Purifying Recombinant Plasmodium falciparum Circumsporozoite Protein

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Solution Overview

Problem

Current methods for purifying recombinant Plasmodium falciparum circumsporozoite protein (rCSP) face challenges such as dimerization, aggregation, and N-terminal degradation, leading to low yields and inefficiencies in scalable production, particularly due to the formation of covalent intermolecular disulfide bonds and the need for denaturing and refolding processes.

Innovation Solution

A process involving the separation of bacterial cell lysate into soluble and insoluble fractions, followed by preferential reducing conditions using mild reducing agents and disaggregating agents to reduce intermolecular disulfide bonds while preserving intramolecular bonds, allowing for the purification of rCSP without denaturation and refolding, thereby maintaining the N-terminus integrity and achieving high yields.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Manufacturing precision

If conventional purification schemes are used to obtain recombinant CSP, then the protein can be purified, but the N-terminal region is highly susceptible to degradation and yields are low

Engineering Contradiction:
ImproveN-terminal region integrityVSAvoidpurification yield
Core Design Contradiction:
Manufacturing precisionVSProductivity

Solution Approach 1:

The patent changes the pH parameter during purification to maintain the N-terminal region integrity. By controlling pH conditions throughout the purification process, the method prevents N-terminal degradation while achieving high yields of intact CSP protein

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent performs preliminary protease inhibition before purification begins. By adding protease inhibitors at the start of the process and maintaining them throughout, the N-terminal region is protected from degradation before it can be damaged, enabling high recovery of intact protein

Inventive Principle:
Principle #10Preliminary action

2Manufacturing precision

If denaturing and refolding steps are used to eliminate dimers and aggregates, then protein purity is improved, but the process becomes complicated and costly with reduced yield

Engineering Contradiction:
Improveprotein purityVSAvoidprocess complexity
Core Design Contradiction:
Manufacturing precisionVSDevice complexity

Solution Approach 1:

The patent extracts and removes dimers and aggregates through size-exclusion chromatography without requiring denaturation. By using a gentle separation method that exploits size differences, the process eliminates the need for harsh denaturing and refolding steps, simplifying the workflow while maintaining purity

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent uses size-exclusion chromatography as an intermediary separation method. This technique acts as a mediator that separates monomers from dimers and aggregates based on hydrodynamic radius without disrupting protein structure, avoiding the need for denaturation while achieving high purity

Inventive Principle:
Principle #24Intermediary (Mediator)

3Manufacturing precision

If denaturing and refolding steps are used to eliminate dimers and aggregates, then protein purity is improved, but yield is reduced and scaling up becomes challenging

Engineering Contradiction:
Improveprotein purityVSAvoidpurification yield
Core Design Contradiction:
Manufacturing precisionVSProductivity

Solution Approach 1:

The patent extracts and removes dimers and aggregates through size-exclusion chromatography without requiring denaturation. By using a gentle separation method that exploits size differences, the process eliminates the need for harsh denaturation and refolding steps, simplifying the workflow while maintaining purity

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent maintains continuous protection of the N-terminal region throughout the entire purification process by keeping protease inhibitors present from start to finish. This continuous protective action prevents degradation at all stages, ensuring high yield of intact protein without interruption or loss

Inventive Principle:
Principle #20Continuity of useful action

4Manufacturing precision

If denaturing and refolding steps are used to eliminate dimers and aggregates, then protein purity is improved, but the process becomes costly

Engineering Contradiction:
Improveprotein purityVSAvoidmanufacturing cost
Core Design Contradiction:
Manufacturing precisionVSEase of manufacture

Solution Approach 1:

The patent extracts and removes dimers and aggregates through size-exclusion chromatography without requiring denaturation. By using a gentle separation method that exploits size differences, the process eliminates the need for harsh denaturation and refolding steps, simplifying the workflow while maintaining purity

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent uses disposable protease inhibitor cocktails that can be added directly to the purification buffer. These inexpensive, ready-to-use inhibitors provide continuous protection without requiring complex recovery or regeneration, reducing overall manufacturing costs while maintaining protein integrity

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

This method effectively purifies rCSP with high yields, maintaining N-terminus integrity and reducing the formation of dimers and aggregates, thus improving the quality and quantity of the purified protein, making it suitable for large-scale production.

Implementation Method 1

subjecting the recombinant P. falciparum circumsporozoite protein dimers to preferential reducing conditions, wherein the preferential reducing conditions comprise a mild reducing agent selected from DTT, cysteine, acetylcysteine, glutathione, monothioglycerol (MTG), thioglycolate, dithiothreitol, dithioerythritol, 2-Mercaptoethanol (β-mercaptoethanol), TCEP-HCl (pure, crystalline Tris(2-carboxyethyl)phosphine hydrochloride), and 2-Mercaptoethylamine-HCl (2-MEA)

Methodology Applied
Scientific EffectRedox Reactions: Redox Reactions

Implementation Method 2

The purified recombinant P. falciparum circumsporozoite protein obtained is N-terminally intact from residue 25 of SEQ ID NO: 1, and wherein not more than 10% of the purified recombinant P. falciparum circumsporozoite protein obtained is dimerized, and not more than 5% of the purified recombinant P. falciparum circumsporozoite protein obtained is present as high molecular weight aggregates

Methodology Applied
Scientific EffectSolvation: Solvation

Data Source

PatentEP2844666B1Process for purifying recombinant plasmodium falciparum circumsporozoite protein
Publication Date: 2019.07.17 PFENEX INC
  • EP2844666B1 patent drawingFigure 1
  • EP2844666B1 patent drawingFigure 2A~2C
  • EP2844666B1 patent drawingFigure 3A~3B

AI summary

The present invention relates to processes for purifying high-quality recombinant Plasmodium falciparum circumsporozoite protein at high yields. This process provides rCSP at high yields without the need for denaturing and refolding the protein. The present invention overcomes obstacles previously encountered in the field, including dimerization, aggregation, and N-terminal degradation of rCSP. The process provided by the invention is scalable, and can be applied to large fermentation batches. The invention also relates to stable liquid formulations of recombinant P. falciparum circumsporozoite protein, and processes for stably maintaining rCSP in a stable liquid formulation.