New analogues of laminin active fragment YIGSR: synthesis and biological activity in vitro and in vivo. |
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Authors: | Ewa Witkowska Alicja Oriowska Jan Izdebski Jan Salwa Joanna Wietrzyk Adam Opolski |
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Institution: | Laboratory of Peptides, Department of Chemistry, Warsaw University, Poland. ewawit@chem.uw.edu.pl |
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Abstract: | Eleven analogues of the laminin pentapeptide amide fragment Tyr-Ile-Gly-Ser-Arg-NH2 (YIGSR-NH2) corresponding to a B1 chain fragment of the glycoprotein laminin have been synthesized by the solid phase method, and their biological activity has been studied in vitro by a cell adhesion assay: all of them inhibited the adhesion of LLC tumor cells to laminin. The analogues were found to be more resistant to enzymatic degradation in human serum than YIGSR-NH2 itself. Analogue DatIGSHar-NH2 was selected for an experimental pulmonary metastasis assay in vivo: it had higher antimetastatic activity than YIGSR-NH2. |
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Keywords: | laminin YIGSR‐NH2 fragment peptide synthesis tumor cell adhesion assay enzymatic degradation antimetastatic activity melanoma |
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