home chevron_right Programs chevron_right UPPBEAT™ Platform

UPPBEAT™ Platform

UPPBEAT™

Our covalent ligand screening platform for novel E3 ligase
① (non-Cys focused) covalent probe library
Probe = Fragment

Cys probe

Lys probe

Tyr probe

77
① Covalent probe integrated PROTAC
'Scout PROTACs' consists of
Warhead (e.g. BRD4 inhibitor)
E3L binder (Covalent probes)
77
② Covalent binding based screening
  1. Probe treats to cells or lysates
  2. Probe covalently binds to proteins including E3Ls with nucleophilic residue
77
② Degradation based screening
  1. Scout PROTACs treats to cells or lysates
  2. PROTAC covalently bound to a certain E3L degrades BRD4
77
③ ABPP method
  1. Reporter tag (biotin or fluorophores conjugation by CuACC)
  2. Trypsin digest
  1. Avidin enrichment
  2. Peptide elution
77
④ E3L deconvolution + binding probe verification

"Chemoproteomics (LC-MS/MS)"

"In-gel fluorescence scanning"