Glucagon superfamily peptides exhibiting nuclear hormone receptor activity
First Claim
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1. A compound comprising the structure Q-L-Y;
- wherein Q is a glucagon superfamily peptide;
Y is a steroid, which antagonizes a Type I nuclear hormone receptor (NHR) activity, with an EC50 of about 1μ
M or less, and has a molecular weight of up to about 1000 daltons; and
L is a linking group or a bond, with the proviso that Y is not a bile salt or cholesterol.
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Abstract
Provided herein are glucagon superfamily peptides conjugated with NHR ligands that are capable of acting at a nuclear hormone receptor. Also provided herein are pharmaceutical compositions and kits of the conjugates of the invention. Further provided herein are methods of treating a disease, e.g., a metabolic disorder, such as diabetes and obesity, comprising administering the conjugates of the invention.
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Citations
21 Claims
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1. A compound comprising the structure Q-L-Y;
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wherein Q is a glucagon superfamily peptide; Y is a steroid, which antagonizes a Type I nuclear hormone receptor (NHR) activity, with an EC50 of about 1μ
M or less, and has a molecular weight of up to about 1000 daltons; andL is a linking group or a bond, with the proviso that Y is not a bile salt or cholesterol. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21)
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Specification