Week_2_-_SPLecture_2_1


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### Week 2 - SPLecture 2_1: Protein Affinity vs Protein Activity

Lecturer: Prof. Karin Hing

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Page 1: Introduction

- Topic: Biocompatibility - Protein Affinity vs Protein Activity

- Recap from Week 1:

- Protein shape is controlled by primary structure and local environment.

- Protein shape regulates its function.

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Page 2: Key Points from Week 1

- Protein adsorption occurs whenever a material is introduced into a biological environment.

- The protein interlayer is influenced by:

- Material properties (physio-chemistry)

- Protein characteristics (structure, chemistry)

- Host environment (composition)

- Key factors behind protein interlayer formation:

- Dehydration & hydrophobicity

- Electrostatics & surface charge

- Conformational changes & protein stabilisation

- Importance of protein interlayers in bioactivity:

- The host interacts with the material through the adsorbed protein layer.

- If the material does not release substances, this interaction becomes the primary biological response driver.

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Page 3: Observed Cell Responses to Materials

- Osteogenic cell adhesion and activity are usually superior on hydrophilic surfaces.

- Example: cp titanium & hydroxyapatite outperform polyethylene.

- Many resorbable polymers are naturally hydrophobic and require surface modification before cell seeding.

- Example: Polystyrene in tissue culture plastics is modified to become hydrophilic to improve cell attachment.

- The protein interlayer quality impacts cell response based on:

- What proteins are present (affinity).

- How proteins are arranged (structure and activity).

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Page 4: Role of the Protein Interlayer in Cell Response

- Protein interlayer quality depends on:

- Affinity/Enrichment (which proteins adsorb preferentially)

- Activity/Activation (whether proteins retain function upon adsorption)

- Affinity/Enrichment:

- Determines how specific proteins adsorb to a material or tissue surface in a given environment.

- Activity/Activation:

- A protein’s ability to function biologically after adsorption, which depends on its conformation and ability to interact with other molecules.

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Page 5: Protein Affinity

- Protein affinity depends on the environment:

- Vitronectin adsorbs equally to hydrophilic and hydrophobic surfaces in pure solutions.

- However, in serum, hydrophilic surfaces adsorb more vitronectin, improving cell attachment and migration.

- Dilution experiments can help identify affinity-driven enrichment.

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Page 6: Environmental Sensitivity of Affinity

- Factors affecting protein affinity:

- Temperature & protein concentration:

- Adsorption levels vary at 18°C vs 37°C.

- Solute composition:

- The presence of different media (MEM, PBS, HA, SA) alters adsorption levels.

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Page 7: Competitive Adsorption

- Co-adsorbants affect protein binding:

- Presence of BSA and whole serum changes adsorption behaviour.

- Activity also matters:

- Same amount of fibronectin adsorbed, but cell attachment rate varies depending on surface pre-conditioning.

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Page 8: Key Protein Characteristics Affecting Affinity & Activity

- Properties influencing protein behaviour at surfaces:

- Composition & Conformation

- Solubility & Hydrophobicity

- Molecular weight

- Charge & Isoelectric point (pI)

- Stability

- Protein stability affects function:

- Tertiary structure influences how a protein behaves when adsorbed.

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Page 9: Protein Molecular Weight & Isoelectric Point (pI)

- Examples of protein molecular weights:

- Fibronectin: 440,000 – 480,000 Da

- Vitronectin: 65,000 – 75,000 Da

- Hemoglobin: 64,500 Da

- Isoelectric point (pI) determines protein charge at a given pH.

- Proteins are less soluble near their pI.

- At pH 7.4, fibronectin and vitronectin carry a net negative charge.

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Page 10-11: Protein Stability

- Proteins are only marginally stable in physiological conditions (ΔG ~ 20-65 kJ/mol).

- Denaturation can occur due to:

- Heating

- Extreme pH

- Chaotropic agents

- Surface adsorption

- Impact of stability on activity:

- A protein’s functionality depends on its structural integrity.

- Orientation & conformation impact biological activity.

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Page 12: Protein Activity & Surface Activation

- Protein function changes upon adsorption:

- Fibronectin and vitronectin may lose or gain function depending on how they adsorb.

- Example: Fibronectin shows reduced cell-binding ability in its soluble form, requiring surface activation.

- Vitronectin partially unfolds upon binding, improving integrin binding.

- Fibrinogen binds to inactivated platelets only when adsorbed.

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Page 13: Modulating Surface Activation

- Competitive adsorption can alter protein function:

- In high-protein environments, adsorption-induced conformational changes can be suppressed.

- Fibronectin on hydrophilic polystyrene supports better osteoblast adhesion than on hydrophobic polystyrene.

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Page 14: Hydrophilic vs Hydrophobic Surfaces

- Cell adhesion and proliferation:

- More successful on moderately hydrophilic surfaces than hydrophobic ones.

- Fibronectin must reorganise after adsorption to support cell function.

- Hydrophobic surfaces limit reorganisation, reducing function.

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Page 15: Enhanced Protein Activity on Hydrophilic Surfaces

- Cell response variation is linked to:

- Surface charge

- Hydrophobicity

- Point of zero charge

- Higher activity on silicate-substituted HA (SA) compared to hydroxyapatite (HA).

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Page 16: Role of Specific Binding Sites

- Protein orientation matters:

- Specifically charged surfaces can control protein orientation.

- Example: Osteopontin’s cell-binding ability is modulated by surface charge.

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Page 17: Summary – Key Factors Influencing Protein Affinity & Activity

- Material characteristics:

- Composition

- Surface chemistry

- Wettability

- Surface charge

- Stability

- Protein characteristics:

- Structure

- Conformation

- Solubility

- Charge & pI

- Molecular weight

- Environmental conditions:

- Ionic & organic composition

- Temperature

- pH, pO₂, pCO₂

Final Key Takeaway:

- Both protein enrichment (affinity) and activation (activity) are crucial for optimising biomaterial-cell interactions.

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### Final Notes