WDB002

**WDB002** is a natural product cyclic polyketide discovered through genome mining of *Streptomyces malaysiensis* isolates, featuring a conserved FKBP12-binding region similar to rapamycin and FK506 but with a unique variable domain and starter unit. It binds with high affinity (~4 nM) to FKBP12 in its hydrophobic pocket, forming a ternary complex that potently and selectively engages the featureless coiled-coil domain of human centrosomal protein 250 (**CEP250**) (~40 nM affinity), disrupting CEP250 function, centrosome organization, and NEK2-mediated centrosome separation in cells. Initially identified by Warp Drive Bio (a Revolution Medicines subsidiary), it exemplifies a "tri-complex" or molecular glue modality for targeting otherwise undruggable flat protein surfaces, with potential antiviral applications against SARS-CoV-2 due to CEP250's interaction with viral Nsp13.

Other names

WDB0011WDB-0011WDB 0011