- Cotton functionalized with peptides: Characterization and synthetic methods
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Three approaches for the chemical ligation of peptides to cotton fibers are described and compared. This investigation was encouraged by the need to create peptide-decorated natural textiles, furnished with useful properties (e.g. antimicrobial activity). IR absorption spectroscopy is proved to be an easy and fast method to check the covalent anchorage of a peptide to cotton, whereas for a quantitative determination, a UV absorption method was employed. We also analyzed the usefulness of electron paramagnetic resonance spectroscopy to characterize our peptide-cotton conjugates. Copyright 2014 European Peptide Society and John Wiley & Sons, Ltd. In this work, three approaches for the chemical ligation of peptides and dendrimers to cotton fibers are described and compared. Characterization of the peptide bound to the cotton was achieved by means of IR absorption, UV, and electron paramagnetic resonance spectroscopies. Copyright
- Orlandin, Andrea,Formaggio, Fernando,Toffoletti, Antonio,Peggion, Cristina
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- Facile access to modified and functionalized PNAs through Ugi-based solid phase oligomerization
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Peptide nucleic acids (PNAs) derivatized with functional molecules are increasingly used in diverse biosupramolecular applications. PNAs have proven to be highly tolerant to modifications and different applications benefit from the use of modified PNAs, in particular modifications at the γ position. Herein we report simple protocols to access modified PNAs from iterative Ugi couplings which allow modular modifications at the α, β or γ position of the PNA backbone from simple starting materials. We demonstrate the utility of the method with the synthesis of several bioactive small molecules (a peptide ligand, a kinase inhibitor and a glycan)-PNA conjugates.
- Saarbach, Jacques,Masi, Daniela,Zambaldo, Claudio,Winssinger, Nicolas
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- Maintaining homogeneity during a sol-gel transition by an autocatalytic enzyme reaction
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Kinetic control over supramolecular gelation by increasing the pH can be achieved using an enzymatic reaction. This method allows us to produce homogeneous hydrogels with superior and improved mechanical properties as compared to gels obtained from simple addition of base.
- Panja, Santanu,Adams, Dave J.
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- SILVESTROL ANTIBODY-DRUG CONJUGATES AND METHODS OF USE
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The invention relates generally to a silvestrol molecule activated with a leaving group. The invention further relates generally to an antibody-drug conjugate comprising an antibody conjugated by a linker to one or more silvestrol drug moieties and methods of treatment.
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Page/Page column 90
(2018/01/15)
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- Flow-mediated synthesis of Boc, Fmoc, and Dd iv monoprotected diamines
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A series of monoprotected aliphatic diamines (21 examples) were synthesized via continuous flow methods. The carbamates and enamines were obtained in 45-91% yields using a 0.5 mm diameter PTFE tubular flow reactor. Using readily accessible protecting group precursors, the procedure serves as an attractive alternative to existing batch-mode synthetic routes by providing direct, multigram access to N-Boc-, N-Fmoc-, and N-Ddiv-protected compounds with productivity indexes of 1.2-3.6 g/h.
- Jong, Thingsoon,Bradley, Mark
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supporting information
p. 422 - 425
(2015/03/03)
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- Structure-affinity relationships of glutamine mimics incorporated into phosphopeptides targeted to the SH2 domain of signal transducer and activator of transcription 3
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In cancer cells, signal transducer and activator of transcription 3 (Stat3) participates in aberrant growth, survival, angiogenesis, and invasion signals and is a validated target for anticancer drug design. We are targeting its SH2 domain to prevent docking to cytokine and growth factor receptors and subsequent signaling. One of the important elements of the recognition sequence, pTyr-Xxx-Xxx-Gln, is glutamine. We incorporated novel Gln mimics into a lead peptide, pCinn-Leu-Pro-Gln-NHBn, and found that a linear, unconstrained side chain and carboxamide are necessary for high affinity, and the benzamide can be eliminated. Replacement of Gln-NHBn with (R)-4-aminopentanamide or 2-aminoethylurea produced inhibitors with equal or greater potency than that of the lead, as judged by fluorescence polarization (IC50 values were 110 and 130 nM, respectively). When Pro was replaced with cis-3,4- methanoproline, the glutamine mimic, (4R,5S)-4-amino-5-benzyloxyhexanamide resulted in an IC50 of 69 nM, the highest affinity Stat3 inhibitor reported to date. 2009 American Chemical Society.
- Mandal, Pijus K.,Ren, Zhiyong,Chen, Xiaomin,Xiong, Chiyi,McMurray, John S.
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scheme or table
p. 6126 - 6141
(2010/03/24)
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