Protein Characterization: Testing to Triage Lead Candidates

Purity/impurity testing, structural characterization (e.g., MS- based protein ID and post translational modification analysis), and SPR/ELISA/cell-based activity assays.

Protein Sciences: Early-Stage R&D Protein Characterization Services

Mass Spectrometry

• Intact Mass/PeptideMap/ Disulfide • N-/O- Glycan Analysis • De Novo Antibody Sequence • Proteomics • HCP

Our experience extends beyond standard monoclonal antibodies to more complex biologics like bispecific and multi-specific antibodies. The most common contaminant in bispecific antibody production are homodimers. Other mispairings can happen that can be revealed by mass intact mass analysis. Detailed characterization of bispecific antibodies by intact mass analysis At WuXi Biologics, our Protein Sciences (PS) Department provides comprehensive protein characterization testing during early-stage R&D activities. Our extensive capabilities cover routine testing of the critical quality attributes and additional product characterization aspects of your lead molecule. Capabilities include purity/impurity testing, structural characterization (e.g., mass spectrometry- based protein ID and post translational modification analysis), and SPR/ELISA/cell-based activity assays. This comprehensive analysis enables our clients to thoroughly assess their molecules much earlier during the discovery stage and triage/optimize the leads more effectively.

Micro Developability Package • Biophysical: DSF, DLS • Polyspecificity/PK Indicating Assay: Baculovirus/DNA/ Insulin Binding

Impurity Test • Residual DNA • Host Cell Protein • Residual Protein A • Endotoxin

Solutions

Binding Activity & MOA Related Bioassay • SPR/BLI Binding Assay • Enzymatic Activity Assay • ELISA/Cell-based Bioassay

Purity Test by LC&CE

• SEC-HPLC • SEC-MALS • CEX-HPLC • NR/R CE-SDS • icIEF

Surface Plasmon Resonance (SPR)

Surface Plasmon Resonance (SPR) is an optical technique used to measure molecular interactions in real time. SPR can occur when plane-polarized light hits a metal film under total internal reflection conditions. Benefits of SPR: an ideal tool for evaluating product characteristics such as binding

Kinetics/A inity

10 15 20 25 30 35 40

HC1 homodimer 150 kDa

HC2 homodimer 150 kDa

0 5

+

+

LC-HC mispair 150 kDa

-5

bsAb

0

-50

5 100150200250300350400450

Epitope Binning/Competition

HC dimer w/o LC 150 kDa

300

200

Target peak (HC1+HC2+LC1+LC2)

100

0 0.1 0.2 0.3 0.4 0.5 0.6 0.7 0.8 0.9 1 1.1

159202.1

affinity and kinetics and product concentration

0

Mispairing (HC1+HC2+LC1+LC1)

0

50 10

150 200 250

HC1+HC2+LC1+Cysteine HC1+HC2

Concentration Analysis

Versatile: capable of detecting most types of molecules

110896.3

4000 6000 8000 10000

Measurement 1 Measurement 2

40 60 80 100 120

100 µL/min

2 4 6 8 10

LC dimer 51267.0 50000

136649.4

5 µL/min

Wide range: capable of analyzing from μM to fM binde

0.01

0.001

20

2000

100000 Counts vs. Deconvoluted Mass (amu)

150000

-10 0 0

10 20

30 40

0.001 0.01 0.1 1 10 100 1000

Disulfide mapping analysis to determine unknown disulfide linkage

Deliverables: • Confirm known disulfide linkage information • Report free cysteine amount and any mis-linked disulfide bond with >5% abundance • Determine unknown disulfide linkage for every cysteine

Purified Protein Samples

Ethanol Precipitation

Alkylation

Digest by Specific Proteases (pH<6.7)

Non-reduced Fraction

LC-MS

Deglycosylation if Necessary

DTT

Profile Comparison to Find Different Peaks

Reduced Fraction

LC-MS

N-glycan analysis by LC-Fluorescence-MS/MS for complex glycosylation

Deliverables: • Report any glycan relative abundance >1% based on fluorescence • Report glycan ID based on mass spec results

N-glycanase Release Glycans HLB Plates

Glycan Pool

Glycoprotein

high mannose hybrid complex

M6P

Convert

Fluorescent 2-AB/Procainamide Labeling

Labeled Glycan Pool + Dye

Glycans with Free Reducing End

Clean

Identification Software Search Manual Interpretation

Liquid Chromatography MS/MS

Component Identification

Glycan Distribution

Quantification by Byomap

Detailed peptide mapping for sequence coverage, PTM, sequence variant analysis

Deliverables: • Confirm protein sequence: sequence coverage map • Software-based identification for PTM, SV and fragment et al analysis • Check sequence homogeneity: manual check for all components with user defined intensity threshold (>1%) for detailed PTM, SV and fragment et al analysis

Identified Major Peaks

Confirmed Peak Identity Sequence Coverage

Database Search

LC-MS/MS

Peak feature detection based on MS1 only

MS2/MS3

LC-MS/MS (tMS2) CID/HCD/ETD

Un-identified Small Peaks

Manual Assignments

m/z

PTM 9%

Variants 2%

Adducts, non-specific digest 89%

1000-2000 components

Learn more: Protein Sciences: Early-Stage R&D Protein Characterization Services

About WuXi Biologics

WuXi Biologics is a leading contract research, development and manufacturing organization (CRDMO) that provides end-to-end capabilities to healthcare organizations worldwide. With operations in China, the United States, Ireland, Germany, and Singapore, we enable our partners to effectively and efficiently bring biologics and vaccines to patients worldwide through our comprehensive and high-quality drug development model.

The world’s leading global single-source platform from concept to commercialization.

wuxibiologics.com | info@wuxibiologics.com

5-9-2024

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