1. No category

SO3Na
HS
F
NH 2
Amine-selective
conjugation
CN
NH
O
O
S
O
CBTF
N
N
N N
CN
N N
Cu
N N
Cu
N
N3
N
ADVANTAGES:
N N
N
Cys-selective
conjugation
N
N
N N
Alkyne-selective
conjugation
G1-Chelazide
- faster reaction rate
- higher selectivity
- full biocompatibility (exogeneous
copper source is not needed)
CN
S
H
N
BIOMOLECULE
(antibody,enzyme, polypeptide, etc)
O
LINKER
ADVANTAGES:
- increased selectivity
- better reproducibility
- higher reliability
- elevated stability of educts and adducts
O
O
O
O
+
+
OH OH
O
+
O
X = H, Cl, Br, I
N
X
X = H, Cl, Br, I
ADVANTAGES:
People suffering
from cancer:
O-
SPSA-click
O
Click&Release4
O
- mild cleavage conditions
- high efficiency of release
- elevated stability of educts and adducts
- possibility of transtagging-cleavage*
13 mln
X
O
O
O
O
N O
N+
SOE-link3
Lysosomal
release
OH OH
FUNCTIONAL TAG
(cytotoxic, contrast, fluorescent agent, etc)
X
N-
2x
ADCs currently
on the market:
O
N+
N
O
—
30x
ADCs in clinical
development:
NH 2 , — CO 2
N
ADVANTAGES:
- Copper-catalyzed or
strain-promoted pathways
- tunable reactivity of sydnone
scaffold (by changing the nature of X)
- the fastest among described strainpromoted couplings (k2 up to 5M-1s-1)5
- generation of a stable pyrazole linkage
1
Bioconjugate Chem. 25, 202–206 (2014);
Patent WO2015001117 (2014).
2
Angew. Chem. Int. Ed. 53, 5872–5876 (2014);
Patent WO2014057201 (2014).
3
Bioconjugate Chem. Submitted (2015).
4
Patent application EP14305933.5 (2014).
5
Angew. Chem. Int. Ed. 52, 12056–12060 (2013);
Chem. Commun. 10.1039/C4CC03816A (2014);
Patent application EP14305726.3 (2014).
Contact SYNDIVIA
Mail : [email protected]
Web : http://www.syndivia.com