Non-Degrading Molecular Glues: A Platform for Finding Novel Chemical Matter for Inhibiting Intracellular & Transmembrane Proteins
Time: 2:00 pm
day: Post-Conference Focus Day
Details:
- The described macrocycles form ternary complexes comprising a presenter protein (FKBP12), the molecular glue, and a target protein. Inhibition through formation of a ternary complex often results in potency, selectivity over homologous proteins and favorable drug like properties such as slow binding kinetics
- The construction of DEL and array libraries of molecular glues will be discussed as well as perspectives on topological diversity
- Screening of the platform has yielded chemical starting points have been discovered for several target classes. One program will described SAR leading to potent, cell permeable macrocycles for the inhibition of an oncology target. Another program will discuss the inhibition of a nucleoside transporter target that has yielded a development candidate
