                         SEQUENCE LISTING

<110>  Eisai R&D Management Co., Ltd.
       Kim, Dae-Shik
       Fang, Frank
       Endo, Atsushi
       Choi, Hyeong-Wook
       Hao, Ming-Hong
       Bao, Xingfeng
       Huang, Kuan-Chun
 
<120>  Compounds for the Treatment of Cancer

<130>  0080171-000371

<150>  62/460562
<151>  2017-02-17

<150>  62/479169
<151>  2017-03-30

<150>  62/551645
<151>  2017-08-29

<150>  62/551647
<151>  2017-08-29

<150>  62/551668
<151>  2017-08-29

<160>  7     

<170>  PatentIn version 3.5

<210>  1
<211>  1140
<212>  DNA
<213>  Homo sapiens

<400>  1
atgccccact ccagcctgca tccatccatc ccgtgtccca ggggtcacgg ggcccagaag       60

gcagccttgg ttctgctgag tgcctgcctg gtgacccttt gggggctagg agagccacca      120

gagcacactc tccggtacct ggtgctccac ctagcctccc tgcagctggg actgctgtta      180

aacggggtct gcagcctggc tgaggagctg cgccacatcc actccaggta ccggggcagc      240

tactggagga ctgtgcgggc ctgcctgggc tgccccctcc gccgtggggc cctgttgctg      300

ctgtccatct atttctacta ctccctccca aatgcggtcg gcccgccctt cacttggatg      360

cttgccctcc tgggcctctc gcaggcactg aacatcctcc tgggcctcaa gggcctggcc      420

ccagctgaga tctctgcagt gtgtgaaaaa gggaatttca acgtggccca tgggctggca      480

tggtcatatt acatcggata tctgcggctg atcctgccag agctccaggc ccggattcga      540

acttacaatc agcattacaa caacctgcta cggggtgcag tgagccagcg gctgtatatt      600

ctcctcccat tggactgtgg ggtgcctgat aacctgagta tggctgaccc caacattcgc      660

ttcctggata aactgcccca gcagaccggt gaccgggctg gcatcaagga tcgggtttac      720

agcaacagca tctatgagct tctggagaac gggcagcggg cgggcacctg tgtcctggag      780

tacgccaccc ccttgcagac tttgtttgcc atgtcacaat acagtcaagc tggctttagc      840

cgggaggata ggcttgagca ggccaaactc ttctgccgga cacttgagga catcctggca      900

gatgcccctg agtctcagaa caactgccgc ctcattgcct accaggaacc tgcagatgac      960

agcagcttct cgctgtccca ggaggttctc cggcacctgc ggcaggagga aaaggaagag     1020

gttactgtgg gcagcttgaa gacctcagcg gtgcccagta cctccacgat gtcccaagag     1080

cctgagctcc tcatcagtgg aatggaaaag cccctccctc tccgcacgga tttctcttga     1140


<210>  2
<211>  1140
<212>  DNA
<213>  Homo sapiens

<400>  2
atgccccact ccagcctgca tccatccatc ccgtgtccca ggggtcacgg ggcccagaag       60

gcagccttgg ttctgctgag tgcctgcctg gtgacccttt gggggctagg agagccacca      120

gagcacactc tccggtacct ggtgctccac ctagcctccc tgcagctggg actgctgtta      180

aacggggtct gcagcctggc tgaggagctg cgccacatcc actccaggta ccggggcagc      240

tactggagga ctgtgcgggc ctgcctgggc tgccccctcc gccgtggggc cctgttgctg      300

ctgtccatct atttctacta ctccctccca aatgcggtcg gcccgccctt cacttggatg      360

cttgccctcc tgggcctctc gcaggcactg aacatcctcc tgggcctcaa gggcctggcc      420

ccagctgaga tctctgcagt gtgtgaaaaa gggaatttca acgtggccca tgggctggca      480

tggtcatatt acatcggata tctgcggctg atcctgccag agctccaggc ccggattcga      540

acttacaatc agcattacaa caacctgcta cggggtgcag tgagccagcg gctgtatatt      600

ctcctcccat tggactgtgg ggtgcctgat aacctgagta tggctgaccc caacattcgc      660

ttcctggata aactgcccca gcagaccggt gaccatgctg gcatcaagga tcgggtttac      720

agcaacagca tctatgagct tctggagaac gggcagcggg cgggcacctg tgtcctggag      780

tacgccaccc ccttgcagac tttgtttgcc atgtcacaat acagtcaagc tggctttagc      840

cgggaggata ggcttgagca ggccaaactc ttctgccgga cacttgagga catcctggca      900

gatgcccctg agtctcagaa caactgccgc ctcattgcct accaggaacc tgcagatgac      960

agcagcttct cgctgtccca ggaggttctc cggcacctgc ggcaggagga aaaggaagag     1020

gttactgtgg gcagcttgaa gacctcagcg gtgcccagta cctccacgat gtcccaagag     1080

cctgagctcc tcatcagtgg aatggaaaag cccctccctc tccgcacgga tttctcttga     1140


<210>  3
<211>  1140
<212>  DNA
<213>  Homo sapiens

<400>  3
atgccccact ccagcctgca tccatccatc ccgtgtccca ggggtcacgg ggcccagaag       60

gcagccttgg ttctgctgag tgcctgcctg gtgacccttt gggggctagg agagccacca      120

gagcacactc tccggtacct ggtgctccac ctagcctccc tgcagctggg actgctgtta      180

aacggggtct gcagcctggc tgaggagctg cgccacatcc actccaggta ccggggcagc      240

tactggagga ctgtgcgggc ctgcctgggc tgccccctcc gccgtggggc cctgttgctg      300

ctgtccatct atttctacta ctccctccca aatgcggtcg gcccgccctt cacttggatg      360

cttgccctcc tgggcctctc gcaggcactg aacatcctcc tgggcctcaa gggcctggcc      420

ccagctgaga tctctgcagt gtgtgaaaaa gggaatttca acgtggccca tgggctggca      480

tggtcatatt acatcggata tctgcggctg atcctgccag agctccaggc ccggattcga      540

acttacaatc agcattacaa caacctgcta cggggtgcag tgagccagcg gctgtatatt      600

ctcctcccat tggactgtgg ggtgcctgat aacctgagta tggctgaccc caacattcgc      660

ttcctggata aactgcccca gcagaccgct gaccgagctg gcatcaagga tcgggtttac      720

agcaacagca tctatgagct tctggagaac gggcagcggg cgggcacctg tgtcctggag      780

tacgccaccc ccttgcagac tttgtttgcc atgtcacaat acagtcaagc tggctttagc      840

cgggaggata ggcttgagca ggccaaactc ttctgccaga cacttgagga catcctggca      900

gatgcccctg agtctcagaa caactgccgc ctcattgcct accaggaacc tgcagatgac      960

agcagcttct cgctgtccca ggaggttctc cggcacctgc ggcaggagga aaaggaagag     1020

gttactgtgg gcagcttgaa gacctcagcg gtgcccagta cctccacgat gtcccaagag     1080

cctgagctcc tcatcagtgg aatggaaaag cccctccctc tccgcacgga tttctcttga     1140


<210>  4
<211>  187
<212>  PRT
<213>  Homo sapiens

<400>  4

Val Ala His Gly Leu Ala Trp Ser Tyr Tyr Ile Gly Tyr Leu Arg Leu 
1               5                   10                  15      


Ile Leu Pro Glu Leu Gln Ala Arg Ile Arg Thr Tyr Asn Gln His Tyr 
            20                  25                  30          


Asn Asn Leu Leu Arg Gly Ala Val Ser Gln Arg Leu Tyr Ile Leu Leu 
        35                  40                  45              


Pro Leu Asp Cys Gly Val Pro Asp Asn Leu Ser Met Ala Asp Pro Asn 
    50                  55                  60                  


Ile Arg Phe Leu Asp Lys Leu Pro Gln Gln Thr Gly Asp Arg Ala Gly 
65                  70                  75                  80  


Ile Lys Asp Arg Val Tyr Ser Asn Ser Ile Tyr Glu Leu Leu Glu Asn 
                85                  90                  95      


Gly Gln Arg Ala Gly Thr Cys Val Leu Glu Tyr Ala Thr Pro Leu Gln 
            100                 105                 110         


Thr Leu Phe Ala Met Ser Gln Tyr Ser Gln Ala Gly Phe Ser Arg Glu 
        115                 120                 125             


Asp Arg Leu Glu Gln Ala Lys Leu Phe Cys Arg Thr Leu Glu Asp Ile 
    130                 135                 140                 


Leu Ala Asp Ala Pro Glu Ser Gln Asn Asn Cys Arg Leu Ile Ala Tyr 
145                 150                 155                 160 


Gln Glu Pro Ala Asp Asp Ser Ser Phe Ser Leu Ser Gln Glu Val Leu 
                165                 170                 175     


Arg His Leu Arg Gln Glu Glu Lys Glu Glu Val 
            180                 185         


<210>  5
<211>  311
<212>  PRT
<213>  Artificial Sequence

<220>
<223>  His-TEV-Sumo-WT STING construct

<400>  5

Met His His His His His His Ser Ser Gly Val Asp Leu Gly Thr Glu 
1               5                   10                  15      


Asn Leu Tyr Phe Gln Ser Asn Ala Met Ser Asp Ser Glu Val Asn Gln 
            20                  25                  30          


Glu Ala Lys Pro Glu Val Lys Pro Glu Val Lys Pro Glu Thr His Ile 
        35                  40                  45              


Asn Leu Lys Val Ser Asp Gly Ser Ser Glu Ile Phe Phe Lys Ile Lys 
    50                  55                  60                  


Lys Thr Thr Pro Leu Arg Arg Leu Met Glu Ala Phe Ala Lys Arg Gln 
65                  70                  75                  80  


Gly Lys Glu Met Asp Ser Leu Arg Phe Leu Tyr Asp Gly Ile Arg Ile 
                85                  90                  95      


Gln Ala Asp Gln Thr Pro Glu Asp Leu Asp Met Glu Asp Asn Asp Ile 
            100                 105                 110         


Ile Glu Ala His Arg Glu Gln Ile Gly Gly Gly Ser Val Ala His Gly 
        115                 120                 125             


Leu Ala Trp Ser Tyr Tyr Ile Gly Tyr Leu Arg Leu Ile Leu Pro Glu 
    130                 135                 140                 


Leu Gln Ala Arg Ile Arg Thr Tyr Asn Gln His Tyr Asn Asn Leu Leu 
145                 150                 155                 160 


Arg Gly Ala Val Ser Gln Arg Leu Tyr Ile Leu Leu Pro Leu Asp Cys 
                165                 170                 175     


Gly Val Pro Asp Asn Leu Ser Met Ala Asp Pro Asn Ile Arg Phe Leu 
            180                 185                 190         


Asp Lys Leu Pro Gln Gln Thr Gly Asp Arg Ala Gly Ile Lys Asp Arg 
        195                 200                 205             


Val Tyr Ser Asn Ser Ile Tyr Glu Leu Leu Glu Asn Gly Gln Arg Ala 
    210                 215                 220                 


Gly Thr Cys Val Leu Glu Tyr Ala Thr Pro Leu Gln Thr Leu Phe Ala 
225                 230                 235                 240 


Met Ser Gln Tyr Ser Gln Ala Gly Phe Ser Arg Glu Asp Arg Leu Glu 
                245                 250                 255     


Gln Ala Lys Leu Phe Cys Arg Thr Leu Glu Asp Ile Leu Ala Asp Ala 
            260                 265                 270         


Pro Glu Ser Gln Asn Asn Cys Arg Leu Ile Ala Tyr Gln Glu Pro Ala 
        275                 280                 285             


Asp Asp Ser Ser Phe Ser Leu Ser Gln Glu Val Leu Arg His Leu Arg 
    290                 295                 300                 


Gln Glu Glu Lys Glu Glu Val 
305                 310     


<210>  6
<211>  187
<212>  PRT
<213>  Homo sapiens

<400>  6

Val Ala His Gly Leu Ala Trp Ser Tyr Tyr Ile Gly Tyr Leu Arg Leu 
1               5                   10                  15      


Ile Leu Pro Glu Leu Gln Ala Arg Ile Arg Thr Tyr Asn Gln His Tyr 
            20                  25                  30          


Asn Asn Leu Leu Arg Gly Ala Val Ser Gln Arg Leu Tyr Ile Leu Leu 
        35                  40                  45              


Pro Leu Asp Cys Gly Val Pro Asp Asn Leu Ser Met Ala Asp Pro Asn 
    50                  55                  60                  


Ile Arg Phe Leu Asp Lys Leu Pro Gln Gln Thr Gly Asp His Ala Gly 
65                  70                  75                  80  


Ile Lys Asp Arg Val Tyr Ser Asn Ser Ile Tyr Glu Leu Leu Glu Asn 
                85                  90                  95      


Gly Gln Arg Ala Gly Thr Cys Val Leu Glu Tyr Ala Thr Pro Leu Gln 
            100                 105                 110         


Thr Leu Phe Ala Met Ser Gln Tyr Ser Gln Ala Gly Phe Ser Arg Glu 
        115                 120                 125             


Asp Arg Leu Glu Gln Ala Lys Leu Phe Cys Arg Thr Leu Glu Asp Ile 
    130                 135                 140                 


Leu Ala Asp Ala Pro Glu Ser Gln Asn Asn Cys Arg Leu Ile Ala Tyr 
145                 150                 155                 160 


Gln Glu Pro Ala Asp Asp Ser Ser Phe Ser Leu Ser Gln Glu Val Leu 
                165                 170                 175     


Arg His Leu Arg Gln Glu Glu Lys Glu Glu Val 
            180                 185         


<210>  7
<211>  311
<212>  PRT
<213>  Artificial Sequence

<220>
<223>  His-TEV-Sumo-REF STING 155-341 construct

<400>  7

Met His His His His His His Ser Ser Gly Val Asp Leu Gly Thr Glu 
1               5                   10                  15      


Asn Leu Tyr Phe Gln Ser Asn Ala Met Ser Asp Ser Glu Val Asn Gln 
            20                  25                  30          


Glu Ala Lys Pro Glu Val Lys Pro Glu Val Lys Pro Glu Thr His Ile 
        35                  40                  45              


Asn Leu Lys Val Ser Asp Gly Ser Ser Glu Ile Phe Phe Lys Ile Lys 
    50                  55                  60                  


Lys Thr Thr Pro Leu Arg Arg Leu Met Glu Ala Phe Ala Lys Arg Gln 
65                  70                  75                  80  


Gly Lys Glu Met Asp Ser Leu Arg Phe Leu Tyr Asp Gly Ile Arg Ile 
                85                  90                  95      


Gln Ala Asp Gln Thr Pro Glu Asp Leu Asp Met Glu Asp Asn Asp Ile 
            100                 105                 110         


Ile Glu Ala His Arg Glu Gln Ile Gly Gly Gly Ser Val Ala His Gly 
        115                 120                 125             


Leu Ala Trp Ser Tyr Tyr Ile Gly Tyr Leu Arg Leu Ile Leu Pro Glu 
    130                 135                 140                 


Leu Gln Ala Arg Ile Arg Thr Tyr Asn Gln His Tyr Asn Asn Leu Leu 
145                 150                 155                 160 


Arg Gly Ala Val Ser Gln Arg Leu Tyr Ile Leu Leu Pro Leu Asp Cys 
                165                 170                 175     


Gly Val Pro Asp Asn Leu Ser Met Ala Asp Pro Asn Ile Arg Phe Leu 
            180                 185                 190         


Asp Lys Leu Pro Gln Gln Thr Gly Asp His Ala Gly Ile Lys Asp Arg 
        195                 200                 205             


Val Tyr Ser Asn Ser Ile Tyr Glu Leu Leu Glu Asn Gly Gln Arg Ala 
    210                 215                 220                 


Gly Thr Cys Val Leu Glu Tyr Ala Thr Pro Leu Gln Thr Leu Phe Ala 
225                 230                 235                 240 


Met Ser Gln Tyr Ser Gln Ala Gly Phe Ser Arg Glu Asp Arg Leu Glu 
                245                 250                 255     


Gln Ala Lys Leu Phe Cys Arg Thr Leu Glu Asp Ile Leu Ala Asp Ala 
            260                 265                 270         


Pro Glu Ser Gln Asn Asn Cys Arg Leu Ile Ala Tyr Gln Glu Pro Ala 
        275                 280                 285             


Asp Asp Ser Ser Phe Ser Leu Ser Gln Glu Val Leu Arg His Leu Arg 
    290                 295                 300                 


Gln Glu Glu Lys Glu Glu Val 
305                 310     


