SelDeg51 in complex with FKBP51FK1 domain and pVHL:EloB:EloC

[(1~{R})-3-(3,4-dimethoxyphenyl)-1-[4-[[1-[3-[2-[[[(2~{S},4~{R})-1-[(2~{S})-2-[(1-fluoranylcyclopropyl)carbonylamino]-3,3-dimethyl-butanoyl]-4-oxidanyl-pyrrolidin-2-yl]carbonylamino]methyl]-5-(4-methyl-1,3-thiazol-5-yl)phenoxy]propyl]-1,2,3-triazol-4-yl]methoxy]phenyl]propyl] (2~{S})-1-[(2~{S})-2-cyclohexyl-2-(3,4,5-trimethoxyphenyl)ethanoyl]piperidine-2-carboxylate

Discovery of a Potent PROTAC Enables Targeting of FKBP51's Scaffolding Functions

von Hippel-Lindau disease tumor suppressor

Peptidyl-prolyl cis-trans isomerase FKBP5

EloC,Elongin 15 kDa subunit,RNA polymerase II transcription factor SIII subunit C,SIII p15,Transcription elongation factor B polypeptide 1

EloB,Elongin 18 kDa subunit,RNA polymerase II transcription factor SIII subunit B,SIII p18,Transcription elongation factor B polypeptide 2

PPIase FKBP5,51 kDa FK506-binding protein,FKBP-51,54 kDa progesterone receptor-associated immunophilin,Androgen-regulated protein 6,FF1 antigen,FK506-binding protein 5,FKBP-5,FKBP54,p54,HSP90-binding immunophilin,Rotamase

15% PEG3350, 0.2 M tri-sodium citrate, 0.1 M HEPES-NaOH pH 7.5 and 10% glycol

German Federal Ministry for Education and Research

Hydrogens have been added in their riding positions

FKBP51, SAFit, Complex, PROTAC, ISOMERASE

Local NCS retraints between domains: 1 2

Local NCS retraints between domains: 3 4

Local NCS retraints between domains: 5 6

Local NCS retraints between domains: 7 8