摘要:

AbstractOver the past several years, new modulators of feeding and body weight have been discovered, and our knowledge of the mechanisms and neurohumoral interactions between anorexigenic and orexigenic compounds has increased dramatically. This review aims to summarize the present knowledge of the role of leptin and several hypothalamic neuropeptides, such as neuropeptide Y (NPY), corticotropin‐releasing hormone (CRH) and melanocortins, in the regulation of appetite and body weight. It also presents the progress made in the design of interactions between leptin and hypothalamic peptides in the regulation of feeding. The role of these compounds in the pathogenesis of obesity in animals and humans, and their potential usefulness in the treatment of this disorder, are discussed. Copyright © 2000 European Peptide Society and John Wiley&Sons, L

ISSN:1075-2617    

DOI:10.1002/psc.354

出版商:John Wiley&Sons, Ltd.    

年代:2001

数据来源: WILEY

摘要:

AbstractTheN‐terminal portion of HIV‐1 Tat covering residues 1–9 is a competitive inhibitor of dipeptidyl peptidase IV (DP IV). We have used1H NMR techniques, coupled with molecular dynamics methods, to determine the conformation of this peptide in the three diverse media: DMSO‐d6, water (pH 2.7) and 40% HFA solution. The results indicate that in both DMSO‐d6and HFA the peptide has a tendency to acquire a type I β‐turn around the segment Asp5‐Pro6‐Asn7‐Ile8. TheN‐terminal end is seen to be as a random coil. In water, the structure is best described as a left‐handed polyproline type II (PPII) helix for the mid segment region Asp2to Pro6. The structures obtained in this study have been compared with an earlier report on Tat (1–9). Copyright © 2000 European Peptide Society

ISSN:1075-2617    

DOI:10.1002/psc.353

出版商:John Wiley&Sons, Ltd.    

年代:2001

数据来源: WILEY

摘要:

AbstractThe HTLV‐I integraseN‐terminal domain [50‐residue peptide (IN50)], and a 35‐residue truncated peptide formed by residues 9–43 (IN35) have been synthesized by solid‐phase peptide synthesis. Formation of the 50‐residue zinc finger type structure through a HHCC motif has been proved by UV‐visible absorption spectroscopy. Its stability was demonstrated by an original method using RP‐HPLC. Similar experiments performed on the 35‐residue peptide showed that the truncation does not prevent zinc complex formation but rather that it significantly influences its stability. As evidenced by CD spectroscopy, the 50‐residue zinc finger is unordered in aqueous solution but adopts a partially helical conformation when trifluoroethanol is added. These results are in agreement with our secondary structure predictions and demonstrate that the HTLV‐I integraseN‐terminal domain is likely to be composed of an helical region (residues 28–42) and a β‐strand (residues 20–23), associated with a HHCC zinc‐binding motif. Size‐exclusion chromatography showed that the structured zinc finger dimerizes through the helical region. Copyright © 2000 European Pep

ISSN:1075-2617    

DOI:10.1002/psc.356

出版商:John Wiley&Sons, Ltd.    

年代:2001

数据来源: WILEY

摘要:

AbstractAnalogues of the nonselective bombesin receptor synthetic agonist H‐D‐Phe‐Gln‐Trp‐Ala‐Val‐βAla‐His‐Phe‐Nle‐NH2were prepared and their biological activity assessed at the NMB‐preferring/bombesin receptor (NMB‐R; BB1), the GRP‐preferring/bombesin receptor (GRP‐R; BB2) and the orphan receptor bombesin receptor subtype‐3 (BRS‐3; BB3). ProgressiveN‐terminal deletions identified the minimumC‐terminal sequences required for maintaining a significant agonist effect, whilst an alanine scan, targeted changes in stereochemistry and other pertinent substitutions identified key side‐chain and stereochemical requirements for activation. Key structural elements required for functional potency at BB1BB2and BB3, and for selectivity between these receptor subtypes were established. Synthetic peptides were discovered, which were highly potent agonists at BB2and extremely selective over both BB1and BB3. Copyright © 2000 European

ISSN:1075-2617    

DOI:10.1002/psc.359

出版商:John Wiley&Sons, Ltd.    

年代:2001

数据来源: WILEY

摘要:

AbstractA hydrophobic analogue of human galanin (1–19) fragment has been synthesized using Boc/Bzl tactics to demonstrate the synthetic utility of the flexible crosslinked polystyrene support prepared by the suspension polymerization of styrene and 1,4‐butanediol dimethacrylate. The copolymer was chloromethylated to 2.36 mmol Cl/g. The functionalized resin was found to possess all the physicochemical properties similar to Merrifield resin. The free peptide was obtained in high yield and purity as judged by RP‐HPLC and characterized by amino acid analysis and ESI‐MS. Copyright © 2000 European Peptide Society and John Wiley&S

ISSN:1075-2617    

DOI:10.1002/psc.357

出版商:John Wiley&Sons, Ltd.    

年代:2001

数据来源: WILEY