Sialyltransferase inhibitors

被引：16

作者：

Jung, KH ^{[1
]}

Schwörer, R ^{[1
]}

Schmidt, RR ^{[1
]}

机构：

[1] Univ Konstanz, Fachbereich Chem, D-78457 Constance, Germany

来源：

TRENDS IN GLYCOSCIENCE AND GLYCOTECHNOLOGY | 2003年 / 15卷 / 85期

关键词：

bisubstrate analogs; glycosyltransferase; inhibitors; mimeticsneuraminic acid; substrate analogs; transition-state analogs;

D O I：

10.4052/tigg.15.275

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 [生物化学与分子生物学]; 081704 [应用化学];

摘要：

Sialylation of glycoproteins and glycolipids plays an important role in many cell surface processes; of special interest in this context are changes in tissue involved in diseases and especially changes during infections. Therefore, inhibitors of sialyltransferases regulating sialylation might be of medicinal interest, especially in the therapy of virus and cancer diseases. The present paper reviews the development of sialyltransferase inhibitors; thus acceptor analogs, donor analogs, transition-state analogs, and bisubstrate analogs were designed based on sialic acid derivatives as well as on structural mimetics. This way, very potent sialyltransferase inhibitors with inhibition constants in the low nanomolar range have been recently found.

引用

页码：275 / 289

页数：15

共 61 条

[1]

Amann F, 1998, CHEM-EUR J, V4, P1106, DOI 10.1002/(SICI)1521-3765(19980615)4:6<1106::AID-CHEM1106>3.0.CO

[2]

2-7

[3]

Use of an altered sugar-nucleotide to unmask the transition state for α(2→6) sialyltransferase [J].

Bruner, M ;

Horenstein, BA .

BIOCHEMISTRY, 2000, 39 (09) :2261-2268

[4]

An α2,3 sialyltransferase (ST3Gal I) is elevated in primary breast carcinomas [J].

Burchell, J ;

Poulsom, R ;

Hanby, A ;

Whitehouse, C ;

Cooper, L ;

Clausen, H ;

Miles, D ;

Taylor-Papadimitriou, J .

GLYCOBIOLOGY, 1999, 9 (12) :1307-1311

[5]

An efficient synthesis of CMP-3-fluoroneuraminic acid [J].

Burkart, MD ;

Vincent, SP ;

Wong, CH .

CHEMICAL COMMUNICATIONS, 1999, (16) :1525-1526

[6]

Chemo-enzymatic synthesis of fluorinated sugar nucleotide:: Useful mechanistic probes for glycosyltransferases [J].

Burkart, MD ;

Vincent, SP ;

Düffels, A ;

Murray, BW ;

Ley, SV ;

Wong, CH .

BIOORGANIC & MEDICINAL CHEMISTRY, 2000, 8 (08) :1937-1946

[7]

Synthesis and characterization of an anomeric sulfur analogue of CMP-sialic acid [J].

Cohen, SB ;

Halcomb, RL .

JOURNAL OF ORGANIC CHEMISTRY, 2000, 65 (19) :6145-6152

[8]

DALLOLIO F, 1989, INT J CANCER, V44, P434

[9]

DAO TL, 1986, TUMOR MARKERS THEIR, P31

[10]

Dennis JW, 1999, BIOESSAYS, V21, P412, DOI 10.1002/(SICI)1521-1878(199905)21:5<412::AID-BIES8>3.0.CO

← 1 2 3 4 5 6 7 →