The targeted delivery of small-molecule drugs through the use of antibodies has required the development of novel synthetic chemistry to selectively modify proteins (bioconjugation) as well as create stable and bioreversible linkers to a wide variety of functional groups found on synthetic drugs. The decoupling of stability and release inherent in disulfide bond linkers has resulted in well-behaved, homogeneous, efficacious antibody-drug conjugates for treating cancer. Expanding the utility of this linker to the alcohol of VHL-containing heterobifunctional protein degraders (or PROTACs) has resulted in a general approach to enabling the target delivery of this class of molecules, overcoming pharmacokinetic challenges inherent in this class of "medium"-sized molecules as well as offering improved selectivity.

Role of organic chemistry in developing new linker and conjugation chemistries for antibody-drug conjugates

Fall 2022 abstracts, posters, and presentations will launch in mid-September.

ACS Fall 2022

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.