               SEQUENCE LISTING

<110> Bayer AG
      Bayer Pharma AG
      Deutsches Krebsforschungszentrum (DKFZ)

<120> SUBSTITUTED AMINOQUINOLONES AS DGKALPHA INHIBITORS FOR IMMUNE ACTIVATION

<130> BHC193047FC

<160> 5

<170> BiSSAP 1.3.6

<210> 1
<211> 743
<212> PRT
<213> human


<220> 
<223> human DGKa M1 to S735 plus C-terminal Flag-Tag

<400> 1
Met Ala Lys Glu Arg Gly Leu Ile Ser Pro Ser Asp Phe Ala Gln Leu 
1               5                   10                  15      
Gln Lys Tyr Met Glu Tyr Ser Thr Lys Lys Val Ser Asp Val Leu Lys 
            20                  25                  30          
Leu Phe Glu Asp Gly Glu Met Ala Lys Tyr Val Gln Gly Asp Ala Ile 
        35                  40                  45              
Gly Tyr Glu Gly Phe Gln Gln Phe Leu Lys Ile Tyr Leu Glu Val Asp 
    50                  55                  60                  
Asn Val Pro Arg His Leu Ser Leu Ala Leu Phe Gln Ser Phe Glu Thr 
65                  70                  75                  80  
Gly His Cys Leu Asn Glu Thr Asn Val Thr Lys Asp Val Val Cys Leu 
                85                  90                  95      
Asn Asp Val Ser Cys Tyr Phe Ser Leu Leu Glu Gly Gly Arg Pro Glu 
            100                 105                 110         
Asp Lys Leu Glu Phe Thr Phe Lys Leu Tyr Asp Thr Asp Arg Asn Gly 
        115                 120                 125             
Ile Leu Asp Ser Ser Glu Val Asp Lys Ile Ile Leu Gln Met Met Arg 
    130                 135                 140                 
Val Ala Glu Tyr Leu Asp Trp Asp Val Ser Glu Leu Arg Pro Ile Leu 
145                 150                 155                 160 
Gln Glu Met Met Lys Glu Ile Asp Tyr Asp Gly Ser Gly Ser Val Ser 
                165                 170                 175     
Gln Ala Glu Trp Val Arg Ala Gly Ala Thr Thr Val Pro Leu Leu Val 
            180                 185                 190         
Leu Leu Gly Leu Glu Met Thr Leu Lys Asp Asp Gly Gln His Met Trp 
        195                 200                 205             
Arg Pro Lys Arg Phe Pro Arg Pro Val Tyr Cys Asn Leu Cys Glu Ser 
    210                 215                 220                 
Ser Ile Gly Leu Gly Lys Gln Gly Leu Ser Cys Asn Leu Cys Lys Tyr 
225                 230                 235                 240 
Thr Val His Asp Gln Cys Ala Met Lys Ala Leu Pro Cys Glu Val Ser 
                245                 250                 255     
Thr Tyr Ala Lys Ser Arg Lys Asp Ile Gly Val Gln Ser His Val Trp 
            260                 265                 270         
Val Arg Gly Gly Cys Glu Ser Gly Arg Cys Asp Arg Cys Gln Lys Lys 
        275                 280                 285             
Ile Arg Ile Tyr His Ser Leu Thr Gly Leu His Cys Val Trp Cys His 
    290                 295                 300                 
Leu Glu Ile His Asp Asp Cys Leu Gln Ala Val Gly His Glu Cys Asp 
305                 310                 315                 320 
Cys Gly Leu Leu Arg Asp His Ile Leu Pro Pro Ser Ser Ile Tyr Pro 
                325                 330                 335     
Ser Val Leu Ala Ser Gly Pro Asp Arg Lys Asn Ser Lys Thr Ser Gln 
            340                 345                 350         
Lys Thr Met Asp Asp Leu Asn Leu Ser Thr Ser Glu Ala Leu Arg Ile 
        355                 360                 365             
Asp Pro Val Pro Asn Thr His Pro Leu Leu Val Phe Val Asn Pro Lys 
    370                 375                 380                 
Ser Gly Gly Lys Gln Gly Gln Arg Val Leu Trp Lys Phe Gln Tyr Ile 
385                 390                 395                 400 
Leu Asn Pro Arg Gln Val Phe Asn Leu Leu Lys Asp Gly Pro Glu Ile 
                405                 410                 415     
Gly Leu Arg Leu Phe Lys Asp Val Pro Asp Ser Arg Ile Leu Val Cys 
            420                 425                 430         
Gly Gly Asp Gly Thr Val Gly Trp Ile Leu Glu Thr Ile Asp Lys Ala 
        435                 440                 445             
Asn Leu Pro Val Leu Pro Pro Val Ala Val Leu Pro Leu Gly Thr Gly 
    450                 455                 460                 
Asn Asp Leu Ala Arg Cys Leu Arg Trp Gly Gly Gly Tyr Glu Gly Gln 
465                 470                 475                 480 
Asn Leu Ala Lys Ile Leu Lys Asp Leu Glu Met Ser Lys Val Val His 
                485                 490                 495     
Met Asp Arg Trp Ser Val Glu Val Ile Pro Gln Gln Thr Glu Glu Lys 
            500                 505                 510         
Ser Asp Pro Val Pro Phe Gln Ile Ile Asn Asn Tyr Phe Ser Ile Gly 
        515                 520                 525             
Val Asp Ala Ser Ile Ala His Arg Phe His Ile Met Arg Glu Lys Tyr 
    530                 535                 540                 
Pro Glu Lys Phe Asn Ser Arg Met Lys Asn Lys Leu Trp Tyr Phe Glu 
545                 550                 555                 560 
Phe Ala Thr Ser Glu Ser Ile Phe Ser Thr Cys Lys Lys Leu Glu Glu 
                565                 570                 575     
Ser Leu Thr Val Glu Ile Cys Gly Lys Pro Leu Asp Leu Ser Asn Leu 
            580                 585                 590         
Ser Leu Glu Gly Ile Ala Val Leu Asn Ile Pro Ser Met His Gly Gly 
        595                 600                 605             
Ser Asn Leu Trp Gly Asp Thr Arg Arg Pro His Gly Asp Ile Tyr Gly 
    610                 615                 620                 
Ile Asn Gln Ala Leu Gly Ala Thr Ala Lys Val Ile Thr Asp Pro Asp 
625                 630                 635                 640 
Ile Leu Lys Thr Cys Val Pro Asp Leu Ser Asp Lys Arg Leu Glu Val 
                645                 650                 655     
Val Gly Leu Glu Gly Ala Ile Glu Met Gly Gln Ile Tyr Thr Lys Leu 
            660                 665                 670         
Lys Asn Ala Gly Arg Arg Leu Ala Lys Cys Ser Glu Ile Thr Phe His 
        675                 680                 685             
Thr Thr Lys Thr Leu Pro Met Gln Ile Asp Gly Glu Pro Trp Met Gln 
    690                 695                 700                 
Thr Pro Cys Thr Ile Lys Ile Thr His Lys Asn Gln Met Pro Met Leu 
705                 710                 715                 720 
Met Gly Pro Pro Pro Arg Ser Thr Asn Phe Phe Gly Phe Leu Ser Asp 
                725                 730                 735     
Tyr Lys Asp Asp Asp Asp Lys 
            740             

<210> 2
<211> 793
<212> PRT
<213> human


<220> 
<223> human DGKa M1 to S735 plus N-terminal Avi-Tag and C-terminal
      Flag-Tag, DGKa_hu_1Avi

<400> 2
Met Thr Ser His His His His His His Ser Ser Met Gly Ser Arg Gly 
1               5                   10                  15      
Ile Glu Gly Arg Gly Gly Leu Asn Asp Ile Phe Glu Ala Gln Lys Ile 
            20                  25                  30          
Glu Trp His Glu Gly Ser Arg Thr Ser Leu Tyr Lys Lys Ala Gly Ser 
        35                  40                  45              
Ala Thr Met Ala Lys Glu Arg Gly Leu Ile Ser Pro Ser Asp Phe Ala 
    50                  55                  60                  
Gln Leu Gln Lys Tyr Met Glu Tyr Ser Thr Lys Lys Val Ser Asp Val 
65                  70                  75                  80  
Leu Lys Leu Phe Glu Asp Gly Glu Met Ala Lys Tyr Val Gln Gly Asp 
                85                  90                  95      
Ala Ile Gly Tyr Glu Gly Phe Gln Gln Phe Leu Lys Ile Tyr Leu Glu 
            100                 105                 110         
Val Asp Asn Val Pro Arg His Leu Ser Leu Ala Leu Phe Gln Ser Phe 
        115                 120                 125             
Glu Thr Gly His Cys Leu Asn Glu Thr Asn Val Thr Lys Asp Val Val 
    130                 135                 140                 
Cys Leu Asn Asp Val Ser Cys Tyr Phe Ser Leu Leu Glu Gly Gly Arg 
145                 150                 155                 160 
Pro Glu Asp Lys Leu Glu Phe Thr Phe Lys Leu Tyr Asp Thr Asp Arg 
                165                 170                 175     
Asn Gly Ile Leu Asp Ser Ser Glu Val Asp Lys Ile Ile Leu Gln Met 
            180                 185                 190         
Met Arg Val Ala Glu Tyr Leu Asp Trp Asp Val Ser Glu Leu Arg Pro 
        195                 200                 205             
Ile Leu Gln Glu Met Met Lys Glu Ile Asp Tyr Asp Gly Ser Gly Ser 
    210                 215                 220                 
Val Ser Gln Ala Glu Trp Val Arg Ala Gly Ala Thr Thr Val Pro Leu 
225                 230                 235                 240 
Leu Val Leu Leu Gly Leu Glu Met Thr Leu Lys Asp Asp Gly Gln His 
                245                 250                 255     
Met Trp Arg Pro Lys Arg Phe Pro Arg Pro Val Tyr Cys Asn Leu Cys 
            260                 265                 270         
Glu Ser Ser Ile Gly Leu Gly Lys Gln Gly Leu Ser Cys Asn Leu Cys 
        275                 280                 285             
Lys Tyr Thr Val His Asp Gln Cys Ala Met Lys Ala Leu Pro Cys Glu 
    290                 295                 300                 
Val Ser Thr Tyr Ala Lys Ser Arg Lys Asp Ile Gly Val Gln Ser His 
305                 310                 315                 320 
Val Trp Val Arg Gly Gly Cys Glu Ser Gly Arg Cys Asp Arg Cys Gln 
                325                 330                 335     
Lys Lys Ile Arg Ile Tyr His Ser Leu Thr Gly Leu His Cys Val Trp 
            340                 345                 350         
Cys His Leu Glu Ile His Asp Asp Cys Leu Gln Ala Val Gly His Glu 
        355                 360                 365             
Cys Asp Cys Gly Leu Leu Arg Asp His Ile Leu Pro Pro Ser Ser Ile 
    370                 375                 380                 
Tyr Pro Ser Val Leu Ala Ser Gly Pro Asp Arg Lys Asn Ser Lys Thr 
385                 390                 395                 400 
Ser Gln Lys Thr Met Asp Asp Leu Asn Leu Ser Thr Ser Glu Ala Leu 
                405                 410                 415     
Arg Ile Asp Pro Val Pro Asn Thr His Pro Leu Leu Val Phe Val Asn 
            420                 425                 430         
Pro Lys Ser Gly Gly Lys Gln Gly Gln Arg Val Leu Trp Lys Phe Gln 
        435                 440                 445             
Tyr Ile Leu Asn Pro Arg Gln Val Phe Asn Leu Leu Lys Asp Gly Pro 
    450                 455                 460                 
Glu Ile Gly Leu Arg Leu Phe Lys Asp Val Pro Asp Ser Arg Ile Leu 
465                 470                 475                 480 
Val Cys Gly Gly Asp Gly Thr Val Gly Trp Ile Leu Glu Thr Ile Asp 
                485                 490                 495     
Lys Ala Asn Leu Pro Val Leu Pro Pro Val Ala Val Leu Pro Leu Gly 
            500                 505                 510         
Thr Gly Asn Asp Leu Ala Arg Cys Leu Arg Trp Gly Gly Gly Tyr Glu 
        515                 520                 525             
Gly Gln Asn Leu Ala Lys Ile Leu Lys Asp Leu Glu Met Ser Lys Val 
    530                 535                 540                 
Val His Met Asp Arg Trp Ser Val Glu Val Ile Pro Gln Gln Thr Glu 
545                 550                 555                 560 
Glu Lys Ser Asp Pro Val Pro Phe Gln Ile Ile Asn Asn Tyr Phe Ser 
                565                 570                 575     
Ile Gly Val Asp Ala Ser Ile Ala His Arg Phe His Ile Met Arg Glu 
            580                 585                 590         
Lys Tyr Pro Glu Lys Phe Asn Ser Arg Met Lys Asn Lys Leu Trp Tyr 
        595                 600                 605             
Phe Glu Phe Ala Thr Ser Glu Ser Ile Phe Ser Thr Cys Lys Lys Leu 
    610                 615                 620                 
Glu Glu Ser Leu Thr Val Glu Ile Cys Gly Lys Pro Leu Asp Leu Ser 
625                 630                 635                 640 
Asn Leu Ser Leu Glu Gly Ile Ala Val Leu Asn Ile Pro Ser Met His 
                645                 650                 655     
Gly Gly Ser Asn Leu Trp Gly Asp Thr Arg Arg Pro His Gly Asp Ile 
            660                 665                 670         
Tyr Gly Ile Asn Gln Ala Leu Gly Ala Thr Ala Lys Val Ile Thr Asp 
        675                 680                 685             
Pro Asp Ile Leu Lys Thr Cys Val Pro Asp Leu Ser Asp Lys Arg Leu 
    690                 695                 700                 
Glu Val Val Gly Leu Glu Gly Ala Ile Glu Met Gly Gln Ile Tyr Thr 
705                 710                 715                 720 
Lys Leu Lys Asn Ala Gly Arg Arg Leu Ala Lys Cys Ser Glu Ile Thr 
                725                 730                 735     
Phe His Thr Thr Lys Thr Leu Pro Met Gln Ile Asp Gly Glu Pro Trp 
            740                 745                 750         
Met Gln Thr Pro Cys Thr Ile Lys Ile Thr His Lys Asn Gln Met Pro 
        755                 760                 765             
Met Leu Met Gly Pro Pro Pro Arg Ser Thr Asn Phe Phe Gly Phe Leu 
    770                 775                 780                 
Ser Asp Tyr Lys Asp Asp Asp Asp Lys 
785                 790             

<210> 3
<211> 8
<212> PRT
<213> human


<220> 
<223> SIINFEKL amino acid sequence

<400> 3
Ser Ile Ile Asn Phe Glu Lys Leu 
1               5               

<210> 4
<211> 8
<212> PRT
<213> human


<220> 
<223> Flag-Tag sequence

<400> 4
Asp Tyr Lys Asp Asp Asp Asp Lys 
1               5               

<210> 5
<211> 30
<212> PRT
<213> human


<220> 
<223> OVA-30 peptide sequence

<400> 5
Ser Met Leu Val Leu Leu Pro Asp Glu Val Ser Gly Leu Glu Gln Leu 
1               5                   10                  15      
Glu Ser Ile Ile Asn Phe Glu Lys Leu Thr Glu Trp Thr Ser 
            20                  25                  30  

