                         SEQUENCE LISTING

<110>  Bayer AG
       Bayer Pharma AG
 
<120>  MASP inhibitory compounds and uses thereof

<130>  BHC171044WO

<160>  10    

<170>  PatentIn version 3.5

<210>  1
<211>  14
<212>  PRT
<213>  Artificial Sequence

<220>
<223>  SFMI-1


<220>
<221>  DISULFID
<222>  (3)..(11)
<223>  disulfide bond;

<220>
<221>  DISULFID
<222>  (3)..(11)
<223>  disulfide bond

<400>  1

Gly Ile Cys Ser Arg Ser Leu Pro Pro Ile Cys Ile Pro Asp 
1               5                   10                  


<210>  2
<211>  430
<212>  PRT
<213>  Artificial Sequence

<220>
<223>  MASP-1_Human_Sequence fragment_C-terminal His Tag and N-terminal 
       Ig-kappa secretion signal

<400>  2

Met Glu Thr Asp Thr Leu Leu Leu Trp Val Leu Leu Leu Trp Val Pro 
1               5                   10                  15      


Gly Ser Thr Gly Asp Ala Gly Asn Glu Cys Pro Glu Leu Gln Pro Pro 
            20                  25                  30          


Val His Gly Lys Ile Glu Pro Ser Gln Ala Lys Tyr Phe Phe Lys Asp 
        35                  40                  45              


Gln Val Leu Val Ser Cys Asp Thr Gly Tyr Lys Val Leu Lys Asp Asn 
    50                  55                  60                  


Val Glu Met Asp Thr Phe Gln Ile Glu Cys Leu Lys Asp Gly Thr Trp 
65                  70                  75                  80  


Ser Asn Lys Ile Pro Thr Cys Lys Ile Val Asp Cys Arg Ala Pro Gly 
                85                  90                  95      


Glu Leu Glu His Gly Leu Ile Thr Phe Ser Thr Arg Asn Asn Leu Thr 
            100                 105                 110         


Thr Tyr Lys Ser Glu Ile Lys Tyr Ser Cys Gln Glu Pro Tyr Tyr Lys 
        115                 120                 125             


Met Leu Asn Asn Asn Thr Gly Ile Tyr Thr Cys Ser Ala Gln Gly Val 
    130                 135                 140                 


Trp Met Asn Lys Val Leu Gly Arg Ser Leu Pro Thr Cys Leu Pro Val 
145                 150                 155                 160 


Cys Gly Leu Pro Lys Phe Ser Arg Lys Leu Met Ala Arg Ile Phe Asn 
                165                 170                 175     


Gly Arg Pro Ala Gln Lys Gly Thr Thr Pro Trp Ile Ala Met Leu Ser 
            180                 185                 190         


His Leu Asn Gly Gln Pro Phe Cys Gly Gly Ser Leu Leu Gly Ser Ser 
        195                 200                 205             


Trp Ile Val Thr Ala Ala His Cys Leu His Gln Ser Leu Asp Pro Glu 
    210                 215                 220                 


Asp Pro Thr Leu Arg Asp Ser Asp Leu Leu Ser Pro Ser Asp Phe Lys 
225                 230                 235                 240 


Ile Ile Leu Gly Lys His Trp Arg Leu Arg Ser Asp Glu Asn Glu Gln 
                245                 250                 255     


His Leu Gly Val Lys His Thr Thr Leu His Pro Gln Tyr Asp Pro Asn 
            260                 265                 270         


Thr Phe Glu Asn Asp Val Ala Leu Val Glu Leu Leu Glu Ser Pro Val 
        275                 280                 285             


Leu Asn Ala Phe Val Met Pro Ile Cys Leu Pro Glu Gly Pro Gln Gln 
    290                 295                 300                 


Glu Gly Ala Met Val Ile Val Ser Gly Trp Gly Lys Gln Phe Leu Gln 
305                 310                 315                 320 


Arg Phe Pro Glu Thr Leu Met Glu Ile Glu Ile Pro Ile Val Asp His 
                325                 330                 335     


Ser Thr Cys Gln Lys Ala Tyr Ala Pro Leu Lys Lys Lys Val Thr Arg 
            340                 345                 350         


Asp Met Ile Cys Ala Gly Glu Lys Glu Gly Gly Lys Asp Ala Cys Ala 
        355                 360                 365             


Gly Asp Ser Gly Gly Pro Met Val Thr Leu Asn Arg Glu Arg Gly Gln 
    370                 375                 380                 


Trp Tyr Leu Val Gly Thr Val Ser Trp Gly Asp Asp Cys Gly Lys Lys 
385                 390                 395                 400 


Asp Arg Tyr Gly Val Tyr Ser Tyr Ile His His Asn Lys Asp Trp Ile 
                405                 410                 415     


Gln Arg Val Thr Gly Val Arg Asn His His His His His His 
            420                 425                 430 


<210>  3
<211>  417
<212>  PRT
<213>  Artificial Sequence

<220>
<223>  MASP-2_Human_Sequence fragment_C-terminal His Tag and N-terminal 
       Ig-kappa secretion signal

<400>  3

Met Glu Thr Asp Thr Leu Leu Leu Trp Val Leu Leu Leu Trp Val Pro 
1               5                   10                  15      


Gly Ser Thr Gly Asp Ala Gln Pro Cys Pro Tyr Pro Met Ala Pro Pro 
            20                  25                  30          


Asn Gly His Val Ser Pro Val Gln Ala Lys Tyr Ile Leu Lys Asp Ser 
        35                  40                  45              


Phe Ser Ile Phe Cys Glu Thr Gly Tyr Glu Leu Leu Gln Gly His Leu 
    50                  55                  60                  


Pro Leu Lys Ser Phe Thr Ala Val Cys Gln Lys Asp Gly Ser Trp Asp 
65                  70                  75                  80  


Arg Pro Met Pro Ala Cys Ser Ile Val Asp Cys Gly Pro Pro Asp Asp 
                85                  90                  95      


Leu Pro Ser Gly Arg Val Glu Tyr Ile Thr Gly Pro Gly Val Thr Thr 
            100                 105                 110         


Tyr Lys Ala Val Ile Gln Tyr Ser Cys Glu Glu Thr Phe Tyr Thr Met 
        115                 120                 125             


Lys Val Asn Asp Gly Lys Tyr Val Cys Glu Ala Asp Gly Phe Trp Thr 
    130                 135                 140                 


Ser Ser Lys Gly Glu Lys Ser Leu Pro Val Cys Glu Pro Val Cys Gly 
145                 150                 155                 160 


Leu Ser Ala Arg Thr Thr Gly Gly Arg Ile Tyr Gly Gly Gln Lys Ala 
                165                 170                 175     


Lys Pro Gly Asp Phe Pro Trp Gln Val Leu Ile Leu Gly Gly Thr Thr 
            180                 185                 190         


Ala Ala Gly Ala Leu Leu Tyr Asp Asn Trp Val Leu Thr Ala Ala His 
        195                 200                 205             


Ala Val Tyr Glu Gln Lys His Asp Ala Ser Ala Leu Asp Ile Arg Met 
    210                 215                 220                 


Gly Thr Leu Lys Arg Leu Ser Pro His Tyr Thr Gln Ala Trp Ser Glu 
225                 230                 235                 240 


Ala Val Phe Ile His Glu Gly Tyr Thr His Asp Ala Gly Phe Asp Asn 
                245                 250                 255     


Asp Ile Ala Leu Ile Lys Leu Asn Asn Lys Val Val Ile Asn Ser Asn 
            260                 265                 270         


Ile Thr Pro Ile Cys Leu Pro Arg Lys Glu Ala Glu Ser Phe Met Arg 
        275                 280                 285             


Thr Asp Asp Ile Gly Thr Ala Ser Gly Trp Gly Leu Thr Gln Arg Gly 
    290                 295                 300                 


Phe Leu Ala Arg Asn Leu Met Tyr Val Asp Ile Pro Ile Val Asp His 
305                 310                 315                 320 


Gln Lys Cys Thr Ala Ala Tyr Glu Lys Pro Pro Tyr Pro Arg Gly Ser 
                325                 330                 335     


Val Thr Ala Asn Met Leu Cys Ala Gly Leu Glu Ser Gly Gly Lys Asp 
            340                 345                 350         


Ser Cys Arg Gly Asp Ser Gly Gly Ala Leu Val Phe Leu Asp Ser Glu 
        355                 360                 365             


Thr Glu Arg Trp Phe Val Gly Gly Ile Val Ser Trp Gly Ser Met Asn 
    370                 375                 380                 


Cys Gly Glu Ala Gly Gln Tyr Gly Val Tyr Thr Lys Val Ile Asn Tyr 
385                 390                 395                 400 


Ile Pro Trp Ile Glu Asn Ile Ile Ser Asp Phe His His His His His 
                405                 410                 415     


His 
    


<210>  4
<211>  430
<212>  PRT
<213>  Artificial Sequence

<220>
<223>  MASP-1_Rat_Sequence fragment_C-terminal His Tag and N-terminal 
       Ig-kappa secretion signal

<400>  4

Met Glu Thr Asp Thr Leu Leu Leu Trp Val Leu Leu Leu Trp Val Pro 
1               5                   10                  15      


Gly Ser Thr Gly Asp Ala Gly Asn Glu Cys Pro Lys Leu Gln Pro Pro 
            20                  25                  30          


Val Tyr Gly Lys Ile Glu Pro Ser Gln Ala Val Tyr Ser Phe Lys Asp 
        35                  40                  45              


Gln Val Leu Ile Ser Cys Asp Thr Gly Tyr Lys Val Leu Lys Asp Asn 
    50                  55                  60                  


Glu Val Met Asp Thr Phe Gln Ile Glu Cys Leu Lys Asp Gly Ala Trp 
65                  70                  75                  80  


Ser Asn Lys Ile Pro Thr Cys Lys Ile Val Asp Cys Gly Val Pro Ala 
                85                  90                  95      


Val Leu Lys His Gly Leu Val Thr Phe Ser Thr Arg Asn Asn Leu Thr 
            100                 105                 110         


Thr Tyr Lys Ser Glu Ile Arg Tyr Ser Cys Gln Gln Pro Tyr Tyr Lys 
        115                 120                 125             


Met Leu His Asn Thr Thr Gly Val Tyr Thr Cys Ser Ala His Gly Thr 
    130                 135                 140                 


Trp Thr Asn Glu Val Leu Lys Arg Ser Leu Pro Thr Cys Leu Pro Val 
145                 150                 155                 160 


Cys Gly Leu Pro Lys Phe Ser Arg Lys His Ile Ser Arg Ile Phe Asn 
                165                 170                 175     


Gly Arg Pro Ala Gln Lys Gly Thr Thr Pro Trp Ile Ala Met Leu Ser 
            180                 185                 190         


Gln Leu Asn Gly Gln Pro Phe Cys Gly Gly Ser Leu Leu Gly Ser Asn 
        195                 200                 205             


Trp Val Leu Thr Ala Ala His Cys Leu His His Pro Leu Asp Pro Glu 
    210                 215                 220                 


Glu Pro Ile Leu His Asn Ser His Leu Leu Ser Pro Ser Asp Phe Lys 
225                 230                 235                 240 


Ile Ile Met Gly Lys His Trp Arg Arg Arg Ser Asp Glu Asp Glu Gln 
                245                 250                 255     


His Leu His Val Lys His Ile Met Leu His Pro Leu Tyr Asn Pro Ser 
            260                 265                 270         


Thr Phe Glu Asn Asp Leu Gly Leu Val Glu Leu Ser Glu Ser Pro Arg 
        275                 280                 285             


Leu Asn Asp Phe Val Met Pro Val Cys Leu Pro Glu His Pro Ser Thr 
    290                 295                 300                 


Glu Gly Thr Met Val Ile Val Ser Gly Trp Gly Lys Gln Phe Leu Gln 
305                 310                 315                 320 


Arg Leu Pro Glu Asn Leu Met Glu Ile Glu Ile Pro Ile Val Asn Tyr 
                325                 330                 335     


His Thr Cys Gln Glu Ala Tyr Thr Pro Leu Gly Lys Lys Val Thr Gln 
            340                 345                 350         


Asp Met Ile Cys Ala Gly Glu Lys Glu Gly Gly Lys Asp Ala Cys Ala 
        355                 360                 365             


Gly Asp Ser Gly Gly Pro Met Val Thr Lys Asp Ala Glu Arg Asp Gln 
    370                 375                 380                 


Trp Tyr Leu Val Gly Val Val Ser Trp Gly Glu Asp Cys Gly Lys Lys 
385                 390                 395                 400 


Asp Arg Tyr Gly Val Tyr Ser Tyr Ile Tyr Pro Asn Lys Asp Trp Ile 
                405                 410                 415     


Gln Arg Val Thr Gly Val Arg Asn His His His His His His 
            420                 425                 430 


<210>  5
<211>  417
<212>  PRT
<213>  Artificial Sequence

<220>
<223>  MASP-2_Rat_Sequence fragment_C-terminal His Tag and N-terminal 
       Ig-kappa secretion signal

<400>  5

Met Glu Thr Asp Thr Leu Leu Leu Trp Val Leu Leu Leu Trp Val Pro 
1               5                   10                  15      


Gly Ser Thr Gly Asp Thr Ala Gln Pro Cys Pro Asp Pro Thr Ala Pro 
            20                  25                  30          


Pro Asn Gly His Ile Ser Pro Val Gln Ala Thr Tyr Val Leu Lys Asp 
        35                  40                  45              


Ser Phe Ser Val Phe Cys Lys Thr Gly Phe Glu Leu Leu Gln Gly Ser 
    50                  55                  60                  


Val Pro Leu Lys Ser Phe Thr Ala Val Cys Gln Lys Asp Gly Ser Trp 
65                  70                  75                  80  


Asp Arg Pro Ile Pro Glu Cys Ser Ile Ile Asp Cys Gly Pro Pro Asp 
                85                  90                  95      


Asp Leu Pro Asn Gly His Val Asp Tyr Ile Thr Gly Pro Glu Val Thr 
            100                 105                 110         


Thr Tyr Lys Ala Val Ile Gln Tyr Ser Cys Glu Glu Thr Phe Tyr Thr 
        115                 120                 125             


Met Ser Ser Asn Gly Lys Tyr Val Cys Glu Ala Asp Gly Phe Trp Thr 
    130                 135                 140                 


Ser Ser Lys Gly Glu Lys Ser Leu Pro Val Cys Lys Pro Val Cys Gly 
145                 150                 155                 160 


Leu Ser Thr His Thr Ser Gly Gly Arg Ile Ile Gly Gly Gln Pro Ala 
                165                 170                 175     


Lys Pro Gly Asp Phe Pro Trp Gln Val Leu Leu Leu Gly Glu Thr Thr 
            180                 185                 190         


Ala Ala Gly Ala Leu Ile His Asp Asp Trp Val Leu Thr Ala Ala His 
        195                 200                 205             


Ala Val Tyr Gly Lys Thr Glu Ala Met Ser Ser Leu Asp Ile Arg Met 
    210                 215                 220                 


Gly Ile Leu Lys Arg Leu Ser Leu Ile Tyr Thr Gln Ala Trp Pro Glu 
225                 230                 235                 240 


Ala Val Phe Ile His Glu Gly Tyr Thr His Gly Ala Gly Phe Asp Asn 
                245                 250                 255     


Asp Ile Ala Leu Ile Lys Leu Lys Asn Lys Val Thr Ile Asn Arg Asn 
            260                 265                 270         


Ile Met Pro Ile Cys Leu Pro Arg Lys Glu Ala Ala Ser Leu Met Lys 
        275                 280                 285             


Thr Asp Phe Val Gly Thr Val Ala Gly Trp Gly Leu Thr Gln Lys Gly 
    290                 295                 300                 


Phe Leu Ala Arg Asn Leu Met Phe Val Asp Ile Pro Ile Val Asp His 
305                 310                 315                 320 


Gln Lys Cys Ala Thr Ala Tyr Thr Lys Gln Pro Tyr Pro Gly Ala Lys 
                325                 330                 335     


Val Thr Val Asn Met Leu Cys Ala Gly Leu Asp Arg Gly Gly Lys Asp 
            340                 345                 350         


Ser Cys Arg Gly Asp Ser Gly Gly Ala Leu Val Phe Leu Asp Asn Glu 
        355                 360                 365             


Thr Gln Arg Trp Phe Val Gly Gly Ile Val Ser Trp Gly Ser Ile Asn 
    370                 375                 380                 


Cys Gly Gly Ser Glu Gln Tyr Gly Val Tyr Thr Lys Val Thr Asn Tyr 
385                 390                 395                 400 


Ile Pro Trp Ile Glu Asn Ile Ile Asn Asn Phe His His His His His 
                405                 410                 415     


His 
    


<210>  6
<211>  11
<212>  PRT
<213>  Artificial Sequence

<220>
<223>  Fluorescence Resonance Energy Transfer substrate


<220>
<221>  Xaa
<222>  (1)..(1)
<223>  Xaa is 2-aminobenzoyl

<220>
<221>  MOD_RES
<222>  (10)..(10)
<223>  AMIDATION

<220>
<221>  Xaa
<222>  (11)..(11)
<223>  Xaa is a non peptidic capping group (2,4-dinitrophenyl; bound to 
       lysine amino group on position 6)

<400>  6

Xaa Met Tyr Gly Gly Ala Arg Arg Leu Lys Xaa 
1               5                   10      


<210>  7
<211>  13
<212>  PRT
<213>  Artificial Sequence

<220>
<223>  Fluorescence resonance energy transfer substrate


<220>
<221>  Xaa
<222>  (1)..(1)
<223>  Xaa is 4-((4-(dimethylamino)phenyl)azo)benzoic acid

<220>
<221>  MOD_RES
<222>  (12)..(12)
<223>  AMIDATION

<220>
<221>  Xaa
<222>  (13)..(13)
<223>  Xaa is 5-[(2-Aminoethyl) amino]naphthalene-1-sulfonyl (bound to 
       Glutamic acid caboxylic acid group on position 5)

<400>  7

Xaa Lys Ile Ser Pro Gln Gly Tyr Gly Arg Arg Glu Xaa 
1               5                   10              


<210>  8
<211>  11
<212>  PRT
<213>  Artificial Sequence

<220>
<223>  Fluorescence resonance energy transfer substrate


<220>
<221>  Xaa
<222>  (1)..(1)
<223>  Xaa is 4-((4-(dimethylamino)phenyl)azo)benzoic acid

<220>
<221>  MOD_RES
<222>  (10)..(10)
<223>  AMIDATION

<220>
<221>  Xaa
<222>  (11)..(11)
<223>  Xaa is 5-[(2-Aminoethyl) amino]naphthalene-1-sulfonyl (bound to 
       Glutamic acid caboxylic acid group on position 5)

<400>  8

Xaa Met Tyr Gly Gly Ala Arg Arg Leu Glu Xaa 
1               5                   10      


<210>  9
<211>  11
<212>  PRT
<213>  Artificial Sequence

<220>
<223>  Fluorescence resonance energy transfer substrate


<220>
<221>  Xaa
<222>  (1)..(1)
<223>  Xaa is 2-aminobenzoyl

<220>
<221>  MOD_RES
<222>  (10)..(10)
<223>  AMIDATION

<220>
<221>  Xaa
<222>  (11)..(11)
<223>  Xaa is a non peptidic capping group (2,4-dinitrophenyl; bound to 
       lysine amino group on position 6)

<400>  9

Xaa Ile Glu Gly Arg Thr Ser Glu Asp Lys Xaa 
1               5                   10      


<210>  10
<211>  14
<212>  PRT
<213>  Artificial Sequence

<220>
<223>  Ala-1 SFMI-1


<220>
<221>  DISULFID
<222>  (3)..(11)

<220>
<221>  DISULFID
<222>  (3)..(11)
<223>  disulfide bond

<400>  10

Ala Ile Cys Ser Arg Ser Leu Pro Pro Ile Cys Ile Pro Asp 
1               5                   10                  


