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Digitale Medien

A β-turn mimic and a thiomethylene dipeptide surrogate employed in the study of cyclic peptide RGD and RCD cell-adhesion inhibitors (1996)

Rishton, Gilbert M. ; Harn, Nancy K. ; Cripps, Stephan J. ; [weitere]

Springer

International journal of peptide research and therapeutics 3 (1996), S. 37-44

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ISSN: 1573-3904

Schlagwort(e): Integrins ; Fibronectin ; Vascular cell-adhesion molecule-1 ; VCAM-1 ; Pseudopeptide ; Peptidomimetic ; Anti-inflammatory agents

Quelle: Springer Online Journal Archives 1860-2000

Thema: Chemie und Pharmazie

Notizen: Summary During an inflammatory response, leukocytes adhere to the blood-vessel wall and to underlying extracellular matrix-protein fibronectin via noncovalent interaction through two distinct cell-surface integrins, α5β1 and α4β1. An Arg-Gly-Asp tripeptide in the cell-binding domain of fibronectin has been demonstrated to be the major site that mediates cell attachment. Our group has previously disclosed Arg-Gly-Asp- and Arg-Cys-Asp-containing cyclic peptide cell-adhesion inhibitors, which are potentially useful as anti-inflammatory agents, particularly in the treatment of asthma and rheumatoid arthritis. Subsequently, we have incorporated a β-turn dipeptide mimic and a suitably protected Arg-Gly thiomethylene dipeptide surrogate into our lead peptides by solid-phase synthesis. The preparation of the surrogates, and the structure-activity studies of the surrogate-containing peptides are described in this paper. Complete loss of cell-adhesion inhibition activity was observed in the case of incorporation of the conformationally constrained β-turn dipeptide into a cyclic Arg-Cys-Asp peptide inhibitor. Incorporation of an Arg-Gly thiomethylene dipeptide surrogate into cyclic Arg-Gly-Asp and Arg-Cys-Asp cyclic disulfide peptide inhibitors was tolerated, resulting in cyclic pseudopeptide cell-adhesion inhibitors lacking the Arg-Gly peptide amide bond.

Materialart: Digitale Medien

URL: http://dx.doi.org/10.1007/BF00131084

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Digitale Medien

Single screw extrusion of poly(vinyl chloride): Effect on fusion and properties (1992)

Covas, J. A. ; Gilbert, M.

Stamford, Conn. [u.a.] : Wiley-Blackwell

Polymer Engineering and Science 32 (1992), S. 743-750

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ISSN: 0032-3888

Schlagwort(e): Chemistry ; Chemical Engineering

Quelle: Wiley InterScience Backfile Collection 1832-2000

Thema: Chemie und Pharmazie , Maschinenbau , Physik

Notizen: The behavior of unplasticized poly(vinyl chloride) (UPVC) during single screw extrusion was studied. The melting and gelation mechanisms under a variety of operating conditions were identified using microscopy, density measurements, and thermal analysis. The compound followed the behavior of wall-slipping materials, the melt forming a pool near the passive flight of the screw. Gelation involved the progressive destruction of the original powder morphology and the development, upon cooling, of an entanglement network with primary and secondary crystallinity. Both the breakdown and internal fusion of the grains were observed, depending on the location of the material around the screw. Tensile yield parameters were found to be independent of the gelation level. The values of the post-yield parameters reached a maximum for gelation levels in the range of 70% to 85%.

Zusätzliches Material: 15 Ill.