摘要:

AbstractAmyloid formation plays a central role in the cause and progression of Alzheimer's disease. The major component of this amyloid is the amyloid‐β (Aβ) peptide, which is currently the subject of intense study. This review discusses some recent studies in the area of Aβ synthesis, purification and structural analysis. Also discussed are proposed mechanisms for Aβ‐induced neurotoxicity and some recent advances in the development of Aβ‐related therapeutic strategies. Copyright © 2001 European Peptide Society and John Wile

ISSN:1075-2617    

DOI:10.1002/psc.324

出版商:John Wiley&Sons, Ltd.    

年代:2001

数据来源: WILEY

摘要:

AbstractA new synthesis of orthogonally protected diaminoglutaric acid containing peptides using the Ugi four component condensation is presented. To demonstrate that this method is useful to replace cystine by diaminoglutaric acid in biologically interesting peptides, we built up two cyclic somatostatin analogues deriving from Sandostatin and from TT‐232. A photolytically cleavable amine derivative of the nitroveratryl type is used for the Ugi four component condensation. Because of a racemic build up of the new stereocentre of the diaminoglutaric acid, and racemization of the isonitrile component, four diastereomeric peptides resulted that were separated by HPLC. The stereochemistry of the cyclopeptides could be easily and unambiguously assigned by chiral gas chromatography and a reference sample of enantiomerically pure (2S,4S)‐diaminoglutaric acid. Copyright © 2001 European Peptide Society and John Wiley&Sons,

ISSN:1075-2617    

DOI:10.1002/psc.306

出版商:John Wiley&Sons, Ltd.    

年代:2001

数据来源: WILEY

摘要:

AbstractDendritic peptides, often presented as multiple antigen peptides (MAPs), are widely used in immunological‐based fields of research, although their synthesis can be extremely challenging. In this paper, a tetrameric dendritic MAP‐like presentation of the retinoblastoma protein [649‐654] sequence (4RB649‐654) has been prepared using solid‐phase peptide synthesis (SPPS) methods. During the synthesis of this dendritic molecule, numerous modifications to the synthetic protocols were examined. These modifications included the introduction of a combination Boc‐ and Fmoc‐chemistry approach and also the use of 1,8‐diazabicyclo[5.4.0]‐undec‐7‐ene as a Fmoc‐deprotection agent. The use in combination of Boc‐ and Fmoc‐based synthetic strategies resulted in the production of the desired peptide molecule, 4RB649‐654, in high purity and acceptable yields following purification by reversed phase HPLC. Copyright © 2001 European Peptide So

ISSN:1075-2617    

DOI:10.1002/psc.314

出版商:John Wiley&Sons, Ltd.    

年代:2001

数据来源: WILEY

摘要:

AbstractWe have designed and synthesized a conformationally homogeneous series of cyclic pentapeptides of the general structurec[Pro‐aai‐

ISSN:1075-2617    

DOI:10.1002/psc.321

出版商:John Wiley&Sons, Ltd.    

年代:2001

数据来源: WILEY

摘要:

AbstractThe tetrapeptideN‐Acetyl‐Ser‐Asp‐Lys‐Pro (AcSDKP), an inhibitor of haematopoietic stem cell proliferation, reducesin vivoandin vitrothe damage to the stem cell compartment resulting from treatment with chemotherapeutic agents or ionizing radiations. In order to provide new molecules likely to improve the myeloprotection displayed by this tetrapeptide, we have prepared a set of analogues of AcSDKP. These compounds are derived from the parent peptide by substitution or modification of theN‐ or of theC‐terminus, or substitution of side chains. We report here that almost all investigated analogues retain the antiproliferative activity reducingin vitrothe proportion of murine Colony‐Forming Units Granulocyte/Macrophage (CFU‐GM) in S‐phase and inhibiting the entry into cycle of High Proliferative Potential Colony‐Forming Cells (HPP‐CFC). This shows that the polar groups of Ser, Asp or Lys are critical for the expression of biological activity, but that the modification of theN‐ orC‐terminus mostly yielded compounds still retaining antiproliferative activity and devoid of toxicity. The efficacy of AcSDKP analogues in preventingin vitrothe primitive haematopoietic cells from entering into cycle makes these molecules new candidates for furtherin vivoinvestigations. Copyright © 2001 European Peptide Soci

ISSN:1075-2617    

DOI:10.1002/psc.322

出版商:John Wiley&Sons, Ltd.    

年代:2001

数据来源: WILEY

ISSN:1075-2617    

DOI:10.1002/psc.332

出版商:John Wiley&Sons, Ltd.    

年代:2001

数据来源: WILEY