Investigation of the Best Conditions to Obtain c(RGDfK) Peptide on Solid Phase(644 views) Saviano M, Del Gatto A, De Simone M, De Paola I, Saviano M, Zaccaro L
Int J Pept Res Ther (ISSN: 1573-3149, 0929-5666), 2011 Mar; 17(1): 39-45.
Keywords: Optimisation, Pharmaceuticals, Reaction, Synthesis, Cyclo(arginylglycylaspartylphenylalanyllysine), Cyclopeptide, Unclassified Drug, Article, Chemical Reaction, Dimerization, Drug Screening, Drug Synthesis, Peptide Synthesis, Process Optimization, Protein Modification, Solid Phase Synthesis, Cyclo (arginylglycylaspartylphenylalanyllysine),
Affiliations: *** IBB - CNR ***
Istituto di Biostrutture e Bioimmagini-CNR, Via Mezzocannone 16, Naples 80134, Italy
Dipartimento Delle Scienze Biologiche, Università Degli Studi di Napoli Federico II, Via Mezzocannone 16, Naples 80134, Italy
Istituto di Cristallografia-CNR, Via Giovanni Amendola 122/O, Bari 70126, Italy
References: Not available.
Investigation of the Best Conditions to Obtain c(RGDfK) Peptide on Solid Phase
The cyclic pentapeptide c(RGDfK) is a high affinity ligand of alphaVbeta3 integrin. It was an analog of Cilengitide (EMD 121974) developed to be employed as tracer for cancer diagnosis and therapy by functionalisation of its Lys side-chain. Solution-phase and solid-phase synthetic approaches were previously reported. In the attempt to improve solid-phase synthesis of the cyclopeptide circumventing cyclodimerisation reactions, a systematic study of the synthetic conditions was performed, evaluating and optimising parameters directly involved in the ring closure step. The three-dimensional orthogonal solid-phase strategy developed in this study yields the desired c(RGDfK) peptide with no cyclodimerisation by-products. The protocols described allow the modification of the peptide directly on the solid support in order to obtain novel derivatives for biomedical applications.
Investigation of the Best Conditions to Obtain c(RGDfK) Peptide on Solid Phase
Petraglia F, Singh AA, Carafa V, Nebbioso A, Conte M, Scisciola L, Valente S, Baldi A, Mandoli A, Petrizzi VB, Ingenito C, De Falco S, Cicatiello V, Apicella I, Janssen-megens EM, Kim B, Yi G, Logie C, Heath S, Ruvo M, Wierenga ATJ, Flicek P, Yaspo ML, Della Valle V, Bernard O, Tomassi S, Novellino E, Feoli A, Sbardella G, Gut I, Vellenga E, Stunnenberg HG, Mai A, Martens JHA, Altucci L * Combined HAT/EZH2 modulation leads to cancer-selective cell death(458 views) Oncotarget (ISSN: 1949-2553electronic, 1949-2553linking), 2018 May 22; 9(39): 25630-25646. Impact Factor:5.008 ViewExport to BibTeXExport to EndNote
Vitiello M, Finamore E, Falanga A, Raieta K, Cantisani M, Galdiero F, Pedone C, Galdiero M, Galdiero S * Fusion in Coq(600 views) Lecture Notes In Computer Science (ISSN: 0302-9743, 0302-974335404636319783540463634, 0302-974335402975459783540297543), 2001; 2178LNCS: 583-596. Impact Factor:0.415 ViewExport to BibTeXExport to EndNote