Hydrophilic sequence-defined cross-linkers for antibody–drug conjugates
… cross-linkers was … hydrophilicity, antigen binding, and in vitro potency. This work establishes
a versatile method for synthesizing multifunctional cross-linkers and identifies cross-linker …
a versatile method for synthesizing multifunctional cross-linkers and identifies cross-linker …
Synthesis and evaluation of hydrophilic linkers for antibody–maytansinoid conjugates
RY Zhao, SD Wilhelm, C Audette, G Jones… - Journal of medicinal …, 2011 - ACS Publications
… hydrophilic linkers suitable for conjugation of a thiol-containing cytotoxic agent. These linkers
… Although the ideal linker for all antibody–drug conjugates may not exist, we believe the …
… Although the ideal linker for all antibody–drug conjugates may not exist, we believe the …
[HTML][HTML] Polyethylene glycol-based linkers as hydrophilicity reservoir for antibody-drug conjugates
T Tedeschini, B Campara, A Grigoletto, M Bellini… - Journal of Controlled …, 2021 - Elsevier
… linker-drug architectures that improve the efficacy and stability of ADCs. In this context, the
use of hydrophilic linkers … of the most used cytotoxic drugs and positively impact the physical …
use of hydrophilic linkers … of the most used cytotoxic drugs and positively impact the physical …
Exatecan antibody drug conjugates based on a hydrophilic polysarcosine drug-linker platform
L Conilh, G Fournet, E Fourmaux, A Murcia, EL Matera… - Pharmaceuticals, 2021 - mdpi.com
… –drug conjugate (ADC) based on the topoisomerase I inhibitor payload exatecan, using our
hydrophilic monodisperse polysarcosine (PSAR) drug-linker … about the drug-linker structure–…
hydrophilic monodisperse polysarcosine (PSAR) drug-linker … about the drug-linker structure–…
Cleavable linkers in antibody–drug conjugates
JD Bargh, A Isidro-Llobet, JS Parker… - Chemical Society …, 2019 - pubs.rsc.org
… The hydrophilic linkers facilitated the conjugation of budesonide, a lipophilic glucocorticoid.
The ADC bearing the linker was active and selective in vitro but there has of yet been no in …
The ADC bearing the linker was active and selective in vitro but there has of yet been no in …
Investigation of hydrophilic auristatin derivatives for use in antibody drug conjugates
BA Mendelsohn, SD Barnscher, JT Snyder… - Bioconjugate …, 2017 - ACS Publications
… drug-linker were generated with increasing DAR. This was done to evaluate whether increased
drug hydrophilicity … our experience, the drug-linkers were conjugated to two human IgG2 …
drug hydrophilicity … our experience, the drug-linkers were conjugated to two human IgG2 …
[HTML][HTML] Antibody–drug conjugates: recent advances in linker chemistry
Z Su, D Xiao, F Xie, L Liu, Y Wang, S Fan… - … Pharmaceutica Sinica B, 2021 - Elsevier
… Moreover, the high hydrophilicity of the linker was … diester linker drug is greater than 5
mg/mL). In an in vitro evaluation, ADCs containing pyrophosphate and triphosphate diester linkers …
mg/mL). In an in vitro evaluation, ADCs containing pyrophosphate and triphosphate diester linkers …
Impact of cathepsin B-sensitive triggers and hydrophilic linkers on in vitro efficacy of novel site-specific antibody–drug conjugates
F Bryden, C Martin, S Letast, E Lles… - Organic & …, 2018 - pubs.rsc.org
… receptor affinity of the resulting antibody–drug conjugates (ADCs), we have demonstrated that
… this type of linker. In addition, while PEGylation augments linker hydrophilicity, this change …
… this type of linker. In addition, while PEGylation augments linker hydrophilicity, this change …
Linker technologies for antibody–drug conjugates
B Nolting - Antibody-drug conjugates, 2013 - Springer
… the conjugation of antibody and drug linker such as drug-to-antibody ratio and site of
conjugation. … the importance of linker hydrophilicity in the design for mAb-MGBA conjugates [111]. …
conjugation. … the importance of linker hydrophilicity in the design for mAb-MGBA conjugates [111]. …
Hydrophilic auristatin glycoside payload enables improved antibody-drug conjugate efficacy and biocompatibility
T Satomaa, H Pynnönen, A Vilkman, T Kotiranta… - Antibodies, 2018 - mdpi.com
… that this effect was due to the hydrophobic character of the current ADC payloads and that
by masking the hydrophobic payloads by hydrophilic linker moieties DAR = 8 ADCs with …
by masking the hydrophobic payloads by hydrophilic linker moieties DAR = 8 ADCs with …
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