US2021054041A1PendingUtilityA1

Glycoprotein Hormone Long-Acting Superagonists

71
Assignee: TROPHOGEN INCPriority: Jul 30, 2012Filed: Sep 4, 2020Published: Feb 25, 2021
Est. expiryJul 30, 2032(~6 yrs left)· nominal 20-yr term from priority
Inventors:Mariusz SzkudlinskiBruce D. Weintraub
C07K 14/59A61P 5/00A61P 15/08A61K 38/00A61P 5/24A61P 5/06A61K 38/24
71
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Claims

Abstract

This invention provides long-acting, superactive analogs of glycoprotein hormones demonstrating enhanced bioactivity both in vitro and in vivo as compared to wild type counterparts. The analogs are particularly useful for treating subjects showing low receptor expression or poor receptor responsiveness, and for the treatment of any condition associated with glycoprotein hormone activity.

Claims

exact text as granted — not AI-modified
What is claimed: 
     
         1 : A modified glycoprotein hormone comprising an amino acid sequence with at least one conservative basic amino acid substitution selected from the group consisting of K15, K17, K20 and K24, and an insert of NVTINV (SEQ ID NO: 1) between F6 and T7 of the alpha subunit of a glycoprotein hormone. 
     
     
         2 : The modified glycoprotein hormone of  claim 1 , comprising at least two basic amino acid substitutions selected from the group consisting of K15, K17, K20 and K24. 
     
     
         3 : The modified glycoprotein hormone of  claim 1 , comprising at least three basic amino acid substitutions selected from the group consisting of K15, K17, K20 and K24. 
     
     
         4 : The modified glycoprotein hormone of  claim 1 , comprising at least four basic amino acid substitutions at K15, K17, K20 and K24. 
     
     
         5 : The modified glycoprotein hormone of  claim 4 , further comprising a basic amino acid substitution at E18. 
     
     
         6 : The modified glycoprotein hormone of  claim 1 , further comprising a basic amino acid substitution at E18. 
     
     
         7 : The modified glycoprotein hormone of  claim 5 , wherein the basic amino acid is arginine. 
     
     
         8 : The modified glycoprotein hormone of  claim 5 , wherein the basic amino acid is histidine. 
     
     
         9 : The modified glycoprotein hormone of  claim 1 , wherein the alpha subunit comprises an amino acid sequence with at least 85% identity to SEQ ID NO: 7. 
     
     
         10 : The modified glycoprotein hormone of  claim 1 , wherein the alpha subunit comprises an amino acid sequence with at least 90% identity to SEQ ID NO: 7. 
     
     
         11 : The modified glycoprotein hormone of  claim 1 , wherein the alpha subunit comprises an amino acid sequence with at least 99% identity to SEQ ID NO: 7. 
     
     
         12 : The modified glycoprotein hormone of  claim 1 , further comprising the beta subunit of follicle-stimulating hormone (FSH). 
     
     
         13 : The modified glycoprotein hormone of  claim 1 , wherein the alpha subunit is derived from a bovine alpha subunit (SEQ ID NO: 2). 
     
     
         14 : The modified glycoprotein hormone of  claim 13 , wherein the basic amino acid is arginine. 
     
     
         15 : The modified glycoprotein hormone of  claim 14 , further comprising an arginine substitution at E18. 
     
     
         16 : The modified glycoprotein hormone of  claim 18 , further comprising the beta subunit of bovine follicle-stimulating hormone (FSH). 
     
     
         17 : The modified glycoprotein hormone of  claim 1 , comprising amino acid substitutions at K15R, K17R, E18R, K20R, and K24R, and the beta subunit of bovine follicle-stimulating hormone (FSH). 
     
     
         18 : The modified glycoprotein hormone of  claim 1  comprising an alpha subunit having a sequence of SEQ ID NO: 7. 
     
     
         19 : The modified glycoprotein hormone of  claim 18 , further comprising the beta subunit of bovine follicle-stimulating hormone (FSH).

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