86,536 research outputs found
Biella. Chiesa della SS. Trinità. Assistenza archeologica ai lavori di manutenzione del sagrato
No full textPyrazolo-isothiazole dioxide: an interesting scaffold for the preparation of peptidomimetics
No full textThere are many examples in literature of peptidomimetics that incorporate a heterocycle scaffold into a peptide, or a peptide-like sequence. The pre-organization of peptide shape, via the introduction of a structural heterocyclic motif that imparts conformational restriction, can enhance binding and hence therapeutic potential.1
Hitherto the standard approach to combine heterocycles and peptides has been to functionalize the side chain or the N/C termini of an amino acid building block with the heterocyclic moiety.2 A few examples have been accomplished in which the heterocycles are part of the peptide backbone itself.3
By the way of a 1,3-dipolar cycloaddition reaction between diazoacetates 2 and the high reactive double bond of the 3-amino isothiazole dioxide partner 1, the adducts 3 are obtained in high yield and complete regioselectivity.
The presence in compounds 3 of the carboxylic substituent and the pyrazole NH group can be exploited for coupling reaction with amino acids. By this way a peptide sequence can be generated characterized by the rigid planar geometry of the heterocyclic system favoring a particular orientation of the growing peptide chain (Figure).
Moreover the presence of the sulfonyl group as well as the NH group at C-3 is of interest. They can behave as hydrogen bond acceptor and donor, respectively, giving raise to interactions with proteins or other potential targets.
The synthesis of model peptidomimetics containing the heterocyclic scaffold, NMR analyses and computational studies are reported
Peptidomimetics based on electrospun nanofibers
No full textElectrospinning is a simple and versatile technique used for the fabrication of continuous micro and nanofibers. This approach is inexpensive, scalable, reliable and mainly used from polymer solutions and polymer melts.
Recent studies have demonstrated that high molar mass polymers are not essential for production of uniform electrospun fibers but that sufficient intermolecular interactions acting as chain entanglements is the primary criterion.
A study on the electrospinnability of short peptide chains containing natural amino acids (Gly, Ala, Leu, Val) together with a heterocyclic scaffold properly functionalized, is here reported
Targeted treatments in advanced renal cell carcinoma: focus on axitinib
No full textElena Verzoni, Paolo Grassi, Isabella Testa, Roberto Iacovelli, Pamela Biondani, Enrico Garanzini , Filippo De Braud, Giuseppe ProcopioDepartment of Medical Oncology 1, Fondazione IRCCS Istituto Nazionale Tumori, Milan, ItalyAbstract: Antiangiogenesis options have evolved rapidly in the last few years, with an increasing number of agents currently approved by the US Food and Drug Administration and European Medicines Agency. Angiogenesis inhibitors have been shown to be very effective for the treatment of metastatic renal cancer cell. Axitinib is a third-generation inhibitor of vascular endothelial growth factor receptor and is currently being developed for the treatment of various malignancies. The pharmacokinetic properties of axitinib may have a selective therapeutic effect, with minimal adverse reactions and enhanced safety. In a large Phase III study of previously treated patients with metastatic renal cell carcinoma, axitinib achieved a longer progression-free survival than sorafenib with an acceptable safety profile and good quality of life. This review focuses on the pharmacology, pharmacokinetics, and clinical activity of axitinib in the current treatment of renal cell carcinoma. The role of axitinib in the adjuvant and/or neoadjuvant setting needs to be evaluated in further clinical trials.Keywords: axitinib, renal cell carcinoma, vascular endothelial growth factor receptor, angiogenesi
Nanofibers from small molecules
No full textElectrospinning is a simple and versatile technique used for the fabrication of continuous micro and nanofibers. This approach is inexpensive, scalable, reliable and mainly used from polymer solutions and polymer melts.
Recent studies have demonstrated that high molar mass polymers are not essential for production of uniform electrospun fibers but that sufficient intermolecular interactions acting as chain entanglements is the primary criterion.
A study on the electrospinnability of non natural small molecules is here reported for the first time
Nanofibers from small molecules
No full textElectrospinning is a simple and versatile technique used for the fabrication of continuous micro and nanofibers. This approach is inexpensive, scalable, reliable and mainly used from polymer solutions and polymer melts.
Recent studies have demonstrated that high molar mass polymers are not essential for production of uniform electrospun fibers but that sufficient intermolecular interactions acting as chain entanglements is the primary criterion.[2]
A study on the electrospinnability of non natural small molecules is here reported for the first time
Livorno Ferraris: alcune considerazioni preliminari a partire dai dati delle campagne di ricognizione 2021 e delle ricerche d’archivio,
No full textanalisi archeologica del territorio dell'attuale Comune di Livorno F
analisi degli Statuti comunal
New evidence of human frequentations in the western Alps: The project "Survey Alta Valsessera (Piedmont-Italy)"
No full textThe Sessera valley is an under-populated Italian alpine valley located in the north-eastern Piedmont (northwest Italy) between the provinces of Biella and Vercelli. We discuss the data obtained during the first and the second year of the project "Survey Alta Val Sessera" held in 2013 and in 2014 under the scientific direction of Soprintendenza Archeologia del Piemonte in collaboration with Associazione Culturale 3P - Progetto Preistoria Piemonte and DocBi - Centro Studi Biellesi that had as its main purpose the identification of new prehistoric human frequentations in the valley. The theoretical scheme employed starts from the one developed for Trentino and the South Tyrolean region (north-eastern Italy) by Broglio and Improta. During the campaigns, surveys in the Sessera and in the neighbouring Dolca valley have been carried out using the patterns of settlement and mobility in the alpine environment developed by Kompatscher and Kompatscher, in order to identify the most interesting areas to investigate. The most important results obtained during the first two survey campaigns indicate that the Sessera valley was occupied by human groups using knapped lithic industries made of local vein quartz. Another important result is the identification of a Late Ancient site located at high altitude (1642 m a.s.l.) along one of the ridge paths investigated. Even if the lithic findings have no diagnostic elements for a precise chronological positioning, the importance of the data obtained consists mainly in having successfully tested a method of research aimed at identifying human frequentations at high altitude in this part of Piedmont, where no comparable research has been carried out until now
Rationale and protocol of RESORT, a randomized, open-label, multicenter phase II study to evaluate the efficacy of sorafenib in patients with advanced renal cell carcinoma after radical resection of the metastases
No full textThe introduction of targeted agents did not totally resolve the approach to the treatment of metastatic renal cell carcinoma (mRCC) because complete response is rarely achieved. Recent findings seem to indicate that metastasectomy may improve survival. The RESORT study was designed to evaluate the additional clinical benefit of metastasectomy followed by sorafenib in a population of mRCC patients. With the aim of evaluating time to recurrence, 132 patients with mRCC who underwent radical resection of metastases at the time of recurrence after nephrectomy will be randomized to receive either sorafenib or best supportive care. Targeted treatment will be administered for up to 52 weeks or discontinued in the case of disease recurrence or unacceptable toxicity. Patients will be followed for a period of 36 months
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