                         SEQUENCE LISTING

<110>  Spitfire Pharma
 
<120>  GLP-1R and GCGR Agonists, Formulations, and Methods of Use

<130>  MED007.PCT

<150>  62/980,093
<151>  2020-02-21

<150>  63/122,108
<151>  2020-12-07

<150>  63/133,540
<151>  2021-01-04

<160>  33    

<170>  PatentIn version 3.5

<210>  1
<211>  29
<212>  PRT
<213>  Artificial sequence

<220>
<223>  Synthetic Peptide


<220>
<221>  MOD_RES
<222>  (2)..(2)
<223>  Aib

<220>
<221>  SITE
<222>  (16)..(16)
<223>  Glu side chain lactam linkage to Lys

<220>
<221>  SITE
<222>  (16)..(20)
<223>  cyclic

<220>
<221>  MOD_RES
<222>  (17)..(17)
<223>  Z17CO2H

<220>
<221>  SITE
<222>  (20)..(20)
<223>  Lys side chain lactam linkage to Glu

<400>  1

His Xaa Gln Gly Thr Phe Thr Ser Asp Tyr Ser Lys Tyr Leu Asp Glu 
1               5                   10                  15      


Lys Ala Ala Lys Glu Phe Ile Gln Trp Leu Leu Gln Thr  
            20                  25                    


<210>  2
<211>  29
<212>  PRT
<213>  Artificial sequence

<220>
<223>  Synthetic Peptide


<220>
<221>  MOD_RES
<222>  (2)..(2)
<223>  Aib

<220>
<221>  SITE
<222>  (16)..(16)
<223>  Glu side chain lactam linkage to Lys

<220>
<221>  SITE
<222>  (16)..(20)
<223>  cyclic

<220>
<221>  MOD_RES
<222>  (17)..(17)
<223>  Me15CO2H

<220>
<221>  SITE
<222>  (20)..(20)
<223>  Lys side chain lactam linkage to Glu

<400>  2

His Xaa Gln Gly Thr Phe Thr Ser Asp Tyr Ser Lys Tyr Leu Asp Glu 
1               5                   10                  15      


Lys Ala Ala Lys Glu Phe Ile Gln Trp Leu Leu Gln Thr  
            20                  25                    


<210>  3
<211>  29
<212>  PRT
<213>  Artificial sequence

<220>
<223>  Synthetic Peptide


<220>
<221>  MOD_RES
<222>  (2)..(2)
<223>  Aib

<220>
<221>  SITE
<222>  (16)..(16)
<223>  Glu side chain lactam linkage to Lys

<220>
<221>  SITE
<222>  (16)..(20)
<223>  cyclic

<220>
<221>  SITE
<222>  (20)..(20)
<223>  Lys side chain lactam linkage to Glu

<220>
<221>  MOD_RES
<222>  (24)..(24)
<223>  Z15CO2H

<400>  3

His Xaa Gln Gly Thr Phe Thr Ser Asp Tyr Ser Lys Tyr Leu Asp Glu 
1               5                   10                  15      


Gln Ala Ala Lys Glu Phe Ile Lys Trp Leu Leu Gln Thr  
            20                  25                    


<210>  4
<211>  29
<212>  PRT
<213>  Artificial sequence

<220>
<223>  Synthetic Peptide


<220>
<221>  MOD_RES
<222>  (2)..(2)
<223>  Aib

<220>
<221>  SITE
<222>  (16)..(16)
<223>  Glu side chain lactam linkage to Lys

<220>
<221>  SITE
<222>  (16)..(20)
<223>  cyclic

<220>
<221>  SITE
<222>  (20)..(20)
<223>  Lys side chain lactam linkage to Glu

<220>
<221>  MOD_RES
<222>  (24)..(24)
<223>  Z17CO2H

<400>  4

His Xaa Gln Gly Thr Phe Thr Ser Asp Tyr Ser Lys Tyr Leu Asp Glu 
1               5                   10                  15      


Gln Ala Ala Lys Glu Phe Ile Lys Trp Leu Leu Gln Thr  
            20                  25                    


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

<220>
<223>  Synthetic Peptide


<220>
<221>  MOD_RES
<222>  (2)..(2)
<223>  Aib

<220>
<221>  SITE
<222>  (16)..(16)
<223>  Glu side chain lactam linkage to Lys

<220>
<221>  SITE
<222>  (16)..(20)
<223>  cyclic

<220>
<221>  MOD_RES
<222>  (17)..(17)
<223>  Z17CO2H

<220>
<221>  SITE
<222>  (20)..(20)
<223>  Lys side chain lactam linkage to Glu

<400>  5

His Xaa Gln Gly Thr Phe Thr Ser Asp Tyr Ser Arg Tyr Leu Asp Glu 
1               5                   10                  15      


Lys Ala Ala Lys Glu Phe Ile Gln Trp Leu Leu Gln Thr  
            20                  25                    


<210>  6
<211>  29
<212>  PRT
<213>  Artificial sequence

<220>
<223>  Synthetic Peptide


<220>
<221>  MOD_RES
<222>  (2)..(2)
<223>  Aib

<220>
<221>  SITE
<222>  (16)..(20)
<223>  cyclic

<220>
<221>  SITE
<222>  (16)..(16)
<223>  Glu side chain lactam linkage to Lys

<220>
<221>  MOD_RES
<222>  (17)..(17)
<223>  Lys(N-omega(1-(17-carboxyl-heptadecyloxy)beta-D-glucuronyl)) or 
       Lys(Z17CO2H)

<220>
<221>  SITE
<222>  (20)..(20)
<223>  Lys side chain lactam linkage to Glu

<400>  6

His Xaa Gln Gly Thr Phe Thr Ser Asp Tyr Ser Lys Tyr Leu Asp Glu 
1               5                   10                  15      


Xaa Ala Ala Lys Glu Phe Ile Gln Trp Leu Leu Gln Thr 
            20                  25                  


<210>  7
<211>  29
<212>  PRT
<213>  Artificial sequence

<220>
<223>  Synthetic Peptide


<220>
<221>  MOD_RES
<222>  (2)..(2)
<223>  Aib

<220>
<221>  SITE
<222>  (16)..(20)
<223>  cyclic

<220>
<221>  SITE
<222>  (16)..(16)
<223>  Glu side chain lactam linkage to Lys

<220>
<221>  MOD_RES
<222>  (17)..(17)
<223>  Me17CO2H

<220>
<221>  SITE
<222>  (20)..(20)
<223>  Lys side chain lactam linkage to Glu

<400>  7

His Xaa Gln Gly Thr Phe Thr Ser Asp Tyr Ser Lys Tyr Leu Asp Glu 
1               5                   10                  15      


Lys Ala Ala Lys Glu Phe Ile Gln Trp Leu Leu Gln Thr 
            20                  25                  


<210>  8
<211>  29
<212>  PRT
<213>  Artificial sequence

<220>
<223>  Synthetic Peptide


<220>
<221>  MOD_RES
<222>  (2)..(2)
<223>  Aib

<220>
<221>  SITE
<222>  (16)..(20)
<223>  cyclic

<220>
<221>  SITE
<222>  (16)..(16)
<223>  Glu side chain lactam linkage to Lys

<220>
<221>  SITE
<222>  (20)..(20)
<223>  Lys side chain lactam linkage to Glu

<220>
<221>  MOD_RES
<222>  (24)..(24)
<223>  Lys(Z15CO2H)

<400>  8

His Xaa Gln Gly Thr Phe Thr Ser Asp Tyr Ser Lys Tyr Leu Asp Glu 
1               5                   10                  15      


Gln Ala Ala Lys Glu Phe Ile Xaa Trp Leu Leu Gln Thr 
            20                  25                  


<210>  9
<211>  29
<212>  PRT
<213>  Artificial sequence

<220>
<223>  Synthetic Peptide


<220>
<221>  MOD_RES
<222>  (2)..(2)
<223>  Aib

<220>
<221>  SITE
<222>  (16)..(20)
<223>  cyclic

<220>
<221>  SITE
<222>  (16)..(16)
<223>  Glu side chain lactam linkage to Lys

<220>
<221>  SITE
<222>  (20)..(20)
<223>  Lys side chain lactam linkage to Glu

<220>
<221>  MOD_RES
<222>  (24)..(24)
<223>  Lys(Z17CO2H)

<400>  9

His Xaa Gln Gly Thr Phe Thr Ser Asp Tyr Ser Lys Tyr Leu Asp Glu 
1               5                   10                  15      


Gln Ala Ala Lys Glu Phe Ile Xaa Trp Leu Leu Gln Thr 
            20                  25                  


<210>  10
<211>  29
<212>  PRT
<213>  Artificial sequence

<220>
<223>  Synthetic Peptide


<220>
<221>  MOD_RES
<222>  (2)..(2)
<223>  Aib

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

<220>
<221>  SITE
<222>  (16)..(20)
<223>  cyclic

<220>
<221>  SITE
<222>  (16)..(16)
<223>  Glu side chain lactam linkage to Lys

<220>
<221>  MOD_RES
<222>  (17)..(17)
<223>  Lys(N-omega(1-(17-carboxyl-heptadecyloxy)beta-D-glucuronyl)) or 
       Lys(Z17CO2H)

<220>
<221>  SITE
<222>  (20)..(20)
<223>  Lys side chain lactam linkage to Glu

<400>  10

His Xaa Gln Gly Thr Phe Thr Ser Asp Tyr Ser Xaa Tyr Leu Asp Glu 
1               5                   10                  15      


Xaa Ala Ala Lys Glu Phe Ile Gln Trp Leu Leu Gln Thr 
            20                  25                  


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

<220>
<223>  Synthetic Peptide


<220>
<221>  MOD_RES
<222>  (2)..(2)
<223>  Aib

<220>
<221>  MOD_RES
<222>  (20)..(20)
<223>  Lys(yGlu-2xOEG)

<400>  11

His Xaa Glu Gly Thr Phe Thr Ser Asp Val Ser Ser Tyr Leu Glu Gly 
1               5                   10                  15      


Gln Ala Ala Xaa Glu Phe Ile Ala Trp Leu Val Arg Gly Arg Gly 
            20                  25                  30      


<210>  12
<211>  29
<212>  PRT
<213>  Artificial sequence

<220>
<223>  Synthetic Peptide


<220>
<221>  MOD_RES
<222>  (2)..(2)
<223>  Aib

<220>
<221>  SITE
<222>  (16)..(20)
<223>  cyclic

<220>
<221>  SITE
<222>  (16)..(16)
<223>  Glu side chain lactam linkage to Lys

<220>
<221>  SITE
<222>  (16)..(20)
<223>  Lys side chain lactam linkage to Glu

<220>
<221>  MOD_RES
<222>  (24)..(24)
<223>  Lys(GC8)

<400>  12

His Xaa Gln Gly Thr Phe Thr Ser Asp Tyr Ser Lys Tyr Leu Asp Glu 
1               5                   10                  15      


Gln Ala Ala Lys Glu Phe Ile Lys Trp Leu Leu Gln Thr 
            20                  25                    


<210>  13
<211>  30
<212>  PRT
<213>  Artificial sequence

<220>
<223>  Synthetic Peptide


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

<220>
<221>  misc_feature
<222>  (30)..(30)
<223>  Xaa can be any naturally occurring amino acid

<400>  13

His Xaa Gln Gly Thr Phe Thr Ser Asp Tyr Ser Lys Tyr Leu Asp Glu 
1               5                   10                  15      


Gln Ala Ala Lys Glu Phe Ile Lys Trp Leu Leu Gln Thr Xaa 
            20                  25                  30  


<210>  14
<211>  30
<212>  PRT
<213>  Artificial sequence

<220>
<223>  Synthetic Peptide


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

<220>
<221>  misc_feature
<222>  (30)..(30)
<223>  Xaa can be any naturally occurring amino acid

<400>  14

His Xaa Gln Gly Thr Phe Thr Ser Asp Tyr Ser Lys Tyr Leu Asp Glu 
1               5                   10                  15      


Gln Ala Ala Lys Glu Phe Ile Lys Trp Leu Leu Gln Thr Xaa 
            20                  25                  30  


<210>  15
<211>  30
<212>  PRT
<213>  Artificial sequence

<220>
<223>  Synthetic Peptide


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

<220>
<221>  misc_feature
<222>  (30)..(30)
<223>  Xaa can be any naturally occurring amino acid

<400>  15

His Xaa Gln Gly Thr Phe Thr Ser Asp Tyr Ser Lys Tyr Leu Asp Glu 
1               5                   10                  15      


Gln Ala Ala Lys Glu Phe Ile Lys Trp Leu Leu Gln Thr Xaa 
            20                  25                  30  


<210>  16
<211>  30
<212>  PRT
<213>  Artificial sequence

<220>
<223>  Synthetic Peptide


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

<220>
<221>  misc_feature
<222>  (30)..(30)
<223>  Xaa can be any naturally occurring amino acid

<400>  16

His Xaa Gln Gly Thr Phe Thr Ser Asp Tyr Ser Lys Tyr Leu Asp Glu 
1               5                   10                  15      


Gln Ala Ala Lys Glu Phe Ile Lys Trp Leu Leu Gln Thr Xaa 
            20                  25                  30  


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

<220>
<223>  Synthetic Peptide


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

<220>
<221>  misc_feature
<222>  (30)..(30)
<223>  Xaa can be any naturally occurring amino acid

<400>  17

His Xaa Gln Gly Thr Phe Thr Ser Asp Tyr Ser Lys Tyr Leu Asp Glu 
1               5                   10                  15      


Gln Ala Ala Lys Glu Phe Ile Lys Trp Leu Leu Gln Thr Xaa 
            20                  25                  30  


<210>  18
<211>  30
<212>  PRT
<213>  Artificial sequence

<220>
<223>  Synthetic Peptide


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

<220>
<221>  misc_feature
<222>  (30)..(30)
<223>  Xaa can be any naturally occurring amino acid

<400>  18

His Xaa Gln Gly Thr Phe Thr Ser Asp Tyr Ser Lys Tyr Leu Asp Glu 
1               5                   10                  15      


Gln Ala Ala Lys Glu Phe Ile Lys Trp Leu Leu Gln Thr Xaa 
            20                  25                  30  


<210>  19
<211>  30
<212>  PRT
<213>  Artificial sequence

<220>
<223>  Synthetic Peptide


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

<220>
<221>  misc_feature
<222>  (30)..(30)
<223>  Xaa can be any naturally occurring amino acid

<400>  19

His Xaa Gln Gly Thr Phe Thr Ser Asp Tyr Ser Lys Tyr Leu Asp Glu 
1               5                   10                  15      


Gln Ala Ala Lys Glu Phe Ile Lys Trp Leu Leu Gln Thr Xaa 
            20                  25                  30  


<210>  20
<211>  30
<212>  PRT
<213>  Artificial sequence

<220>
<223>  Synthetic Peptide


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

<220>
<221>  misc_feature
<222>  (30)..(30)
<223>  Xaa can be any naturally occurring amino acid

<400>  20

His Xaa Gln Gly Thr Phe Thr Ser Asp Tyr Ser Lys Tyr Leu Asp Glu 
1               5                   10                  15      


Gln Ala Ala Lys Glu Phe Ile Lys Trp Leu Leu Gln Thr Xaa 
            20                  25                  30  


<210>  21
<211>  30
<212>  PRT
<213>  Artificial sequence

<220>
<223>  Synthetic Peptide


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

<220>
<221>  misc_feature
<222>  (30)..(30)
<223>  Xaa can be any naturally occurring amino acid

<400>  21

His Xaa Gln Gly Thr Phe Thr Ser Asp Tyr Ser Lys Tyr Leu Asp Glu 
1               5                   10                  15      


Gln Ala Ala Lys Glu Phe Ile Lys Trp Leu Leu Gln Thr Xaa 
            20                  25                  30  


<210>  22
<211>  30
<212>  PRT
<213>  Artificial sequence

<220>
<223>  Synthetic Peptide


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

<220>
<221>  misc_feature
<222>  (30)..(30)
<223>  Xaa can be any naturally occurring amino acid

<400>  22

His Xaa Gln Gly Thr Phe Thr Ser Asp Tyr Ser Lys Tyr Leu Asp Glu 
1               5                   10                  15      


Gln Ala Ala Lys Glu Phe Ile Lys Trp Leu Leu Gln Thr Xaa 
            20                  25                  30  


<210>  23
<211>  30
<212>  PRT
<213>  Artificial sequence

<220>
<223>  Synthetic Peptide


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

<220>
<221>  misc_feature
<222>  (30)..(30)
<223>  Xaa can be any naturally occurring amino acid

<400>  23

His Xaa Gln Gly Thr Phe Thr Ser Asp Tyr Ser Lys Tyr Leu Asp Glu 
1               5                   10                  15      


Lys Ala Ala Lys Glu Phe Ile Gln Trp Leu Leu Gln Thr Xaa 
            20                  25                  30  


<210>  24
<211>  30
<212>  PRT
<213>  Artificial sequence

<220>
<223>  Synthetic Peptide


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

<220>
<221>  misc_feature
<222>  (30)..(30)
<223>  Xaa can be any naturally occurring amino acid

<400>  24

His Xaa Gln Gly Thr Phe Thr Ser Asp Tyr Ser Lys Tyr Leu Asp Glu 
1               5                   10                  15      


Gln Ala Ala Lys Glu Phe Ile Lys Trp Leu Leu Gln Thr Xaa 
            20                  25                  30  


<210>  25
<211>  30
<212>  PRT
<213>  Artificial sequence

<220>
<223>  Synthetic Peptide


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

<220>
<221>  misc_feature
<222>  (30)..(30)
<223>  Xaa can be any naturally occurring amino acid

<400>  25

His Xaa Gln Gly Thr Phe Thr Ser Asp Tyr Ser Lys Tyr Leu Asp Glu 
1               5                   10                  15      


Gln Ala Ala Lys Glu Phe Ile Lys Trp Leu Leu Gln Thr Xaa 
            20                  25                  30  


<210>  26
<211>  30
<212>  PRT
<213>  Artificial sequence

<220>
<223>  Synthetic Peptide


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

<220>
<221>  misc_feature
<222>  (30)..(30)
<223>  Xaa can be any naturally occurring amino acid

<400>  26

His Xaa Gln Gly Thr Phe Thr Ser Asp Tyr Ser Lys Tyr Leu Asp Glu 
1               5                   10                  15      


Gln Ala Ala Lys Glu Phe Ile Lys Trp Leu Leu Gln Thr Xaa 
            20                  25                  30  


<210>  27
<211>  30
<212>  PRT
<213>  Artificial sequence

<220>
<223>  Synthetic Peptide


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

<220>
<221>  misc_feature
<222>  (30)..(30)
<223>  Xaa can be any naturally occurring amino acid

<400>  27

His Xaa Gln Gly Thr Phe Thr Ser Asp Tyr Ser Lys Tyr Leu Asp Glu 
1               5                   10                  15      


Gln Ala Ala Lys Glu Phe Ile Lys Trp Leu Leu Gln Thr Xaa 
            20                  25                  30  


<210>  28
<400>  28
000

<210>  29
<400>  29
000

<210>  30
<211>  31
<212>  PRT
<213>  Artificial sequence

<220>
<223>  Synthetic Peptide

<400>  30

His Ala Glu Gly Thr Phe Thr Ser Asp Val Ser Ser Tyr Leu Glu Gly 
1               5                   10                  15      


Gln Ala Ala Lys Glu Phe Ile Ala Trp Leu Val Lys Gly Arg Gly 
            20                  25                  30      


<210>  31
<211>  29
<212>  PRT
<213>  Artificial sequence

<220>
<223>  Synthetic Peptide

<400>  31

His Ser Gln Gly Thr Phe Thr Ser Asp Tyr Ser Lys Tyr Leu Asp Ser 
1               5                   10                  15      


Arg Arg Ala Gln Asp Phe Val Gln Trp Leu Met Asn Thr 
            20                  25                  


<210>  32
<211>  30
<212>  PRT
<213>  Artificial sequence

<220>
<223>  Synthetic Peptide


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

<220>
<221>  misc_feature
<222>  (30)..(30)
<223>  Xaa can be any naturally occurring amino acid

<400>  32

His Xaa Gln Gly Thr Phe Thr Ser Asp Tyr Ser Lys Tyr Leu Asp Glu 
1               5                   10                  15      


Gln Ala Ala Lys Glu Phe Ile Cys Trp Leu Met Asn Thr Xaa 
            20                  25                  30  


<210>  33
<211>  30
<212>  PRT
<213>  Artificial sequence

<220>
<223>  Synthetic Peptide


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

<220>
<221>  misc_feature
<222>  (30)..(30)
<223>  Xaa can be any naturally occurring amino acid

<400>  33

His Xaa Gln Gly Thr Phe Thr Ser Asp Tyr Ser Lys Tyr Leu Asp Glu 
1               5                   10                  15      


Lys Ala Ala Lys Glu Phe Ile Lys Trp Lys Lys Gln Thr Xaa 
            20                  25                  30  


