                         SEQUENCE LISTING

<110>  Mainline Biosciences
 
<120>  HIGH AFFINITY CXCR4 SELECTIVE BINDING CONJUGATE AND METHOD FOR 
       USING THE SAME

<130>  MLB-000300PC

<150>  62/554,354
<151>  2017-09-05

<160>  12    

<170>  PatentIn version 3.5

<210>  1
<211>  11
<212>  PRT
<213>  Artificial Sequence

<220>
<223>  Compound of Formula II


<220>
<221>  MISC_FEATURE
<222>  (1)..(1)
<223>  Along with the sulfur atom that is attached to is 
       3-mercaptopropionic acid (MPA), optionally N-substituted cysteine
       or optionally N-substituted homocysteine

<220>
<221>  MISC_FEATURE
<222>  (1)..(7)
<223>  Forms cyclic structure via sulfur atoms and a linker 
       -(CH2-Ar1-CH2)-, where Ar1 is an optionally substituted aryl

<220>
<221>  MISC_FEATURE
<222>  (3)..(3)
<223>  can be Arg, Dap, Dab, Orn, Lys, Dap(iPr), Dab(iPr), Orn(iPr), or 
       Lys(iPr)

<220>
<221>  MISC_FEATURE
<222>  (4)..(4)
<223>  D-isomer

<220>
<221>  MISC_FEATURE
<222>  (5)..(5)
<223>  2Nal

<220>
<221>  MISC_FEATURE
<222>  (7)..(7)
<223>  Along with the sulfur atom that is attached to is cysteine or 
       homocysteine

<220>
<221>  MISC_FEATURE
<222>  (8)..(8)
<223>  can be Arg, Dap, Dab, Orn, Lys, Dap(iPr), Dab(iPr), Orn(iPr), 
       Lys(iPr), D-Arg, D-Dap, D-Dab, D-Orn, D-Lys, D-Dap(iPr), 
       D-Dab(iPr), D-Orn(iPr), D-Lys(iPr), or absent

<220>
<221>  MISC_FEATURE
<222>  (9)..(9)
<223>  can be Gly or absent

<220>
<221>  MISC_FEATURE
<222>  (10)..(10)
<223>  can be Lys, Phe, 2Nal, 1Nal, the D-isomer thereof, Gly, or absent

<220>
<221>  MISC_FEATURE
<222>  (11)..(11)
<223>  Lys, Gly or absent

<220>
<221>  MISC_FEATURE
<222>  (11)..(11)
<223>  terminal -OH group is replaced with -OR4 or -NHR5, wherein R4 and
       R5 is H, alkyl, optionally substituted aryl, or optionally 
       substituted aralkyl

<400>  1

Xaa Tyr Xaa Arg Xaa Gly Xaa Xaa Xaa Xaa Xaa 
1               5                   10      


<210>  2
<211>  8
<212>  PRT
<213>  Artificial Sequence

<220>
<223>  Compound of Formula III


<220>
<221>  MISC_FEATURE
<222>  (1)..(1)
<223>  along with the sulfur atom that is attached thereto is 
       3-mercaptopropionic acid, optionally substituted cysteine, or 
       optionally substituted homocysteine

<220>
<221>  MISC_FEATURE
<222>  (1)..(7)
<223>  Forms cyclic structure via sulfur atoms and a linker 
       -(CH2-Ar1-CH2)-, where Ar1 is an optionally substituted aryl

<220>
<221>  MISC_FEATURE
<222>  (3)..(3)
<223>  can be Arg, Dap, Dab, Orn, Lys, Dap(iPr), Dab(iPr), Orn(iPr), or 
       Lys(iPr)

<220>
<221>  MISC_FEATURE
<222>  (4)..(4)
<223>  D-isomer

<220>
<221>  MISC_FEATURE
<222>  (5)..(5)
<223>  2Nal

<220>
<221>  MISC_FEATURE
<222>  (7)..(7)
<223>  along with the sulfur atom that is attached thereto is cysteine 
       or homocysteine

<220>
<221>  MISC_FEATURE
<222>  (7)..(7)
<223>  along with the sulfur atom that is attached thereto is cysteine 
       or homocysteine

<220>
<221>  MISC_FEATURE
<222>  (8)..(8)
<223>  can be Arg, Dap, Dab, Orn, Lys, Dap(iPr), Dab(iPr), Orn(iPr), 
       Lys(iPr), D-Arg, D-Dap, D-Dab, D-Orn, D-Lys, D-Dap(iPr), 
       D-Dab(iPr), D-Orn(iPr), D-Lys(iPr), or absent

<400>  2

Xaa Tyr Xaa Arg Xaa Gly Xaa Xaa 
1               5               


<210>  3
<211>  8
<212>  PRT
<213>  Artificial Sequence

<220>
<223>  S-Paclitaxel


<220>
<221>  MISC_FEATURE
<222>  (1)..(7)
<223>  cyclic structure is formed between the alpha-amino of 
       phenylalanince

<220>
<221>  MISC_FEATURE
<222>  (3)..(3)
<223>  side-chain amino acid of lysine is substituted with iso-propyl 
       group

<220>
<221>  MISC_FEATURE
<222>  (4)..(4)
<223>  D-isomer

<220>
<221>  MISC_FEATURE
<222>  (5)..(5)
<223>  2NaI

<220>
<221>  MISC_FEATURE
<222>  (7)..(7)
<223>  D-isomer

<220>
<221>  MISC_FEATURE
<222>  (8)..(8)
<223>  side-chain amino group is substituted with iso-propyl.

<400>  3

Phe Tyr Lys Arg Xaa Gly Gln Lys 
1               5               


<210>  4
<211>  8
<212>  PRT
<213>  Artificial Sequence

<220>
<223>  linked to paclitaxel


<220>
<221>  MISC_FEATURE
<222>  (1)..(7)
<223>  cyclic structure is formed by formation of a di-sulfide linkage 
       between sulfur atoms of two cysteine groups.

<220>
<221>  MISC_FEATURE
<222>  (3)..(3)
<223>  side-chain amino group is substituted with isopropyl

<220>
<221>  MISC_FEATURE
<222>  (4)..(4)
<223>  D-isomer

<220>
<221>  MISC_FEATURE
<222>  (5)..(5)
<223>  NaI

<220>
<221>  MISC_FEATURE
<222>  (8)..(8)
<223>  side-chain amino group is substituted with isopropyl

<400>  4

Cys Tyr Lys Arg Xaa Gly Cys Lys 
1               5               


<210>  5
<211>  8
<212>  PRT
<213>  Artificial Sequence

<220>
<223>  linked to paclitaxel


<220>
<221>  MISC_FEATURE
<222>  (1)..(1)
<223>  homocysteine

<220>
<221>  MISC_FEATURE
<222>  (1)..(7)
<223>  cyclic structure is formed by formation of a di-sulfide linkage 
       between sulfur atoms of homocysteine and cysteine

<220>
<221>  MISC_FEATURE
<222>  (3)..(3)
<223>  side-chain amino group is substituted with isopropyl

<220>
<221>  MISC_FEATURE
<222>  (4)..(4)
<223>  D-isome

<220>
<221>  MISC_FEATURE
<222>  (5)..(5)
<223>  2NaI

<220>
<221>  MISC_FEATURE
<222>  (8)..(8)
<223>  side-chain amino group is substituted with isopropyl

<400>  5

Xaa Tyr Lys Arg Xaa Gly Cys Lys 
1               5               


<210>  6
<211>  8
<212>  PRT
<213>  Artificial Sequence

<220>
<223>  linked to paclitaxel


<220>
<221>  MISC_FEATURE
<222>  (1)..(7)
<223>  cyclic structure is formed by formation of a di-sulfide linkage 
       between sulfur atoms of cysteine and homocysteine

<220>
<221>  MISC_FEATURE
<222>  (3)..(3)
<223>  side-chain amino group is substituted with isopropyl

<220>
<221>  MISC_FEATURE
<222>  (4)..(4)
<223>  D-isomer

<220>
<221>  MISC_FEATURE
<222>  (5)..(5)
<223>  2NaI

<220>
<221>  MISC_FEATURE
<222>  (7)..(7)
<223>  homocysteine

<220>
<221>  MISC_FEATURE
<222>  (8)..(8)
<223>  side-chain amino group is substituted with isopropyl

<400>  6

Cys Tyr Lys Arg Xaa Gly Xaa Lys 
1               5               


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

<220>
<223>  linked to paclitaxel


<220>
<221>  MISC_FEATURE
<222>  (1)..(7)
<223>  Forms cyclic structure via sulfur atoms and a linker 
       -(CH2-(1,2-Ph)-CH2)-.

<220>
<221>  MISC_FEATURE
<222>  (3)..(3)
<223>  side-chain amino group is substituted with isopropyl

<220>
<221>  MISC_FEATURE
<222>  (4)..(4)
<223>  D-isomer

<220>
<221>  MISC_FEATURE
<222>  (5)..(5)
<223>  2NaI

<220>
<221>  MISC_FEATURE
<222>  (8)..(8)
<223>  side-chain amino group is substituted with isopropyl

<400>  7

Cys Tyr Lys Arg Xaa Gly Cys Leu 
1               5               


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

<220>
<223>  Example 1 statring material


<220>
<221>  MISC_FEATURE
<222>  (1)..(1)
<223>  protected with Mmt

<220>
<221>  MISC_FEATURE
<222>  (2)..(2)
<223>  protected with tBu

<220>
<221>  MISC_FEATURE
<222>  (3)..(3)
<223>  side-chain amino group is substituted with isopropyl

<220>
<221>  MISC_FEATURE
<222>  (3)..(3)
<223>  protected with Boc

<220>
<221>  MISC_FEATURE
<222>  (4)..(4)
<223>  D-isomer

<220>
<221>  MISC_FEATURE
<222>  (4)..(4)
<223>  protected with Pbf

<220>
<221>  MISC_FEATURE
<222>  (5)..(5)
<223>  2NaI

<220>
<221>  MISC_FEATURE
<222>  (6)..(6)
<223>  side-chain amino group is substituted with isopropyl

<220>
<221>  MISC_FEATURE
<222>  (6)..(6)
<223>  protected with Boc

<220>
<221>  MISC_FEATURE
<222>  (6)..(6)
<223>  linked to -(mini-PEG6)-Cys(Trt)

<400>  8

Cys Tyr Lys Arg Xaa Cys Lys 
1               5           


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

<220>
<223>  Reagent of Example 2


<220>
<221>  MISC_FEATURE
<222>  (1)..(1)
<223>  protected with Trt

<220>
<221>  MISC_FEATURE
<222>  (2)..(2)
<223>  protected with Mmt

<220>
<221>  MISC_FEATURE
<222>  (3)..(3)
<223>  protected with tBu

<220>
<221>  MISC_FEATURE
<222>  (4)..(4)
<223>  side-chain amino group is substituted with isopropyl

<220>
<221>  MISC_FEATURE
<222>  (4)..(4)
<223>  protected with Boc

<220>
<221>  MISC_FEATURE
<222>  (5)..(5)
<223>  D-isomer

<220>
<221>  MISC_FEATURE
<222>  (5)..(5)
<223>  protected with Pbf

<220>
<221>  MISC_FEATURE
<222>  (6)..(6)
<223>  2NaI

<220>
<221>  MISC_FEATURE
<222>  (8)..(8)
<223>  protected with Mmt

<220>
<221>  MISC_FEATURE
<222>  (9)..(9)
<223>  side-chain amino group is substituted with isopropyl

<220>
<221>  MISC_FEATURE
<222>  (9)..(9)
<223>  protected with Boc

<400>  9

Cys Cys Tyr Lys Arg Xaa Gly Cys Lys Gly 
1               5                   10  


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

<220>
<223>  reagent for example 4


<220>
<221>  MISC_FEATURE
<222>  (1)..(1)
<223>  protected with Trt

<220>
<221>  MISC_FEATURE
<222>  (1)..(2)
<223>  linker (mini-PEG6) is present between two cysteine groups

<220>
<221>  MISC_FEATURE
<222>  (2)..(2)
<223>  protected wtih Mmt

<220>
<221>  MISC_FEATURE
<222>  (3)..(3)
<223>  protected wtih tBu

<220>
<221>  MISC_FEATURE
<222>  (4)..(4)
<223>  side-chain amino group is substituted with isopropyl

<220>
<221>  MISC_FEATURE
<222>  (4)..(4)
<223>  protected with Boc

<220>
<221>  MISC_FEATURE
<222>  (5)..(5)
<223>  D-isomer

<220>
<221>  MISC_FEATURE
<222>  (5)..(5)
<223>  protected with Pbf

<220>
<221>  MISC_FEATURE
<222>  (6)..(6)
<223>  2NaI

<220>
<221>  MISC_FEATURE
<222>  (8)..(8)
<223>  protected with Mmt

<220>
<221>  MISC_FEATURE
<222>  (9)..(9)
<223>  side-chain amino group is substituted with isopropyl

<220>
<221>  MISC_FEATURE
<222>  (9)..(9)
<223>  protected with Boc

<400>  10

Cys Cys Tyr Leu Arg Xaa Gly Cys Leu Gly 
1               5                   10  


<210>  11
<211>  10
<212>  PRT
<213>  Artificial Sequence

<220>
<223>  reagent for example 5


<220>
<221>  MISC_FEATURE
<222>  (2)..(2)
<223>  protected with tBu

<220>
<221>  MISC_FEATURE
<222>  (3)..(3)
<223>  side-chain amino group is substituted with isopropyl

<220>
<221>  MISC_FEATURE
<222>  (3)..(3)
<223>  protected with Boc

<220>
<221>  MISC_FEATURE
<222>  (4)..(4)
<223>  protected with Pbf

<220>
<221>  MISC_FEATURE
<222>  (4)..(4)
<223>  D-isomer

<220>
<221>  MISC_FEATURE
<222>  (5)..(5)
<223>  2NaI

<220>
<221>  MISC_FEATURE
<222>  (7)..(7)
<223>  protected with OAll

<220>
<221>  MISC_FEATURE
<222>  (7)..(7)
<223>  D-isomer

<220>
<221>  MISC_FEATURE
<222>  (8)..(8)
<223>  side-chain amino group is substituted with isopropyl

<220>
<221>  MISC_FEATURE
<222>  (8)..(8)
<223>  protected with Boc

<220>
<221>  MISC_FEATURE
<222>  (8)..(9)
<223>  linker (mini-PEG6) is present between lysine and cysteine

<220>
<221>  MISC_FEATURE
<222>  (9)..(9)
<223>  protected with Trt

<400>  11

Phe Tyr Lys Arg Xaa Gly Gln Lys Cys Gly 
1               5                   10  


<210>  12
<211>  10
<212>  PRT
<213>  Artificial Sequence

<220>
<223>  reagent for Example 6


<220>
<221>  MISC_FEATURE
<222>  (1)..(1)
<223>  protected with Mmt

<220>
<221>  MISC_FEATURE
<222>  (2)..(2)
<223>  protected with tBu

<220>
<221>  MISC_FEATURE
<222>  (3)..(3)
<223>  side-chain amino group is substituted with isopropyl

<220>
<221>  MISC_FEATURE
<222>  (3)..(3)
<223>  protected with Boc

<220>
<221>  MISC_FEATURE
<222>  (4)..(4)
<223>  protected with Pbf

<220>
<221>  MISC_FEATURE
<222>  (4)..(4)
<223>  D-isomer

<220>
<221>  MISC_FEATURE
<222>  (5)..(5)
<223>  2NaI

<220>
<221>  MISC_FEATURE
<222>  (7)..(7)
<223>  protected with Mmt

<220>
<221>  MISC_FEATURE
<222>  (8)..(8)
<223>  protected with Boc

<220>
<221>  MISC_FEATURE
<222>  (8)..(8)
<223>  side-chain amino group is substituted with isopropyl

<220>
<221>  MISC_FEATURE
<222>  (10)..(10)
<223>  protected with Trt

<400>  12

Cys Tyr Lys Arg Xaa Gly Cys Lys Gly Cys 
1               5                   10  


