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 …

We report on the synthesis, in vitro and in vivo biological evaluations of a dimeric β-
glucuronidase-responsive albumin-binding prodrug designed for the double release of …

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 …

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 …

Monomethyl auristatin E and monomethyl auristatin F are widely used cytotoxic agents in
antibody–drug conjugates (ADCs), a group of promising cancer drugs. The ADCs …

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 …

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 …

A prodrug is bioreversible medication that is specifically converted to the active drugs by
enzymes overexpressed in the tumor microenvironment, which can considerably reduce the …

Background: Breast cancer is a heterogeneous disease characterized by differential
responses to targeted and chemotherapeutic agents. Antibody-drug conjugates are one of …

Effective antibody-drug conjugates (ADC) combine high drug-linker stability in circulation
and efficient intratumoral release of drug. Conjugation of monomethyl auristatin E (MMAE) to …