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1.
Bioorg Med Chem Lett ; 14(15): 4001-4, 2004 Aug 02.
Article in English | MEDLINE | ID: mdl-15225715

ABSTRACT

An affinity column immobilizing a decapeptide H(2)N-RGDSPASSKP-CO(2)H was used to select RGD-binding aptamers from a pool of 86-mer single-strand oligodeoxynucleotides (ODNs) containing a random 40-mer sequence. The enriched library thus obtained was further selected against adsorbed fibronectin and individual aptamers were monocloned in E. coli and sequenced to give a couple of highly homologous ODNs, which indeed inhibited fibronectin-integrin mediated cell adhesion.


Subject(s)
Cell Adhesion/drug effects , Fibronectins/physiology , Oligopeptides/chemical synthesis , Oligopeptides/pharmacology , Amino Acid Sequence , Animals , Base Sequence , Cell Line , Cricetinae , Fibronectins/antagonists & inhibitors , Kidney , Models, Molecular , Molecular Sequence Data , Protein Conformation
2.
Bioorg Med Chem Lett ; 14(9): 2087-90, 2004 May 03.
Article in English | MEDLINE | ID: mdl-15080984

ABSTRACT

Tailed calix[4]resorcarene macrocycle (tail=undecyl) can be used as a platform to assemble four glycosaminoglycan polysaccharide chains to give a new type of proteoglycan mimics. A tetra(chondroitin sulfate) derivative thus obtained from the reaction of macrocyclic octaamine and chondroitin sulfate lactone is readily immobilized on a tissue culture plastic (polystyrene) plate and inhibits fibronectin-mediated adhesion of BHK (baby hamster kidney) cells thereon remarkably strongly with 50% inhibition occurring at a 10 ng/mL or 40 pM concentration range.


Subject(s)
Calixarenes/chemistry , Cell Adhesion/drug effects , Chondroitin Sulfates/pharmacology , Macrocyclic Compounds/chemistry , Molecular Mimicry , Proteoglycans/pharmacology , Animals , Cell Line , Chondroitin Sulfates/chemistry , Cricetinae , Proteoglycans/chemistry
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