Trifunctional conjugates
First Claim
1. A trifunctional conjugate having a first member, a second member and a third member, each member being attached to an organic spacer moiety, wherein:
- (a) the first member is a reactive member capable of binding to at least one macromolecule, said macromolecule having at least one binding site for a ligand, said ligand being distinct from the first member, the second member and the third member,(b) the second member comprises at least one substituted boronic acid group capable of binding to said macromolecule having at least one binding site for a ligand, said ligand being distinct from the first member, the second member and the third member, said substituted bormic acid group not being capable of binding to ligand binding sites on said macromolecule;
(c) the third member is a label; and
(d) the spacer moiety is selected such that the binding of the second member to a macromolecule does not prevent binding of the reactive member to the same macromolecule.
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Accused Products
Abstract
A trifunctional conjugate is provided having three chemical moieties, attached through a spacer moiety. At least two of the chemical moieties are relatively small molecules, usually less than about 7,000 Daltons in size. The spacer moiety is selected to impart certain steric properties to the conjugate. In one embodiment, the binding of a macromolecular specific binding partner to one of the chemical mouths sterically inhibits the binding of a different macromolecule to another chemical moiety. In another embodiment, the binding of a first chemical moiety to a macromolecule restricts the subsequent binding of a second chemical moiety to a proximate location on the same macromolecule.
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Citations
30 Claims
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1. A trifunctional conjugate having a first member, a second member and a third member, each member being attached to an organic spacer moiety, wherein:
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(a) the first member is a reactive member capable of binding to at least one macromolecule, said macromolecule having at least one binding site for a ligand, said ligand being distinct from the first member, the second member and the third member, (b) the second member comprises at least one substituted boronic acid group capable of binding to said macromolecule having at least one binding site for a ligand, said ligand being distinct from the first member, the second member and the third member, said substituted bormic acid group not being capable of binding to ligand binding sites on said macromolecule; (c) the third member is a label; and (d) the spacer moiety is selected such that the binding of the second member to a macromolecule does not prevent binding of the reactive member to the same macromolecule. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20)
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21. A preparation comprising at least two trifunctional conjugate molecules, each trifunctional molecule having three members, a first member, a second member and a third member, each member being attached together through an organic spacer moiety such that the three members are separated each from the other by distances controlled to within about one bond length, the controlled distances being substantially uniform for all molecules of the preparation, wherein at least two of the members are small molecules capable of binding with at least one small molecule binding partner and one of the members is a modulating member, wherein at least two of the members are separated from each other by at least about 28 Å
- , and the modulating member is separated from two of the members by less than about 22 Å
, and the binding of a modulating member specific binding partner to said modulating member prevents, by steric inhibition, the binding of at least one of the members to a binding partner of that member. - View Dependent Claims (22, 23, 24)
- , and the modulating member is separated from two of the members by less than about 22 Å
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25. A preparation comprising at least two trifunctional conjugate molecules, each trifunctional conjugate having a first member, a modulating member and a third member, each member being attached to an organic spacer moiety;
- wherein;
the organic spacer moiety comprises ω
-carbobenzoxylysine;(ii) the first member is biotin; (iii) the modulating member is theophylline; and (iv) the third member is dinitrophenol.
- wherein;
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26. A trifunctional conjugate having a first member, a second member and a third member, each member being attached to an organic spacer moiety, wherein:
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(a) the first member is an azide residue capable of binding to at least one macromolecule; (b) the second member is a phenyl boronic acid residue capable of binding to at least one macromolecule; (c) the third member is selected from the group consisting of labels and solid supports; and (d) the spacer moiety is selected such that the binding of the azide residue to a macromolecule does not prevent the binding of the phenyl boronic acid residue to said macromolecule. - View Dependent Claims (27, 28, 29, 30)
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Specification