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
Herein we describe the synthesis and evaluation of four novel HER2-targeting, cathepsin B-
sensitive antibody–drug conjugates bearing a monomethylauristatin E (MMAE) cytotoxic …
sensitive antibody–drug conjugates bearing a monomethylauristatin E (MMAE) cytotoxic …
Rapid, high-yielding solid-phase synthesis of cathepsin-B cleavable linkers for targeted cancer therapeutics
A Pryyma, S Gunasekera, J Lewin… - Bioconjugate …, 2020 - ACS Publications
Antibody–drug conjugates (ADCs) constitute an emerging class of anticancer agents that
deliver potent payloads selectively to tumors while avoiding systemic toxicity associated with …
deliver potent payloads selectively to tumors while avoiding systemic toxicity associated with …
Site selection: a case study in the identification of optimal cysteine engineered antibody drug conjugates
As the antibody drug conjugate (ADC) community continues to shift towards site-specific
conjugation technology, there is a growing need to understand how the site of conjugation …
conjugation technology, there is a growing need to understand how the site of conjugation …
Discovery of peptidomimetic antibody–drug conjugate linkers with enhanced protease specificity
BQ Wei, J Gunzner-Toste, H Yao, T Wang… - Journal of medicinal …, 2018 - ACS Publications
Antibody–drug conjugates (ADCs) have become an important therapeutic modality for
oncology, with three approved by the FDA and over 60 others in clinical trials. Despite the …
oncology, with three approved by the FDA and over 60 others in clinical trials. Despite the …
Exploring the effects of linker composition on site-specifically modified antibody–drug conjugates
AE Albers, AW Garofalo, PM Drake, R Kudirka… - European Journal of …, 2014 - Elsevier
In the context of antibody–drug conjugates (ADCs), noncleavable linkers provide a means to
deliver cytotoxic small molecules to cell targets while reducing systemic toxicity caused by …
deliver cytotoxic small molecules to cell targets while reducing systemic toxicity caused by …
Chemical generation of small molecule-based bispecific antibody-drug conjugates for broadening the target scope
Antibody-drug conjugates (ADCs) hold great therapeutic promise for cancer indications;
however, treating tumors with intratumor heterogeneity remains challenging. We …
however, treating tumors with intratumor heterogeneity remains challenging. We …
Construction of homogeneous antibody–drug conjugates using site-selective protein chemistry
P Akkapeddi, SA Azizi, AM Freedy, PMSD Cal… - Chemical …, 2016 - pubs.rsc.org
Systemic chemotherapy, the current standard of care for the treatment of cancer, is rarely
curative and is often accompanied by debilitating side effects. Targeted drug delivery stands …
curative and is often accompanied by debilitating side effects. Targeted drug delivery stands …
Incorporation of Hydrophilic Macrocycles Into Drug-Linker Reagents Produces Antibody-Drug Conjugates With Enhanced in vivo Performance
N Evans, R Grygorash, P Williams, A Kyle… - Frontiers in …, 2022 - frontiersin.org
Antibody-drug conjugates (ADCs) have begun to fulfil their promise as targeted cancer
therapeutics with ten clinical approvals to date. As the field matures, much attention has …
therapeutics with ten clinical approvals to date. As the field matures, much attention has …
Aldehyde tag coupled with HIPS chemistry enables the production of ADCs conjugated site-specifically to different antibody regions with distinct in vivo efficacy and …
PM Drake, AE Albers, J Baker, S Banas… - Bioconjugate …, 2014 - ACS Publications
It is becoming increasingly clear that site-specific conjugation offers significant advantages
over conventional conjugation chemistries used to make antibody–drug conjugates (ADCs) …
over conventional conjugation chemistries used to make antibody–drug conjugates (ADCs) …
Development of a facile antibody–drug conjugate platform for increased stability and homogeneity
Despite the advances in the design of antibody–drug conjugates (ADCs), the search is still
ongoing for novel approaches that lead to increased stability and homogeneity of the ADCs …
ongoing for novel approaches that lead to increased stability and homogeneity of the ADCs …