cyclin A/B RxL inhibitor CID-078

An orally bioavailable macrocycle inhibitor of cyclin A and B RxL, with potential antineoplastic activity. Upon oral administration, cyclin A/B RxL inhibitor CID-078 selectively targets and binds to the hydrophobic patch (HP) of cyclins A and B and prevents cyclin A and B substrates containing RxL motifs from binding to cyclins A and B, thereby preventing their interaction, including the interaction of the cyclin A substrate E2F1 with cyclin A-cyclin-dependent kinase 2 (CDK2) and the cyclin B substrate Myt1 with cyclin B-CDK1. This may lead to DNA cell damage and cell cycle arrest during the G1/S transition, induce apoptosis, and inhibit proliferation of susceptible tumor cells. Cyclins A and B play a key role in the regulation and progression of the cell cycle and their function is dysregulated in certain tumor cell types.