[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 …

Auristatin PYE, a novel synthetic derivative of dolastatin 10, is highly effective in human colon tumour models

SD Shnyder, PA Cooper… - International …, 2007 - spandidos-publications.com
Despite promising early data, the natural product dolastatin 10 has not been successful as a
single agent in phase II clinical trials. Herein the mechanism of action and efficacy of a …

Targeting cell surface alpha (v) beta (3) integrin increases therapeutic efficacies of a legumain protease-activated auristatin prodrug

Y Liu, KM Bajjuri, C Liu, SC Sinha - Molecular pharmaceutics, 2012 - ACS Publications
Novel monomethylauristatin E (MMAE) prodrug 8 was designed and prepared that bound
cell surface glycoprotein integrin αvβ3, and was activated using legumain protease as a …

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 …

Discovery of cytotoxic dolastatin 10 analogues with N-terminal modifications

A Maderna, M Doroski, C Subramanyam… - Journal of medicinal …, 2014 - ACS Publications
Auristatins, synthetic analogues of the antineoplastic natural product Dolastatin 10, are
ultrapotent cytotoxic microtubule inhibitors that are clinically used as payloads in antibody …

Development of potent monoclonal antibody auristatin conjugates for cancer therapy

SO Doronina, BE Toki, MY Torgov… - Nature …, 2003 - nature.com
We describe the in vitro and in vivo properties of monoclonal antibody (mAb)-drug
conjugates consisting of the potent synthetic dolastatin 10 analogs auristatin E (AE) and …

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 …

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 …

Recent advances in the development of new auristatins: structural modifications and application in antibody drug conjugates

A Maderna, CA Leverett - Molecular pharmaceutics, 2015 - ACS Publications
Dolastatin 10 is a powerful antineoplastic agent and microtubule inhibitor that was
discovered by Pettit et al. and published in 1987. Since then, many research groups have …

Investigation of hydrophilic auristatin derivatives for use in antibody drug conjugates

BA Mendelsohn, SD Barnscher, JT Snyder… - Bioconjugate …, 2017 - ACS Publications
Antibody drug conjugates offer a targeted cancer treatment for the delivery of potent
cytotoxic drugs. Derivatives of the natural product dolastatin 10 containing pyridines and …