Optimizing PROTAC design: BRPF1 degraders as a treatment for AML

Live webinar 29 March 2022

The development of proteolysis targeting chimera (PROTAC) molecules is at the forefront of modern drug discovery. The field has matured to the extent that first-generation compounds have progressed into clinic and proven efficacy. We are now in an era of competitive PROTAC drug discovery, where an ability to understand the design concepts, specialist assays and the required triage cascades provides an advantage.

Join Dr. Daniel Glynn as he presents how Concept Life Sciences (CLS) approached the design and synthesis of a range of BRPF1 degraders targeting acute myeloid leukemia (AML). The designed degraders sit in highly desirable physicochemical space, and we showcase our degrader focused in-silico modeling. The prepared degraders, which utilize multiple E3 ligases, were screened against cell lines harboring mixed-lineage leukemia (MLL) translocations (for example the THP-1 cell line). Additionally, you’ll learn how the team investigated the ability of the compounds to effectively degrade the target and the suitability of our degraders for potential in-vivo exposure through a panel of routine ADMET assays.

During this webinar, you will learn:

how to design and synthesize PROTACs

the optimal design space for PROTACs

how CLS can support you with our services

You can register for free to all our webinars and you will automatically receive the On-Demand version