US 12,128,110 B2
Transglutaminase conjugation method and linker
Philipp Spycher, Zurich (CH); Roger Schibli, Baden (CH); Martin Behe, Gelterkinde (CH); and Jori Wehrmuller, Zurich (CH)
Assigned to PAUL SCHERRER INSTITUT, Villigen PSI (CH)
Appl. No. 16/648,636
Filed by Paul Scherrer Institut, Villigen PSI (CH)
PCT Filed Sep. 19, 2018, PCT No. PCT/EP2018/075350
§ 371(c)(1), (2) Date Mar. 18, 2020,
PCT Pub. No. WO2019/057772, PCT Pub. Date Mar. 28, 2019.
Claims priority of application No. 17191825 (EP), filed on Sep. 19, 2017; and application No. 1800878 (GB), filed on Jan. 19, 2018.
Prior Publication US 2021/0128743 A1, May 6, 2021
Int. Cl. C07K 16/32 (2006.01); A61K 47/68 (2017.01); C07K 16/28 (2006.01); C12P 21/00 (2006.01)
CPC A61K 47/6855 (2017.08) [A61K 47/6803 (2017.08); A61K 47/6889 (2017.08); C07K 16/2878 (2013.01); C07K 16/32 (2013.01); C12P 21/00 (2013.01); C07K 2317/24 (2013.01); C07K 2317/41 (2013.01)] 31 Claims
 
1. An antibody conjugate comprising
a) one or more linker constructs comprising a linker having the peptide structure (shown in N->C direction):

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and
b) an antibody comprising at least one Gln residue (Q295) at position 295 (EU numbering) of the CH2 domain of the antibody, wherein the antibody is N-glycosylated in position N297 (EU numbering) of the CH2 domain;
wherein:
m is an integer between ≥0 and ≤12;
n is an integer between ≥0 and ≤12;
o is an integer between ≥0 and ≤12;
m+n+o is an integer between ≥1 and ≤12;
Aax is any naturally or non-naturally occurring L- or D-amino acid, or amino acid derivative or mimetic;

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is a lysine or a lysine derivative or a lysine mimetic having a primary amine group;
B is a payload or a linking moiety
and wherein:
the linker construct is conjugated to the Gln residue Q295 of the CH2 domain of the antibody via the primary amine group of

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