28 Result(s)
within
Jean Martinez
Life Sciences
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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
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
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
Microwave-assisted Solid Phase Peptide Synthesis on High Loaded Resins
Kinetic of diffusion of reactants from the solution into the resin beads is a key factor of the efficiency of reaction in solid phase synthesis. We demonstrated in this paper that stirring is required to obtai...
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Article
Solid Phase Synthesis of a Hydroxypyrrolidine Derivative and its Use in Solid Phase Peptide Synthesis as Constrained Statine Mimic
As part of our efforts to design constrained peptide mimics and introduce them in peptide sequences, we set up the synthesis of racemic N-Fmoc protected hydroxypyrrolidine by reduction of the corresponding oxo...
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Article
A Novel Route to Pseudoproline (ΨH,HPro)-Containing Dipeptides Building Blocks
In view of the synthetic and biological interest of pseudoproline (ΨR,RPro)-containing peptides, we have investigated a new strategy to these target compounds, taking into account the existence of the well-known ...
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Protocol
Fundamentals of Modern Peptide Synthesis
The purpose of this chapter is to delineate strategic considerations and provide practical procedures to enable non-experts to synthesize peptides with a reasonable chance of success. This chapter focuses on F...
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Protocol
Automated vs Manual Profiling of Peptide Libraries by Mass Spectrometry
Combinatorial chemistry (1–7) has evolved from the synthesis of very large mixtures to the preparation of collections of isolated compounds by parallel syntheses. Peptides constitute ideal materials because their...
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Protocol
Quality Control of Solid-Phase Synthesis by Mass Spectrometry
Combinatorial chemistry (1–7) has drastically modified the drug discovery process by allowing the rapid simultaneous preparation of numerous organic molecules to feed bioassays. Most of the time, syntheses are ca...
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Chapter
Solid phase synthesis of peptide aldehydes
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Chapter
Synthesis and in Vivo pharmacological profile of dimeric HOE 140 bradykinin antagonists
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Chapter
A Novel Series of Growth Hormone Secretagogues
Growth Hormone (GH), secreted by the pituitary gland, acts directly or indirectly on the peripheral organs by stimulating the synthesis of growth factors (insulin-like growth factor-I or IGF-I). The direct act...
