You have full text access to this contentNeuropeptide Y receptors: ligand binding and trafficking suggest novel approaches in drug development (pages 233–246)
Cornelia Walther, Karin Mörl and Annette G. Beck-Sickinger
Article first published online: 24 FEB 2011 | DOI: 10.1002/psc.1357
The members of the NPY hormone family have been shown to exhibit critical effects in the regulation of many important physiological functions by acting through YRs. Therefore the NPY system emerged as one of the main targets in modern drug development. Recent advances in understanding YR functionality and YR-targeted diagnostics and therapy are reviewed.
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Protocols
You have full text access to this contentSynthesis of multiple antigenic peptides (MAPs)—strategies and limitations (pages 247–251)
Wioleta Kowalczyk, Marta Monsó, Beatriz G. de la Torre and David Andreu
Article first published online: 29 NOV 2010 | DOI: 10.1002/psc.1310
MAPs can be made either by all-solid phase methods or by ligation in solution of preformed, SPPS-made components. Although MAP and MAP-like constructs are successfully used for many biological applications, reports tend to be vague on synthetic data. This protocol provides detailed information on the chemical synthesis and analytical documentation of MAPs and similar dendrimers made by either all-SPPS or thioether ligation methods.
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You have full text access to this contentScope and limitation of side-chain assisted ligation (pages 252–255)
Liat Spasser, K. S. Ajish Kumar and Ashraf Brik
Article first published online: 3 FEB 2011 | DOI: 10.1002/psc.1336
Side-chain assisted ligation is an auxiliary-mediated ligation strategy in which a thiol bearing cyclohexane or cyclopentane is attached to the side-chain of Asp, Glu, Ser or Thr to function in a similar manner to Cys in a native chemical ligation. Following the ligation step, the auxiliary is removed, without product isolation, under alkaline conditions.
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Research Articles
You have full text access to this contentSynthesis of peptides containing 5-hydroxytryptophan, oxindolylalanine, N-formylkynurenine and kynurenine (pages 256–262)
Toni Todorovski, Maria Fedorova, Lothar Hennig and Ralf Hoffmann
Article first published online: 19 JAN 2011 | DOI: 10.1002/psc.1322
Tryptophan residues are often irreversibly oxidized by ROS in mammalian cells. To study the functional and structural aspects of these oxidation pathways and to provide standard compounds for LC-MS-based proteomics studies, we have specifically incorporated four Trp-oxidation products (5-HTP, Oia, Kyn and NFK) in high yields in various sequences using the Fmoc/tBu-strategy on solid phase. Isobaric peptides containing 5-HTP and Oia were always well separated on a C18-phase by ion-pair RP-HPLC (acetonitrile gradient, 0.1% TFA).
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You have full text access to this contentStructural determinants of protein translocation in bacteria: conformational flexibility of SecA IRA1 loop region (pages 263–269)
Pasquale Palladino, Gabriella Saviano, Teodorico Tancredi, Ettore Benedetti, Filomena Rossi and Raffaele Ragone
Article first published online: 18 FEB 2011 | DOI: 10.1002/psc.1324
Conformational analysis of the main functional region of SecA motor protein by bioinformatics, CD, and NMR.
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You have full text access to this contentDPP-IV-resistant, long-acting oxyntomodulin derivatives (pages 270–280)
Alessia Santoprete, Elena Capitò, Paul E. Carrington, Alessandro Pocai, Marco Finotto, Annunziata Langella, Paolo Ingallinella, Karolina Zytko, Simone Bufali, Simona Cianetti, Maria Veneziano, Fabio Bonelli, Lan Zhu, Edith Monteagudo, Donald J. Marsh, Ranabir SinhaRoy, Elisabetta Bianchi and Antonello Pessi
Article first published online: 3 FEB 2011 | DOI: 10.1002/psc.1328
DPP-IV-resistant, long-acting oxyntomodulin derivatives were developed as candidate peptide therapeutics for diabetes and obesity.
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You have full text access to this contentAnalogues of trypsin inhibitor SFTI-1 modified in the conserved P1′ position by synthetic or non-proteinogenic amino acids retain their inhibitory activity (pages 281–287)
Łukajtis Rafał, Łȩgowska Anna, Wysocka Magdalena, Dȩbowski Dawid, Lesner Adam and Rolka Krzysztof
Article first published online: 3 FEB 2011 | DOI: 10.1002/psc.1330
A series of linear and monocyclic (with a disulfide bridge only) analogues of trypsin inhibitor SFTI-1 modified in the P1 and/or P1′ positions were synthesized by the solid-phase method. In the substrate specificity P1 position, Phe or N-benzylglycine (Nphe) were introduced, whereas the conserved Ser6 in Bownam-Birk (BBI) inhibitors was replaced by Hse (L-homoserine), Nhse [N-(2-hydroxyethyl)glycine], Sar, and Ala.
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You have full text access to this contentExamination of the active secondary structure of the peptide 101.10, an allosteric modulator of the interleukin-1 receptor, by positional scanning using β-amino γ-lactams (pages 288–296)
Nicolas Boutard, Stéphane Turcotte, Kim Beauregard, Christiane Quiniou, Sylvain Chemtob and William D. Lubell
Article first published online: 4 FEB 2011 | DOI: 10.1002/psc.1337
The IL-1R allosteric modulator APG-101.10 has been studied by positional scanning using (S)- and (R)-Bgl as a β-turn mimic. Certain analogs exhibited retained and improved potency in inhibiting IL-1β-induced thymocyte cell proliferation. CD spectroscopy indicated that the presence of a fold about the central residues of the parent peptide may be important for activity.