Evotec Munich

More documents

Recommendations

Info

0,01 0,1 1 K d[µM] PAGE 13 DDR1 BCR ABL1 ABL2 PIP4K2A PIP4K2C Target profile of imatinib in K562 cells KinAffinity Native kinome profiling of type II inhibitors Imatinib (Gleevec , Novartis) is approved for the treatment of CML and GIST and is known to inhibit several tyrosine kinases KinAffinity identified imatinib’s main kinase targets with the exception of PDGFR, which is not expressed in K562 cells N N N N NH H O N N
0,1 1 10 K d M PAGE 14 K d [µM] MIER3 C16orf87 SIN3A SIN3B MIER1 NCOR1 RCOR2 NCOR2 MIER2 CHD3 GPS2 BHC80 ZNF217 GSE1 BRAF35 CoREST HDAC1 RERE ZNF261 AOF2 GATAD2A RCOR3 HDAC2 IRA1 WDR5 MTA3 TBL1 GATAD2B CHD4 MTA1 MBD3 RBBP4 HMG20A HDAC3 MTA2 ISOC2 ZNF198 RBBP7 HDAC6 DBP5 MBD2 KPNA3 PP3476 HDAC10 KPNA4 LAMB2 ALDH2 MBLAC2 CK2a1 ALDH1B1 TTC38 HDAC8 Epigenetics Target Profiling Profiling of SAHA (Vorinostat) using a generic matrix 80 80 60 60 40 40 HDAC1 20 20 0,19 120 100 100 80 80 60 60 40 HDAC4 40 - 20 20 % Bound 0 -20 120 20 0 -20 1 10 102 Conc [µM] 120 120 100 100 80 80 60 60 40 HDAC5 40 - 20 20 100 100 80 80 60 60 HDAC7 - 40 40 % Bound % Bound 0 -20 120 20 0 -20 1 10 102 Conc [µM] 120 100 100 80 80 60 60 HDAC6 40 0,43 40 1 10 102 Conc [µM] 120 100 100 80 80 60 60 HDAC8 6,5 40 40 % Bound 120 20 0 -20 1 10 102 Conc [µM] 100 100 80 80 60 60 HDAC10 0,79 40 40 % Bound % Bound % Bound 120 100 0 -20 120 100 0 -20 120 20 0 -20 1 10 102 Conc [µM] 80 80 60 60 40 40 HDAC2 0,24 20 20 % Bound 120 100 0 -20 1 10 102 Conc [µM] 80 80 60 60 40 40 HDAC3 0,35 20 20 HDAC Known HDAC complex partner Other proteins Target profile in human ovarian cancer (A2780) cells % Bound Binding Competition K d M 1 10 102 Conc [µM] 1 10 102 Conc [µM] 1 10 102 Conc [µM] % Bound % Bound % Bound % Bound % Bound % Bound % Bound % Bound % Bound 120 100 0 -20 120 100 0 -20 120 100 0 -20 120 0 -20 0 -20 20 0 -20 120 20 0 -20 20 0 -20 120 20 0 -20 -2 10 10-1 100 101 Conc [µM] -2 10 10-1 100 101 Conc [µM] -2 10 10-1 100 101 Conc [µM] -2 10 10-1 100 101 Conc [µM] -2 10 10-1 100 101 Conc [µM] -2 10 10-1 Conc [µM] 100 101 -2 10 10-1 100 101 Conc [µM] -2 10 10-1 100 101 Conc [µM] -2 10 10-1 100 101 Conc [µM] Epigenetics Target Profiling allows for maximum HDAC coverage and constitutes a native assay under conditions that preserve the integrity of HDAC complexes
Page 1 and 2: Evotec Munich Building innovative d
Page 3 and 4: PAGE 2 Evotec Munich Technology Off
Page 5 and 6: PAGE 4 Cellular Target Profiling R
Page 7 and 8: Kd [µM] 0.01 0.1 1.0 10 PAGE 6 PI3
Page 9 and 10: 0,1 1 10 K d [µM] PAGE 8 Parafibro
Page 11 and 12: PAGE 10 Cellular Target Profiling
Page 13: 0,01 0,1 1 10 K d[µM] PAGE 12 MAP4
Page 17 and 18: PAGE 16 Complete Proteome Analysis
Page 19 and 20: PAGE 18 PhosphoScout ® - Case Stud
Page 21 and 22: N O N PAGE 20 O N O N F F F Cl Phos
Page 23 and 24: Test sample set (cell lines, xenogr
Page 25: Your contact: proteomics@evotec.com

Evotec Munich

You also want an ePaper? Increase the reach of your titles

Delete template?

Save as template?