Ligand Binding Heterogeneity and Cooperativity in Receptor Systems

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18 Questions

What is one way to assess ligand specificity?

Competitive-binding assay

What is the property of biological receptors binding tightly to a single natural ligand called?

Specificity

How can receptor specificity be confirmed in a competitive-binding assay?

The amount of ligand bound is not affected by the presence of other ligands

What is the reason behind proteins tending to stick to glass?

Polar surfaces interacting with each other

What is the reason behind proteins having some affinity for cell surfaces?

Cell surfaces being quite polar

How do molecules interact with each other?

Noncovalently

What special statistical effects need to be considered when interpreting the nonlinear Scatchard plots that arise from lattice binding?

Special statistical effects need to be considered when interpreting the nonlinear Scatchard plots that arise from lattice binding.

How can Scatchard plots alone not distinguish between heterogeneous binding sites and cooperativity?

Scatchard plots alone cannot distinguish between heterogeneous binding sites and cooperativity because they both result in nonlinear plots.

How can cooperativity and receptor heterogeneity be distinguished?

Cooperativity and receptor heterogeneity can be distinguished by measuring the effect of bound ligand on the value of the dissociation rate constant, koff.

How is the value of koff measured?

The value of koff can be measured by allowing ligand and receptor to reach equilibrium, removing free ligand, and then measuring the dissociation of ligand over time.

In practice, how is the decrease in the concentration of bound ligand usually measured?

In practice, the decrease in the concentration of bound ligand is usually measured.

What might limit the access of additional molecules of ligand to free sites on the lattice?

Certain arrangements of large ligands on lattice-like receptors may limit the access of additional molecules of ligand to free sites on the lattice.

What are the types of electrostatic forces that contribute to the innate affinity between molecules?

Coulombic attractions, hydrogen bonds, and dispersion forces

Why are noncovalent interactions important in biological processes?

They are important for catalysis of chemical reactions, neutralization of foreign toxins, and stimulation of cellular activities.

What do receptors and ligands exchange interactions with before interacting with each other?

Solvent and solute molecules

What are biological chemists trying to understand regarding receptor-ligand interactions?

The molecular details

What is the goal of medicinal chemists in relation to receptor-ligand interactions?

To develop useful pharmaceutics

Why are organic chemists trying to develop synthetic systems that mimic biological interactions?

To mimic biological interactions

Explore the concepts of heterogeneous binding sites and cooperativity in receptor systems. Understand how ligands may bind to multiple sites with different dissociation constants and how ligand binding can influence the affinity of receptors for subsequent ligands. Learn how Scatchard plots alone cannot differentiate between heterogeneous binding sites and cooperativity.

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