                         SEQUENCE LISTING

<110>  SOCPRA Sciences sante et Humaines s.e.c.
       RICHTER, Martin
       LEDUC, Richard
       COLOMBO, Eloic
       MARSAULT, Eric
 
<120>  MATRIPTASE INHIBITORS AND USES THEREOF AGAINST ORTHOMYXOVIRIDAE 
       INFECTIONS

<130>  765/14692.25

<150>  US 61/492,556
<151>  2011-06-02

<160>  8     

<170>  PatentIn version 3.5

<210>  1
<211>  2568
<212>  DNA
<213>  Homo sapiens


<220>
<221>  CDS
<222>  (1)..(2568)

<400>  1
atg ggg agc gat cgg gcc cgc aag ggc gga ggg ggc ccg aag gac ttc         48
Met Gly Ser Asp Arg Ala Arg Lys Gly Gly Gly Gly Pro Lys Asp Phe           
1               5                   10                  15                

ggc gcg gga ctc aag tac aac tcc cgg cac gag aaa gtg aat ggc ttg         96
Gly Ala Gly Leu Lys Tyr Asn Ser Arg His Glu Lys Val Asn Gly Leu           
            20                  25                  30                    

gag gaa ggc gtg gag ttc ctg cca gtc aac aac gtc aag aag gtg gaa        144
Glu Glu Gly Val Glu Phe Leu Pro Val Asn Asn Val Lys Lys Val Glu           
        35                  40                  45                        

aag cat ggc ccg ggg cgc tgg gtg gtg ctg gca gcc gtg ctg atc ggc        192
Lys His Gly Pro Gly Arg Trp Val Val Leu Ala Ala Val Leu Ile Gly           
    50                  55                  60                            

ctc ctc ttg gtc ttg ctg ggg atc ggc ttc ctg gtg tgg cat ttg cag        240
Leu Leu Leu Val Leu Leu Gly Ile Gly Phe Leu Val Trp His Leu Gln           
65                  70                  75                  80            

tac cgg gac gtg cgt gtc cag aag gtc ttc aat ggc tac atg agg atc        288
Tyr Arg Asp Val Arg Val Gln Lys Val Phe Asn Gly Tyr Met Arg Ile           
                85                  90                  95                

aca aat gag aat ttt gtg gat gcc tac gag aac tcc aac tcc act gag        336
Thr Asn Glu Asn Phe Val Asp Ala Tyr Glu Asn Ser Asn Ser Thr Glu           
            100                 105                 110                   

ttt gta agc ctg gcc agc aag gtg aag gac gcg ctg aag ctg ctg tac        384
Phe Val Ser Leu Ala Ser Lys Val Lys Asp Ala Leu Lys Leu Leu Tyr           
        115                 120                 125                       

agc gga gtc cca ttc ctg ggc ccc tac cac aag gag tcg gct gtg acg        432
Ser Gly Val Pro Phe Leu Gly Pro Tyr His Lys Glu Ser Ala Val Thr           
    130                 135                 140                           

gcc ttc agc gag ggc agc gtc atc gcc tac tac tgg tct gag ttc agc        480
Ala Phe Ser Glu Gly Ser Val Ile Ala Tyr Tyr Trp Ser Glu Phe Ser           
145                 150                 155                 160           

atc ccg cag cac ctg gtg gag gag gcc gag cgc gtc atg gcc gag gag        528
Ile Pro Gln His Leu Val Glu Glu Ala Glu Arg Val Met Ala Glu Glu           
                165                 170                 175               

cgc gta gtc atg ctg ccc ccg cgg gcg cgc tcc ttg aag tcc ttt gtg        576
Arg Val Val Met Leu Pro Pro Arg Ala Arg Ser Leu Lys Ser Phe Val           
            180                 185                 190                   

gtc acc tca gtg gtg gct ttc ccc acg gac tcc aaa aca gta cag agg        624
Val Thr Ser Val Val Ala Phe Pro Thr Asp Ser Lys Thr Val Gln Arg           
        195                 200                 205                       

acc cag gac aac agc tgc agc ttt ggc ctg cac gcc cgc ggt gtg gag        672
Thr Gln Asp Asn Ser Cys Ser Phe Gly Leu His Ala Arg Gly Val Glu           
    210                 215                 220                           

ctg atg cgc ttc acc acg ccc ggc ttc cct gac agc ccc tac ccc gct        720
Leu Met Arg Phe Thr Thr Pro Gly Phe Pro Asp Ser Pro Tyr Pro Ala           
225                 230                 235                 240           

cat gcc cgc tgc cag tgg gcc ctg cgg ggg gac gcc gac tca gtg ctg        768
His Ala Arg Cys Gln Trp Ala Leu Arg Gly Asp Ala Asp Ser Val Leu           
                245                 250                 255               

agc ctc acc ttc cgc agc ttt gac ctt gcg tcc tgc gac gag cgc ggc        816
Ser Leu Thr Phe Arg Ser Phe Asp Leu Ala Ser Cys Asp Glu Arg Gly           
            260                 265                 270                   

agc gac ctg gtg acg gtg tac aac acc ctg agc ccc atg gag ccc cac        864
Ser Asp Leu Val Thr Val Tyr Asn Thr Leu Ser Pro Met Glu Pro His           
        275                 280                 285                       

gcc ctg gtg cag ttg tgt ggc acc tac cct ccc tcc tac aac ctg acc        912
Ala Leu Val Gln Leu Cys Gly Thr Tyr Pro Pro Ser Tyr Asn Leu Thr           
    290                 295                 300                           

ttc cac tcc tcc cag aac gtc ctg ctc atc aca ctg ata acc aac act        960
Phe His Ser Ser Gln Asn Val Leu Leu Ile Thr Leu Ile Thr Asn Thr           
305                 310                 315                 320           

gag cgg cgg cat ccc ggc ttt gag gcc acc ttc ttc cag ctg cct agg       1008
Glu Arg Arg His Pro Gly Phe Glu Ala Thr Phe Phe Gln Leu Pro Arg           
                325                 330                 335               

atg agc agc tgt gga ggc cgc tta cgt aaa gcc cag ggg aca ttc aac       1056
Met Ser Ser Cys Gly Gly Arg Leu Arg Lys Ala Gln Gly Thr Phe Asn           
            340                 345                 350                   

agc ccc tac tac cca ggc cac tac cca ccc aac att gac tgc aca tgg       1104
Ser Pro Tyr Tyr Pro Gly His Tyr Pro Pro Asn Ile Asp Cys Thr Trp           
        355                 360                 365                       

aac att gag gtg ccc aac aac cag cat gtg aag gtg cgc ttc aaa ttc       1152
Asn Ile Glu Val Pro Asn Asn Gln His Val Lys Val Arg Phe Lys Phe           
    370                 375                 380                           

ttc tac ctg ctg gag ccc ggc gtg cct gcg ggc acc tgc ccc aag gac       1200
Phe Tyr Leu Leu Glu Pro Gly Val Pro Ala Gly Thr Cys Pro Lys Asp           
385                 390                 395                 400           

tac gtg gag atc aat ggg gag aaa tac tgc gga gag agg tcc cag ttc       1248
Tyr Val Glu Ile Asn Gly Glu Lys Tyr Cys Gly Glu Arg Ser Gln Phe           
                405                 410                 415               

gtc gtc acc agc aac agc aac aag atc aca gtt cgc ttc cac tca gat       1296
Val Val Thr Ser Asn Ser Asn Lys Ile Thr Val Arg Phe His Ser Asp           
            420                 425                 430                   

cag tcc tac acc gac acc ggc ttc tta gct gaa tac ctc tcc tac gac       1344
Gln Ser Tyr Thr Asp Thr Gly Phe Leu Ala Glu Tyr Leu Ser Tyr Asp           
        435                 440                 445                       

tcc agt gac cca tgc ccg ggg cag ttc acg tgc cgc acg ggg cgg tgt       1392
Ser Ser Asp Pro Cys Pro Gly Gln Phe Thr Cys Arg Thr Gly Arg Cys           
    450                 455                 460                           

atc cgg aag gag ctg cgc tgt gat ggc tgg gcc gac tgc acc gac cac       1440
Ile Arg Lys Glu Leu Arg Cys Asp Gly Trp Ala Asp Cys Thr Asp His           
465                 470                 475                 480           

agc gat gag ctc aac tgc agt tgc gac gcc ggc cac cag ttc acg tgc       1488
Ser Asp Glu Leu Asn Cys Ser Cys Asp Ala Gly His Gln Phe Thr Cys           
                485                 490                 495               

aag aac aag ttc tgc aag ccc ctc ttc tgg gtc tgc gac agt gtg aac       1536
Lys Asn Lys Phe Cys Lys Pro Leu Phe Trp Val Cys Asp Ser Val Asn           
            500                 505                 510                   

gac tgc gga gac aac agc gac gag cag ggg tgc agt tgt ccg gcc cag       1584
Asp Cys Gly Asp Asn Ser Asp Glu Gln Gly Cys Ser Cys Pro Ala Gln           
        515                 520                 525                       

acc ttc agg tgt tcc aat ggg aag tgc ctc tcg aaa agc cag cag tgc       1632
Thr Phe Arg Cys Ser Asn Gly Lys Cys Leu Ser Lys Ser Gln Gln Cys           
    530                 535                 540                           

aat ggg aag gac gac tgt ggg gac ggg tcc gac gag gcc tcc tgc ccc       1680
Asn Gly Lys Asp Asp Cys Gly Asp Gly Ser Asp Glu Ala Ser Cys Pro           
545                 550                 555                 560           

aag gtg aac gtc gtc act tgt acc aaa cac acc tac cgc tgc ctc aat       1728
Lys Val Asn Val Val Thr Cys Thr Lys His Thr Tyr Arg Cys Leu Asn           
                565                 570                 575               

ggg ctc tgc ttg agc aag ggc aac cct gag tgt gac ggg aag gag gac       1776
Gly Leu Cys Leu Ser Lys Gly Asn Pro Glu Cys Asp Gly Lys Glu Asp           
            580                 585                 590                   

tgt agc gac ggc tca gat gag aag gac tgc gac tgt ggg ctg cgg tca       1824
Cys Ser Asp Gly Ser Asp Glu Lys Asp Cys Asp Cys Gly Leu Arg Ser           
        595                 600                 605                       

ttc acg aga cag gct cgt gtt gtt ggg ggc acg gat gcg gat gag ggc       1872
Phe Thr Arg Gln Ala Arg Val Val Gly Gly Thr Asp Ala Asp Glu Gly           
    610                 615                 620                           

gag tgg ccc tgg cag gta agc ctg cat gct ctg ggc cag ggc cac atc       1920
Glu Trp Pro Trp Gln Val Ser Leu His Ala Leu Gly Gln Gly His Ile           
625                 630                 635                 640           

tgc ggt gct tcc ctc atc tct ccc aac tgg ctg gtc tct gcc gca cac       1968
Cys Gly Ala Ser Leu Ile Ser Pro Asn Trp Leu Val Ser Ala Ala His           
                645                 650                 655               

tgc tac atc gat gac aga gga ttc agg tac tca gac ccc acg cag tgg       2016
Cys Tyr Ile Asp Asp Arg Gly Phe Arg Tyr Ser Asp Pro Thr Gln Trp           
            660                 665                 670                   

acg gcc ttc ctg ggc ttg cac gac cag agc cag cgc agc gcc cct ggg       2064
Thr Ala Phe Leu Gly Leu His Asp Gln Ser Gln Arg Ser Ala Pro Gly           
        675                 680                 685                       

gtg cag gag cgc agg ctc aag cgc atc atc tcc cac ccc ttc ttc aat       2112
Val Gln Glu Arg Arg Leu Lys Arg Ile Ile Ser His Pro Phe Phe Asn           
    690                 695                 700                           

gac ttc acc ttc gac tat gac atc gcg ctg ctg gag ctg gag aaa ccg       2160
Asp Phe Thr Phe Asp Tyr Asp Ile Ala Leu Leu Glu Leu Glu Lys Pro           
705                 710                 715                 720           

gca gag tac agc tcc atg gtg cgg ccc atc tgc ctg ccg gac gcc tcc       2208
Ala Glu Tyr Ser Ser Met Val Arg Pro Ile Cys Leu Pro Asp Ala Ser           
                725                 730                 735               

cat gtc ttc cct gcc ggc aag gcc atc tgg gtc acg ggc tgg gga cac       2256
His Val Phe Pro Ala Gly Lys Ala Ile Trp Val Thr Gly Trp Gly His           
            740                 745                 750                   

acc cag tat gga ggc act ggc gcg ctg atc ctg caa aag ggt gag atc       2304
Thr Gln Tyr Gly Gly Thr Gly Ala Leu Ile Leu Gln Lys Gly Glu Ile           
        755                 760                 765                       

cgc gtc atc aac cag acc acc tgc gag aac ctc ctg ccg cag cag atc       2352
Arg Val Ile Asn Gln Thr Thr Cys Glu Asn Leu Leu Pro Gln Gln Ile           
    770                 775                 780                           

acg ccg cgc atg atg tgc gtg ggc ttc ctc agc ggc ggc gtg gac tcc       2400
Thr Pro Arg Met Met Cys Val Gly Phe Leu Ser Gly Gly Val Asp Ser           
785                 790                 795                 800           

tgc cag ggt gat tcc ggg gga ccc ctg tcc agc gtg gag gcg gat ggg       2448
Cys Gln Gly Asp Ser Gly Gly Pro Leu Ser Ser Val Glu Ala Asp Gly           
                805                 810                 815               

cgg atc ttc cag gcc ggt gtg gtg agc tgg gga gac ggc tgc gct cag       2496
Arg Ile Phe Gln Ala Gly Val Val Ser Trp Gly Asp Gly Cys Ala Gln           
            820                 825                 830                   

agg aac aag cca ggc gtg tac aca agg ctc cct ctg ttt cgg gac tgg       2544
Arg Asn Lys Pro Gly Val Tyr Thr Arg Leu Pro Leu Phe Arg Asp Trp           
        835                 840                 845                       

atc aaa gag aac act ggg gta tag                                       2568
Ile Lys Glu Asn Thr Gly Val                                               
    850                 855                                               


<210>  2
<211>  855
<212>  PRT
<213>  Homo sapiens

<400>  2

Met Gly Ser Asp Arg Ala Arg Lys Gly Gly Gly Gly Pro Lys Asp Phe 
1               5                   10                  15      


Gly Ala Gly Leu Lys Tyr Asn Ser Arg His Glu Lys Val Asn Gly Leu 
            20                  25                  30          


Glu Glu Gly Val Glu Phe Leu Pro Val Asn Asn Val Lys Lys Val Glu 
        35                  40                  45              


Lys His Gly Pro Gly Arg Trp Val Val Leu Ala Ala Val Leu Ile Gly 
    50                  55                  60                  


Leu Leu Leu Val Leu Leu Gly Ile Gly Phe Leu Val Trp His Leu Gln 
65                  70                  75                  80  


Tyr Arg Asp Val Arg Val Gln Lys Val Phe Asn Gly Tyr Met Arg Ile 
                85                  90                  95      


Thr Asn Glu Asn Phe Val Asp Ala Tyr Glu Asn Ser Asn Ser Thr Glu 
            100                 105                 110         


Phe Val Ser Leu Ala Ser Lys Val Lys Asp Ala Leu Lys Leu Leu Tyr 
        115                 120                 125             


Ser Gly Val Pro Phe Leu Gly Pro Tyr His Lys Glu Ser Ala Val Thr 
    130                 135                 140                 


Ala Phe Ser Glu Gly Ser Val Ile Ala Tyr Tyr Trp Ser Glu Phe Ser 
145                 150                 155                 160 


Ile Pro Gln His Leu Val Glu Glu Ala Glu Arg Val Met Ala Glu Glu 
                165                 170                 175     


Arg Val Val Met Leu Pro Pro Arg Ala Arg Ser Leu Lys Ser Phe Val 
            180                 185                 190         


Val Thr Ser Val Val Ala Phe Pro Thr Asp Ser Lys Thr Val Gln Arg 
        195                 200                 205             


Thr Gln Asp Asn Ser Cys Ser Phe Gly Leu His Ala Arg Gly Val Glu 
    210                 215                 220                 


Leu Met Arg Phe Thr Thr Pro Gly Phe Pro Asp Ser Pro Tyr Pro Ala 
225                 230                 235                 240 


His Ala Arg Cys Gln Trp Ala Leu Arg Gly Asp Ala Asp Ser Val Leu 
                245                 250                 255     


Ser Leu Thr Phe Arg Ser Phe Asp Leu Ala Ser Cys Asp Glu Arg Gly 
            260                 265                 270         


Ser Asp Leu Val Thr Val Tyr Asn Thr Leu Ser Pro Met Glu Pro His 
        275                 280                 285             


Ala Leu Val Gln Leu Cys Gly Thr Tyr Pro Pro Ser Tyr Asn Leu Thr 
    290                 295                 300                 


Phe His Ser Ser Gln Asn Val Leu Leu Ile Thr Leu Ile Thr Asn Thr 
305                 310                 315                 320 


Glu Arg Arg His Pro Gly Phe Glu Ala Thr Phe Phe Gln Leu Pro Arg 
                325                 330                 335     


Met Ser Ser Cys Gly Gly Arg Leu Arg Lys Ala Gln Gly Thr Phe Asn 
            340                 345                 350         


Ser Pro Tyr Tyr Pro Gly His Tyr Pro Pro Asn Ile Asp Cys Thr Trp 
        355                 360                 365             


Asn Ile Glu Val Pro Asn Asn Gln His Val Lys Val Arg Phe Lys Phe 
    370                 375                 380                 


Phe Tyr Leu Leu Glu Pro Gly Val Pro Ala Gly Thr Cys Pro Lys Asp 
385                 390                 395                 400 


Tyr Val Glu Ile Asn Gly Glu Lys Tyr Cys Gly Glu Arg Ser Gln Phe 
                405                 410                 415     


Val Val Thr Ser Asn Ser Asn Lys Ile Thr Val Arg Phe His Ser Asp 
            420                 425                 430         


Gln Ser Tyr Thr Asp Thr Gly Phe Leu Ala Glu Tyr Leu Ser Tyr Asp 
        435                 440                 445             


Ser Ser Asp Pro Cys Pro Gly Gln Phe Thr Cys Arg Thr Gly Arg Cys 
    450                 455                 460                 


Ile Arg Lys Glu Leu Arg Cys Asp Gly Trp Ala Asp Cys Thr Asp His 
465                 470                 475                 480 


Ser Asp Glu Leu Asn Cys Ser Cys Asp Ala Gly His Gln Phe Thr Cys 
                485                 490                 495     


Lys Asn Lys Phe Cys Lys Pro Leu Phe Trp Val Cys Asp Ser Val Asn 
            500                 505                 510         


Asp Cys Gly Asp Asn Ser Asp Glu Gln Gly Cys Ser Cys Pro Ala Gln 
        515                 520                 525             


Thr Phe Arg Cys Ser Asn Gly Lys Cys Leu Ser Lys Ser Gln Gln Cys 
    530                 535                 540                 


Asn Gly Lys Asp Asp Cys Gly Asp Gly Ser Asp Glu Ala Ser Cys Pro 
545                 550                 555                 560 


Lys Val Asn Val Val Thr Cys Thr Lys His Thr Tyr Arg Cys Leu Asn 
                565                 570                 575     


Gly Leu Cys Leu Ser Lys Gly Asn Pro Glu Cys Asp Gly Lys Glu Asp 
            580                 585                 590         


Cys Ser Asp Gly Ser Asp Glu Lys Asp Cys Asp Cys Gly Leu Arg Ser 
        595                 600                 605             


Phe Thr Arg Gln Ala Arg Val Val Gly Gly Thr Asp Ala Asp Glu Gly 
    610                 615                 620                 


Glu Trp Pro Trp Gln Val Ser Leu His Ala Leu Gly Gln Gly His Ile 
625                 630                 635                 640 


Cys Gly Ala Ser Leu Ile Ser Pro Asn Trp Leu Val Ser Ala Ala His 
                645                 650                 655     


Cys Tyr Ile Asp Asp Arg Gly Phe Arg Tyr Ser Asp Pro Thr Gln Trp 
            660                 665                 670         


Thr Ala Phe Leu Gly Leu His Asp Gln Ser Gln Arg Ser Ala Pro Gly 
        675                 680                 685             


Val Gln Glu Arg Arg Leu Lys Arg Ile Ile Ser His Pro Phe Phe Asn 
    690                 695                 700                 


Asp Phe Thr Phe Asp Tyr Asp Ile Ala Leu Leu Glu Leu Glu Lys Pro 
705                 710                 715                 720 


Ala Glu Tyr Ser Ser Met Val Arg Pro Ile Cys Leu Pro Asp Ala Ser 
                725                 730                 735     


His Val Phe Pro Ala Gly Lys Ala Ile Trp Val Thr Gly Trp Gly His 
            740                 745                 750         


Thr Gln Tyr Gly Gly Thr Gly Ala Leu Ile Leu Gln Lys Gly Glu Ile 
        755                 760                 765             


Arg Val Ile Asn Gln Thr Thr Cys Glu Asn Leu Leu Pro Gln Gln Ile 
    770                 775                 780                 


Thr Pro Arg Met Met Cys Val Gly Phe Leu Ser Gly Gly Val Asp Ser 
785                 790                 795                 800 


Cys Gln Gly Asp Ser Gly Gly Pro Leu Ser Ser Val Glu Ala Asp Gly 
                805                 810                 815     


Arg Ile Phe Gln Ala Gly Val Val Ser Trp Gly Asp Gly Cys Ala Gln 
            820                 825                 830         


Arg Asn Lys Pro Gly Val Tyr Thr Arg Leu Pro Leu Phe Arg Asp Trp 
        835                 840                 845             


Ile Lys Glu Asn Thr Gly Val 
    850                 855 


<210>  3
<211>  20
<212>  DNA
<213>  Artificial Sequence

<220>
<223>  Synthetic oligonucleotide

<400>  3
ctaggatgag cagctgtgga                                                   20


<210>  4
<211>  20
<212>  DNA
<213>  Artificial Sequence

<220>
<223>  Synthetic oligonucleotide

<400>  4
aagaatttga agcgcacctt                                                   20


<210>  5
<211>  255
<212>  DNA
<213>  Homo sapiens

<400>  5
acgtcctgct catcacactg ataaccaaca ctgagcggcg gcatcccggc tttgaggcca       60

ccttcttcca gctgcctagg atgagcagct gtggaggccg cttacgtaaa gcccagggga      120

cattcaacag cccctactac ccaggccact acccacccaa cattgactgc acatggaaca      180

ttgaggtgcc caacaaccag catgtgaagg tgcgcttcaa attcttctac ctgctggagc      240

ccggcgtgcc tgcgg                                                       255


<210>  6
<211>  9
<212>  PRT
<213>  Artificial sequence

<220>
<223>  Artificial sequence


<220>
<221>  MISC_FEATURE
<222>  (1)..(1)
<223>  ortho-Aminobenzoic acid (Abz)

<220>
<221>  misc_feature
<222>  (2)..(3)
<223>  Xaa can be any naturally occurring amino acid

<220>
<221>  MISC_FEATURE
<222>  (9)..(9)
<223>  3-NO2

<400>  6

Xaa Xaa Xaa Arg Gly Leu Phe Gly Tyr 
1               5                   


<210>  7
<211>  9
<212>  PRT
<213>  Artificial sequence

<220>
<223>  Artificial sequence


<220>
<221>  MISC_FEATURE
<222>  (1)..(1)
<223>  ortho-Aminobenzoic acid (Abz)

<220>
<221>  MISC_FEATURE
<222>  (9)..(9)
<223>  3-NO2

<400>  7

Ile Gln Ser Arg Gly Leu Phe Gly Tyr 
1               5                   


<210>  8
<211>  9
<212>  PRT
<213>  Artificial sequence

<220>
<223>  Artificial sequence


<220>
<221>  MISC_FEATURE
<222>  (1)..(1)
<223>  ortho-Aminobenzoic acid (Abz)

<220>
<221>  MISC_FEATURE
<222>  (9)..(9)
<223>  3-NO2

<400>  8

Lys Gln Thr Arg Gly Leu Phe Gly Tyr 
1               5                   


