                         SEQUENCE LISTING

<110>  Merck Patent GmbH
 
<120>  BISPECIFIC ANTIBODY-DRUG CONJUGATES TARGETING EGFR AND MUC1 AND 
       USES THEREOF

<130>  EMD-016

<150>  63/034,296
<151>  2020-06-03

<160>  48    

<170>  PatentIn version 3.5

<210>  1
<211>  478
<212>  PRT
<213>  Artificial

<220>
<223>  anti-MUC1 scFvFc (AG SEED)

<400>  1

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


Ala Ser Val Lys Val Ser Cys Lys Ala Ser Gly Tyr Ser Phe Thr Ser 
            20                  25                  30          


His Phe Met His Trp Val Arg Gln Ala Pro Gly Gln Gly Leu Glu Trp 
        35                  40                  45              


Met Gly Trp Ile Asp Pro Val Thr Gly Gly Thr Lys Tyr Ala Gln Asn 
    50                  55                  60                  


Phe Gln Gly Trp Val Thr Met Thr Arg Asp Thr Ser Ile Arg Thr Ala 
65                  70                  75                  80  


Tyr Leu Glu Leu Ser Arg Leu Arg Ser Asp Asp Thr Ala Met Tyr Tyr 
                85                  90                  95      


Cys Ala Arg Glu Ala Arg Ala Asp Arg Gly Gln Phe Asp Lys Trp Gly 
            100                 105                 110         


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


Gly Gly Ser Gly Gly Gly Gly Ser Gln Ser Val Leu Thr Gln Pro Pro 
    130                 135                 140                 


Ser Val Ser Val Ala Pro Gly Lys Thr Ala Arg Ile Thr Cys Gly Gly 
145                 150                 155                 160 


Asn Asn Ile Gly Ser Lys Ser Val His Trp Tyr Gln Gln Lys Pro Gly 
                165                 170                 175     


Gln Ala Pro Ala Leu Val Ile Tyr Tyr Gly Ser Asn Arg Pro Ser Gly 
            180                 185                 190         


Ile Pro Glu Arg Phe Ser Gly Ser Asn Ser Gly Asn Thr Ala Thr Leu 
        195                 200                 205             


Thr Ile Ser Arg Val Glu Ala Gly Asp Glu Ala Asp Tyr Tyr Cys Gln 
    210                 215                 220                 


Val Trp Asp Ser Ser Ser Asp Trp Val Phe Gly Gly Gly Thr Lys Leu 
225                 230                 235                 240 


Thr Val Leu Lys Pro Lys Ser Ser Asp Lys Thr His Thr Cys Pro Pro 
                245                 250                 255     


Cys Pro Ala Pro Glu Leu Leu Gly Gly Pro Ser Val Phe Leu Phe Pro 
            260                 265                 270         


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


Cys Val Val Val Asp Val Ser His Glu Asp Pro Glu Val Lys Phe Asn 
    290                 295                 300                 


Trp Tyr Val Asp Gly Val Glu Val His Asn Ala Lys Thr Lys Pro Arg 
305                 310                 315                 320 


Glu Glu Gln Tyr Asn Ser Thr Tyr Arg Val Val Ser Val Leu Thr Val 
                325                 330                 335     


Leu His Gln Asp Trp Leu Asn Gly Lys Glu Tyr Lys Cys Lys Val Ser 
            340                 345                 350         


Asn Lys Ala Leu Pro Ala Pro Ile Glu Lys Thr Ile Ser Lys Ala Lys 
        355                 360                 365             


Gly Gln Pro Phe Arg Pro Glu Val His Leu Leu Pro Pro Ser Arg Glu 
    370                 375                 380                 


Glu Met Thr Lys Asn Gln Val Ser Leu Thr Cys Leu Ala Arg Gly Phe 
385                 390                 395                 400 


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


Asn Asn Tyr Lys Thr Thr Pro Ser Arg Gln Glu Pro Ser Gln Gly Thr 
            420                 425                 430         


Thr Thr Phe Ala Val Thr Ser Lys Leu Thr Val Asp Lys Ser Arg Trp 
        435                 440                 445             


Gln Gln Gly Asn Val Phe Ser Cys Ser Val Met His Glu Ala Leu His 
    450                 455                 460                 


Asn His Tyr Thr Gln Lys Thr Ile Ser Leu Ser Pro Gly Lys 
465                 470                 475             


<210>  2
<211>  453
<212>  PRT
<213>  Artificial

<220>
<223>  anti-EGFR Fab(heavy)Fc (GA SEED)

<400>  2

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


Ala Ser Val Lys Val Ser Cys Lys Ala Ser Gly Phe Ser Leu Thr Asn 
            20                  25                  30          


Tyr Gly Val His Trp Met Arg Gln Ala Pro Gly Gln Gly Leu Glu Trp 
        35                  40                  45              


Ile Gly Val Ile Trp Ser Gly Gly Asn Thr Asp Tyr Asn Thr Pro Phe 
    50                  55                  60                  


Thr Ser Arg Val Thr Ile Thr Ser Asp Lys Ser Thr Ser Thr Ala Tyr 
65                  70                  75                  80  


Met Glu Leu Ser Ser Leu Arg Ser Glu Asp Thr Ala Val Tyr Tyr Cys 
                85                  90                  95      


Ala Arg Ala Leu Thr Tyr Tyr Asp Tyr Glu Phe Ala Tyr Trp Gly Gln 
            100                 105                 110         


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


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


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


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


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


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


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


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


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


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


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


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


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


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


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


Thr Leu Pro Pro Pro Ser Glu Glu Leu Ala Leu Asn Glu Leu Val Thr 
        355                 360                 365             


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


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


Ala Pro Val Leu Asp Ser Asp Gly Ser Phe Phe Leu Tyr Ser Ile Leu 
                405                 410                 415     


Arg Val Ala Ala Glu Asp Trp Lys Lys Gly Asp Thr Phe Ser Cys Ser 
            420                 425                 430         


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


Arg Ser Pro Gly Lys 
    450             


<210>  3
<211>  215
<212>  PRT
<213>  Artificial

<220>
<223>  anti-EGFR Fab(light chain)

<400>  3

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


Gly Asp Arg Val Thr Ile Thr Cys Arg Ala Ser Gln Ser Ile Gly Thr 
            20                  25                  30          


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


Ile Lys Tyr Ala Ser Glu Ser Ile Ser Gly Val Pro Ser Arg Phe Ser 
    50                  55                  60                  


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


Pro Glu Asp Val Ala Thr Tyr Tyr Cys Gln Gln Asn Asn Asn Trp Pro 
                85                  90                  95      


Thr Thr Phe Gly Gln Gly Thr Lys Val Glu Ile Lys Arg Thr Val Ala 
            100                 105                 110         


Ala Pro Ser Val Phe Ile Phe Pro Pro Ser Asp Glu Gln Leu Lys Ser 
        115                 120                 125             


Gly Thr Ala Ser Val Val Cys Leu Leu Asn Asn Phe Tyr Pro Arg Glu 
    130                 135                 140                 


Ala Lys Val Gln Trp Lys Val Asp Asn Ala Leu Gln Ser Gly Asn Ser 
145                 150                 155                 160 


Gln Glu Ser Val Thr Glu Gln Asp Ser Lys Asp Ser Thr Tyr Ser Leu 
                165                 170                 175     


Ser Ser Thr Leu Thr Leu Ser Lys Ala Asp Tyr Glu Lys His Lys Val 
            180                 185                 190         


Tyr Ala Cys Glu Val Thr His Gln Gly Leu Ser Ser Pro Val Thr Lys 
        195                 200                 205             


Ser Phe Asn Arg Gly Glu Cys 
    210                 215 


<210>  4
<211>  10
<212>  PRT
<213>  Artificial

<220>
<223>  CDRH1 motif for HT186-D11 and 1993 series antibodies


<220>
<221>  VARIANT
<222>  (3)..(3)
<223>  Xaa is Ser or Pro

<220>
<221>  VARIANT
<222>  (5)..(5)
<223>  Xaa is Thr or Asn

<220>
<221>  VARIANT
<222>  (6)..(6)
<223>  Xaa is Gly, Asp, or Ser

<220>
<221>  VARIANT
<222>  (7)..(7)
<223>  Xaa is His or Asn

<220>
<221>  VARIANT
<222>  (8)..(8)
<223>  Xaa is Tyr or Phe

<400>  4

Gly Tyr Xaa Phe Xaa Xaa Xaa Xaa Met His 
1               5                   10  


<210>  5
<211>  17
<212>  PRT
<213>  Artificial

<220>
<223>  CDRH2 motif for HT186-D11 and 1993 series antibodies


<220>
<221>  VARIANT
<222>  (8)..(8)
<223>  Xaa is Gly or Glu

<220>
<221>  VARIANT
<222>  (10)..(10)
<223>  Xaa is Lys or Arg

<220>
<221>  VARIANT
<222>  (14)..(14)
<223>  Xaa is Asn or Asp

<400>  5

Trp Ile Asp Pro Val Thr Gly Xaa Thr Xaa Tyr Ala Gln Xaa Phe Gln 
1               5                   10                  15      


Gly 
    


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

<220>
<223>  CDRH3 motif for HT186-D11 and 1993 series antibodies


<220>
<221>  VARIANT
<222>  (2)..(2)
<223>  Xaa is Val or Ala

<220>
<221>  VARIANT
<222>  (3)..(3)
<223>  Xaa is Thr or Arg

<220>
<221>  VARIANT
<222>  (4)..(4)
<223>  Xaa is Gly or Ala

<220>
<221>  VARIANT
<222>  (5)..(5)
<223>  Xaa is Asp or Ser

<400>  6

Glu Xaa Xaa Xaa Xaa Arg Gly Gln Phe Asp Lys 
1               5                   10      


<210>  7
<211>  11
<212>  PRT
<213>  Artificial

<220>
<223>  CDRL1 for HT186-D11 and 1993 series antibodies

<400>  7
000

Gly Gly Asn Asn Ile Gly Ser Lys Ser Val His 
1               5                   10      


<210>  8
<211>  7
<212>  PRT
<213>  Artificial

<220>
<223>  CDRL2 for HT186-D11 and 1993 series antibodies

<400>  8
000

Tyr Gly Ser Asn Arg Pro Ser 
1               5           


<210>  9
<211>  10
<212>  PRT
<213>  Artificial

<220>
<223>  CDRL3 for HT186-D11 and 1993 series antibodies

<400>  9

Gln Val Trp Asp Ser Ser Ser Asp Trp Val 
1               5                   10  


<210>  10
<211>  16
<212>  PRT
<213>  Artificial

<220>
<223>  VNTR peptide of MUC1

<400>  10

Ala Pro Asp Thr Arg Pro Ala Pro Gly Ser Thr Ala Pro Pro Ala Cys 
1               5                   10                  15      


<210>  11
<211>  478
<212>  PRT
<213>  Artificial

<220>
<223>  anti-MUC1 scFvFc (AG SEED) with non-natural amino acids (e.g., 
       pAMF) introduced at Xaa sites


<220>
<221>  MUTAGEN
<222>  (269)..(269)
<223>  Non-natural amino acid, e.g., para azidomethyl L-phenylalanine 
       (pAMF)

<220>
<221>  MUTAGEN
<222>  (435)..(435)
<223>  Non-natural amino acid, e.g., para azidomethyl L-phenylalanine 
       (pAMF)

<400>  11

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


Ala Ser Val Lys Val Ser Cys Lys Ala Ser Gly Tyr Ser Phe Thr Ser 
            20                  25                  30          


His Phe Met His Trp Val Arg Gln Ala Pro Gly Gln Gly Leu Glu Trp 
        35                  40                  45              


Met Gly Trp Ile Asp Pro Val Thr Gly Gly Thr Lys Tyr Ala Gln Asn 
    50                  55                  60                  


Phe Gln Gly Trp Val Thr Met Thr Arg Asp Thr Ser Ile Arg Thr Ala 
65                  70                  75                  80  


Tyr Leu Glu Leu Ser Arg Leu Arg Ser Asp Asp Thr Ala Met Tyr Tyr 
                85                  90                  95      


Cys Ala Arg Glu Ala Arg Ala Asp Arg Gly Gln Phe Asp Lys Trp Gly 
            100                 105                 110         


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


Gly Gly Ser Gly Gly Gly Gly Ser Gln Ser Val Leu Thr Gln Pro Pro 
    130                 135                 140                 


Ser Val Ser Val Ala Pro Gly Lys Thr Ala Arg Ile Thr Cys Gly Gly 
145                 150                 155                 160 


Asn Asn Ile Gly Ser Lys Ser Val His Trp Tyr Gln Gln Lys Pro Gly 
                165                 170                 175     


Gln Ala Pro Ala Leu Val Ile Tyr Tyr Gly Ser Asn Arg Pro Ser Gly 
            180                 185                 190         


Ile Pro Glu Arg Phe Ser Gly Ser Asn Ser Gly Asn Thr Ala Thr Leu 
        195                 200                 205             


Thr Ile Ser Arg Val Glu Ala Gly Asp Glu Ala Asp Tyr Tyr Cys Gln 
    210                 215                 220                 


Val Trp Asp Ser Ser Ser Asp Trp Val Phe Gly Gly Gly Thr Lys Leu 
225                 230                 235                 240 


Thr Val Leu Lys Pro Lys Ser Ser Asp Lys Thr His Thr Cys Pro Pro 
                245                 250                 255     


Cys Pro Ala Pro Glu Leu Leu Gly Gly Pro Ser Val Xaa Leu Phe Pro 
            260                 265                 270         


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


Cys Val Val Val Asp Val Ser His Glu Asp Pro Glu Val Lys Phe Asn 
    290                 295                 300                 


Trp Tyr Val Asp Gly Val Glu Val His Asn Ala Lys Thr Lys Pro Arg 
305                 310                 315                 320 


Glu Glu Gln Tyr Asn Ser Thr Tyr Arg Val Val Ser Val Leu Thr Val 
                325                 330                 335     


Leu His Gln Asp Trp Leu Asn Gly Lys Glu Tyr Lys Cys Lys Val Ser 
            340                 345                 350         


Asn Lys Ala Leu Pro Ala Pro Ile Glu Lys Thr Ile Ser Lys Ala Lys 
        355                 360                 365             


Gly Gln Pro Phe Arg Pro Glu Val His Leu Leu Pro Pro Ser Arg Glu 
    370                 375                 380                 


Glu Met Thr Lys Asn Gln Val Ser Leu Thr Cys Leu Ala Arg Gly Phe 
385                 390                 395                 400 


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


Asn Asn Tyr Lys Thr Thr Pro Ser Arg Gln Glu Pro Ser Gln Gly Thr 
            420                 425                 430         


Thr Thr Xaa Ala Val Thr Ser Lys Leu Thr Val Asp Lys Ser Arg Trp 
        435                 440                 445             


Gln Gln Gly Asn Val Phe Ser Cys Ser Val Met His Glu Ala Leu His 
    450                 455                 460                 


Asn His Tyr Thr Gln Lys Thr Ile Ser Leu Ser Pro Gly Lys 
465                 470                 475             


<210>  12
<211>  453
<212>  PRT
<213>  Artificial

<220>
<223>  anti-EGFR Fab(heavy)Fc (GA SEED) with non-natural amino acids 
       (e.g., pAMF) introduced at Xaa sites


<220>
<221>  MUTAGEN
<222>  (183)..(183)
<223>  Xaa is an unnatural amino acid, e.g., para azidomethyl 
       L-phenylalanine (pAMF)

<220>
<221>  MUTAGEN
<222>  (244)..(244)
<223>  Xaa is an unnatural amino acid, e.g., para azidomethyl 
       L-phenylalanine (pAMF)

<400>  12

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


Ala Ser Val Lys Val Ser Cys Lys Ala Ser Gly Phe Ser Leu Thr Asn 
            20                  25                  30          


Tyr Gly Val His Trp Met Arg Gln Ala Pro Gly Gln Gly Leu Glu Trp 
        35                  40                  45              


Ile Gly Val Ile Trp Ser Gly Gly Asn Thr Asp Tyr Asn Thr Pro Phe 
    50                  55                  60                  


Thr Ser Arg Val Thr Ile Thr Ser Asp Lys Ser Thr Ser Thr Ala Tyr 
65                  70                  75                  80  


Met Glu Leu Ser Ser Leu Arg Ser Glu Asp Thr Ala Val Tyr Tyr Cys 
                85                  90                  95      


Ala Arg Ala Leu Thr Tyr Tyr Asp Tyr Glu Phe Ala Tyr Trp Gly Gln 
            100                 105                 110         


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


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


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


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


Leu Gln Ser Ser Gly Leu Xaa Ser Leu Ser Ser Val Val Thr Val Pro 
            180                 185                 190         


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


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


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


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


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


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


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


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


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


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


Thr Leu Pro Pro Pro Ser Glu Glu Leu Ala Leu Asn Glu Leu Val Thr 
        355                 360                 365             


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


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


Ala Pro Val Leu Asp Ser Asp Gly Ser Phe Phe Leu Tyr Ser Ile Leu 
                405                 410                 415     


Arg Val Ala Ala Glu Asp Trp Lys Lys Gly Asp Thr Phe Ser Cys Ser 
            420                 425                 430         


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


Arg Ser Pro Gly Lys 
    450             


<210>  13
<211>  8
<212>  PRT
<213>  Artificial

<220>
<223>  CDRH1 for hC225

<400>  13
000

Gly Phe Ser Leu Thr Asn Tyr Gly 
1               5               


<210>  14
<211>  7
<212>  PRT
<213>  Artificial

<220>
<223>  CDRH2 for hC225

<400>  14
000

Ile Trp Ser Gly Gly Asn Thr 
1               5           


<210>  15
<211>  13
<212>  PRT
<213>  Artificial

<220>
<223>  CDRH3 for hC225

<400>  15
000

Ala Arg Ala Leu Thr Tyr Tyr Asp Tyr Glu Phe Ala Tyr 
1               5                   10              


<210>  16
<211>  6
<212>  PRT
<213>  Artificial

<220>
<223>  CDRL1 for hC225

<400>  16
000

Gln Ser Ile Gly Thr Asn 
1               5       


<210>  17
<211>  4
<212>  PRT
<213>  Artificial

<220>
<223>  CDRL2 for hC225

<400>  17
000

Tyr Ala Ser Glu 
1               


<210>  18
<211>  9
<212>  PRT
<213>  Artificial

<220>
<223>  CDRL3 for hC225

<400>  18
000

Gln Gln Asn Asn Asn Trp Pro Thr Thr 
1               5                   


<210>  19
<211>  98
<212>  PRT
<213>  Artificial

<220>
<223>  CH1 within hC225 heavy chain

<400>  19
000

Ala Ser Thr Lys Gly Pro Ser Val Phe Pro Leu Ala Pro Ser Ser Lys 
1               5                   10                  15      


Ser Thr Ser Gly Gly Thr Ala Ala Leu Gly Cys Leu Val Lys Asp Tyr 
            20                  25                  30          


Phe Pro Glu Pro Val Thr Val Ser Trp Asn Ser Gly Ala Leu Thr Ser 
        35                  40                  45              


Gly Val His Thr Phe Pro Ala Val Leu Gln Ser Ser Gly Leu Tyr Ser 
    50                  55                  60                  


Leu Ser Ser Val Val Thr Val Pro Ser Ser Ser Leu Gly Thr Gln Thr 
65                  70                  75                  80  


Tyr Ile Cys Asn Val Asn His Lys Pro Ser Asn Thr Lys Val Asp Lys 
                85                  90                  95      


Arg Val 
        


<210>  20
<211>  98
<212>  PRT
<213>  Artificial

<220>
<223>  CH1 within hC225 heavy chain with non-natural amino acid (e.g., 
       pAMF) introduced at Xaa


<220>
<221>  MUTAGEN
<222>  (63)..(63)
<223>  Xaa is a non-natural amino acid, e.g., para azidomethyl 
       L-phenylalanine (pAMF)

<400>  20
000

Ala Ser Thr Lys Gly Pro Ser Val Phe Pro Leu Ala Pro Ser Ser Lys 
1               5                   10                  15      


Ser Thr Ser Gly Gly Thr Ala Ala Leu Gly Cys Leu Val Lys Asp Tyr 
            20                  25                  30          


Phe Pro Glu Pro Val Thr Val Ser Trp Asn Ser Gly Ala Leu Thr Ser 
        35                  40                  45              


Gly Val His Thr Phe Pro Ala Val Leu Gln Ser Ser Gly Leu Xaa Ser 
    50                  55                  60                  


Leu Ser Ser Val Val Thr Val Pro Ser Ser Ser Leu Gly Thr Gln Thr 
65                  70                  75                  80  


Tyr Ile Cys Asn Val Asn His Lys Pro Ser Asn Thr Lys Val Asp Lys 
                85                  90                  95      


Arg Val 
        


<210>  21
<211>  107
<212>  PRT
<213>  Artificial

<220>
<223>  CL1 within hC225 light chain

<400>  21
000

Arg Thr Val Ala Ala Pro Ser Val Phe Ile Phe Pro Pro Ser Asp Glu 
1               5                   10                  15      


Gln Leu Lys Ser Gly Thr Ala Ser Val Val Cys Leu Leu Asn Asn Phe 
            20                  25                  30          


Tyr Pro Arg Glu Ala Lys Val Gln Trp Lys Val Asp Asn Ala Leu Gln 
        35                  40                  45              


Ser Gly Asn Ser Gln Glu Ser Val Thr Glu Gln Asp Ser Lys Asp Ser 
    50                  55                  60                  


Thr Tyr Ser Leu Ser Ser Thr Leu Thr Leu Ser Lys Ala Asp Tyr Glu 
65                  70                  75                  80  


Lys His Lys Val Tyr Ala Cys Glu Val Thr His Gln Gly Leu Ser Ser 
                85                  90                  95      


Pro Val Thr Lys Ser Phe Asn Arg Gly Glu Cys 
            100                 105         


<210>  22
<211>  40
<212>  PRT
<213>  Artificial

<220>
<223>  peptide from human MUC1

<400>  22
000

Ala Pro Asp Thr Arg Pro Ala Pro Gly Ser Thr Ala Pro Pro Ala His 
1               5                   10                  15      


Gly Val Thr Ser Ala Pro Asp Thr Arg Pro Ala Pro Gly Ser Thr Ala 
            20                  25                  30          


Pro Pro Ala His Gly Val Thr Ser 
        35                  40  


<210>  23
<211>  15
<212>  PRT
<213>  Artificial

<220>
<223>  human MUC1 truncated peptide

<400>  23
000

Ala Pro Asp Thr Arg Pro Ala Pro Gly Ser Thr Ala Pro Pro Ala 
1               5                   10                  15  


<210>  24
<211>  15
<212>  PRT
<213>  Artificial

<220>
<223>  human MUC1 truncated peptide

<400>  24
000

Pro Ala Pro Gly Ser Thr Ala Pro Pro Ala His Gly Val Thr Ser 
1               5                   10                  15  


<210>  25
<211>  15
<212>  PRT
<213>  Artificial

<220>
<223>  human MUC1 truncated peptide

<400>  25
000

Thr Ala Pro Pro Ala His Gly Val Thr Ser Ala Pro Asp Thr Arg 
1               5                   10                  15  


<210>  26
<211>  15
<212>  PRT
<213>  Artificial

<220>
<223>  human MUC1 truncated peptide

<400>  26
000

His Gly Val Thr Ser Ala Pro Asp Thr Arg Pro Ala Pro Gly Ser 
1               5                   10                  15  


<210>  27
<211>  5
<212>  PRT
<213>  Artificial

<220>
<223>  human MUC1 minimal consensus motif

<400>  27
000

Thr Arg Pro Ala Pro 
1               5   


<210>  28
<211>  6
<212>  PRT
<213>  Artificial

<220>
<223>  human MUC1 minimal consensus motif

<400>  28
000

Asp Thr Arg Pro Ala Pro 
1               5       


<210>  29
<211>  5
<212>  PRT
<213>  Artificial

<220>
<223>  CDRH1 for HT186-D11 - Kabat

<400>  29
000

Gly His Tyr Met His 
1               5   


<210>  30
<211>  17
<212>  PRT
<213>  Artificial

<220>
<223>  CDRH2 for HT186-D11 - Kabat

<400>  30
000

Trp Ile Asp Pro Val Thr Gly Gly Thr Lys Tyr Ala Gln Asn Phe Gln 
1               5                   10                  15      


Gly 
    


<210>  31
<211>  11
<212>  PRT
<213>  Artificial

<220>
<223>  CDRH3 for HT186-D11 - Kabat

<400>  31
000

Glu Val Thr Gly Asp Arg Gly Gln Phe Asp Lys 
1               5                   10      


<210>  32
<211>  7
<212>  PRT
<213>  Artificial

<220>
<223>  CDRH1 for HT186-D11 - Chothia

<400>  32
000

Gly Tyr Ser Phe Thr Gly His 
1               5           


<210>  33
<211>  6
<212>  PRT
<213>  Artificial

<220>
<223>  CDRH2 for HT186-D11 - Chothia

<400>  33
000

Asp Pro Val Thr Gly Gly 
1               5       


<210>  34
<211>  11
<212>  PRT
<213>  Artificial

<220>
<223>  CDRH3 for HT186-D11 - Chothia

<400>  34
000

Glu Val Thr Gly Asp Arg Gly Gln Phe Asp Lys 
1               5                   10      


<210>  35
<211>  5
<212>  PRT
<213>  Artificial

<220>
<223>  CDRH1 for 1993-H02 - Kabat

<400>  35
000

Ser His Phe Met His 
1               5   


<210>  36
<211>  17
<212>  PRT
<213>  Artificial

<220>
<223>  CDRH2 for 1993-H02 - Kabat

<400>  36
000

Trp Ile Asp Pro Val Thr Gly Gly Thr Lys Tyr Ala Gln Asn Phe Gln 
1               5                   10                  15      


Gly 
    


<210>  37
<211>  11
<212>  PRT
<213>  Artificial

<220>
<223>  CDRH3 for 1993-H02 - Kabat

<400>  37
000

Glu Ala Arg Ala Asp Arg Gly Gln Phe Asp Lys 
1               5                   10      


<210>  38
<211>  7
<212>  PRT
<213>  Artificial

<220>
<223>  CDRH1 for 1993-H02 - Chothia

<400>  38
000

Gly Tyr Ser Phe Thr Ser His 
1               5           


<210>  39
<211>  6
<212>  PRT
<213>  Artificial

<220>
<223>  CDRH2 for 1993-H02 - Chothia

<400>  39
000

Asp Pro Val Thr Gly Gly 
1               5       


<210>  40
<211>  11
<212>  PRT
<213>  Artificial

<220>
<223>  CDRH3 for 1993-H02 - Chothia

<400>  40
000

Glu Ala Arg Ala Asp Arg Gly Gln Phe Asp Lys 
1               5                   10      


<210>  41
<211>  120
<212>  PRT
<213>  Artificial

<220>
<223>  VH for HT186-D11

<400>  41
000

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


Ser Val Lys Val Ser Cys Lys Ala Ser Gly Tyr Ser Phe Thr Gly His 
            20                  25                  30          


Tyr Met His Trp Val Arg Gln Ala Pro Gly Gln Gly Leu Glu Trp Met 
        35                  40                  45              


Gly Trp Ile Asp Pro Val Thr Gly Gly Thr Lys Tyr Ala Gln Asn Phe 
    50                  55                  60                  


Gln Gly Trp Val Thr Met Thr Arg Asp Thr Ser Ile Arg Thr Ala Tyr 
65                  70                  75                  80  


Leu Glu Leu Ser Arg Leu Arg Ser Asp Asp Thr Ala Met Tyr Tyr Cys 
                85                  90                  95      


Ala Arg Glu Val Thr Gly Asp Arg Gly Gln Phe Asp Lys Trp Gly Gln 
            100                 105                 110         


Gly Thr Leu Val Thr Val Ala Ser 
        115                 120 


<210>  42
<211>  120
<212>  PRT
<213>  Artificial

<220>
<223>  VH for 1993-H02

<400>  42
000

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


Ser Val Lys Val Ser Cys Lys Ala Ser Gly Tyr Ser Phe Thr Ser His 
            20                  25                  30          


Phe Met His Trp Val Arg Gln Ala Pro Gly Gln Gly Leu Glu Trp Met 
        35                  40                  45              


Gly Trp Ile Asp Pro Val Thr Gly Gly Thr Lys Tyr Ala Gln Asn Phe 
    50                  55                  60                  


Gln Gly Trp Val Thr Met Thr Arg Asp Thr Ser Ile Arg Thr Ala Tyr 
65                  70                  75                  80  


Leu Glu Leu Ser Arg Leu Arg Ser Asp Asp Thr Ala Met Tyr Tyr Cys 
                85                  90                  95      


Ala Arg Glu Ala Arg Ala Asp Arg Gly Gln Phe Asp Lys Trp Gly Gln 
            100                 105                 110         


Gly Thr Leu Val Thr Val Ala Ser 
        115                 120 


<210>  43
<211>  107
<212>  PRT
<213>  Artificial

<220>
<223>  VL for HT186-D11 and for 1993-H02

<400>  43
000

Gln Ser Val Leu Thr Gln Pro Pro Ser Val Ser Val Ala Pro Gly Lys 
1               5                   10                  15      


Thr Ala Arg Ile Thr Cys Gly Gly Asn Asn Ile Gly Ser Lys Ser Val 
            20                  25                  30          


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


Tyr Gly Ser Asn Arg Pro Ser Gly Ile Pro Glu Arg Phe Ser Gly Ser 
    50                  55                  60                  


Asn Ser Gly Asn Thr Ala Thr Leu Thr Ile Ser Arg Val Glu Ala Gly 
65                  70                  75                  80  


Asp Glu Ala Asp Tyr Tyr Cys Gln Val Trp Asp Ser Ser Ser Asp Trp 
                85                  90                  95      


Val Phe Gly Gly Gly Thr Lys Leu Thr Val Leu 
            100                 105         


<210>  44
<211>  120
<212>  PRT
<213>  Artificial

<220>
<223>  VH for 1993-E03

<400>  44
000

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


Ser Val Lys Val Ser Cys Lys Ala Ser Gly Tyr Ser Phe Asn Asp His 
            20                  25                  30          


Phe Met His Trp Val Arg Gln Ala Pro Gly Gln Gly Leu Glu Trp Met 
        35                  40                  45              


Gly Trp Ile Asp Pro Val Thr Gly Gly Thr Lys Tyr Ala Gln Asn Phe 
    50                  55                  60                  


Gln Gly Trp Val Thr Met Thr Arg Asp Thr Ser Ile Arg Thr Ala Tyr 
65                  70                  75                  80  


Leu Glu Leu Ser Arg Leu Arg Ser Asp Asp Thr Ala Met Tyr Tyr Cys 
                85                  90                  95      


Ala Arg Glu Ala Arg Ala Asp Arg Gly Gln Phe Asp Lys Trp Gly Gln 
            100                 105                 110         


Gly Thr Leu Val Thr Val Ala Ser 
        115                 120 


<210>  45
<211>  120
<212>  PRT
<213>  Artificial

<220>
<223>  VH for 1993-H08

<400>  45
000

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


Ser Val Lys Val Ser Cys Lys Ala Ser Gly Tyr Ser Phe Thr Gly His 
            20                  25                  30          


Tyr Met His Trp Val Arg Gln Ala Pro Gly Gln Gly Leu Glu Trp Met 
        35                  40                  45              


Gly Trp Ile Asp Pro Val Thr Gly Glu Thr Lys Tyr Ala Gln Asn Phe 
    50                  55                  60                  


Gln Gly Trp Val Thr Met Thr Arg Asp Thr Ser Ile Arg Thr Ala Tyr 
65                  70                  75                  80  


Leu Glu Leu Ser Arg Leu Arg Ser Asp Asp Thr Ala Met Tyr Tyr Cys 
                85                  90                  95      


Ala Arg Glu Ala Arg Ala Asp Arg Gly Gln Phe Asp Lys Trp Gly Gln 
            100                 105                 110         


Gly Thr Leu Val Thr Val Ala Ser 
        115                 120 


<210>  46
<211>  120
<212>  PRT
<213>  Artificial

<220>
<223>  VH for 1993-G09

<400>  46
000

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


Ser Val Lys Val Ser Cys Lys Ala Ser Gly Tyr Ser Phe Thr Asp His 
            20                  25                  30          


Tyr Met His Trp Val Arg Gln Ala Pro Gly Gln Gly Leu Glu Trp Met 
        35                  40                  45              


Gly Trp Ile Asp Pro Val Thr Gly Glu Thr Lys Tyr Ala Gln Asp Phe 
    50                  55                  60                  


Gln Gly Trp Val Thr Met Thr Arg Asp Thr Ser Ile Arg Thr Ala Tyr 
65                  70                  75                  80  


Leu Glu Leu Ser Arg Leu Arg Ser Asp Asp Thr Ala Met Tyr Tyr Cys 
                85                  90                  95      


Ala Arg Glu Ala Arg Ala Asp Arg Gly Gln Phe Asp Lys Trp Gly Gln 
            100                 105                 110         


Gly Thr Leu Val Thr Val Ala Ser 
        115                 120 


<210>  47
<211>  120
<212>  PRT
<213>  Artificial

<220>
<223>  VH for 1993-E04

<400>  47
000

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


Ser Val Lys Val Ser Cys Lys Ala Ser Gly Tyr Ser Phe Thr Gly Asn 
            20                  25                  30          


Tyr Met His Trp Val Arg Gln Ala Pro Gly Gln Gly Pro Glu Trp Met 
        35                  40                  45              


Gly Trp Ile Asp Pro Val Thr Gly Glu Thr Lys Tyr Ala Gln Asn Phe 
    50                  55                  60                  


Gln Gly Trp Val Thr Met Thr Arg Asp Thr Ser Ile Arg Thr Ala Tyr 
65                  70                  75                  80  


Leu Glu Leu Ser Arg Leu Arg Ser Asp Asp Thr Ala Met Tyr Tyr Cys 
                85                  90                  95      


Ala Arg Glu Ala Arg Ala Ser Arg Gly Gln Phe Asp Lys Trp Gly Gln 
            100                 105                 110         


Gly Thr Leu Val Thr Val Ala Ser 
        115                 120 


<210>  48
<211>  120
<212>  PRT
<213>  Artificial

<220>
<223>  VH for 1993-D01

<400>  48
000

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


Ser Val Lys Val Ser Cys Lys Ala Ser Gly Tyr Pro Phe Thr Gly His 
            20                  25                  30          


Tyr Met His Trp Val Arg Gln Ala Pro Gly Gln Gly Pro Glu Trp Met 
        35                  40                  45              


Gly Trp Ile Asp Pro Val Thr Gly Glu Thr Arg Tyr Ala Gln Asn Phe 
    50                  55                  60                  


Gln Gly Trp Val Thr Met Thr Arg Asp Thr Ser Ile Arg Thr Ala Tyr 
65                  70                  75                  80  


Leu Glu Leu Ser Arg Leu Arg Ser Asp Asp Thr Ala Met Tyr Tyr Cys 
                85                  90                  95      


Ala Arg Glu Ala Arg Ala Asp Arg Gly Gln Phe Asp Lys Trp Gly Gln 
            100                 105                 110         


Gly Thr Leu Val Thr Val Ala Ser 
        115                 120 


