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......
Role of A β and the α 7 nicotinic acetylcholine receptor in regulating synaptic plasticity in Alzheimer's disease
Letters in Peptide Science - Tập 10 - Trang 401-404 - 2003
Alzheimer's disease (AD) is caused by the accumulation of β-amyloid protein (Aβ) in the brain. The aggregation of β-amyloid protein to higher molecular weight fibrillar forms is also considered to be an important step in the pathogenesis of the disease. The memory problems associated with AD are likely to be caused by changes in synaptic plasticity. Recent studies suggest that Aβ binds to the α 7 ......
New antitumor leads from a peptidomimetic library
Letters in Peptide Science - - 1999
A parallel combinatorial library of over 1600 compounds has been designed and synthesized for the development of new potential peptidomimetic protein tyrosine kinase (PTK) inhibitor leads. These peptidomimetic molecules are aimed at intervening with the substrate binding site of the pp60c−src enzyme. The new structures were based on kown PTK inhibtors with at least two variously substituted aromat......
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......
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