Letters in Peptide Science
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Base-induced side reactions in Fmoc-solid phase peptide synthesis:Minimization by use of piperazine as Nα-deprotectionreagent
Letters in Peptide Science - Tập 7 - Trang 107-112 - 2000
Base-induced aspartimide (cyclic imide) and subsequentbase adduct formation in the Fmoc-solid phasesynthesis of sensitive sequences are serious sidereactions that are difficult to both anticipate andcontrol. The effect of extended treatment ofpiperazine as Nα-Fmoc deprotection reagenton two sensitive peptide sequences was examined. Forcomparison, other bases were also investigated,including piperi......
Novel naphthoquinonyl derivatives: Potential structural components for the synthesis of cytotoxic peptides
Letters in Peptide Science - Tập 3 - Trang 263-274 - 1996
Syntheses and physicochemical properties are described of several novel naphthoquinonyl amino acid derivatives, which are potential components in cytotoxic peptide conjugates. These compounds include N
ε- and N
α-naphthoquinonyl derivatives of lysine as well as N-naphthoquinonyl-carboxylic derivatives. The former class of compounds can be employed as building blocks in a stepwise peptide synthesis......
Use of thiazolidine-mediated ligation for site specific biotinylation of mouse EGF for biosensor immobilisation
Letters in Peptide Science - Tập 8 - Trang 211-220 - 2001
Biosensors provide a sophisticated and discriminating means of probing biomolecular interactions. Specific ligands such as peptides and proteins can be immobilized onto sensor surfaces by a number of means including covalent attachment via amine, thiol or aldehyde chemistry, capture via biotin-avidin interaction or the use of specific tags. We have devised a simple chemoselective ligation method t......
Evaluation of strategies for ‘one-pot’ deprotection, cleavage and disulfide bond formation in the preparation of cystine-containing peptides
Letters in Peptide Science - Tập 3 - Trang 327-332 - 1997
Oxytocin, a nonapeptide amide, was synthesized on a PEGA-resin using the Fmoc-tBu strategy. The sulfhydryl groups of the two cysteine residues were protected with trityl groups. Different oxidation reagents such as DMSO, I2 and thallium (III) trifluoroacetate mixed with TFA were evaluated in order to obtain oxytocin in a one-pot reaction. The mixture of TFA and DMSO (5:1) in which oxytocin was for......
Cytotoxic Peptides: Naphthoquinonyl Derivatives of Luteinizing Hormone-Releasing Hormone
Letters in Peptide Science - Tập 5 - Trang 421-427 - 1998
In an attempt to produce efficient cytotoxic derivatives of luteinizing hormone-releasing hormone (LH-RH), two novel 1,4-naphthoquinone derivatives of [D-Lys6]-LH-RH were synthesized primarily by solid-phase peptide synthesis, in good yield and high purity. The ability of each analog to produce reactive oxygen species using enzymatic reduction, i.e. NADPH-cytochrome P-450 reductase, was evaluated ......
A method for the facile solid-phase synthesis of gramicidin S and its analogs
Letters in Peptide Science - Tập 3 - Trang 53-60 - 1996
A simple method is described for the facile synthesis of gramicidin S and six other analogs, using standard solidphase synthetic technology and a single solution-phase cyclization step. The peptides were purified to homogeneity and characterized by plasma desorption time-of-flight mass spectrometry and NMR spectroscopy. Complete 1H NMR assignments for all seven peptides (in aqueous solution) are p......
Design of specific antagonists of the fibrinogen receptor
Letters in Peptide Science - Tập 4 - Trang 463-466 - 1997
The aim of this work was to elucidate, using molecular modeling, structural and electrostatic common parameters of several selective fibrinogen receptor antagonists. From this theoretical pattern, we are currently designing and synthesizing original non-peptidic and selective carbohydrate-based antagonists of the fibrinogen receptor.
Computational binding assays of antigenic peptides
Letters in Peptide Science - Tập 6 - Trang 313-324 - 1999
Computer models can be combined with laboratory experiments for the efficient determination of (i) peptides that bind MHC molecules and (ii) T-cell epitopes. For maximum benefit, the use of computer models must be treated as experiments analogous to standard laboratory procedures. This requires the definition of standards and experimental protocols for model application. We describe the requiremen......
p56lck SH2 domain binding motifs from bead binding screening of peptide libraries containing phosphotyrosine surrogates
Letters in Peptide Science - Tập 6 - Trang 335-341 - 1999
Phosphorylation reactions are key meditors in a variety of biochemical signal processes. Research into the selective inhibition of protein tyrosine kinases to generate anticancer agents has madeO-phosphotyrosyl analogues important pharmacological tools. The simple procedures reported here involving the formation of interative peptide libraries together with the development of a selective and sensi......
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