Benovic, J.L., Regulation of receptor trafficking by GRKs and arrestins (2007) Annual Review of Physiology, 69, pp. 451-482. , DOI 10.1146/annurev.physiol.69.022405.154712
Ribas, C., Penela, P., Murga, C., Salcedo, A., Garcia-Hoz, C., Jurado-Pueyo, M., Aymerich, I., Mayor Jr., F., The G protein-coupled receptor kinase (GRK) interactome: Role of GRKs in GPCR regulation and signaling (2007) Biochimica et Biophysica Acta - Biomembranes, 1768 (4), pp. 913-922. , DOI 10.1016/j.bbamem.2006.09.019, PII S0005273606003774
Lefkowitz, R.J., Shenoy, S.K., Transduction of receptor signals by beta-arrestins (2005) Science, 308, pp. 512-517
Hupfeld, C.J., Olefsky, J.M., Regulation of receptor tyrosine kinase signaling by GRKs and β-arrestins (2007) Annual Review of Physiology, 69, pp. 561-577. , DOI 10.1146/annurev.physiol.69.022405.154626
Oppermann, M., Diverse-Pierluissi, M., Drazner, M.H., Dyer, S.L., Freedman, N.J., Peppel, K.C., Lefkowitz, R.J., Monoclonal antibodies reveal receptor specificity among G-protein coupled receptor kinases (1996) Proc. Natl. Acad. Sci. U. S. A., 93, pp. 7649-7654
Willets, J.M., Challiss, R.A.J., Nahorski, S.R., Non-visual GRKs: Are we seeing the whole picture? (2003) Trends in Pharmacological Sciences, 24 (12), pp. 626-633. , DOI 10.1016/j.tips.2003.10.003
Inglese, J., Freedman, N.J., Koch, W.J., Lefkowitz, R.J., Structure and mechanism of the G protein-coupled receptor kinases (1993) Journal of Biological Chemistry, 268 (32), pp. 23735-23738
Evron, T., Daigle, T.L., Caron, M.G., GRK2: Multiple roles beyond G protein-coupled receptor desensitization (2012) Trends Pharmacol. Sci., 33, pp. 154-164
Dzimiri, N., Muiya, P., Andres, E., Al-Halees, Z., Differential functional expression of human myocardial G protein receptor kinases in left ventricular cardiac diseases (2004) European Journal of Pharmacology, 489 (3), pp. 167-177. , DOI 10.1016/j.ejphar.2004.03.015, PII S0014299904002286
Ungerer, M., Kessebohm, K., Kronsbein, K., Lohse, M.J., Richardt, G., Activation of β-adrenergic receptor kinase during myocardial ischemia (1996) Circulation Research, 79 (3), pp. 455-460
Choi, D.-J., Koch, W.J., Hunter, J.J., Rockman, H.A., Mechanism of β-adrenergic receptor desensitization in cardiac hypertrophy is increased β-adrenergic receptor kinase (1997) Journal of Biological Chemistry, 272 (27), pp. 17223-17229. , DOI 10.1074/jbc.272.27.17223
Gros, R., Benovic, J.L., Tan, C.M., Feldman, R.D., G-protein-coupled receptor kinase activity is increased in hypertension (1997) Journal of Clinical Investigation, 99 (9), pp. 2087-2093
Theilade, J., Strom, C., Christiansen, T., Haunso, S., Sheikh, S.P., Differential G protein receptor kinase 2 expression in compensated hypertrophy and heart failure after myocardial infarction in the rat (2003) Basic Research in Cardiology, 98 (2), pp. 97-103. , DOI 10.1007/s00395-003-0395-x
Harris, C.A., Chuang, T.-T., Scorer, C.A., Expression of GRK2 is increased in the left ventricles of cardiomyopathic hamsters (2001) Basic Research in Cardiology, 96 (4), pp. 364-368. , DOI 10.1007/s003950170044
Yi, X.P., Gerdes, A.M., Li, F., Myocyte redistribution of GRK2 and GRK5 in hypertensive, heart-failure-prone rats (2002) Hypertension, 39 (6), pp. 1058-1063. , DOI 10.1161/01.HYP.0000019130.09167.3B
Anderson, K.M., Eckhart, A.D., Willette, R.N., Koch, W.J., The myocardial β-adrenergic system in spontaneously hypertensive heart failure (SHHF) rats (1999) Hypertension, 33 (1), pp. 402-407
Iaccarino, G., Barbato, E., Cipolletta, E., De Amicis, V., Margulies, K.B., Leosco, D., Trimarco, B., Koch, W.J., Elevated myocardial and lymphocyte GRK2 expression and activity in human heart failure (2005) European Heart Journal, 26 (17), pp. 1752-1758. , DOI 10.1093/eurheartj/ehi429
Hata, J.A., Williams, M.L., Schroder, J.N., Lima, B., Keys, J.R., Blaxall, B.C., Petrofski, J.A., Koch, W.J., Lymphocyte Levels of GRK2 (βARK1) Mirror Changes in the LVAD-Supported Failing Human Heart: Lower GRK2 Associated With Improved β-Adrenergic Signaling After Mechanical Unloading (2006) Journal of Cardiac Failure, 12 (5), pp. 360-368. , DOI 10.1016/j.cardfail.2006.02.011, PII S1071916406001308
Bonita, R.E., Raake, P.W., Otis, N.J., Chuprun, J.K., Spivack, T., Dasgupta, A., Whellan, D.J., Koch, W.J., Dynamic changes in lymphocyte GRK2 levels in cardiac transplant patients: A biomarker for left ventricular function (2010) Clin. Transl. Sci., 3, pp. 14-18
Iaccarino, G., Koch, W.J., Therapeutic potential of G-protein coupled receptor kinases in the heart (1999) Expert Opinion on Investigational Drugs, 8 (5), pp. 545-554. , DOI 10.1517/13543784.8.5.545
Rengo, G., Lymperopoulos, A., Leosco, D., Koch, W.J., GRK2 as a novel gene therapy target in heart failure (2011) J. Mol. Cell Cardiol., 50, pp. 785-792
Rockman, H.A., Chien, K.R., Choi, D.-J.U., Iaccarino, G., Hunter, J.J., John Ross, J.R., Lefkowitz, R.J., Koch, W.J., Expression of a β-adrenergic receptor kinase 1 inhibitor prevents the development of myocardial failure in gene-targeted mice (1998) Proceedings of the National Academy of Sciences of the United States of America, 95 (12), pp. 7000-7005. , DOI 10.1073/pnas.95.12.7000
Setyawan, J., Koide, K., Diller, T.C., Bunnage, M.E., Taylor, S.S., Nicolaou, K.C., Brunton, L.L., Inhibition of protein kinases by balanol: Specificity within the serine/threonine protein kinase subfamily (1999) Molecular Pharmacology, 56 (2), pp. 370-376
Iino, M., Furugori, T., Mori, T., Moriyama, S., Fukuzawa, A., Shibano, T., Rational design and evaluation of new lead compound structures for selective βARK1 inhibitors (2002) Journal of Medicinal Chemistry, 45 (11), pp. 2150-2159. , DOI 10.1021/jm010093a
Benovic, J.L., Stone, W.C., Caron, M.G., Lefkowitz, R.J., Inhibition of the β-adrenergic receptor kinase by polyanions (1989) Journal of Biological Chemistry, 264 (12), pp. 6707-6710
Ikeda, S., Kaneko, M., Fujiwara, S., Cardiotonic Agents Comprising GRK Inhibitor, , Takeda Pharmaceuticals Company Limited World Patent WO2007034846
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Eur J Med Chem (ISSN: 0223-5234, 1768-3254, 1768-3254electronic), 2013; 69: 384-392.
Export to BibTeX Export to EndNote
Paper type: Journal Article,
Impact factor: 3.432, 5-year impact factor: 4.071
Url: http://www.scopus.com/inward/record.url?eid=2-s2.0-84884612383&partnerID=40&md5=063cc3be44019c0b56a4b4f89b7435ab
Keywords: Cardiovascular System, Cyclic Peptides, Grk2 Inhibitors, Nmr Conformational Analysis, Cyclopeptide, G Protein Coupled Receptor Kinase 2, G Protein Coupled Receptor Kinase 2 Inhibitor, Lactam Derivative, Protein Serine Threonine Kinase Inhibitor, Unclassified Drug, Article, Controlled Study, Drug Conformation, Drug Design, Drug Efficacy, Drug Potency, Drug Selectivity, Drug Synthesis, Enzyme Inhibition, Enzyme Structure, Human, Human Cell, Nuclear Magnetic Resonance Spectroscopy, Nuclear Overhauser Effect, Peptide Library, Protein Structure, 7-Pentamethyldihydro Benzofuran-5-Sulfonyl, 2-(1h-Benzotriazole-1-Yl)-1, 3-Tetramethyluronium Hexafluoro-Phosphate, 9-Fluorenyl-Methoxycarbonyl, Adenosine Triphosphate, Cyclic Adenosine Monophosphate, Dichloromethane, Dipea, Dodecylphosphocholine, Egta, Electrospray Ionization, Ethylene Diamine Tetraacetic Acid, Ethylene Glycol Tetraacetic Acid, Fmoc, Hbtu, Liquid Chromatography Quadrupole Mass Spectrometry, N-Diisopropylethyl-Amine, N-Dimethylformamide, N-Hydroxy-Benzotriazole, Pr(3)sih Or Tis, Reversed-Phase High Performance Liquid Chromatography, Rp-Hplc, Structure-Activity Relationship, Trifluoroacetic Acid, Triisopropylsilane, Trityl, Dose-Response Relationship, G-Protein-Coupled Receptor Kinase 2, Models, Molecular, Protein Kinase Inhibitors,
Affiliations:
*** IBB - CNR ***
Dipartimento di Farmacia Federico II, University of Naples, Italy
Dipartimento di Scienze Biomediche Avanzate Federico II, University of Naples, Italy
Dipartimento di Medicina e Chirurgia, University of Salerno, Italy
IRCCS Multimedica, Milano, Italy
Pharmaceutical Science, University of Salerno, Salerno, Italy
References:
Pitcher, J.A., Freedman, N.J., Lefkowitz, R.J., G protein-coupled receptor kinases (1998) Annual Review of Biochemistry, 67, pp. 653-692. , DOI 10.1146/annurev.biochem.67.1.65
Ferguson, S.S.G., Evolving concepts in G protein-coupled receptor endocytosis: The role in receptor desensitization and signaling (2001) Pharmacological Reviews, 53 (1), pp. 1-24
Reiter, E., Lefkowitz, R.J., GRKs and beta-arrestins: Roles in receptor silencing, trafficking and signalling (2006) Trends Endocrinol. Metab., 17, pp. 159-165
Moore, C.A.C., Milano, S.K., Benovic, J.L., Regulation of receptor trafficking by GRKs and arrestins (2007) Annual Review of Physiology, 69, pp. 451-482. , DOI 10.1146/annurev.physiol.69.022405.154712
Ribas, C., Penela, P., Murga, C., Salcedo, A., Garcia-Hoz, C., Jurado-Pueyo, M., Aymerich, I., Mayor Jr., F., The G protein-coupled receptor kinase (GRK) interactome: Role of GRKs in GPCR regulation and signaling (2007) Biochimica et Biophysica Acta - Biomembranes, 1768 (4), pp. 913-922. , DOI 10.1016/j.bbamem.2006.09.019, PII S0005273606003774
Lefkowitz, R.J., Shenoy, S.K., Transduction of receptor signals by beta-arrestins (2005) Science, 308, pp. 512-517
Hupfeld, C.J., Olefsky, J.M., Regulation of receptor tyrosine kinase signaling by GRKs and β-arrestins (2007) Annual Review of Physiology, 69, pp. 561-577. , DOI 10.1146/annurev.physiol.69.022405.154626
Oppermann, M., Diverse-Pierluissi, M., Drazner, M.H., Dyer, S.L., Freedman, N.J., Peppel, K.C., Lefkowitz, R.J., Monoclonal antibodies reveal receptor specificity among G-protein coupled receptor kinases (1996) Proc. Natl. Acad. Sci. U. S. A., 93, pp. 7649-7654
Willets, J.M., Challiss, R.A.J., Nahorski, S.R., Non-visual GRKs: Are we seeing the whole picture? (2003) Trends in Pharmacological Sciences, 24 (12), pp. 626-633. , DOI 10.1016/j.tips.2003.10.003
Inglese, J., Freedman, N.J., Koch, W.J., Lefkowitz, R.J., Structure and mechanism of the G protein-coupled receptor kinases (1993) Journal of Biological Chemistry, 268 (32), pp. 23735-23738
Evron, T., Daigle, T.L., Caron, M.G., GRK2: Multiple roles beyond G protein-coupled receptor desensitization (2012) Trends Pharmacol. Sci., 33, pp. 154-164
Dzimiri, N., Muiya, P., Andres, E., Al-Halees, Z., Differential functional expression of human myocardial G protein receptor kinases in left ventricular cardiac diseases (2004) European Journal of Pharmacology, 489 (3), pp. 167-177. , DOI 10.1016/j.ejphar.2004.03.015, PII S0014299904002286
Ungerer, M., Kessebohm, K., Kronsbein, K., Lohse, M.J., Richardt, G., Activation of β-adrenergic receptor kinase during myocardial ischemia (1996) Circulation Research, 79 (3), pp. 455-460
Choi, D.-J., Koch, W.J., Hunter, J.J., Rockman, H.A., Mechanism of β-adrenergic receptor desensitization in cardiac hypertrophy is increased β-adrenergic receptor kinase (1997) Journal of Biological Chemistry, 272 (27), pp. 17223-17229. , DOI 10.1074/jbc.272.27.17223
Gros, R., Benovic, J.L., Tan, C.M., Feldman, R.D., G-protein-coupled receptor kinase activity is increased in hypertension (1997) Journal of Clinical Investigation, 99 (9), pp. 2087-2093
Theilade, J., Strom, C., Christiansen, T., Haunso, S., Sheikh, S.P., Differential G protein receptor kinase 2 expression in compensated hypertrophy and heart failure after myocardial infarction in the rat (2003) Basic Research in Cardiology, 98 (2), pp. 97-103. , DOI 10.1007/s00395-003-0395-x
Harris, C.A., Chuang, T.-T., Scorer, C.A., Expression of GRK2 is increased in the left ventricles of cardiomyopathic hamsters (2001) Basic Research in Cardiology, 96 (4), pp. 364-368. , DOI 10.1007/s003950170044
Yi, X.P., Gerdes, A.M., Li, F., Myocyte redistribution of GRK2 and GRK5 in hypertensive, heart-failure-prone rats (2002) Hypertension, 39 (6), pp. 1058-1063. , DOI 10.1161/01.HYP.0000019130.09167.3B
Anderson, K.M., Eckhart, A.D., Willette, R.N., Koch, W.J., The myocardial β-adrenergic system in spontaneously hypertensive heart failure (SHHF) rats (1999) Hypertension, 33 (1), pp. 402-407
Iaccarino, G., Barbato, E., Cipolletta, E., De Amicis, V., Margulies, K.B., Leosco, D., Trimarco, B., Koch, W.J., Elevated myocardial and lymphocyte GRK2 expression and activity in human heart failure (2005) European Heart Journal, 26 (17), pp. 1752-1758. , DOI 10.1093/eurheartj/ehi429
Hata, J.A., Williams, M.L., Schroder, J.N., Lima, B., Keys, J.R., Blaxall, B.C., Petrofski, J.A., Koch, W.J., Lymphocyte Levels of GRK2 (βARK1) Mirror Changes in the LVAD-Supported Failing Human Heart: Lower GRK2 Associated With Improved β-Adrenergic Signaling After Mechanical Unloading (2006) Journal of Cardiac Failure, 12 (5), pp. 360-368. , DOI 10.1016/j.cardfail.2006.02.011, PII S1071916406001308
Bonita, R.E., Raake, P.W., Otis, N.J., Chuprun, J.K., Spivack, T., Dasgupta, A., Whellan, D.J., Koch, W.J., Dynamic changes in lymphocyte GRK2 levels in cardiac transplant patients: A biomarker for left ventricular function (2010) Clin. Transl. Sci., 3, pp. 14-18
Iaccarino, G., Koch, W.J., Therapeutic potential of G-protein coupled receptor kinases in the heart (1999) Expert Opinion on Investigational Drugs, 8 (5), pp. 545-554. , DOI 10.1517/13543784.8.5.545
Rengo, G., Lymperopoulos, A., Leosco, D., Koch, W.J., GRK2 as a novel gene therapy target in heart failure (2011) J. Mol. Cell Cardiol., 50, pp. 785-792
Rockman, H.A., Chien, K.R., Choi, D.-J.U., Iaccarino, G., Hunter, J.J., John Ross, J.R., Lefkowitz, R.J., Koch, W.J., Expression of a β-adrenergic receptor kinase 1 inhibitor prevents the development of myocardial failure in gene-targeted mice (1998) Proceedings of the National Academy of Sciences of the United States of America, 95 (12), pp. 7000-7005. , DOI 10.1073/pnas.95.12.7000
Setyawan, J., Koide, K., Diller, T.C., Bunnage, M.E., Taylor, S.S., Nicolaou, K.C., Brunton, L.L., Inhibition of protein kinases by balanol: Specificity within the serine/threonine protein kinase subfamily (1999) Molecular Pharmacology, 56 (2), pp. 370-376
Iino, M., Furugori, T., Mori, T., Moriyama, S., Fukuzawa, A., Shibano, T., Rational design and evaluation of new lead compound structures for selective βARK1 inhibitors (2002) Journal of Medicinal Chemistry, 45 (11), pp. 2150-2159. , DOI 10.1021/jm010093a
Benovic, J.L., Stone, W.C., Caron, M.G., Lefkowitz, R.J., Inhibition of the β-adrenergic receptor kinase by polyanions (1989) Journal of Biological Chemistry, 264 (12), pp. 6707-6710
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Design, synthesis and efficacy of novel G protein-coupled receptor kinase 2 inhibitors
G protein-coupled receptor kinase 2 (GRK2) is a relevant signaling node of the cellular transduction network, playing major roles in the physiology of various organs/tissues including the heart and blood vessels. Emerging evidence suggests that GRK2 is up regulated in pathological situations such as heart failure, hypertrophy and hypertension, and its inhibition offers a potential therapeutic solution to these diseases. We explored the GRK2 inhibitory activity of a library of cyclic peptides derived from the HJ loop of G protein-coupled receptor kinases 2 (GRK2). The design of these cyclic compounds was based on the conformation of the HJ loop within the X-ray structure of GRK2. One of these compounds, the cyclic peptide 7, inhibited potently and selectively the GRK2 activity, being more active than its linear precursor. In a cellular system, this peptide confirms the beneficial signaling properties of a potent GRK2 inhibitor. Preferred conformations of the most potent analog were investigated by NMR spectroscopy. © 2013 Published by Elsevier Masson SAS.
G protein-coupled receptor kinase 2 (GRK2) is a relevant signaling node of the cellular transduction network, playing major roles in the physiology of various organs/tissues including the heart and blood vessels. Emerging evidence suggests that GRK2 is up regulated in pathological situations such as heart failure, hypertrophy and hypertension, and its inhibition offers a potential therapeutic solution to these diseases. We explored the GRK2 inhibitory activity of a library of cyclic peptides derived from the HJ loop of G protein-coupled receptor kinases 2 (GRK2). The design of these cyclic compounds was based on the conformation of the HJ loop within the X-ray structure of GRK2. One of these compounds, the cyclic peptide 7, inhibited potently and selectively the GRK2 activity, being more active than its linear precursor. In a cellular system, this peptide confirms the beneficial signaling properties of a potent GRK2 inhibitor. Preferred conformations of the most potent analog were investigated by NMR spectroscopy. © 2013 Published by Elsevier Masson SAS.
Design, synthesis and efficacy of novel G protein-coupled receptor kinase 2 inhibitors
| ▼ Design of New FSHR-Specific Peptides for therapeutic and diagnostic applications |
Design, synthesis and efficacy of novel G protein-coupled receptor kinase 2 inhibitors
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Fattorusso R, Morelli G, Lombardi A, Nastri F, maglio O, D'Auria G, Pedone C, Pavone V
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Biopolymers (ISSN: 0006-3525, 0006-6352, 0006-3525print), 1995; 37(6): 401-410.
Impact Factor: 2.425
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Pavone V, Lombardi A, Saviano M, Nastri F, Fattorusso R, Maglio O, Isernia C, Paolillo L, Pedone C
β-alanine containing cyclic peptides with turned structure: The 'pseudo type II β-turn. ' VI (463 views)
Biopolymers (ISSN: 0006-3525, 0006-6352, 0006-3525print), 1994 Nov; 34(11): 1517-1526.
Impact Factor: 2.425
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Rossi F, Saviano M, Di Blasio B, Zanotti G, Maione AM, Tancredi T, Pedone C
BIOACTIVE PEPTIDES - SOLID-STATE, SOLUTION AND MOLECULAR-DYNAMICS STUDIES OF A CYCLOLINOPEPTIDE-A RELATED CYSTINYL CYCLOPENTAPEPTIDE (455 views)
Biopolymers (ISSN: 0006-3525, 0006-6352, 0006-3525print), 1994 Feb; 34(2): 273-284.
Impact Factor: 2.425
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Di Blasio B, Lombardi A, D'Auria G, Saviano M, Isernia C, Maglio O, Paolillo L, Pedone C, Pavone V
Beta-Alanine Containing Peptides: Gamma-Turns In Cyclotetrapeptides (560 views)
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Impact Factor: 2.425
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DIBLASIO B, ROSSI F, BENEDETTI E, PAVONE V, SAVIANO M, PEDONE C, ZANOTTI G, TANCREDI T
BIOACTIVE PEPTIDES - X-RAY AND NMR CONFORMATIONAL STUDY OF [AIB(5, 6)-D-ALA(8)]CYCLOLINOPEPTIDE-A (441 views)
J Am Chem Soc (ISSN: 0002-7863, 0002-2786, 1520-5126), 1992 Oct 7; 114(21): 8277-8283.
Impact Factor: 5.65
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Tancredi T, Benedetti E, Grimaldi M, Pedone C, Rossi F, Saviano M, Temussi PA, Zanotti G
Ion binding of cyclolinopeptide A: An NMR and CD conformational study (633 views)
Biopolymers (ISSN: 0006-3525, 0006-6352, 0006-3525print), 1991 May; 31(6): 761-767.
Impact Factor: 2.425
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Cucinotta V, D'Alessandro F, Impellizzeri G, Pappalardo G, Rizzarelli E, Vecchio G
Cyclopeptide Functionalized beta-Cyclodextrin. A New Class of Potentially Enzyme Mimicking Compound with Two Recognition Sites (267 views)
Chem Commun, 1991; N/D: 293-294.
Impact Factor: 0
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Tancredi T, Zanotti G, Rossi F, Benedetti E, Pedone C, Temussi PA
Comparison of the conformations of cyclolinopeptide A in the solid state and in solution (423 views)
Biopolymers (ISSN: 0006-3525, 0006-6352, 0006-3525print), 1989 Jan; 28(1): 513-523.
Impact Factor: 2.425
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Arena G, Impellizzeri G, Maccarrone G, Pappalardo G, Sciotto D, Rizzarelli E
Non-Covalent Interactions in Cyclopeptide Proton Complex Formation in Aqueous Solution (308 views)
Thermochim Acta, 1989; 154: 97-106.
Impact Factor: 0
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Betocchi S, Cuocolo A, Pace L, Chiariello M, Trimarco B, Alfano B, Ricciardelli B, Salvatore M, Condorelli M
Effects of intravenous verapamil administration on left ventricular diastolic function in systemic hypertension (767 views)
Am J Cardiol (ISSN: 0002-9149), 1987 Mar 1; 59(6): 624-629.
Impact Factor: 2.402
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Ferrara LA, Mancini M, Marotta T, Pasanisi F, Fasano ML
Interference by sulphinpyrazone with the antihypertensive effects of oxprenolol (943 views)
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Impact Factor: 1.219
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Ferrara LA, Strazzullo P, Scillitani A, Mancini M, Gagliardi R
Cross-over study of muzolimine and hydrochlorothiazide-amiloride in hypertensive patients (731 views)
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Impact Factor: 1.219
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Vosa C, Lapenta L, Caianiello G, Esposito V, de LucaL, D'Angelo TS, Salvatore M
Pre- and postoperative Tc 99m scanning in monitoring pulmonary perfusion in the tetralogy of Fallot (701 views)
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Impact Factor: 0
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* Exploring the ability of cyclic peptides to target SAM domains: a computational and experimental study (266 views)
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Impact Factor: 2.641
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Lanza V, Milardi D, Di Natale G, Pappalardo G
* Repurposing of Copper(II)-chelating Drugs for the Treatment of Neurodegenerative Diseases (708 views)
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Impact Factor: 3.249
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Diana D, Di Salvo C, Celentano V, De Rosa L, Romanelli A, Fattorusso R, D'Andrea LD
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Impact Factor: 3.451
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Calvanese L, Caporale A, Focà G, Iaccarino E, Sandomenico A, Doti N, Apicella I, Incisivo GM, De Falco S, Falcigno L, D’auria G, Ruvo M
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Impact Factor: 2.906
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Greco A, Coda ARD, Albanese S, Ragucci M, Liuzzi R, Auletta L, Gargiulo S, Lamagna F, Salvatore M, Mancini M
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Impact Factor: 2.429
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di Villa Bianca R, Mitidieri E, Donnarumma E, Fusco F, Longo N, Rosa GD, Novellino E, Grieco P, Mirone V, Cirino G, Sorrentino R
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Impact Factor: 2.644
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De Rosa L, Diana D, Basile A, Russomanno A, Isernia C, Turco MC, Fattorusso R, D'Andrea LD
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Impact Factor: 3.447
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Bellia F, GrassoG
* The role of copper(II) and zinc(II) in the degradation of human and murine IAPP by insulin-degrading enzyme (520 views)
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Impact Factor: 2.379
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Portella L, Vitale R, De Luca S, D'Alterio C, Ieranò C, Napolitano M, Riccio A, Polimeno MN, Monfregola L, Barbieri A, Luciano A, Ciarmiello A, Arra C, Castello G, Amodeo P, Scala S
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Impact Factor: 3.534
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Saviano M, Del Gatto A, De Simone M, De Paola I, Saviano M, Zaccaro L
* Investigation of the Best Conditions to Obtain c(RGDfK) Peptide on Solid Phase (508 views)
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Impact Factor: 0.986
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Accardo A, Morisco A, Gianolio E, Tesauro D, Mangiapia G, Radulescu A, Brandt A, Morelli G
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Impact Factor: 1.799
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Santulli G, Basilicata MF, De Simone M, Del Giudice C, Anastasio A, Sorriento D, Saviano M, Del Gatto A, Trimarco B, Pedone C, Zaccaro L, Iaccarino G
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Impact Factor: 3.474
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Barile E, Leone M, Barile E, Dahl R, Pellecchia M
* Design and NMR Studies of Cyclic Peptides Targeting the N-Terminal Domain of the Protein Tyrosine Phosphatase YopH (2177 views)
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Impact Factor: 2.282
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Gautier B, Goncalves V, Diana D, Di Stasi R, Teillet F, Lenoir C, Huguenot F, Garbay C, Fattorusso R, D'Andrea LD, Vidal M, Inguimbert N
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Impact Factor: 5.207
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Amodeo P, Castello G, De Luca S, Scala S, Siani A, Vitale RM
* CYCLIC PEPTIDES BINDING CXCR4 RECEPTOR AND RELATIVE MEDICAL AND DIAGNOSTIC USES (470 views)
Patent, 2010; PctWo2011092575: Pct-Pct.
Impact Factor: 0
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Kaczmarek K, Farina B, Zubrzak P, Jankowski S, Zimecki M, Suder P, Benedetti E, Fattorusso R, Saviano M, Zabrocki J
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Impact Factor: 1.807
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Goldfine ID, Maddux BA, Youngren JF, Reaven G, Accili D, Trischitta V, Vigneri R, Frittitta L
* The role of membrane glycoprotein plasma cell antigen 1 ectonucleotide pyrophosphatase phosphodiesterase 1 in the pathogenesis of insulin resistance and related abnormalities (874 views)
Endocrine Reviews (ISSN: 0163-769x), 2008 Feb; 29(1): 62-75.
Impact Factor: 18.562
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De Luca S, De Capua A, Saviano M, Della Moglie R, Aloj L, Tarallo L, Pedone C, Morelli G
* Synthesis and biological evaluation of cyclic and branched peptide analogues as ligands for cholecystokinin type 1 receptor (398 views)
Bioorg Med Chem (ISSN: 0968-0896, 1464-3391, 1464-3391electronic), 2007 Sep 1; 15(17): 5845-5853.
Impact Factor: 2.662
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Galdiero S, Vitiello M, Amodeo P, D'Isanto M, Cantisani M, Pedone C, Galdiero M
* Structural requirements for proinflammatory activity of porin P2 loop 7 from Haemophilus influenzae (514 views)
Biochemistry (ISSN: 0006-2960, 1520-4995, 1520-4995electronic), 2006 Apr 11; 45(14): 4491-4501.
Impact Factor: 3.633
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Colao A, Di Somma C, Cuocolo A, Spinelli L, Acampa W, Spiezia S, Rota F, Savanelli MC, Lombardi G
* Does a gender-related effect of growth hormone (GH) replacement exist on cardiovascular risk factors, cardiac morphology, and performance and atherosclerosis? Results of a two-year open, prospective study in young adult men and women with severe GH deficiency (422 views)
J Clin Endocrinol Metab (ISSN: 0021-972x), 2005 Sep; 90(9): 5146-5155.
Impact Factor: 6.02
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Benedetti E, Pedone C
* Cyclolinopeptide A: inhibitor, immunosuppressor or other? (567 views)
J Pept Sci (ISSN: 1075-2617, 1099-1387, 1075-2617print), 2005 May; 11(5): 268-272.
Impact Factor: 1.803
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Cozzolino R, Palladino P, Rossi F, Cali G, Benedetti E, Laccetti P
* Antineoplastic cyclic astin analogues kill tumour cells via caspase-mediated induction of apoptosis (524 views)
Carcinogenesis (ISSN: 0143-3334), 2005 Apr; 26(4): 733-739.
Impact Factor: 5.108
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De Luca S, Morelli G
* Synthesis and characterization of a sulfated and a non-sulfated cyclic CCK8 analogue functionalized with a chelating group for metal labelling (395 views)
J Pept Sci (ISSN: 1075-2617, 1099-1387, 1075-2617print), 2004 May; 10(5): 265-273.
Impact Factor: 1.652
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Clemente F, D'Avino E, Guaragno M, Menichetti A
* An on line technique to detect cardiac output variations and cardiovascular performances during abdominal aortic surgery (495 views)
Journal Of Clinical Monitoring And Computing (ISSN: 1387-1307), 2004 Apr; 18(2): 81-87.
Impact Factor: 0.888
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De Luca S, Ragone R, Bracco C, Digilio G, Aloj L, Tesauro D, Saviano M, Pedone C, Morelli G
* A cyclic CCK8 analogue selective for the cholecystokinin type A receptor: design, synthesis, NMR structure and binding measurements (472 views)
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Impact Factor: 3.992
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Kozarski M, Ferrari G, Clemente F, Gorczynska K, De Lazzari C, Darowski M, Mimmo R, Tosti G, Guaragno M
* A hybrid mock circulatory system: development and testing of an electro-hydraulic impedance simulator (354 views)
Int J Artif Organs (ISSN: 0391-3988, 0391-3988print), 2003 Jan; 26(1): 53-63.
Impact Factor: 0.964
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Biondi B, Palmieri EA, Pagano L, Klain M, Scherillo G, Salvatore M, Fenzi G, Lombardi G, Fazio S
* Cardiovascular safety of acute recombinant human thyrotropin administration to patients monitored for differentiated thyroid cancer (388 views)
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Impact Factor: 5.873
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Ferrari G, De Lazzari C, Kozarski M, Clemente F, Górczy ska K, Mimmo R, Monnanni E, Tosti G, Guaragno M
* A hybrid mock circulatory system: Testing a prototype under physiologic and pathological conditions (250 views)
Asaio Journal (ISSN: 1058-2916), 2002 Sep; 48(5): 487-494.
Impact Factor: 1.043
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Colao A, Spinelli L, Cuocolo A, Spiezia S, Pivonello R, Di Somma C, Bonaduce D, Salvatore M, Lombardi G
* Cardiovascular consequences of early-onset growth hormone excess (420 views)
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Impact Factor: 5.199
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De Lazzari C, Darowski M, Ferrari G, Clemente F, Guaragno M
* Energetic parameter changes with mechanical ventilation in conjunction with BVAD assistance (399 views)
J Med Eng Technol (ISSN: 0309-1902), 2002 Mar; 26(2): 63-70.
Impact Factor: 0.538
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Saviano G, Rossi F, Benedetti E, Pedone C, Mierke DF, Maione A, Zanotti G, Tancredi T, Saviano M
* Structural consequences of metal complexation of cyclo[Pro-Phe-Phe-Ala-Xaa]2 decapeptides (447 views)
Chemistry (ISSN: 0947-6539, 1521-3765, 1521-3765electronic), 2001 Mar 16; 7(6): 1176-1183.
Impact Factor: 4.614
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Monti SM, Gallo M, Ferracane R, Borrelli RC, Ritieni A, Greco ML, Graniti A, Fogliano V
* Analysis of bacterial lipodepsipeptides by matrix-assisted laser desorption/ionisation time-of-flight and high-performance liquid chromatography with electrospray mass spectrometry (437 views)
Rapid Commun Mass Sp (ISSN: 0951-4198, 1097-0231electronic), 2001; 15(8): 623-628.
Impact Factor: 2.478
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Gallo P, Rossi F, Saviano M, Pedone C, Colonna G, Ragone R
Specific interaction between bovine cyclophilin A and synthetic analogues of cyclolinopeptide (393 views)
Journal Of Biochemistry (ISSN: 0021-924x), 1998 Nov; 124(5): 880-885.
Impact Factor: 2.189
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Zanotti G, Saviano M, Saviano G, Tancredi T, Rossi F, Pedone C, Benedetti E
Structure of cyclic peptides: the crystal and solution conformation of cyclo(Phe-Phe-Aib-Leu-Pro) (592 views)
Journal Of Peptide Research (ISSN: 1397-002x), 1998 Jun; 51(6): 460-466.
Impact Factor: 1.125
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Lombardi A, D'Agostino B, Nastri F, D'Andrea LD, Filippelli A, Falciani M, Rossi F, Pavone V
A novel super-potent neurokinin A receptor antagonist containing dehydroalanine (463 views)
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Impact Factor: 1.5
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Lombardi A, D'Auria G, Maglio O, Nastri F, Quartara L, Pedone C, Pavone V
A novel rigid β-turn molecular scaffold (454 views)
J Am Chem Soc (ISSN: 0002-7863, 0002-2786, 1520-5126), 1998; 120(24): 5879-5886.
Impact Factor: 5.725
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Bonomo RP, Impellizzeri G, Pappalardo G, Purrello R, Rizzarelli E, Tabbì G
Co-ordinating properties of cyclopeptides. Thermodynamic and spectroscopic study on the formation of copper(II) complexes with cyclo(Gly-His)4 and cyclo(Gly-His-Gly)2 and their superoxide dismutase-like activity (452 views)
Journal Of The Chemical Society Dalton Transactions (ISSN: 0300-9246), 1998; (22): 3851-3857.
Impact Factor: 2.507
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D'Andrea LD, Mazzeo M, Isernia C, Rossi F, Saviano M, Gallo P, Paolillo L, Pedone C
Solution conformational preferences of a peptidic analogue of a natural macrolide (382 views)
Biopolymers (ISSN: 0006-3525, 0006-6352, 0006-3525print), 1997; 42(3): 349-361.
Impact Factor: 2.425
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Lombardi A, Saviano M, Nastri F, Maglio O, Mazzeo M, Pedone C, Isernia C, Pavone V
Unusual conformational preferences of β-alanine containing cyclic peptides. VII (456 views)
Biopolymers (ISSN: 0006-3525, 0006-6352, 0006-3525print), 1996 Jun; 38(6): 683-691.
Impact Factor: 2.425
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Lombardi A, D'Auria G, Saviano M, Maglio O, Nastri F, Quartara L, Pedone C, Pavone V
Bicyclic Peptides As Type I/Type Ii Beta-Turn Scaffolds (512 views)
Biopolym Pept Sci Sect, 1996; 40(5): 505-518.
Impact Factor: 0
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Saviano M, Rossi F, Filizola M, Isernia C, Di Blasio B, Benedetti E, Pedone C, Siemion IZ, Pedyczak A
Bioactive peptides: conformational studies of [Tyr4] cyclolinopeptide (406 views)
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Impact Factor: 2.572
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Mazzeo M, Isernia C, Rossi F, Saviano M, Pedone C, Paolillo L, Benedetti E, Pavone V
Conformational Behaviour of a Cyclolinopeptide A Analogue: Two-dimensional NMR study of cyclo(Pro(1)-Pro-Phe-Phe-Ac(6)c-Ile-ala-Val(8)) (320 views)
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Impact Factor: 1.311
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Gallo P, Saviano M, Rossi F, Pavone V, Pedone C, Ragone R, Stiuso P, Colonna G
SPECIFIC INTERACTION BETWEEN CYCLOPHILIN AND CYCLIC-PEPTIDES (484 views)
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Impact Factor: 2.425
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Saviano M, Rossi F, Filizola M, Di Blasio B, Pedone C
[Aib5, 6-D-Ala8]-cyclolinopeptide A, grown from a benzene/acetonitrile mixture (324 views)
Acta Crystallogr Sect C Cryst Struct Commun (ISSN: 0108-2701), 1995 Apr 15; 51: Pt-Pt.
Impact Factor: 0.459
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Fattorusso R, Morelli G, Lombardi A, Nastri F, maglio O, D'Auria G, Pedone C, Pavone V
Design of metal ion binding peptides (614 views)
Biopolymers (ISSN: 0006-3525, 0006-6352, 0006-3525print), 1995; 37(6): 401-410.
Impact Factor: 2.425
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Pavone V, Lombardi A, Saviano M, Nastri F, Fattorusso R, Maglio O, Isernia C, Paolillo L, Pedone C
β-alanine containing cyclic peptides with turned structure: The 'pseudo type II β-turn. ' VI (463 views)
Biopolymers (ISSN: 0006-3525, 0006-6352, 0006-3525print), 1994 Nov; 34(11): 1517-1526.
Impact Factor: 2.425
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Rossi F, Saviano M, Di Blasio B, Zanotti G, Maione AM, Tancredi T, Pedone C
BIOACTIVE PEPTIDES - SOLID-STATE, SOLUTION AND MOLECULAR-DYNAMICS STUDIES OF A CYCLOLINOPEPTIDE-A RELATED CYSTINYL CYCLOPENTAPEPTIDE (455 views)
Biopolymers (ISSN: 0006-3525, 0006-6352, 0006-3525print), 1994 Feb; 34(2): 273-284.
Impact Factor: 2.425
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Di Blasio B, Lombardi A, D'Auria G, Saviano M, Isernia C, Maglio O, Paolillo L, Pedone C, Pavone V
Beta-Alanine Containing Peptides: Gamma-Turns In Cyclotetrapeptides (560 views)
Biopolymers (ISSN: 0006-3525, 0006-6352, 0006-3525print), 1993 Apr; 31(10): 621-631.
Impact Factor: 2.425
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DIBLASIO B, ROSSI F, BENEDETTI E, PAVONE V, SAVIANO M, PEDONE C, ZANOTTI G, TANCREDI T
BIOACTIVE PEPTIDES - X-RAY AND NMR CONFORMATIONAL STUDY OF [AIB(5, 6)-D-ALA(8)]CYCLOLINOPEPTIDE-A (441 views)
J Am Chem Soc (ISSN: 0002-7863, 0002-2786, 1520-5126), 1992 Oct 7; 114(21): 8277-8283.
Impact Factor: 5.65
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Tancredi T, Benedetti E, Grimaldi M, Pedone C, Rossi F, Saviano M, Temussi PA, Zanotti G
Ion binding of cyclolinopeptide A: An NMR and CD conformational study (633 views)
Biopolymers (ISSN: 0006-3525, 0006-6352, 0006-3525print), 1991 May; 31(6): 761-767.
Impact Factor: 2.425
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Cucinotta V, D'Alessandro F, Impellizzeri G, Pappalardo G, Rizzarelli E, Vecchio G
Cyclopeptide Functionalized beta-Cyclodextrin. A New Class of Potentially Enzyme Mimicking Compound with Two Recognition Sites (267 views)
Chem Commun, 1991; N/D: 293-294.
Impact Factor: 0
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Tancredi T, Zanotti G, Rossi F, Benedetti E, Pedone C, Temussi PA
Comparison of the conformations of cyclolinopeptide A in the solid state and in solution (423 views)
Biopolymers (ISSN: 0006-3525, 0006-6352, 0006-3525print), 1989 Jan; 28(1): 513-523.
Impact Factor: 2.425
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Arena G, Impellizzeri G, Maccarrone G, Pappalardo G, Sciotto D, Rizzarelli E
Non-Covalent Interactions in Cyclopeptide Proton Complex Formation in Aqueous Solution (308 views)
Thermochim Acta, 1989; 154: 97-106.
Impact Factor: 0
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Betocchi S, Cuocolo A, Pace L, Chiariello M, Trimarco B, Alfano B, Ricciardelli B, Salvatore M, Condorelli M
Effects of intravenous verapamil administration on left ventricular diastolic function in systemic hypertension (767 views)
Am J Cardiol (ISSN: 0002-9149), 1987 Mar 1; 59(6): 624-629.
Impact Factor: 2.402
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Ferrara LA, Mancini M, Marotta T, Pasanisi F, Fasano ML
Interference by sulphinpyrazone with the antihypertensive effects of oxprenolol (943 views)
Eur J Clin Pharmacol Springer Verlag (ISSN: 0031-6970, 1432-1041), 1986; 29(6): 717-719.
Impact Factor: 1.219
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Ferrara LA, Strazzullo P, Scillitani A, Mancini M, Gagliardi R
Cross-over study of muzolimine and hydrochlorothiazide-amiloride in hypertensive patients (731 views)
Eur J Clin Pharmacol Springer Verlag (ISSN: 0031-6970, 1432-1041), 1985; 28(3): 241-244.
Impact Factor: 1.219
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Vosa C, Lapenta L, Caianiello G, Esposito V, de LucaL, D'Angelo TS, Salvatore M
Pre- and postoperative Tc 99m scanning in monitoring pulmonary perfusion in the tetralogy of Fallot (701 views)
Ital J Surg Sci (ISSN: 0392-3525), 1984; 14(1): 21-24.
Impact Factor: 0
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57 Records (55 excluding Abstracts).
Total impact factor: 156.967 (152.974 excluding Abstracts).
Total 5 year impact factor: 161.75 (157.083 excluding Abstracts).
Total impact factor: 156.967 (152.974 excluding Abstracts).
Total 5 year impact factor: 161.75 (157.083 excluding Abstracts).
527 views. Last view on Monday 27 March 2023, 11:40:19
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