A new therapeutic approach to erectile dysfunction: urotensin-II receptor high affinity agonist ligands (529 views)
Asian J Androl (ISSN: 1008-682x), 2015 Jan; 17(1): 81-85.
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Paper type: Journal Article,
Impact factor: 2.644, 5-year impact factor: 2.579
Url: http://www.scopus.com/inward/record.url?eid=2-s2.0-84920484346&partnerID=40&md5=aa9aafb6905edf4e905afcb91f2eef47
Keywords: Erectile Dysfunction, Intracavernous Pressure, Urotensin-Ii, Urotensin-Ii Ligands, Cyclopeptide, Unclassified Drug, Upg 84, Urotensin Ii, Agonist, Animal Cell, Animal Experiment, Animal Model, Article, Binding Affinity, Controlled Study, Dose Response, Drug Effect, Drug Efficacy, Drug Receptor Binding, Nonhuman,
Affiliations:
*** IBB - CNR ***
Department of Pharmacy, University of Naples, Federico II, Via D. Montesano 49, Naples, Italy
Interdepartmental Centre for Sexual Medicine, University of Naples, Federico II, Via S. Pansini 5, Naples, Italy
Department of Neurosciences, Human Reproduction and Odontostomatology, University of Naples Federico II, Via S. Pansini 5, Naples, Italy
References:
Not available.
Asian J Androl (ISSN: 1008-682x), 2015 Jan; 17(1): 81-85.
Export to BibTeX Export to EndNote
Paper type: Journal Article,
Impact factor: 2.644, 5-year impact factor: 2.579
Url: http://www.scopus.com/inward/record.url?eid=2-s2.0-84920484346&partnerID=40&md5=aa9aafb6905edf4e905afcb91f2eef47
Keywords: Erectile Dysfunction, Intracavernous Pressure, Urotensin-Ii, Urotensin-Ii Ligands, Cyclopeptide, Unclassified Drug, Upg 84, Urotensin Ii, Agonist, Animal Cell, Animal Experiment, Animal Model, Article, Binding Affinity, Controlled Study, Dose Response, Drug Effect, Drug Efficacy, Drug Receptor Binding, Nonhuman,
Affiliations:
*** IBB - CNR ***
Department of Pharmacy, University of Naples, Federico II, Via D. Montesano 49, Naples, Italy
Interdepartmental Centre for Sexual Medicine, University of Naples, Federico II, Via S. Pansini 5, Naples, Italy
Department of Neurosciences, Human Reproduction and Odontostomatology, University of Naples Federico II, Via S. Pansini 5, Naples, Italy
References:
Not available.
A new therapeutic approach to erectile dysfunction: urotensin-II receptor high affinity agonist ligands
Urotensin-II (U-II) is a cyclic peptide that acts through a G protein-coupled receptor (urotensin-II receptor [UTR]) mainly involved in cardiovascular function in humans. The urotensinergic system is also implicated in the urogenital tract. Indeed, U-II relaxes human corpus cavernosum strips and causes an increase in intracavernous pressure (ICP) in rats. In light of this, the U-II/UTR pathway can be considered a new target for the treatment of erectile dysfunction. On this hypothesis, herein we report on two new UTR high affinity-agonists, P5U (H-Asp-c[Pen-Phe-Trp-Lys-Tyr-Cys]-Val-OH) and UPG84(H-Asp-c[Pen-Phe-DTrp-Orn-(pNH 2 ) Phe-Cys]-Val-OH). The effects of P5U and UPG84 were each compared separately with U-II by monitoring the ICP in anesthetized rats. Intracavernous injection of U-II (0.03-1 nmol), P5U (0.03-1 nmol) or UPG84 (0.03-1 nmol) caused an increase in ICP. P5U, in particular, elicited a significant increase in ICP as compared to U-II. The observed effect by using P5U at a dose of 0.1 nmol per rat was comparable to the effect elicited by U-II at a dose of 0.3 nmol. Moreover, UPG84 at the lowest dose (0.03 nmol) showed an effect similar to the highest dose of U-II (1 nmol). Furthermore, UPG84 was found to be more effective than P5U. Indeed, while the lowest dose of P5U (0.03 nmol) did not affect the ICP, UPG84, at the same dose, induced a prominent penile erection in rat. These compounds did not modify the blood pressure, which indicates a good safety profile. In conclusion, UPG84 and P5U may open new perspectives for the management of erectile dysfunction.
Urotensin-II (U-II) is a cyclic peptide that acts through a G protein-coupled receptor (urotensin-II receptor [UTR]) mainly involved in cardiovascular function in humans. The urotensinergic system is also implicated in the urogenital tract. Indeed, U-II relaxes human corpus cavernosum strips and causes an increase in intracavernous pressure (ICP) in rats. In light of this, the U-II/UTR pathway can be considered a new target for the treatment of erectile dysfunction. On this hypothesis, herein we report on two new UTR high affinity-agonists, P5U (H-Asp-c[Pen-Phe-Trp-Lys-Tyr-Cys]-Val-OH) and UPG84(H-Asp-c[Pen-Phe-DTrp-Orn-(pNH 2 ) Phe-Cys]-Val-OH). The effects of P5U and UPG84 were each compared separately with U-II by monitoring the ICP in anesthetized rats. Intracavernous injection of U-II (0.03-1 nmol), P5U (0.03-1 nmol) or UPG84 (0.03-1 nmol) caused an increase in ICP. P5U, in particular, elicited a significant increase in ICP as compared to U-II. The observed effect by using P5U at a dose of 0.1 nmol per rat was comparable to the effect elicited by U-II at a dose of 0.3 nmol. Moreover, UPG84 at the lowest dose (0.03 nmol) showed an effect similar to the highest dose of U-II (1 nmol). Furthermore, UPG84 was found to be more effective than P5U. Indeed, while the lowest dose of P5U (0.03 nmol) did not affect the ICP, UPG84, at the same dose, induced a prominent penile erection in rat. These compounds did not modify the blood pressure, which indicates a good safety profile. In conclusion, UPG84 and P5U may open new perspectives for the management of erectile dysfunction.
A new therapeutic approach to erectile dysfunction: urotensin-II receptor high affinity agonist ligands
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A new therapeutic approach to erectile dysfunction: urotensin-II receptor high affinity agonist ligands
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View Export to BibTeX Export to EndNote
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Impact Factor: 5.447
View Export to BibTeX Export to EndNote
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Impact Factor: 2.734
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De Rosa L, Diana D, Basile A, Russomanno A, Isernia C, Turco MC, Fattorusso R, D'Andrea LD
* Design, Structural And Biological Characterization Of A Vegf Inhibitor Beta-Hairpin-Constrained Peptide (614 views)
Eur J Med Chem (ISSN: 0223-5234, 1768-3254, 0223-5234linking), 2014; 73: 210-216.
Impact Factor: 3.447
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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
* Preclinical Development of a Novel Class of CXCR4 Antagonist Impairing Solid Tumors Growth and Metastases (586 views)
Plosone (ISSN: 1932-6203, 1932-6203electronic, 1932-6203linking), 2013 Sep 13; 8(9): N/D-N/D.
Impact Factor: 3.534
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Carotenuto A, Auriemma L, Merlino F, Limatola A, Campiglia P, Gomez-monterrey I, Di Villa Bianca R, Brancaccio D, Santicioli P, Meini S, Maggi CA, Novellino E, Grieco P
* New insight into the binding mode of peptides at urotensin-II receptor by Trp-constrained analogues of P5U and urantide (606 views)
J Pept Sci (ISSN: 1075-2617, 1099-1387electronic, 1075-2617linking), 2013 May; 19(5): 293-300.
Impact Factor: 1.862
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Carotenuto A, Cipolletta E, Gomez-Monterrey I, Sala M, Vernieri E, Limatola A, Bertamino A, Musella S, Sorriento D, Grieco P, Trimarco B, Novellino E, Iaccarino G, Campiglia P
* Design, synthesis and efficacy of novel G protein-coupled receptor kinase 2 inhibitors (711 views)
Eur J Med Chem (ISSN: 0223-5234, 1768-3254, 1768-3254electronic), 2013; 69: 384-392.
Impact Factor: 3.432
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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 (611 views)
Int J Pept Res Ther (ISSN: 1573-3149, 0929-5666), 2011 Mar; 17(1): 39-45.
Impact Factor: 0.986
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Accardo A, Morisco A, Gianolio E, Tesauro D, Mangiapia G, Radulescu A, Brandt A, Morelli G
* Nanoparticles containing octreotide peptides and gadolinium complexes for MRI applications (591 views)
J Pept Sci (ISSN: 1075-2617, 1099-1387, 1075-2617print), 2011 Feb; 17(2): 154-162.
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
* Evaluation of the anti-angiogenic properties of the new selective alphaVbeta3 integrin antagonist RGDechiHCit (598 views)
J Transl Med (ISSN: 1479-5876electronic, 1479-5876linking), 2011 Jan 13; 9: 7-7.
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 (2326 views)
Chem Biol Drug Des (ISSN: 1747-0277, 1747-0285), 2011 Jan; 77(1): 12-19.
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
* Biochemical and Structural Analysis of the Binding Determinants of a Vascular Endothelial Growth Factor Receptor Peptidic Antagonist (668 views)
J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2010 Jun 10; 53(11): 4428-4440.
Impact Factor: 5.207
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Kaczmarek K, Farina B, Zubrzak P, Jankowski S, Zimecki M, Suder P, Benedetti E, Fattorusso R, Saviano M, Zabrocki J
* Synthesis, conformational analysis and immunological activity of β3Phe-substituted Cyclolinopeptide A analogues (592 views)
J Pept Sci (ISSN: 1075-2617, 1099-1387, 1075-2617print), 2009 Mar; 15(3): 166-174.
Impact Factor: 1.807
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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 (511 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 (685 views)
Biochemistry (ISSN: 0006-2960, 1520-4995, 1520-4995electronic), 2006 Apr 11; 45(14): 4491-4501.
Impact Factor: 3.633
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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 (629 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 (442 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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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 (530 views)
Chembiochem (ISSN: 1439-7633, 1439-4227, 1439-7633electronic), 2003 Nov 7; 4(11): 1176-1187.
Impact Factor: 3.992
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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 (522 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 (520 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 (470 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) (1200 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 (628 views)
Bioorg Med Chem Lett Bioorganic And Medicinal Chemistry Letters (ISSN: 0960-894xprint, 0960-894xlinking), 1998 May 19; 8(10): 1153-1156.
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 (582 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 (519 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 (420 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 (538 views)
Biopolymers (ISSN: 0006-3525, 0006-6352, 0006-3525print), 1996 Jun; 38(6): 683-691.
Impact Factor: 2.425
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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 (535 views)
Biopolymers (ISSN: 0006-3525print, 0006-3525linking, 1097-0282electronic), 1995 Oct; 26(12): 453-460.
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)) (384 views)
J Pept Sci (ISSN: 1075-2617, 1099-1387, 1075-2617print), 1995 Sep; 1(5): 330-340.
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 (533 views)
Biopolymers (ISSN: 0006-3525, 0006-6352, 0006-3525print), 1995 Sep; 36(3): 273-281.
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 (391 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 (731 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 (680 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 (595 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 (649 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 (513 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 (719 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 (325 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 (479 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 (334 views)
Thermochim Acta, 1989; 154: 97-106.
Impact Factor: 0
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43 Records (40 excluding Abstracts).
Total impact factor: 116.344 (110.4 excluding Abstracts).
Total 5 year impact factor: 123.887 (117.513 excluding Abstracts).
Total impact factor: 116.344 (110.4 excluding Abstracts).
Total 5 year impact factor: 123.887 (117.513 excluding Abstracts).
529 views. Last view on Sunday 18 August 2024, 8:34:52
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