Research
Cyclic Peptides
Synthetic methods
Permeability
Therapeutic applications
Abstract 1560: Orally bioavailable macrocycles that target cyclins A and B RxL motifs cause tumor regression in xenograft models and in vitro show activity across multiple cancer types
Using structure-guided design we have developed cell-permeable macrocycle compounds that inhibit the RxL-mediated binding of substrates to both Cyclin A/CDK2 and Cyclin B/CDK1 complexes (Cyclin A/B RxL inhibitors) and have demonstrated that synthetic lethality requires inhibition of both Cyclins A and B
Cyclative Release of Peptidic Compounds
The present disclosure provides efficient and reliable methods for preparing cyclized peptidic compounds. Advantageously, the currently described methods allow for on-resin cyclization using a limited number of processing steps, while increasing the chemical diversity available for the cyclized peptidic compounds produced.
Synthetic Receptors
Cucurbiturils
Molecular recognition of peptides and proteins
Aromatic interactions