                         SEQUENCE LISTING

<110>  MediaPharma S.r.l.
 
<120>  LGALS3BP antibody-drug-conjugate and its use for the treatment of
        cancer

<130>  65940P WO

<150>  EP 18166980
<151>  2018-04-12

<160>  15    

<170>  PatentIn version 3.5

<210>  1
<211>  121
<212>  PRT
<213>  Artificial Sequence

<220>
<223>  Humanized 1959 VH

<400>  1

Gln Val Gln Leu Gln Glu Ser Gly Pro Gly Leu Val Lys Pro Ser Glu 
1               5                   10                  15      


Thr Leu Ser Leu Thr Cys Ala Val Ser Gly Tyr Ser Ile Ser Ser Gly 
            20                  25                  30          


Tyr Tyr Trp Thr Trp Ile Arg Gln Pro Pro Gly Lys Gly Leu Glu Trp 
        35                  40                  45              


Ile Gly Tyr Ile Thr Tyr Asp Gly Lys Asn Asn Tyr Ser Pro Ser Leu 
    50                  55                  60                  


Lys Asn Arg Val Thr Ile Ser Val Asp Thr Ser Lys Asn Gln Phe Ser 
65                  70                  75                  80  


Leu Lys Leu Ser Ser Val Thr Ala Ala Asp Thr Ala Val Tyr Tyr Cys 
                85                  90                  95      


Ala Arg Glu Gly Ser Ser Val Ile Thr Thr Gly Phe Thr Phe Trp Gly 
            100                 105                 110         


Gln Gly Thr Leu Val Thr Val Ser Ser 
        115                 120     


<210>  2
<211>  106
<212>  PRT
<213>  Artificial Sequence

<220>
<223>  Humanized 1959 VL

<400>  2

Asp Ile Gln Met Thr Gln Ser Pro Ser Thr Leu Ser Ala Ser Val Gly 
1               5                   10                  15      


Asp Arg Val Thr Ile Thr Cys Ser Ala Ser Ser Arg Val Ser Tyr Met 
            20                  25                  30          


Tyr Trp Tyr Gln Gln Lys Pro Gly Lys Ala Pro Lys Leu Leu Ile Tyr 
        35                  40                  45              


Leu Thr Ser Asn Leu Ala Ser Gly Val Pro Ala Arg Phe Ser Gly Ser 
    50                  55                  60                  


Gly Ser Gly Thr Glu Phe Thr Leu Thr Ile Ser Ser Leu Gln Pro Asp 
65                  70                  75                  80  


Asp Phe Ala Thr Tyr Tyr Cys Gln Gln Trp Thr Ser His Pro Pro Thr 
                85                  90                  95      


Phe Gly Gln Gly Thr Lys Val Glu Val Lys 
            100                 105     


<210>  3
<211>  11
<212>  PRT
<213>  Artificial Sequence

<220>
<223>  Heavy Chain CDR1

<400>  3

Gly Tyr Ser Ile Ser Ser Gly Tyr Tyr Trp Thr 
1               5                   10      


<210>  4
<211>  16
<212>  PRT
<213>  Artificial Sequence

<220>
<223>  Heavy Chain CDR2

<400>  4

Tyr Ile Thr Tyr Asp Gly Lys Asn Asn Tyr Ser Pro Ser Leu Lys Asn 
1               5                   10                  15      


<210>  5
<211>  12
<212>  PRT
<213>  Artificial Sequence

<220>
<223>  Heavy Chain CDR3

<400>  5

Glu Gly Ser Ser Val Ile Thr Thr Gly Phe Thr Phe 
1               5                   10          


<210>  6
<211>  10
<212>  PRT
<213>  Artificial Sequence

<220>
<223>  Light Chain CDR1

<400>  6

Ser Ala Ser Ser Arg Val Ser Tyr Met Tyr 
1               5                   10  


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

<220>
<223>  Light Chain CDR2

<400>  7

Leu Thr Ser Asn Leu Ala Ser 
1               5           


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

<220>
<223>  Light Chain CDR3

<400>  8

Gln Gln Trp Thr Ser His Pro Pro Thr 
1               5                   


<210>  9
<211>  470
<212>  PRT
<213>  Artificial Sequence

<220>
<223>  Humanized 1959 HC (wt)

<400>  9

Met Asn Phe Gly Leu Arg Leu Ile Phe Leu Val Leu Thr Leu Lys Gly 
1               5                   10                  15      


Val Gln Cys Gln Val Gln Leu Gln Glu Ser Gly Pro Gly Leu Val Lys 
            20                  25                  30          


Pro Ser Glu Thr Leu Ser Leu Thr Cys Ala Val Ser Gly Tyr Ser Ile 
        35                  40                  45              


Ser Ser Gly Tyr Tyr Trp Thr Trp Ile Arg Gln Pro Pro Gly Lys Gly 
    50                  55                  60                  


Leu Glu Trp Ile Gly Tyr Ile Thr Tyr Asp Gly Lys Asn Asn Tyr Ser 
65                  70                  75                  80  


Pro Ser Leu Lys Asn Arg Val Thr Ile Ser Val Asp Thr Ser Lys Asn 
                85                  90                  95      


Gln Phe Ser Leu Lys Leu Ser Ser Val Thr Ala Ala Asp Thr Ala Val 
            100                 105                 110         


Tyr Tyr Cys Ala Arg Glu Gly Ser Ser Val Ile Thr Thr Gly Phe Thr 
        115                 120                 125             


Phe Trp Gly Gln Gly Thr Leu Val Thr Val Ser Ser Ala Ser Thr Lys 
    130                 135                 140                 


Gly Pro Ser Val Phe Pro Leu Ala Pro Ser Ser Lys Ser Thr Ser Gly 
145                 150                 155                 160 


Gly Thr Ala Ala Leu Gly Cys Leu Val Lys Asp Tyr Phe Pro Glu Pro 
                165                 170                 175     


Val Thr Val Ser Trp Asn Ser Gly Ala Leu Thr Ser Gly Val His Thr 
            180                 185                 190         


Phe Pro Ala Val Leu Gln Ser Ser Gly Leu Tyr Ser Leu Ser Ser Val 
        195                 200                 205             


Val Thr Val Pro Ser Ser Ser Leu Gly Thr Gln Thr Tyr Ile Cys Asn 
    210                 215                 220                 


Val Asn His Lys Pro Ser Asn Thr Lys Val Asp Lys Lys Val Glu Pro 
225                 230                 235                 240 


Lys Ser Cys Asp Lys Thr His Thr Cys Pro Pro Cys Pro Ala Pro Glu 
                245                 250                 255     


Leu Leu Gly Gly Pro Ser Val Phe Leu Phe Pro Pro Lys Pro Lys Asp 
            260                 265                 270         


Thr Leu Met Ile Ser Arg Thr Pro Glu Val Thr Cys Val Val Val Asp 
        275                 280                 285             


Val Ser His Glu Asp Pro Glu Val Lys Phe Asn Trp Tyr Val Asp Gly 
    290                 295                 300                 


Val Glu Val His Asn Ala Lys Thr Lys Pro Arg Glu Glu Gln Tyr Asn 
305                 310                 315                 320 


Ser Thr Tyr Arg Val Val Ser Val Leu Thr Val Leu His Gln Asp Trp 
                325                 330                 335     


Leu Asn Gly Lys Glu Tyr Lys Cys Lys Val Ser Asn Lys Ala Leu Pro 
            340                 345                 350         


Ala Pro Ile Glu Lys Thr Ile Ser Lys Ala Lys Gly Gln Pro Arg Glu 
        355                 360                 365             


Pro Gln Val Tyr Thr Leu Pro Pro Ser Arg Glu Glu Met Thr Lys Asn 
    370                 375                 380                 


Gln Val Ser Leu Thr Cys Leu Val Lys Gly Phe Tyr Pro Ser Asp Ile 
385                 390                 395                 400 


Ala Val Glu Trp Glu Ser Asn Gly Gln Pro Glu Asn Asn Tyr Lys Thr 
                405                 410                 415     


Thr Pro Pro Val Leu Asp Ser Asp Gly Ser Phe Phe Leu Tyr Ser Lys 
            420                 425                 430         


Leu Thr Val Asp Lys Ser Arg Trp Gln Gln Gly Asn Val Phe Ser Cys 
        435                 440                 445             


Ser Val Met His Glu Ala Leu His Asn His Tyr Thr Gln Lys Ser Leu 
    450                 455                 460                 


Ser Leu Ser Pro Gly Lys 
465                 470 


<210>  10
<211>  232
<212>  PRT
<213>  Artificial Sequence

<220>
<223>  Humanized 1959 LC

<400>  10

Met Asn Phe Gly Leu Arg Leu Ile Phe Leu Val Leu Thr Leu Lys Gly 
1               5                   10                  15      


Val Gln Cys Asp Ile Gln Met Thr Gln Ser Pro Ser Thr Leu Ser Ala 
            20                  25                  30          


Ser Val Gly Asp Arg Val Thr Ile Thr Cys Ser Ala Ser Ser Arg Val 
        35                  40                  45              


Ser Tyr Met Tyr Trp Tyr Gln Gln Lys Pro Gly Lys Ala Pro Lys Leu 
    50                  55                  60                  


Leu Ile Tyr Leu Thr Ser Asn Leu Ala Ser Gly Val Pro Ala Arg Phe 
65                  70                  75                  80  


Ser Gly Ser Gly Ser Gly Thr Glu Phe Thr Leu Thr Ile Ser Ser Leu 
                85                  90                  95      


Gln Pro Asp Asp Phe Ala Thr Tyr Tyr Cys Gln Gln Trp Thr Ser His 
            100                 105                 110         


Pro Pro Thr Phe Gly Gln Gly Thr Lys Val Glu Val Lys Arg Thr Val 
        115                 120                 125             


Ala Ala Pro Ser Val Phe Ile Phe Pro Pro Ser Asp Glu Gln Leu Lys 
    130                 135                 140                 


Ser Gly Thr Ala Ser Val Val Cys Leu Leu Asn Asn Phe Tyr Pro Arg 
145                 150                 155                 160 


Glu Ala Lys Val Gln Trp Lys Val Asp Asn Ala Leu Gln Ser Gly Asn 
                165                 170                 175     


Ser Gln Glu Ser Val Thr Glu Gln Asp Ser Lys Asp Ser Thr Tyr Ser 
            180                 185                 190         


Leu Ser Ser Thr Leu Thr Leu Ser Lys Ala Asp Tyr Glu Lys His Lys 
        195                 200                 205             


Val Tyr Ala Cys Glu Val Thr His Gln Gly Leu Ser Ser Pro Val Thr 
    210                 215                 220                 


Lys Ser Phe Asn Arg Gly Glu Cys 
225                 230         


<210>  11
<211>  451
<212>  PRT
<213>  Artificial Sequence

<220>
<223>  Human 1959sss  HC (C220S  C226S  C229S)

<400>  11

Gln Val Gln Leu Gln Glu Ser Gly Pro Gly Leu Val Lys Pro Ser Glu 
1               5                   10                  15      


Thr Leu Ser Leu Thr Cys Ala Val Ser Gly Tyr Ser Ile Ser Ser Gly 
            20                  25                  30          


Tyr Tyr Trp Thr Trp Ile Arg Gln Pro Pro Gly Lys Gly Leu Glu Trp 
        35                  40                  45              


Ile Gly Tyr Ile Thr Tyr Asp Gly Lys Asn Asn Tyr Ser Pro Ser Leu 
    50                  55                  60                  


Lys Asn Arg Val Thr Ile Ser Val Asp Thr Ser Lys Asn Gln Phe Ser 
65                  70                  75                  80  


Leu Lys Leu Ser Ser Val Thr Ala Ala Asp Thr Ala Val Tyr Tyr Cys 
                85                  90                  95      


Ala Arg Glu Gly Ser Ser Val Ile Thr Thr Gly Phe Thr Phe Trp Gly 
            100                 105                 110         


Gln Gly Thr Leu Val Thr Val Ser Ser Ala Ser Thr Lys Gly Pro Ser 
        115                 120                 125             


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


Ala Leu Gly Cys Leu Val Lys Asp Tyr Phe Pro Glu Pro Val Thr Val 
145                 150                 155                 160 


Ser Trp Asn Ser Gly Ala Leu Thr Ser Gly Val His Thr Phe Pro Ala 
                165                 170                 175     


Val Leu Gln Ser Ser Gly Leu Tyr Ser Leu Ser Ser Val Val Thr Val 
            180                 185                 190         


Pro Ser Ser Ser Leu Gly Thr Gln Thr Tyr Ile Cys Asn Val Asn His 
        195                 200                 205             


Lys Pro Ser Asn Thr Lys Val Asp Lys Lys Val Glu Pro Lys Ser Ser 
    210                 215                 220                 


Asp Lys Thr His Thr Ser Pro Pro Ser Pro Ala Pro Glu Leu Leu Gly 
225                 230                 235                 240 


Gly Pro Ser Val Phe Leu Phe Pro Pro Lys Pro Lys Asp Thr Leu Met 
                245                 250                 255     


Ile Ser Arg Thr Pro Glu Val Thr Cys Val Val Val Asp Val Ser His 
            260                 265                 270         


Glu Asp Pro Glu Val Lys Phe Asn Trp Tyr Val Asp Gly Val Glu Val 
        275                 280                 285             


His Asn Ala Lys Thr Lys Pro Arg Glu Glu Gln Tyr Asn Ser Thr Tyr 
    290                 295                 300                 


Arg Val Val Ser Val Leu Thr Val Leu His Gln Asp Trp Leu Asn Gly 
305                 310                 315                 320 


Lys Glu Tyr Lys Cys Lys Val Ser Asn Lys Ala Leu Pro Ala Pro Ile 
                325                 330                 335     


Glu Lys Thr Ile Ser Lys Ala Lys Gly Gln Pro Arg Glu Pro Gln Val 
            340                 345                 350         


Tyr Thr Leu Pro Pro Ser Arg Glu Glu Met Thr Lys Asn Gln Val Ser 
        355                 360                 365             


Leu Thr Cys Leu Val Lys Gly Phe Tyr Pro Ser Asp Ile Ala Val Glu 
    370                 375                 380                 


Trp Glu Ser Asn Gly Gln Pro Glu Asn Asn Tyr Lys Thr Thr Pro Pro 
385                 390                 395                 400 


Val Leu Asp Ser Asp Gly Ser Phe Phe Leu Tyr Ser Lys Leu Thr Val 
                405                 410                 415     


Asp Lys Ser Arg Trp Gln Gln Gly Asn Val Phe Ser Cys Ser Val Met 
            420                 425                 430         


His Glu Ala Leu His Asn His Tyr Thr Gln Lys Ser Leu Ser Leu Ser 
        435                 440                 445             


Pro Gly Lys 
    450     


<210>  12
<211>  20
<212>  DNA
<213>  Artificial Sequence

<220>
<223>  Primer LGALS3BP Fw

<400>  12
gaacccaagg cgtgaacgat                                                   20


<210>  13
<211>  20
<212>  DNA
<213>  Artificial Sequence

<220>
<223>  Primer LGALS3BP Rw

<400>  13
gtcccacagg ttgtcacaca                                                   20


<210>  14
<211>  24
<212>  DNA
<213>  Artificial Sequence

<220>
<223>  Primer Act Fw

<400>  14
cagctcacca tggatgatga tatc                                              24


<210>  15
<211>  17
<212>  DNA
<213>  Artificial Sequence

<220>
<223>  Primer Act Rw

<400>  15
aagccggcct tgcacat                                                      17


