Click chemistry selectively activates an auristatin protodrug with either intratumoral or systemic tumor-targeting agents

JM McFarland, M Aleckovic, G Coricor… - ACS Central …, 2023 - ACS Publications
The Click Activated Protodrugs Against Cancer (CAPAC) platform enables the activation of
powerful cancer drugs at tumors. CAPAC utilizes a click chemistry reaction between …

Molecular, macromolecular, and supramolecular glucuronide prodrugs: Lead identified for anticancer prodrug monotherapy

MT Jarlstad Olesen, R Walther, PP Poier… - Angewandte Chemie …, 2020 - Wiley Online Library
In this work, a tumor growth intervention by localized drug synthesis within the tumor volume,
using the enzymatic repertoire of the tumor itself, is presented. Towards the overall success …

Site-Specific Conjugation of Auristatins onto Engineered scFv Using Second Generation Maleimide to Target HER2-positive Breast Cancer in Vitro

N Aubrey, E Allard-Vannier, C Martin… - Bioconjugate …, 2018 - ACS Publications
Antibody-drug conjugates (ADC) are spearheading vectorized chemotherapy against
cancer, with 4 FDA-approved ADCs and 79 in clinical trials. However, most ADCs are …

[HTML][HTML] The legumain protease-activated auristatin prodrugs suppress tumor growth and metastasis without toxicity

KM Bajjuri, Y Liu, C Liu, SC Sinha - ChemMedChem, 2011 - ncbi.nlm.nih.gov
Naturally occurring antimitotic pentapeptide dolastatin 10 (1, Figure 1)[1] and its synthetic
analogue auristatin E (AE, 2)[2] possess subnanomolar cytotoxicity against many human …

A new delivery system for auristatin in STxB-drug conjugate therapy

C Batisse, E Dransart, RA Sarkouh, L Brulle… - European journal of …, 2015 - Elsevier
A key challenge in anticancer therapy is to gain control over the biodistribution of cytotoxic
drugs. The most promising strategy consists in conjugating drugs to tumor-targeting carriers …

Novel peptide linkers for highly potent antibody− auristatin conjugate

SO Doronina, TD Bovee, DW Meyer… - Bioconjugate …, 2008 - ACS Publications
Auristatins are highly potent antimitotic agents that have received considerable attention
because of their activities when targeted to tumor cells in the form of antibody− drug …

Novel auristatin E-based albumin-binding prodrugs with superior anticancer efficacy in vivo compared to the parent compound

L Pes, SD Koester, JP Magnusson, S Chercheja… - Journal of controlled …, 2019 - Elsevier
Auristatins are a class of highly cytotoxic tubulin-disrupting peptides, which have shown
limited therapeutic effect as free agents in clinical trials. In our continuing effort to develop …

Antibody–drug conjugate payloads; study of auristatin derivatives

M Akaiwa, J Dugal-Tessier… - Chemical and …, 2020 - jstage.jst.go.jp
Auristatins are important payloads used in antibody drug conjugates (ADCs), and the most
well-known compound family member, monomethyl auristatin (MMAE), is used in two Food …

Specific Cytotoxic Effect of an Auristatin Nanoconjugate Towards CXCR4+ Diffuse Large B-Cell Lymphoma Cells

A Falgàs, V Pallarès, U Unzueta, Y Núñez… - International Journal …, 2021 - Taylor & Francis
Background and Purpose Around 40–50% of diffuse large-B cell lymphoma (DLBCL)
patients suffer from refractory disease or relapse after R-CHOP first-line treatment. Many …

Novel Auristatins with High Bystander and Cytotoxic Activities in Drug Efflux–Positive Tumor Models

PN Moquist, TD Bovee, AB Waight, JA Mitchell… - Molecular Cancer …, 2021 - AACR
Auristatins, a class of clinically validated anti-tubulin agents utilized as payloads in antibody–
drug conjugates, are generally classified by their membrane permeability and the extent of …