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, the organic spacer moiety being attached to all three members so that the first member is attached to the second member through covalent bonds, the first member is attached to the third member through covalent bonds, and the second member is attached to the third member through covalent bonds, wherein:
- a) the first member is a small molecule capable of noncovalently binding to a first member binding partner;
b) the second member is a modulating member capable of noncovalently binding to a modulating member specific binding partner;
c) the third member is a small molecule capable of binding to a third member binding partner; and
d) the organic spacer moiety is selected such that the binding of the modulating member to the modulating member binding partner prevents, by steric inhibition, at least one of the first member binding partner or the third member binding partner from binding to the first member or the third member, respectively.
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Abstract
A trifunctional conjugate is providing 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 moieties sterically inhibits the binding of a different macromolecule to another chemical moieties. In another embodiment, the binding of a first chemical moiety to a macromolecule restricts the subsequent binding of a second tridentate member to a proximate location on the same macromolecule. The three chemical moieties are preferably a nitrophenylazido residue, a phenyl boronic acid residue, and a solid support or a label such as biotin. The spacer is preferably cysteine, lysine, glutamic acid, pyroglutamic acid, S-acetylmercaptosuccinic anhydride or ω-carbobenzoxylysine. The conjugate is useful in immunoassays and for targeted labeling of proteins.
43 Citations
13 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, the organic spacer moiety being attached to all three members so that the first member is attached to the second member through covalent bonds, the first member is attached to the third member through covalent bonds, and the second member is attached to the third member through covalent bonds, wherein:
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a) the first member is a small molecule capable of noncovalently binding to a first member binding partner; b) the second member is a modulating member capable of noncovalently binding to a modulating member specific binding partner; c) the third member is a small molecule capable of binding to a third member binding partner; and d) the organic spacer moiety is selected such that the binding of the modulating member to the modulating member binding partner prevents, by steric inhibition, at least one of the first member binding partner or the third member binding partner from binding to the first member or the third member, respectively. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12)
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13. A trifunctional conjugate having a first member, a second member, and a third member, each member being attached to an organic spacer moiety, the organic spacer moiety being attached to all three members so that the first member is attached to the second member through covalent bonds, the first member is attached to the third member through covalent bonds, and the second member is attached to the third member through covalent bonds, wherein:
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a) the first member is a small molecule ligand capable of noncovalently binding to a small molecule ligand binding partner having at least one proximity label conjugated thereto; b) the second member is a modulating member capable of noncovalently binding to a modulating member specific binding partner; c) the third member is selected from the group consisting of; i) at least one second proximity label, and ii) at least one solid support having at least one second proximity label conjugated thereto; and d) the organic spacer moiety is selected such that the binding of the modulating member to the modulating member specific binding partner prevents, by steric inhibition, the generation of a measurable reaction between said first proximity label and said second proximity label.
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Specification