WO 2025/099157 A1 — Absolute Quantification of Protein Isoforms by Internal Calibration (Top-Down LC-MS)

Bibliographic Data

FieldValue
Publication numberWO 2025/099157 A1
TypePCT Application (A1 = first publication before grant)
Published2025
Filed~2024 (PCT filing date)
InventorsSouleiman El Balkhi et al. (Limoges, FR)
ApplicantsINSERM, CHU Limoges, Université de Limoges
PDFImage-based (no text layer) — content reconstructed from technology-transfer strategic report

Title

“Absolute Quantification of the Isoforms of a Protein of Interest by Internal Calibration Based on a Top-Down LC-MS Approach”

Core Problem Solved

Top-Down proteomics has historically faced two major barriers to clinical use:

  1. Insufficient mass accuracy on routine instruments (1–5 Da drift for ~66 kDa proteins like albumin)
  2. No absolute quantification without expensive isotope-labeled standards

This patent solves both by using myoglobin (Mb, ~16.7 kDa) as a multifunction internal standard.

Technical Mechanism

Step 1: Real-Time Mass Recalibration

Myoglobin is co-injected with each patient sample. Its multiple charge states generate peaks at precisely known theoretical masses. The software uses these peaks to recalibrate the albumin (~66.4 kDa) or hemoglobin (~64.5 kDa) spectrum in real time, every injection.

Result: mass error reduced from 1–5 Da to <3 ppm (<0.3 Da for albumin). This enables reliable distinction of near-isobaric modifications that were previously unresolvable in routine settings.

Step 2: Absolute Quantification

With myoglobin at a known concentration as the internal reference, the relative signal ratio of each albumin isoform peak to the myoglobin signal directly yields absolute molar concentration of each isoform — without isotope labeling.

Example output: HSA-Cys = 12.4 µmol/L; HSA-Native = 38.1 µmol/L; HSA-Glyc = 3.2 µmol/L (in a cirrhotic patient).

Applications Covered

Primary: Albumin Isoform Absolute Quantification

Extended: Hemoglobin / HbA1c Precision Testing

The patent explicitly covers hemoglobin isoforms. Key application:

HbA1c in hemoglobin variant populations:

  • Standard HbA1c methods (HPLC, immunoassays) fail in patients with HbS, HbC, HbE (common in African, Hispanic, Mediterranean populations)
  • Top-Down approach directly quantifies the glycated β-chain of hemoglobin regardless of variant background
  • Potential reference method for national metrology institutes and proficiency testing programs

Connection to lakis-2024

The published paper lakis-2024 (Lakis et al., Analytica Chimica Acta, 2024) is the peer-reviewed validation of this patent’s core methodology. The CQFD-PTM pipeline implements the quantification algorithm developed in this patent.

Comparison to Prior Art

ApproachMass accuracyAbsolute quantPractical cost
Standard Top-Down (no IS)1–5 DaNoLow
Isotope-labeled IS (SILAC)<1 DaYesVery high (synthesis cost)
This patent (Mb IS)<3 ppm (<0.3 Da)YesLow (Mb is cheap)
SRM/MRM peptide-levelSub-ppmYesModerate

Commercialization Angle

Primary targets per technology-transfer:

  • Thermo Fisher — integrate myoglobin IS calibration natively into Xcalibur/BioPharma Finder software; enables Orbitrap-based clinical Top-Down
  • Shimadzu — adapt method for CLAM-2040 (automated sample prep) to create “sample-to-result” HbA1c / albumin platform for hospital labs
  • Quest Diagnostics — HbA1c precision test for hemoglobin variant populations (unmet need in diverse US patient demographics)
  • Bruker — timsTOF Pro2 clinical proteomics package validation

Position in the 3-Level Platform

This is Level 3 of the albuminomics platform:

  • Level 1 (US20220018852, SEB Test) — answers “is albumin functional?”
  • Level 2 (WO2024074685) — answers “which disease caused the damage?”
  • Level 3 (this patent) — answers “exactly how much of each isoform, in absolute terms?”