Akzo Nobel N.v.

Other

University of Glasgow

Peter Diederik Grootenhuis

Maurice Petitou

Constant A Van Boeckel

Anton Egbert Adang

Adrianus Petrus De Man

Deborah Claire Harris

Pieter Westerduin

Adrian Jonathan Lapthorn

Neil William Isaacs

Serine protease inhibitors

The three-dimensional structure of human chorionic gonadotrophin (hCG) has been determined by X-ray crystallography and the coordinates of the individual atoms are presented. Analogues of hCG and other glycoprotein hormones sharing a similar .alpha.-subunit structure are produced by inputting chemical changes to the structure into a computer loaded with three-dimensional molecular simulation software and representing visually on a computer display. The three-dimensional structures of the original glycoprotein and the chemically modified analogues are compared, and those analogues wherein the three-dimensional configuration and spatial arrangement of regions involved in receptor binding and signal transduction remain substantially preserved are selected for synthesis by molecular biology techniques and screening for biological activity. Glycoprotein analogues with additional glycosylation sites, and deletion of non-essential hairpins are disclosed.

Three dimensional glycoprotein hormone structure representation using a

The invention relates to a tuneable bisconjugate comprising two saccharides and a spacer, each saccharide being the same or different and comprising two to six monosaccharide units, at least one unit being uronic acid, characterized in that at least one of the saccharides per se has anti-thrombotic activity, and that the spacer connects at least one saccharide to the other through its non-reducing end, the chain length of the spacer being 20-120 atoms.

Bisconjugates comprising two saccharides and a spacer

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Oss, Netherlands

Peter Diederik Grootenhuis