1 research outputs found
The Development and Scale-Up of an Antibody Drug Conjugate Tubulysin Payload
Significant development and scale-up
work was completed on the
synthesis of an antibody drug conjugate payload based on the tubulysin
natural products. This work included the development of new routes
to the tubuvaline and tubuphenylaniline portions of the molecules,
as well as extensive optimization of the solid phase peptide synthesis
used to assemble the molecule. The initial route (21 steps longest
linear sequence, 0.01% overall yield) was improved to a new, more
robust route (19 steps longest linear sequence, 2.4% overall yield)
affording a 240-fold increase in overall yield and allowing delivery
of over 86 g of the required molecule