Structure of conformationally constrained peptides: From model compounds to bioactive peptides
β Scribed by C. Toniolo
- Book ID
- 102762416
- Publisher
- Wiley (John Wiley & Sons)
- Year
- 1989
- Tongue
- English
- Weight
- 541 KB
- Volume
- 28
- Category
- Article
- ISSN
- 0006-3525
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β¦ Synopsis
The use of backbone conformational constraints has acquired increasing importance in the design and synthesis of structurally restricted agonists and antagonists of bioactive peptides.
Here I discuss the preferred conformations of four among the most popular types of such peptide surrogates: (a) Peptides from Ca~a-dialkylated residues, (b) tetrazolyl peptides, (c) ( y -and 6-) lactam-containing peptides, and (d) thiated peptides. Emphasis i s given to conformational energy computations and x-ray diffraction analyses of selected model compounds and analogues of small bioactive peptides such L U the formylmethionyl tripeptide chemoattractant and MIF.
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In the quest for a greater understandlng of the relationship between "drug" structure and biologlcal actlvlty the study of conformationally constrained peptldes has received considerable attention. 1 Ma~~llan hornOn systems 'have been a particularly fruitful field for investigation of the effects of