Study Notes on Non-Covalent Interactions in Proteins

Non-Covalent Interactions in Proteins

Overview of Protein Conformation

  • The unique properties of a protein are attributed to its specific three-dimensional (3D) conformation.

  • This conformation is stabilized by different types of non-covalent interactions.

  • Proteins have evolved such that one folded conformation is more stable than any other, known as the native state.

  • There exist some proteins without stable structures, referred to as intrinsically disordered proteins.

  • Certain diseases, such as Alzheimer's and Parkinson's, involve high molecular weight (MW) alternative low-energy folded states (e.g., amyloid fibers).

Main Classes of Non-Covalent Interactions

  • There are four principal classes of non-covalent interactions:

    1. Salt Bridges

    2. Hydrogen Bonds

    3. Van der Waals Interactions

    4. Hydrophobic Effect

Salt Bridges

  • Definition: Electrostatic interactions occurring between fully ionized negative and positive charges.

  • At neutral pH, proteins contain several charged groups:

    • Negatively Charged Groups:

    • $ ext{a-COOH}$ (C-terminus) with pKa = 3.5-4.3

    • Aspartate (Asp) and Glutamate (Glu) sidechains (carboxyl) with pKa = 3.9-4.5

    • Positively Charged Groups:

    • Histidine (His) sidechain (imidazole) with pKa = 6.0-7.0

    • $ ext{a-NH2}$ (N-terminus) with pKa = 6.8-8.0

    • Lysine (Lys) sidechain (amino) with pKa = 10.4-11.1

    • Arginine (Arg) sidechain (guanidinium) with pKa = 12.0

Characteristics of Salt Bridges
  • Salt bridge formation stabilizes the charges and modifies the individual pKa values of the interacting groups.

  • Charged groups do not remain buried in proteins unless they are 'neutralized' by forming a salt bridge.

    • The contribution of a salt bridge to overall protein stability depends on its burial or exposure on the surface.

  • A change in pH can cause charged groups to titrate, initiating or disrupting salt bridges, resulting in protein unfolding at extreme pH levels.

  • The dielectric constant of the solvent increases with the addition of salt, influencing salt bridge interaction strength.

Hydrogen Bonding

  • Definition: A hydrogen bond occurs when two electronegative atoms compete for the same hydrogen atom.

  • Structure of a hydrogen bond:

    • Donor Atom: Covalently bonded to the hydrogen atom.

    • Acceptor Atom: Interacts favorably with the hydrogen atom.

  • Notable properties:

    • The small size of the hydrogen atom allows for high polarization during bonding.

    • Strong hydrogen bonds exhibit near covalent characteristics due to notable electron redistribution.

  • Common Hydrogen Bonds in Proteins:

    • **Amine - Carbonyl

    • Amine - Hydroxyl

    • Amine - Imidazole

    • Hydroxyl - Carbonyl**

    • Backbone-to-backbone interactions are crucial for secondary structure formation.

Directionality of Hydrogen Bonds
  • Hydrogen bonds demonstrate unique directionality, with the interaction strength being maximum when the angle (q) between the atoms involved is 180 degrees; typically q is greater than 120 degrees.

  • The length of a hydrogen bond is approximately 3 Å, with specific distances (e.g., 2.9 Å for backbone-to-backbone H-bonds).

  • Hydrogen bonds are affected by the dielectric properties of the medium, resulting in varied strengths depending on the environment (e.g., presence of water).

Van der Waals Interactions

  • Definition: All atoms generate transient dipoles due to fluctuating electron clouds, inducing attractive forces in nearby atoms.

  • Characteristics:

    • The attractive forces diminish rapidly with increasing distance, following the relationship \( ext{attraction} \sim rac{1}{ ext{distance}^6} \$.

    • As atoms approach each other, repulsive forces increase steeply, represented by \( ext{repulsion} \sim rac{1}{ ext{distance}^{12}} \$.

    • Optimal attraction occurs when atoms are 0.3 to 0.5 Å apart (close to the sum of their van der Waals radii).

The Hydrophobic Effect

  • Definition: The hydrophobic effect refers to the entropic increase associated with non-polar molecules aggregating in aqueous solutions, resulting in a thermodynamically favorable state.

  • Water is a polar solvent that forms hydrogen bonds, creating a network that influences the solvation of polar and non-polar molecules:

    • Non-polar molecules do not form hydrogen bonds with water, causing them to be insoluble.

    • The energy change (ΔH) for transferring a non-polar molecule from the liquid to aqueous solution is approximately zero, while the process is unfavorable in terms of entropy (ΔS < 0).

    • Example: Cyclohexane at 25°C illustrates this effect, with Gibbs free energy (ΔG) calculations confirming entropy-driven hydrophobic interactions.

Water-Ordering Effect
  • When non-polar molecules are introduced into water, cavities form, and the resulting ordering of water molecules reduces system entropy.

  • The aqueous environment will exclude non-polar molecules, reducing their surface area to minimize the associated water-ordering effect.

Amino Acid Hydrophobicity Scale

  • Hydrophobicity varies among amino acid side chains, influencing protein folding and stability:

    • Trp: 2.25

    • Ile: 1.80

    • Phe: 1.79

    • Leu: 1.70

    • Cys: 1.54

    • Met: 1.22

    • Val: 0.96

    • Tyr: 0.72

    • Pro: 0.31

    • Ala: 0.26

    • His: 0.00

    • Gly: -0.04

    • Ser: -0.22

    • Gln: -0.60

    • Asn: -0.64

    • Glu: -0.77

    • Asp: -0.99

    • Lys: -1.01

    • Arg: -1.01

  • Note: Despite containing a polar group, Trp ranks as the most hydrophobic amino acid.

Implications of Non-Covalent Interactions

  • The collective strength of non-covalent interactions in proteins creates a robust network essential for maintaining protein structure.

  • Proteins are marginally stable, with conformational stability estimated to be only 20-60 kJ/mol, equivalent to a few hydrogen bonds.

  • Stability is contingent on a narrow range of external conditions, including pH, temperature, and solvent type. Deviations from these conditions can lead to loss of non-covalent interactions, resulting in protein unfolding or denaturation.