SUPRAMOLECULAR AGGREGATES COMPRISING MALEIMIDO CORES

The invention relates to a supramolecular aggregate of formula (VI) wherein A is an active substance, and X1, X2, X3 and X4, independently to each other, are a moiety of Formula (I) containing a maleimido functionalization 5 and at least one among X1, X2, X3 and X4 is present in Formula (VI). In a preferred embodiment the maleimido-funzionalized core is PWT2. The supramolecular aggregate can be used in the field of drugs, vaccines, as ligands for GPCR, i.e. agonists as well as antagonist, as antibiotics and as diagnostics eventually in complex with 10 radionuclides

Supramolecular aggregates comprising maleimido cores

The invention relates to a supramolecular aggregate of formula (VI) wherein A is an active substance, and X1, X2, X3 and X4, independently to each other, are a moiety of Formula (I) containing a maleimido functionalization and at least one among X1, X2, X3 and X4 is present in Formula (VI). In a preferred embodiment the maleimido-funzionalized core is PWT2. The supra-molecular aggregate can be used in the field of drugs, vaccines, as ligands for GPCR, i.e. agonists as well as antagonist, as antibiotics and as diagnostics eventually in complex with radionuclides

SUPRAMOLECULAR AGGREGATES COMPRISING MALEIMIDO CORES

The invention relates to a supramolecular aggregate of formula (VI) wherein A is an active substance, and X1, X2, X3 and X4, independently to each other, are a moiety of Formula (I) containing a maleimido functionalization 5 and at least one among X1, X2, X3 and X4 is present in Formula (VI). In a preferred embodiment the maleimido-funzionalized core is PWT2. The supramolecular aggregate can be used in the field of drugs, vaccines, as ligands for GPCR, i.e. agonists as well as antagonist, as antibiotics and as diagnostics eventually in complex with 10 radionuclides

The effects of dermorphin on the endocrine system in man

This paper summarizes the results of our recent studies in a group of healthy subjects on the endocrine effects of the new potent opioid peptide, dermorphin (H-Tyr-D-Ala-Phe-Gly-Tyr-Pro-Ser-NH2), originally isolated from amphibian skin. Intravenous infusion (5.5 μg/kg/min for 30 min) of dermorphin (D) significantly increased plasma levels of prolactin (PRL), growth hormone (GH), thyrotropin (TSH) and renin activity (PRA), but decreased plasma levels of cortisol. D produced a small decrease in ACTH, and a small increase in plasma aldosterone. Pretreatment with the opioid receptor antagonist naloxone (N) suppressed the PRL and TSH response to D, blunted the D-induced GH and PRA increase, and completely prevented the D-induced plasma cortisol decrease, but enhanced plasma cortisol and ACTH levels. These data indicate that the action of D is mediated through opioid receptors, and are consistent with the conclusion that: (1) D, a new opioid peptide, can stimulate PRL, GH, and TSH release in humans; (2) D increases PRA levels, perhaps via activation of the sympathetic nervous system, providing evidence that opioid peptides may exert an influence on renin secretion; (3) D suppresses plasma cortisol levels, by affecting ACTH secretion, corroborating previous observations that opioid peptides might affect the function of the pituitary-adrenocortical axis. © 1985

Peptides and proteins in a confined environment: NMR spectra at natural isotopic abundance

Confinement of proteins and peptides in a small inert space mimics the natural environment of the cell, allowing structural studies in conditions that stabilize folded conformations. We have previously shown that confinement in polyacrylamide gels (PAGs) is sufficient to induce a change in the viscosity of the aqueous solution without changing the composition and temperature of the solvent. The main limitation of a PAG to run NMR experiments in a confined environment is the need for labelling the peptides. Here we report the use of the agarose gel to run the NMR spectra of proteins and peptides. We show that agarose gels are completely transparent in NMR experiments, relieving the need for labelling. Although it is necessary to expose biomolecules to fairly high temperatures during sample preparation, we believe that this is not generally an obstacle to the study of peptides, and found that the method is also compatible with temperature-resistant proteins. The mesh of agarose gels is too wide for direct effects of confinement on the stability of proteins but confinement can be easily exploited to interact the proteins with other reagents, including crowding macromolecules that can eventually lead to fold stabilization. The use of these gels is ideally suited for low-temperature studies; we show that a very flexible peptide at subzero temperatures is stabilized into a well-folded conformation

Supramolecular aggregates comprising maleimido cores

The invention relates to a supramolecular aggregate of formula (VI) wherein A is an active substance, and X1, X2, X3 and X4, independently to each other, are a moiety of Formula (I) containing a maleimido functionalization and at least one among X1, X2, X3 and X4 is present in Formula (VI). In a preferred embodiment the maleimido-funzionalized core is PWT2. The supra-molecular aggregate can be used in the field of drugs, vaccines, as ligands for GPCR, i.e. agonists as well as antagonist, as antibiotics and as diagnostics eventually in complex with radionuclides

Effect of somatostatin on growth hormone and prolactin response to dermorphin in man

Effect of somatostatin on growth hormone and prolactin response to dermorphin in ma

AGONISTI PIENI E PARZIALI ED ANTAGONISTI DEL RECETTORE PER NOCICETTINA/ORFANINA FQ AD ELEVATA POTENZA”

La prsente invenzione riguarda peptidi analoghi di nocicettina/orfanina FQ (N/OFQ) in grado di modulare l'attività del recettore del peptide N/OFQ (recettore NOP), composizioni farmaceutiche che li contengono e loro impiego nel trattamento di dsfunzioni, condizioni o stati patologici in cui è coinvolto lo stesso recettore

Synthesis and antimicrobial activity of dermaseptin S1 analogues

Dermaseptins are peptides found in the skin secretions of Phyllomedusinae frogs. These peptides exert lytic action on some microorganisms without substantial haemolysis. In an attempt to understand the antimicrobial activity of these peptides we designed several dermaseptin S1 (ALWKTMLKKLGTMALHAGKAALGAAADTISQGTQ) (DS1) analogues. All peptides were tested on the growth of prokaryotic (Grampositive and Gram-negative bacteria) and eukaryotic (the yeast Candida albicans and the protozoon Leishmania major) organisms. Our data showed a dose-dependent killing effect by most DS1 derivatives. Maximal antibacterial activity was displayed by a 16-mer peptide that was more active than native DS1

Identificazione di un agonista parziale del recettore per il neuropeptide S

La presente invenzione riguarda la sintesi di una molecola di natura peptidica in grado di modulare l’attività del recettore per il neuropeptide S, le composizioni farmaceutiche che la contengono e il loro impiego nel trattamento di disfunzioni, condizioni o stati patologici in cui lo stesso recettore è coinvolto