Iodothyronine enzyme conjugates
First Claim
1. A thyroxine conjugate to an enzyme at other than the active site of the enzyme, having on the average from about 1 to 20 of said thyroxines bonded to said enzyme, wherein said thyroxine conjugated enzyme undergoes a substantial change in the enzymatic activity of said enzyme upon binding of receptor for said thyroxine to the thyroxine conjugated to said enzyme.
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Abstract
Polyiodothyronine conjugates to enzymes are provided which find use in the determination of polyiodothyronine compounds, particularly thyroxine, normally in physiological fluids, such as serum. The enzymes can provide substantial variation in activity when bound to protein receptors for polyiodothyronine as compared to the free or unbound polyiodothyronine conjugated to the enzyme. Various linking groups are provided for linking the polyiodothyronine to the enzyme.
119 Citations
16 Claims
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1. A thyroxine conjugate to an enzyme at other than the active site of the enzyme, having on the average from about 1 to 20 of said thyroxines bonded to said enzyme, wherein said thyroxine conjugated enzyme undergoes a substantial change in the enzymatic activity of said enzyme upon binding of receptor for said thyroxine to the thyroxine conjugated to said enzyme.
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2. A thyroxine enzyme conjugate of the formula ##STR4## wherein:
- any one of the W groups can be X or an H of any one of the W groups may be replaced by X, wherein X is a bond or linking group;
X is 0 or 1, being 0 when W1 is the linking group; A is an enzyme bonded at other than its active site; n is on the average in the range of 1 to the molecular weight by A divided by 2,000; α
1-4 are iodine;L is hydrogen or when W2 is the linking group, lower alkyl of from 1 to 3 carbon atoms or a protective acyl group; when other than a linking group; W and W2 are hydrogen, with the proviso that when L is lower alkyl, W is lower alkyl of from 1 to 3 carbon atoms; and W1 is hydroxyl or lower alkoxyl of from 1 to 3 carbon atoms. - View Dependent Claims (3, 4, 5, 6)
- any one of the W groups can be X or an H of any one of the W groups may be replaced by X, wherein X is a bond or linking group;
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7. A polyiodothyronine enzyme conjugate according to the formula ##STR5## wherein:
- Y is hydrogen or lower alkyl of from 1 to 3 carbon atoms;
n is on the average in the range of 1 to 20; A is an enzyme bonded at other than the active site to the polyiodothyronine group in the parenthesis; W is a linking group which is a bond or aliphatic group of from 1 to 16 atoms other than hydrogen, which are carbon, oxygen, nitrogen, or sulphur, the oxygen and sulphur being present as oxy or oxo or thioanalogs thereof and the nitrogen being present as amido or tertiary amino. - View Dependent Claims (8, 9, 10)
- Y is hydrogen or lower alkyl of from 1 to 3 carbon atoms;
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11. A thyroxine conjugate to an enzyme at other than the active site of the enzyme, having on the average from about 1 to 20 of said thyroxine bonded to said enzyme.
- 12. A thyroxine conjugate to glucose-6-phosphate dehydrogenase having from 1 to 12 thyroxine groups bonded to said glucose-6-phosphate dehydrogenase by amide linkages or the nitrogen or thio analog thereof.
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14. A thyroxine conjugate to glucose oxidase having from 1 to 12 thyroxine groups bonded to said glucose oxidase by amido linkages or the nitrogen or thio analogs thereof.
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15. A thyroxine conjugate to lysozyme having from 1 to 5 thyroxine groups bonded to said lysozyme by amide linkages or the nitrogen or thio analogs thereof.
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16. A desaminothyrozine conjugate to glucose-6-dehydrogenase having from 1 to 12 desaminothyroxine groups bonded to said glucose-6-phosphate dehydrogenase by amide linkages or the nitrogen or thio analog thereof.
Specification