Bivalent thrombin binding molecules comprising linkers

Details Bivalent thrombin binding molecules comprising linkers Bivalent thrombin binding molecules comprising linkers

2005-06-20

2011-11-22

Li, Ruixiang (Department: 1646)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

C530S350000

Reexamination Certificate

active

08063018

ABSTRACT:
There is provided herein a multivalent binding molecule and uses thereof. The molecule is useful in binding a target under certain conditions and releasing it under other conditions. The molecule has the general formula (1) of BM1-L-(BM2)n(1) wherein, BM1 is a binding moiety 1 having an affinity for site 1 on the target, BM2 is a binding moiety 2 having an affinity for a site other than site 1 on the target, n is 1 or greater, and L is a linker joining BM1 and BM2, said linker being adapted to respond to a change in its environment with a change in conformation and/or flexibility, wherein BM1 and BM2 may be the same or different and are selected such that in use each of the BM1 and BM2 existing separately has a lower binding affinity then the complex of BM1 and BM2 does when they are linked to form the molecule. BM2 may have a single binding region or multiple binding regions with affinity for the target. The binding affinity of BM1 or BM2 to the target alone is no more than ½ the binding affinity of the molecule of formula (1). The molecule of formula (1) can be constructed using an oligomeric or polymeric linker, such as a polypeptide sequence. Such molecules can be useful in the delayed release of drugs, in screening assays, for stabilizing enzymes such as proteases, and for controlling reactions such as blood clotting.

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Truong, K. Sawano, A., Mizuno, H., Hama, H., Tong,

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