US2022017586A1PendingUtilityA1

Exposed collagen-targeted fusion cytokine for immune modulation in invasive cancers and lesions of infections

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Assignee: COUNTERPOINT BIOMEDICA LLCPriority: Jan 25, 2017Filed: Jan 19, 2021Published: Jan 20, 2022
Est. expiryJan 25, 2037(~10.5 yrs left)· nominal 20-yr term from priority
A61K 38/193A61K 38/37C07K 14/78C07K 14/56C07K 14/52C07K 2319/21C07K 14/535C07K 2319/01C07K 2319/02C12N 2800/22C07K 14/55C07K 2319/33C12N 15/85A61P 35/00C07K 14/755
61
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Claims

Abstract

Provided herein are new compositions and methods to target pharmaceutical agents to pathological areas by utilizing fusion polypeptides. These fusion polypeptides contain two or more domains: (i) aptamer sequences that bind to exposed collagenous (XC-) proteins present in pathological areas, including cancerous and viral lesions, (ii) immunomodulators, such as cytokines, and optionally (iii) at least one linker joining the two domains or at the terminus of the polypeptide. In some cases, the linker is a rigid linker, e.g., a rigid helical linker. Also provided herein are methods of treating cancer and/or infectious diseases using the new fusion polypeptides.

Claims

exact text as granted — not AI-modified
1 - 84 . (canceled) 
     
     
         85 . A method of treating an infection in a subject comprising administering to a subject in need of such treatment a fusion polypeptide comprising an amino acid sequence selected from the group consisting of:
 APARSPSPSTQPWEHVNAIQEARRLLNLSRDTAAEMNETVEVISEMFDLQEPTCLQTRLE LYKQGLRGSLTKLKGPLTMMASHYKQHCPPTPETSCATQIITFESFKENLKDFLLVIPFDC WEPVQEGAEAAAKEAAAKAGARRGVRVAWREPGRMELNMPHGQE (SEQ ID NO: 17);   APARSPSPSTQPWEHVNAIQEARRLLNLSRDTAAEMNETVEVISEMFDLQEPTCLQTRLE LYKQGLRGSLTKLKGPLTMMASHYKQHCPPTPETSCATQIITFESFKENLKDFLLVIPFDC WEPVQEGSAGSAAGSGARRGVRVAWREPGRMELNMPHGQE (SEQ ID NO: 18);   METDTLLLWVLLLWVPGSTGREEFEEEFEHREEFEFEENLYFQGAPARSPSPSTQPWEHVNAIQE ARRLLNLSRDTAAEMNETVEVISEMFDLQEPTCLQTRLELYKQGLRGSLTKLKGPLTMM ASHYKQHCPPTPETSCATQIITFESFKENLKDFLLVIPFDCWEPVQEGAEAAAKEAAAKA GARRGVRVAWREPGRMELNMPHGQE (SEQ ID NO: 19);   1VIETDTLLLWVLLLWVPGSTGREEFEEEFEHREEFEFEENLYFQGAPARSPSPSTQPWEHVNAIQE ARRLLNLSRDTAAEMNETVEVISEMFDLQEPTCLQTRLELYKQGLRGSLTKLKGPLTMM ASHYKQHCPPTPETSCATQIITFESFKENLKDFLLVIPFDCWEPVQEGSAGSAAGSGARR GVRVAWREPGRMELNMPHGQE (SEQ ID NO: 40);   METDTLLLWVLLLWVPGSTGREEFEEEFEHREEFEHENLYFQGARRGVHVGWREPGRMELN MPHGGAEAAAKEAAAKAGAPARSPSPSTQPWEHVNAIQEARRLLNLSRDTAAEMNET VEVISEMFDLQEPTCLQTRLELYKQGLRGSLTKLKGPLTMMASHYKQHCPPTPETSCAT QIITFESFKENLKDFLLVIPFDCWEPVQE (SEQ ID NO: 36); and   RRGVHVGWREPGRMELNMPHGGAEAAAKEAAAKAGAPARSPSPSTQPWEHVNAIQEA RRLLNLSRDTAAEMNETVEVISEMFDLQEPTCLQTRLELYKQGLRGSLTKLKGPLTMMA SHYKQHCPPTPETSCATQIITFESFKENLKDFLLVIPFDCWEPVQE (SEQ ID NO: 39) in an amount sufficient to treat the infection.   
     
     
         86 . The method of  claim 85 , wherein the fusion polypeptide further comprises a purification tag or an export signal peptide. 
     
     
         87 . The method of  claim 85 , wherein fusion polypeptide comprises the amino acid sequence: 
       
         
           
                 
               
                   (SEQ ID NO: 17) 
                 
                   APARSPSPSTQPWEHVNAIQEARRLLNLSRDTAAEMNETVEVISEMFDL 
                 
                     
                 
                   QEPTCLQTRLELYKQGLRGSLTKLKGPLTMMASHYKQHCPPTPETSCAT 
                 
                     
                 
                   QIITFESFKENLKDFLLVIPFDCWEPVQEGAEAAAKEAAAKAGARRGVR 
                 
                     
                 
                   VAWREPGRMELNMPHGQE. 
                 
             
                
                
                
                
                
                
                
                
               
            
           
         
       
     
     
         88 . The method of  claim 87 , wherein the fusion polypeptide further comprises a purification tag or an export signal peptide. 
     
     
         89 . The method of  claim 85 , wherein fusion polypeptide comprises the amino acid sequence: 
       
         
           
                 
               
                   (SEQ ID NO: 18) 
                 
                   APARSPSPSTQPWEHVNAIQEARRLLNLSRDTAAEMNETVEVISEMFDL 
                 
                     
                 
                   QEPTCLQTRLELYKQGLRGSLTKLKGPLTMMASHYKQHCPPTPETSCAT 
                 
                     
                 
                   QIITFESFKENLKDFLLVIPFDCWEPVQEGSAGSAAGSGARRGVRVAWR 
                 
                     
                 
                   EPGRMELNMPHGQE. 
                 
             
                
                
                
                
                
                
                
                
               
            
           
         
       
     
     
         90 . The method of  claim 89 , wherein the fusion polypeptide further comprises a purification tag or an export signal peptide. 
     
     
         91 . The method of  claim 85 , wherein fusion polypeptide comprises the amino acid sequence: 
       
         
           
                 
               
                   (SEQ ID NO: 19) 
                 
                   METDTLLLWVLLLWVPGSTGHHHHHHHHHHENLYFQGAPARSPSPSTQPW 
                 
                     
                 
                   EHVNAIQEARRLLNLSRDTAAEMNETVEVISEMFDLQEPTCLQTRLELYK 
                 
                     
                 
                   QGLRGSLTKLKGPLTMIVIASHYKQHCPPTPETSCATQIITFESFKENLK 
                 
                     
                 
                   DFLLVIPFDCWEPVQEGAEAAAKEAAAKAGARRGVRVAWREPGRMELNMP 
                 
                     
                 
                   HGQE. 
                 
             
                
                
                
                
                
                
                
                
                
                
               
            
           
         
       
     
     
         92 . The method of  claim 91 , wherein the fusion polypeptide further comprises a purification tag or an export signal peptide. 
     
     
         93 . The method of  claim 85 , wherein fusion polypeptide comprises the amino acid sequence: 
       
         
           
                 
               
                   (SEQ ID NO: 40) 
                 
                   METDTLLLWVLLLWVPGSTGHHHHHHHHHHENLYFQGAPARSPSPSTQP 
                 
                     
                 
                   WEHVNAIQEARRLLNLSRDTAAEMNETVEVISEWDLQEPTCLQTRLELY 
                 
                     
                 
                   KQGLRGSLTKLKGPLTMMASHYKQHCPPTPETSCATQIITFESFKENLK 
                 
                     
                 
                   DFLLVIPFDCWEPVQEGSAGSAAGSGARRGVRVAWREPGRMELNMPHGQ 
                 
                     
                 
                   E. 
                 
             
                
                
                
                
                
                
                
                
                
                
               
            
           
         
       
     
     
         94 . The method of  claim 93 , wherein the fusion polypeptide further comprises a purification tag or an export signal peptide. 
     
     
         95 . The method of  claim 85 , wherein fusion polypeptide comprises the amino acid sequence: 
       
         
           
                 
               
                   (SEQ ID NO: 36) 
                 
                   METDTLLLWVLLLWVPGSTGHHHHHHHHHHENLYFQGARRGVHVGWREP 
                 
                     
                 
                   GRMELNMPHGGAEAAAKEAAAKAGAPARSPSPSTQPWEHVNAIQEARRL 
                 
                     
                 
                   LNLSRDTAAEMNETVEVISEMFDLQEPTCLQTRLELYKQGLRGSLTKLK 
                 
                     
                 
                   GPLTMMASHYKQHCPPTPETSCATQIITFESFKENLKDFLLVIPFDCWE 
                 
                     
                 
                   PVQE. 
                 
             
                
                
                
                
                
                
                
                
                
                
               
            
           
         
       
     
     
         96 . The method of  claim 95 , wherein the fusion polypeptide further comprises a purification tag or an export signal peptide. 
     
     
         97 . The method of  claim 85 , wherein fusion polypeptide comprises the amino acid sequence: 
       
         
           
                 
               
                   (SEQ ID NO: 39) 
                 
                   RRGVHVGWREPGRMELNMPHGGAEAAAKEAAAKAGAPARSPSPSTQPWE 
                 
                     
                 
                   HVNAIQEARRLLNLSRDTAAEMNETVEVISEWDLQEPTCLQTRLELYKQ 
                 
                     
                 
                   GLRGSLTKLKGPLTMMASHYKQHCPPTPETSCATQIITFESFKENLKDF 
                 
                     
                 
                   LLVIPFDCWEPVQE. 
                 
             
                
                
                
                
                
                
                
                
               
            
           
         
       
     
     
         98 . The method of  claim 97 , wherein the fusion polypeptide further comprises a purification tag or an export signal peptide. 
     
     
         99 . The method of  claim 85 , wherein the infection is selected from the group consisting of a viral infection, a bacterial infection, a protozoal infection, and a fungal infection. 
     
     
         100 . The method of  claim 99 , wherein the infection is a viral infection and the virus is selected from the group consisting of hepatitis, human immunodeficiency virus (HIV, e.g., HIV-1), and herpesvirus (e.g., HHV-8). 
     
     
         101 . The method of  claim 99 , wherein the infection is a bacterial infection and the bacteria is tuberculosis. 
     
     
         102 . The method of  claim 99 , wherein the infection is a protozoal infection and the protozoa is  mycoplasma  or  chlamydia.    
     
     
         103 . The method of  claim 99 , wherein the infection is a fungal infection and the fungus is  aspergillus.    
     
     
         104 . A method of treating cancer in a subject comprising administering to a subject in need of such treatment a fusion polypeptide comprising an amino acid sequence selected from the group consisting of:
 APARSPSPSTQPWEHVNAIQEARRLLNLSRDTAAEMNETVEVISEMFDLQEPTCLQTRLE LYKQGLRGSLTKLKGPLTMMASHYKQHCPPTPETSCATQIITFESFKENLKDFLLVIPFDC WEPVQEGAEAAAKEAAAKAGARRGVRVAWREPGRMELNMPHGQE (SEQ ID NO: 17);   APARSPSPSTQPWEHVNAIQEARRLLNLSRDTAAEMNETVEVISEMFDLQEPTCLQTRLE LYKQGLRGSLTKLKGPLTMMASHYKQHCPPTPETSCATQIITFESFKENLKDFLLVIPFDC WEPVQEGSAGSAAGSGARRGVRVAWREPGRMELNMPHGQE (SEQ ID NO: 18);   METDTLLLWVLLLWVPGSTGEEFEHTEHTIEEHTEHENLYFQGAPARSPSPSTQPWEHVNAIQE ARRLLNLSRDTAAEMNETVEVISEWDLQEPTCLQTRLELYKQGLRGSLTKLKGPLTMM ASHYKQHCPPTPETSCATQIITFESFKENLKDFLLVIPFDCWEPVQEGAEAAAKEAAAKA GARRGVRVAWREPGRMELNMPHGQE (SEQ ID NO: 19);   METDTLLLWVLLLWVPGSTGEEFEHTEHTIRFEFEHENLYFQGAPARSPSPSTQPWEHVNAIQE ARRLLNLSRDTAAEMNETVEVISEWDLQEPTCLQTRLELYKQGLRGSLTKLKGPLTMM ASHYKQHCPPTPETSCATQIITFESFKENLKDFLLVIPFDCWEPVQEGSAGSAAGSGARR GVRVAWREPGRMELNMPHGQE (SEQ ID NO: 40);   METDTLLLWVLLLWVPGSTGEEFEHTEHTIRFEFEHENLYFQGARRGVHVGWREPGRMELN MPHGGAEAAAKEAAAKAGAPARSPSPSTQPWEHVNAIQEARRLLNLSRDTAAEMNET VEVISEMFDLQEPTCLQTRLELYKQGLRGSLTKLKGPLTMMASHYKQHCPPTPETSCAT QIITFESFKENLKDFLLVIPFDCWEPVQE (SEQ ID NO: 36); and   RRGVHVGWREPGRMELNMPHGGAEAAAKEAAAKAGAPARSPSPSTQPWEHVNAIQEA RRLLNLSRDTAAEMNETVEVISEWDLQEPTCLQTRLELYKQGLRGSLTKLKGPLTMMA SHYKQHCPPTPETSCATQIITFESFKENLKDFLLVIPFDCWEPVQE (SEQ ID NO: 39) in an amount sufficient to treat the cancer.   
     
     
         105 . The method of  claim 104 , wherein the fusion polypeptide further comprises a purification tag or an export signal peptide. 
     
     
         106 . The method of  claim 104 , wherein fusion polypeptide comprises the amino acid sequence: 
       
         
           
                 
               
                   (SEQ ID NO: 17) 
                 
                   APARSPSPSTQPWEHVNAIQEARRLLNLSRDTAAEMNETVEVISEMFDL 
                 
                     
                 
                   QEPTCLQTRLELYKQGLRGSLTKLKGPLTMMASHYKQHCPPTPETSCAT 
                 
                     
                 
                   QIITFESFKENLKDFLLVIPFDCWEPVQEGAEAAAKEAAAKAGARRGVR 
                 
                     
                 
                   VAWREPGRMELNMPHGQE. 
                 
             
                
                
                
                
                
                
                
                
               
            
           
         
       
     
     
         107 . The method of  claim 106 , wherein the fusion polypeptide further comprises a purification tag or an export signal peptide. 
     
     
         108 . The method of  claim 104 , wherein fusion polypeptide comprises the amino acid sequence: 
       
         
           
                 
               
                   (SEQ ID NO: 18) 
                 
                   APARSPSPSTQPWEHVNAIQEARRLLNLSRDTAAEMNETVEVISEMFDL 
                 
                     
                 
                   QEPTCLQTRLELYKQGLRGSLTKLKGPLTMMASHYKQHCPPTPETSCAT 
                 
                     
                 
                   QIITFESFKENLKDFLLVIPFDCWEPVQEGSAGSAAGSGARRGVRVAWR 
                 
                     
                 
                   EPGRMELNMPHGQE. 
                 
             
                
                
                
                
                
                
                
                
               
            
           
         
       
     
     
         109 . The method of  claim 108 , wherein the fusion polypeptide further comprises a purification tag or an export signal peptide. 
     
     
         110 . The method of  claim 104 , wherein fusion polypeptide comprises the amino acid sequence: 
       
         
           
                 
               
                   (SEQ ID NO: 19) 
                 
                   METDTLLLWVLLLWVPGSTGHHHHHHHHHHENLYFQGAPARSPSPSTQP 
                 
                     
                 
                   WEHVNAIQEARRLLNLSRDTAAEMNETVEVISEWDLQEPTCLQTRLELY 
                 
                     
                 
                   KQGLRGSLTKLKGPLTIMMASHYKQHCPPTPETSCATQIITFESFKENL 
                 
                     
                 
                   KDFLLVIPFDCWEPVQEGAEAAAKEAAAKAGARRGVRVAWREPGRMELN 
                 
                     
                 
                   MPHGQE. 
                 
             
                
                
                
                
                
                
                
                
                
                
               
            
           
         
       
     
     
         111 . The method of  claim 110 , wherein the fusion polypeptide further comprises a purification tag or an export signal peptide. 
     
     
         112 . The method of  claim 104 , wherein fusion polypeptide comprises the amino acid sequence: 
       
         
           
                 
               
                   (SEQ ID NO: 40) 
                 
                   METDTLLLWVLLLWVPGSTGRHHHHHHHHHHENLYFQGAPARSPSPSTQ 
                 
                     
                 
                   PWEHVNAIQEARRLLNLSRDTAAEMNETVEVISEWDLQEPTCLQTRLEL 
                 
                     
                 
                   YKQGLRGSLTKLKGPLTMMASHYKQHCPPTPETSCATQIITFESFKENL 
                 
                     
                 
                   KDFLLVIPFDCWEPVQEGSAGSAAGSGARRGVRVAWREPGRMELNMPHG 
                 
                     
                 
                   QE. 
                 
             
                
                
                
                
                
                
                
                
                
                
               
            
           
         
       
     
     
         113 . The method of  claim 112 , wherein the fusion polypeptide further comprises a purification tag or an export signal peptide. 
     
     
         114 . The method of  claim 104 , wherein fusion polypeptide comprises the amino acid sequence: 
       
         
           
                 
               
                   (SEQ ID NO: 36) 
                 
                   METDTLLLWVLLLWVPGSTGEHHHHHHHHHHEENLYFQGARRGVHVGWR 
                 
                     
                 
                   EPGRMELNMPHGGAEAAAKEAAAKAGAPARSPSPSTQPWEHVNAIQEAR 
                 
                     
                 
                   RLLNLSRDTAAEMNETVEVISEMFDLQEPTCLQTRLELYKQGLRGSLTK 
                 
                     
                 
                   LKGPLTMMASHYKQHCPPTPETSCATQIITFESFKENLKDFLLVIPFDC 
                 
                     
                 
                   WEPVQE. 
                 
             
                
                
                
                
                
                
                
                
                
                
               
            
           
         
       
     
     
         115 . The method of  claim 114 , wherein the fusion polypeptide further comprises a purification tag or an export signal peptide. 
     
     
         116 . The method of  claim 104 , wherein fusion polypeptide comprises the amino acid sequence: 
       
         
           
                 
               
                   (SEQ ID NO: 39) 
                 
                   RRGVHVGWREPGRMELNMPHGGAEAAAKEAAAKAGAPARSPSPSTQPWE 
                 
                     
                 
                   HVNAIQEARRLLNLSRDTAAEMNETVEVISEWDLQEPTCLQTRLELYKQ 
                 
                     
                 
                   GLRGSLTKLKGPLTMMASHYKQHCPPTPETSCATQIITFESFKENLKDF 
                 
                     
                 
                   LLVIPFDCWEPVQE. 
                 
             
                
                
                
                
                
                
                
                
               
            
           
         
       
     
     
         117 . The method of  claim 116 , wherein the fusion polypeptide further comprises a purification tag or an export signal peptide.

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