The Bioactivity of Glycocluster and Glycodendrimer

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1 PROGRESS IN CHEMISTRY Vol. 17 No. 6 Nov., ( ) 3 3 ( ), : Q53 ; O62911 : A : X(2005) The Bioactivity of Glycocluster and Glycodendrimer Lu Weishen ( Institute of Marine Drugs and Food, Ocean University of China, Qingdao , China) Zhang Xiaoru 3 3 (College of Chemistry and Molecular Engineering, Qingdao University of Science & Technology, Qingdao , China) Abstract A new type of glycoconjugate2glycocluster and glycodendrimer has been designed as mimics for the multivalent effect in nature. The recent advances in bioactivity of glycocluster and glycodendrimer and their potential applications are reviewed in this article. Key words carbohydrate ; glycocluster ; glycodendrimer ; multivalent effect ; bioactivity,,, ( ), 2,, [1 ], ( multivalent effect ) ( cluster effect) [3,4 ], K d mmolπl molπl, ;, 2,,,,, ( glycocluster ) [2 2 ] (glycodendrimer), 1 : , : (No. 2001CCA01600) 3 3 e2mail com

2 [5, ] 4 5, [9 ],,,,, [7 ], 1983 Lee [8 ],,, (2), (HA) 11 (1) (HA), [13 ],, :, (CRD), ;,, [14 16 ] Roy [16 ] PAMAM 6a 6d, ( enzymelinked lectin assay,, ELLA) 2acid Limax flavus, 1,,,, IC 50,, 1 (type 1, fimbriae), Lindhorst [9 12 ] (3), ELISA ( )

3 acid Limax flavus Table 1 Inhibition of Binding of Human 2Acid Glycoprotein to Limax flavus by sialodendrimers compound IC 50 (nmolπl) a relative potency a phenyl 22thio2 2sialoside PAMAM2based 4mer 6a 6912 (277) 315 (0187) PAMAM2based 8mer 6b 2115 (172) 11 (114) PAMAM2based 16mer 6c 2189 (46. 2) 84 (512) PAMAM2based 32mer 6d 1113 (36. 2) 210 (617) a : values in parentheses are based on a per sialoside residue SLT2 SLT2,N2, [21 AB 5, ] A 5 B ASGPR 5 B, A [18 ] Gb3[ 2D2Gal (1 4) 2D2Gal (1 4) 2D2Glc (1 O2ceramide) ] Gb3, Gb3, 5, Kitov O157 H7 (SLT2 ) B5, [3,19,20 ], (starfish,7), 30!,, B, SLT2 IC , SLT2 IC ,, 21 N2 ASGPR,,

4 6 1057, Gal 1 3GalNAc 1, PAMAM( N2 ) T (13a 13d), [22 ] Lee N2 YEE (8), N2 IgG , [23 ], [24 ] Schuber, ELISA (9) [25 ], IgG T N2, 13a 13b 13c 13d IC nmol, 460 (10 12), ,,, = 2753, , G219 [26, ASGPR ] 41 31,, MUC1,,,, (HAR) HAR, Gal,, anti2 Gal,,, anti2 Gal [4 ] ( TACAs) : anti2 Gal Tn ( GalNAc 1 O2SerΠThr), stn (NeuAc 2 2GalOR, 6GalNAc 1 O2SerΠThr ) T ( Gal 1 anti2 Gal, Gal 1 3GalNAc 1 O2SerΠThr) [27 ], [28 3Gal 1 4GlcNAc 1 3Gal 1 4Glc 12 [32,33 ] ( ] ), Gal 1 Tn Tatsushi 3Gal, [27 ] GalNAc 1 O2Ser [34 ], starburst Wang : GalNAc 1 O2,1999 2Gal Ser, pnas( N2 ), starburst 7 ( ), T, [35 ] 14, ( ELISA), C anti2t stn, IC Danishefsky [29 ] 50 = 710nmolΠL,, stn T,Roy [30,31 ],Wang 2Gal T BSA,,

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