Journal of Peptide Science

Cover image for Journal of Peptide Science

June 2010

Volume 16, Issue 6

Pages 257–313

  1. Rapid Communications

    1. Top of page
    2. Rapid Communications
    3. Research Articles
    1. Tetrapeptides, as small-sized peptidic inhibitors; synthesis and their inhibitory activity against BACE1 (pages 257–262)

      Taeko Kakizawa, Koushi Hidaka, Daisuke Hamada, Ryoji Yamaguchi, Tsuyoshi Uemura, Hitomi Kitamura, Harichandra D. Tagad, Takashi Hamada, Zyta Ziora, Yoshio Hamada, Tooru Kimura and Prof. Yoshiaki Kiso

      Version of Record online: 7 MAY 2010 | DOI: 10.1002/psc.1238

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      Tetrapeptidic BACE1 inhibitors were designed and synthesized. Inhibitory activity was determined by in vitro enzymatic assay. Our tetrapeptides exhibited high potency, with the highest IC50 value of 34.6 nM from KMI-927.

  2. Research Articles

    1. Top of page
    2. Rapid Communications
    3. Research Articles
    1. Binding of synthetic peptide TPLVTLFK to nonopioid beta-endorphin receptor on rat brain membranes (pages 263–268)

      Yuliia N. Nekrasova, Vladimir B. Sadovnikov, Yury A. Zolotarev and Elena V. Navolotskaya

      Version of Record online: 21 APR 2010 | DOI: 10.1002/psc.1231

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      The synthetic peptide TPLVTLFK corresponding to the sequence 12–19 of β-endorphin (referred to as octarphin) was found to bind to high-affinity naloxone-insensitive binding sites on membranes isolated from the rat brain cortex (Kd = 2.6 ± 0.2 nM). The binding specificity study revealed that these binding sites were insensitive not only to naloxone but also to α-endorphin, γ-endorphin, [Met5]enkephalin, and [Leu5]enkephalin, as well.

    2. Structural characterization of a new statherin from pig parotid granules (pages 269–275)

      Barbara Manconi, Chiara Fanali, Tiziana Cabras, Rosanna Inzitari, Maria Patamia, Emanuele Scarano, Antonella Fiorita, Alberto Vitali, Massimo Castagnola, Irene Messana and Maria Teresa Sanna

      Version of Record online: 7 MAY 2010 | DOI: 10.1002/psc.1232

      Thumbnail image of graphical abstract

      HPLC– ESI-MS analysis on pig parotid secretory granule extracts evidenced a peptide with a molecular mass value of 5381.1 ± 0.6 Da and its truncated form, devoid of the C-terminal Ala, with typical structural features of the four statherins characterized till now. Pig statherin is mono-phoshorylated on Ser-3, while primate statherins already characterized are di-phosphorylated on Ser-2 and Ser-3. This difference, probably, connected to the Asp-4 [RIGHTWARDS ARROW] Glu substitution, suggests the involvement of the Golgi-casein kinase, which strictly recognizes the SX(E/pS) consensus sequence.

    3. Double helix formation in α-peptides: a theoretical study (pages 276–283)

      Peter Schramm and Hans-Jörg Hofmann

      Version of Record online: 7 MAY 2010 | DOI: 10.1002/psc.1234

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      An overview on all possible hydrogen bonding patterns of antiparallel and parallel double helices in α-peptides and their stability relationships is given on the basis of ab initio MO theory.

    4. Solution-phase submonomer diversification of aza-dipeptide building blocks and their application in aza-peptide and aza-DKP synthesis (pages 284–296)

      Carine B. Bourguet, Caroline Proulx, Sophie Klocek, David Sabatino and Prof. William D. Lubell

      Version of Record online: 10 MAY 2010 | DOI: 10.1002/psc.1235

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      Direct alkylation and diversification of protected aza-Gly dipeptides has provide a useful solution-phase strategy for preparing building blocks, which are suitable for incorporation into longer aza-peptides as well as for synthesis of aza-diketopiperazines.

    5. A study to assess the cross-reactivity of cellulose membrane-bound peptides with detection systems: an analysis at the amino acid level (pages 297–302)

      Carsten C. Mahrenholz, Victor Tapia, Rolf D. Stigler and Rudolf Volkmer

      Version of Record online: 7 MAY 2010 | DOI: 10.1002/psc.1237

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      The most important application of the SPOT synthesis technique is to simultaneously detect a high number of peptides that have a strong binding affinity to defined targets. The validity of the results, however, depends on the ability of the detection system to indicate binding events while not interfering with the experiment itself through cross-reaction. We tested three common read-out systems (TAMRA, FITC, and biotin/streptavidin) for their ability to interact with cellulose-bound peptides. Our approach identified several amino acids interacting with different detection systems.

    6. Synthesis and conformation of an analog of the helix-loop-helix domain of the Id1 protein containing the O-acyl iso-prolyl-seryl switch motif (pages 303–308)

      Michael Beisswenger, Taku Yoshiya, Yoshiaki Kiso and Chiara Cabrele

      Version of Record online: 10 MAY 2010 | DOI: 10.1002/psc.1239

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      An analog of the Id1 HLH domain containing the O-acyl iso-dipeptide motif Pro-Ser has been successfully synthesized by solid-phase Fmoc chemistry upon suppression of diketopiperazine formation. No secondary structure could be detected for the O-acyl iso-peptide before its conversion into the native form by O [RIGHTWARDS ARROW] N acyl shift.

    7. The application of an aryl hydrazine linker prevents ß-elimination side products in the SPPS of C-terminal cysteine peptides (pages 309–313)

      Shuaijian Ni, Huibin Zhang, Wenlong Huang, Jinpei Zhou, Hai Qian and Wei Chen

      Version of Record online: 7 MAY 2010 | DOI: 10.1002/psc.1240

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      Solid-phase synthesis allows for the preparation of some complex cysteine-containing peptides with both a high yield and purity. However, side reactions during chain elongation such as modification of amino acid residues have been found in C-terminal cysteine peptides. We identified 3-(1-piperidinyl)-alanine peptides, corroborated the mechanism of the side reaction, and introduced an efficient approach for the Fmoc-based synthesis of C-terminal cysteine peptides using an aryl hydrazine linker.

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