US2006111293A1PendingUtilityA1

Antagonists for human prolactin

40
Individually held — no corporate assignee on recordPriority: Dec 13, 2002Filed: Nov 7, 2005Published: May 25, 2006
Est. expiryDec 13, 2022(expired)· nominal 20-yr term from priority
Inventors:Charles BrooksFrancis C. Peterson
A61P 35/00A61P 15/14A61K 38/00C07K 14/57554
40
PatentIndex Score
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Claims

Abstract

Modified prolactin molecules wherein the prolactin molecule comprises at least one mutation in a region selected from i) amino acids 41-57, ii) amino acids 94-110, and iii) amino acids 160-173; and wherein the at least one mutation is selected from deletions, replacements, and insertions. The modified prolactins are prolactin antagonists, and can be used in treating cancer, among other conditions.

Claims

exact text as granted — not AI-modified
1 . A modified human prolactin molecule comprising the following amino acid sequence:  
       
         
           
                 
                 
                 
               
                     
                     
                 
                     
                   LPICPGGAAR CQVTLRDLFD RAVVLSHYIH NLSSEMFSEF    DKRYTHGRGF     
                     
                 
                     
                           10         20         30         40         50 
                 
                     
                     
                 
                     
                       ITKAINS   CHT SSLATPEDKE QAQQMNQKDF LSLIVSILRS WNE   PLYHLVT     
                 
                     
                           60         70         80         90        100 
                 
                     
                     
                 
                     
                       EVRGMQEAPE    AILSKAVEIE EQTKRLLEGM ELIVSQVHPE TKENEIYPVW 
                 
                     
                          110        120        130        140        150 
                 
                     
                     
                 
                     
                   SGLPSLQMA   D       EESRLSAYYN       LLH   CLRRDSH KIDNYLKLLK CRIIHNNNC 
                 
                     
                          160        170        180        190       199 
                 
                     
                     
                 
             
                
                
                
                
                
                
                
                
                
                
                
                
                
               
            
           
         
       
       wherein the prolactin molecule comprises at least one mutation in a region selected from i) at least one replacement, deletion, or insertion in-amino acids 41-57, ii) at least one replacement, deletion, or insertion in amino acids 94-110, and iii) at least on deletion or insertion in amino acids 160-173, or replacement of an amino acid chosen from A, V, L, I, P, F, W, M, G, S, T, C, Y, N, Q, K, R, H in amino acids 160-173 with an amino acid chosen from D and E.  
     
     
         2 . The modified human prolactin molecule according to  claim 1 , wherein the prolactin molecule comprises at least one replacement mutation in region i), ii), and/or iii).  
     
     
         3 . The modified human prolactin molecule according to  claim 2 , wherein at least one replacement mutation comprises replacing an amino acid chosen from A, V, L, I, P, F, and M, with an amino acid chosen from D and E.  
     
     
         4 . The modified human prolactin molecule according to  claim 3 , wherein at least one replacement mutation is chosen from F44E,_F50E, 151E, A54E, 155E, L95E, L98E, V99E, V102E, L165E, L171E, and L172E.  
     
     
         5 . The modified human prolactin molecule according to  claim 2 , wherein at least one replacement mutation comprises replacing an amino acid chosen from G, S, T, Y, N, and Q, with an_amino acid chosen from D and E.  
     
     
         6 . The modified human prolactin molecule according to  claim 5 , wherein at least one replacement mutation is chosen from T45E, T52E, N56E, S57E, Y96E, Y168E, and Y169E.  
     
     
         7 . The modified human prolactin molecule according to  claim 2 , wherein at least one replacement mutation comprises replacing an amino acid chosen from K, R, and H, with an amino acid chosen from D and E.  
     
     
         8 . The modified human prolactin molecule according to  claim 7 , wherein at least one replacement mutation is chosen from H46E, R48E, K53E, H97E, and H173E.  
     
     
         9 . The modified human prolactin molecule according to  claim 2 , wherein at least one replacement mutation comprises replacing an amino acid chosen from G, S, T, Y, N, and Q, with an amino acid chosen from A, V, L, I, P, F, and M.  
     
     
         10 . The modified human prolactin molecule according to  claim 9 , wherein at least one mutation is chosen from G47F and_G49F.  
     
     
         11 . The modified human prolactin molecule according to  claim 2 , wherein at least one replacement mutation comprises replacing an amino acid chosen from K, R, and H, with an amino acid chosen from A, V, L, I, P, F, and M.  
     
     
         12 . The modified human prolactin molecule according to  claim 9 , wherein at least one mutation is chosen from H46A and R48A.  
     
     
         13 . The modified human prolactin molecule according to  claim 1 , wherein the prolactin molecule comprises at least one deletion mutation in region i), ii), and/or iii).  
     
     
         14 . The modified human prolactin molecule according to  claim 13 , wherein at least one deletion mutation comprises a single deletion of an amino acid chosen from amino acids 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 160, 161, 162, 163, 164, 165, 166, 167, 168,169, 170, 171, 172, and 173.  
     
     
         15 . The modified human prolactin molecule according to  claim 14 , wherein at least one deletion mutation comprises a deletion of F50.  
     
     
         16 . The modified human prolactin molecule according to  claim 13 , wherein at least one deletion mutation comprises deletion of more than one amino acid chosen from amino acids 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, and 173.  
     
     
         17 . The modified human prolactin molecule according to  claim 16 , wherein at least one deletion mutation comprises a deletion of amino acids chosen from 41-57, 94-110, 160-173, 41-49, 50-57, 41-42, 41-43, 41-44, 41-45, 41-46, 41-47, 41-48, 41-50, 41-51, 41-53, 41-54, 41-55, and 41-56.  
     
     
         18 . The modified human prolactin molecule according to  claim 1 , wherein the prolactin molecule comprises at least one insertion mutation in region i), ii), and/or iii).  
     
     
         19 - 21 . (canceled)  
     
     
         22 . A pharmaceutical composition comprising the modified human prolactin molecule according to  claim 1  and at least one pharmaceutically acceptable excipient.  
     
     
         23 . A method of treating a cancer comprising administering an effective therapeutic amount of the modified human prolactin molecule according to  claim 1 .  
     
     
         24 . The method according to  claim 23 , wherein the cancer is breast cancer or leukemia.  
     
     
         25 . The modified human prolactin molecule according to  claim 1 , with the proviso that the deletion is not of amino acids 41-52.  
     
     
         26 . A method for reducing or suppressing lactation comprising administering an effective therapeutic amount of the modified human prolactin molecule according to  claim 1.

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