Simplified purification of secreted histidine-tagged proteins Marianne Carlsson GE Healthcare Life Sciences Outline Introduction Applications Summary 2 WT North America 17/04/2012 Immobilized Metal Ion Affinity Chromatography (IMAC) Histidine-tag Ligand Matrix Me2+ Protein Advantages of IMAC Histidine-tag Small with low charge Stable Compatible with many chemicals Compatible with denaturing conditions Chromatography medium High binding capacity Controllable selectivity Mild elution conditions Matrix 4 WT North America A challenge in IMAC purification Secretion into cultivation media for eukaryotic cells • Interfering substances: Chelators (e.g. EDTA), histidine, arginine, etc. • Low target protein concentration Large sample volumes (> 5 L) Issue: Stripping of immobilized Me2+ from conventional IMAC resins No or low binding of histidine-tagged protein 5 Conventional IMAC Protein secreted into CHO cell culture medium Resin: Sample: System: Ni Sepharose™ 6 Fast Flow (FF), 1 ml (column Ø=5 mm) 250 ml of mPAI-1-(his)8 secreted into GIBCO™ CD CHO medium, pH 7.0 ÄKTA™ avant 25 Mr x 103 97.0 66.0 45.0 30.0 20.1 14.4 1 Equilibration buffer: Wash buffer: Elution buffer: 2 3 4 5 20 mM sodium phosphate, 500 mM NaCl, pH 7.4 20 mM sodium phosphate, 500 mM NaCl, 10 mM imidazole, pH 7.4 20 mM sodium phosphate, 500 mM NaCl, 500 mM imidazole, pH 7.4 6 Remedy Common workflow Cell cultivation Removal of cells Diafiltration Final concentration and clarification IMAC with conventional Me2+ resin 7 Remedy Common workflow Cell cultivation Removal of cells Diafiltration Final concentration and clarification IMAC with conventional Me2+ resin 8 Remedy Common workflow Simplified workflow Cell cultivation Cell cultivation Removal of cells Removal of cells Diafiltration Final concentration and clarification IMAC with conventional Me2+ resin IMAC with Ni Sepharose™ excel HisTrap™ excel His Mag Sepharose excel Conventional IMAC Protein secreted into CHO cell culture medium Resin: Sample: System: Ni Sepharose™ 6 Fast Flow (FF), 1 ml (column Ø=5 mm) 250 ml of mPAI-1-(his)8 secreted into GIBCO™ CD CHO medium, pH 7.0 ÄKTA™ avant 25 Mr x 103 97.0 66.0 45.0 30.0 20.1 14.4 1 Equilibration buffer: Wash buffer: Elution buffer: 2 3 4 5 20 mM sodium phosphate, 500 mM NaCl, pH 7.4 20 mM sodium phosphate, 500 mM NaCl, 10 mM imidazole, pH 7.4 20 mM sodium phosphate, 500 mM NaCl, 500 mM imidazole, pH 7.4 10 Simplified IMAC Protein secreted into CHO cell culture medium Resins: Sample: System: Ni Sepharose™ excel (blue) and Ni Sepharose 6 FF (green), 1 ml (column Ø=5 mm) 250 ml of mPAI-1-(his)8 secreted into GIBCO™ CD CHO medium, pH 7.0 ÄKTA™ avant 25 Ni Sepharose 6 FF excel Mr x 103 97.0 66.0 45.0 30.0 20.1 14.4 1 2 3 4 5 6 7 8 Equilibration buffer: 20 mM sodium phosphate, 500 mM NaCl, 0 mM (excel) or 20 mM (FF) imidazole, pH 7.4 Wash buffer: 20 mM sodium phosphate, 500 mM NaCl, 10 mM (excel) or 20 mM (FF) imidazole, pH 7.4 Elution buffer: 20 mM sodium phosphate, 500 mM NaCl, 500 mM imidazole, pH 7.4 11 Nickel leakage (%) Nickel leakage 45 40 35 30 25 20 15 10 5 0 Ni Sepharose™ excel Ni Sepharose 6 FF EX-CELL™ 420 (SIGMA-ALDRICH) GIBCO™ CD CHO (Invitrogen) TC 100 (PAA) Cultivation medium Test: Analysis: 1 ml of each resin, incubated in 5 ml cultivation media for 24h at room temperature. Nickel leakage was determined by elemental analysis. 12 Compatibility with EDTA Column: Sample: System: HisTrap™ excel 1 ml 250 ml of proCPU-(his)8 secreted into GIBCO™ Sf-900 II insect cell medium, pH 6.8, later supplemented with 0 mM (dark blue), 2 mM (purple), or 10 mM (pale blue) EDTA ÄKTA™ avant 25 Eluates Mr x 103 97.0 66.0 45.0 30.0 20.1 14.4 1 Equilibration buffer: Wash buffer: Elution buffer: 2 3 4 20 mM sodium phosphate, 500 mM NaCl, pH 7.4 20 mM sodium phosphate, 500 mM NaCl, 15 mM imidazole, pH 7.4 20 mM sodium phosphate, 500 mM NaCl, 500 mM imidazole, pH 7.4 13 Outline Introduction Applications Summary 14 Protein secreted into insect cell culture medium Columns: Sample: Sample volumes: System: HisTrap™ excel 5 ml (blue) and HisTrap FF crude 5 ml (purple) (his)6-HA secreted into GIBCO™ Sf-900 II SFM insect cell culture medium, pH 6.6 1020 ml and 1012 ml, respectively ÄKTA™ M SW HisTrap excel 5 ml : Yield 8.9 mg of target protein HisTrap FF crude 5 ml: Yield too low to be quantified excel E M: Molecular Weight Standard S: Sample W: Wash E: Elution fractions Data from Dr. Linda Lua et al., UQ Protein Expression Facility, the University of Queensland, Brisbane, Australia. FF SW E Effect of sample pH on yield Ni Sepharose™ excel, 0.25 ml (column Ø=5 mm) 35 ml of 0.1 mg/ml MBP-(his)6 added to SAFC EX-CELL™ 405 culture medium, pH 5 to 8 ÄKTA™ avant 25 Eluted peak area (mAu*ml) Resin: Sample: System: 5000 MBP-(his)6 in EX-CELL 4000 3000 MBP-(his)6 in control buffer 2000 1000 0 4,5 5,5 6,5 pH 7,5 8,5 Yields are equal at sample pH values ranging from 6.0-7.5 16 Impact of imidazole on purity and yield Resin: Sample: His Mag Sepharose™ excel, 200 µl 10% medium slurry 10 ml PRCP-(his)9 secreted into SAFC EX-CELL™ 405 culture medium, pH 6.9 Wash Eluates Wash Eluates Wash Eluates Wash Eluates 97.0 66.0 45.0 30.0 20.1 14.4 0 mM imidazole 10 mM imidazole 30 mM imidazole 50 mM imidazole 100 80 80 60 60 40 40 20 20 0 0 Purity (%) Mr x 103 Relative yield (%) Imidazole conc was varied in the wash buffer: 0 mM (red), 10 mM (purple), 30 mM (green) and 50 mM (blue) 0 10 20 30 40 50 Wash buffer imidazole conc (mM) Higher imidazole concentration higher purity & lower yield 17 50-fold scale-up His Mag Sepharose™ excel HisTrap™ excel column Resin/column: His Mag Sepharose excel, 200 µl 10% medium slurry (blue) scaled up to HisTrap excel, 1 ml column (purple) Sample: 10 and 500 ml PRCP-(his)9 secreted into SAFC EX-CELL™ 405 culture medium, pH 6.9 30 mM imidazole was used in wash buffer for scale-up experiment Mr x 103 LMW His Mag HisTrap S 200 µl 1 ml 97.0 66.0 45.0 30.0 20.1 14.4 LMW: LMW-SDS Marker Kit S: Sample 18 Outline Introduction Applications Summary 17/04/2012 Summary IMAC purification of proteins secreted into eukaryotic cell culture media is simplified using Nickel Sepharose™ excel • Exceptionally strong binding of Ni2+ • Minimal sample pretreatment • No diafiltration or other buffer-exchange procedures needed • Broad pH range • Flexibility Acknowledgements • Dr. Linda Lua and members of UQ Protein Expression Facility, the University of Queensland, Brisbane, Australia • Dr. Wolfgang Knecht, CVGI iMed Bioscience and Dr. Paul Wan, Discovery Sciences, AstraZeneca R&D, Mölndal, Sweden 21 Thank you! ÄKTA, HisTrap, and Sepharose are trademarks of GE Healthcare companies. GE and GE Monogram are trademarks of General Electric Company. GIBCO is a trademark of Life Technologies Corporation. EX-CELL is a trademark of Sigma-Aldrich Co. Purification and preparation of fusion proteins and affinity peptides comprising at least two adjacent histidine residues may require a license under US patent numbers 5,284,933 and 5,310,663, and equivalent patents and patent applications in other countries assignee: Hoffman La Roche, Inc.). Ni Sepharose 6 Fast Flow products are sold under a license from Sigma-Aldrich under patent number EP 1277616 (Metal chelating compositions) and equivalent patents and patent applications in other countries. All goods and services are sold subject to the terms and conditions of sale of the company within GE Healthcare which supplies them. A copy of these terms and conditions is available on request. 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