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Article
Open AccessCombining adoptive NK cell infusion with a dopamine-releasing peptide reduces senescent cells in aged mice
Aging inducing the development of senescent cells (SNCs) in various tissues is considered as the main cause of the age-related diseases. Senotherapy has become a promising anti-aging therapy. However, the effe...
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Protocol
Hybrid Silylated Peptides for the Design of Bio-functionalized Materials
Hybrid silylated peptides are useful starting compounds for the design of functionalized materials. Indeed, silylated peptides may react in soft conditions with other silylated species through Si–O–Si bonds, o...
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Article
Open AccessGrowth hormone secretagogues hexarelin and JMV2894 protect skeletal muscle from mitochondrial damages in a rat model of cisplatin-induced cachexia
Chemotherapy can cause cachexia, which consists of weight loss associated with muscle atrophy. The exact mechanisms underlying this skeletal muscle toxicity are largely unknown and co-therapies to attenuate ch...
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Article
JMV2894, a novel growth hormone secretagogue, accelerates body mass recovery in an experimental model of cachexia
Oncologic patients subjected to chemotherapy frequently present aphagia, malnutrition, and cachexia. The purpose of this study was to investigate whether selected growth hormone secretagogues including hexarel...
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Chapter
Silaproline, a Silicon-Containing Proline Surrogate
Silaproline (Sip) is a proline analogue that exhibits similar conformational properties as the natural amino acid in peptides. Moreover, the presence of a dimethylsilyl group confers to silaproline higher lipo...
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Article
Stereoselective synthesis of unsaturated α-amino acids
Stereoselective synthesis of unsaturated α-amino acids was performed by asymmetric alkylation. Two methods were investigated and their enantiomeric excess measured and compared. The first route consisted of an...
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Article
Heating and microwave assisted SPPS of C-terminal acid peptides on trityl resin: the truth behind the yield
Despite correct purity of crude peptides prepared on trityl resin by Fmoc/tBu microwave assisted solid phase peptide synthesis, surprisingly, lower yields than those expected were obtained while preparing C-te...
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Article
Synthesis and analgesic effects of novel β2-tryptophan hexapeptide analogs
Aiming to develop more potent analgesic substances a new series of hexapeptides containing β2-tryptophan analogues was synthesized. The Trp in position 4 and 5, respectively in Ac-Arg-Phe-Met-Trp-Met-Lys-NH2 (opi...
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Article
Supported oligomethionine sulfoxide and Ellman’s reagent for cysteine bridges formation
A large number of bioactive peptides are cyclized through a disulfide bridge. This structural feature is very important for both bioactivity and stability. The oxidation of cysteine side chains is challenging ...
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Article
The 1,2,4-triazole as a scaffold for the design of ghrelin receptor ligands: development of JMV 2959, a potent antagonist
Ghrelin is a 28-residue peptide acylated with an n-octanoyl group on the Ser 3 residue, predominantly produced by the stomach. Ghrelin displays strong growth hormone (GH) releasing activity, which is mediated by ...
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Article
Cytotoxic activity of new racemic and optically active N-phosphonoalkyl bicyclic β-amino acids against human malignant cell lines
The cytotoxic effects of novel racemic and optically active constrained N-phosphonoalkyl bicyclic β-amino acids were tested against a panel of human tumor cell lines. All of the compounds investigated exhibited d...
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Article
New 1,3-amino alcohols derived from enantiopure bridgehead β-aminobicyclo[2.2.2]oct-5-ene-2-carboxylic acids
Constrained enantiopure bicyclic β-amino acids derived from the asymmetric Diels–Alder reaction of the (R)-benzyl-4-(3-acryloyloxy-4,4-dimethyl-2-oxopyrrolidin-1-yl)-benzoate and the 1-(benzyloxycarbonylamino)cyc...
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Article
Chemoenzymatic routes to enantiomerically pure 2-azatyrosine and 2-, 3- and 4-pyridylalanine derivatives
Enantiomerically pure 2-, 3- or 4-pyridylalanine (pya) and 2-azatyrosine (azatyr) are known to present various biological activities. After incorporation into appropriate peptide sequences, these heterocyclic ...
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Article
Occurrence of C-Terminal Residue Exclusion in Peptide Fragmentation by ESI and MALDI Tandem Mass Spectrometry
By screening a data set of 392 synthetic peptides MS/MS spectra, we found that a known C-terminal rearrangement was unexpectedly frequently occurring from monoprotonated molecular ions in both ESI and MALDI ta...
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Article
Synthesis of C5-tetrazole derivatives of 2-amino-adipic acid displaying NMDA glutamate receptor antagonism
Five derivatives of 2-amino-adipic acid bearing a tetrazole-substituted in C5 position were synthesized. These compounds displayed selective antagonism towards N-methyl-d-aspartate (NMDA) receptors compared with ...
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Article
Sequencing Lys-N Proteolytic Peptides by ESI and MALDI Tandem Mass Spectrometry
In this study, we explored the MS/MS behavior of various synthetic peptides that possess a lysine residue at the N-terminal position. These peptides were designed to mimic peptides produced upon proteolysis by...
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Article
Open AccessEvidence for a role of NTS2 receptors in the modulation of tonic pain sensitivity
Central neurotensin (NT) administration results in a naloxone-insensitive antinociceptive response in animal models of acute and persistent pain. Both NTS1 and NTS2 receptors were shown to be required for diff...
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Chapter and Conference Paper
Thieno[3,2-e]diazepinediones and 3-Thienylimidazolidinediones Syntheses: Regio-Controlled Ring Opening of Thiaisatoic Anhydride by α-Amino Acids.
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Chapter and Conference Paper
Solid-phase synthesis of dipeptidic and pseudo-dipeptidic potential NOS inhibitors through a side-chain anchoring approach
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Chapter and Conference Paper
Synthesis and Biological Activity of Nicotianamine and Analogues
