Receptors: structure and function

25 important questions on Receptors: structure and function

What happens with a receptor after binding a neurotransmitter or hormone?

Binding results in an induced-fit that changes the shape of the receptor. This leads to a series of events that in the end result in a change in cellular chemistry.

What happens with neurotransmitters and hormones when they bind?

Hormones and neurotransmitters bind, do not undergo any reaction, and leave unchanged. They only pass on their message.

What is crucial in binding a chemical messenger?

The binding should be strong enough to pass the message but should also be weak enough to allow the chemical messenger to leave.
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What are binding groups?

Binding groups are functional groups on the messenger molecules.

How do ion-channel receptors look like?

Ion-channel receptors are an integral part of the ion channel. Brining results in induced fit with conformational change with opens the channel.

What are ligand-gated ion channel receptors?

Ligand-gated ion channel receptors are receptors controlling ion channels. They consist of five protein subunits with the binding site on one or more subunits.

How is an ion channel opened?

The binding of a messenger causes a conformational change. The second transmembrane domain of each subunit rotates to open the channel.

What are G-protein coupled receptors?

G-protein coupled receptors are membrane-bound receptors with seven transmembrane sections. The C-terminus chain is within the cell and the N-terminus is exctracellular.

What happens when a messenger binds to a G-protein coupled receptor?

The G-protein coupled receptor activates signal proteins, G-proteins. The binding of a messenger opens the binding site for the G-protein. The G-protein binds and then fragments. One of the fragments then activates a membrane-bound enzyme in turn.

What can be said about the binding site of G-protein coupled receptors?


The location of these binding sites differs for different G-protein coupled receptors.

What is the difference between types and subtypes of receptors?

They are able to bind the same chemical messenger but differ in structural shape so the binding is not equally effective. This is an advantage in designing selective drugs.

Is it possible for G-protein coupled receptors to exist as dimeric structures?

Yes.

How do kinase-linked receptors look like?

Kinase-linked receptors have an external binding site for the chemical messenger and an internal enzymatic active site. The internal active site is able to phosphorylate tyrosine residues in protein substrates.

What happens when the epidermal growth factor (EGF) binds?

When EGF binds dimerization takes place and the kinase active site is opened. The active site on one half of the dimer catalyzes the phosphorylation of tyrosine on the C-terminal chain on the other half of the dimer.

What is the insulin receptor?

The insulin receptor is a heterotetrameric structure that acts as a tyrosine kinase receptor.

What happens after biding the growth hormone?

The growth hormone receptor dimerizes after binding which activates the tyrosine kinase receptors enzyme in the cytoplasm.

Why are tyrosine kinase receptors important?

Tyrosine kinase receptors are important because they are important targets for anticancer medication.

Why are intracellular receptors important?

Intracellular receptors are important in regulating transcription.

What is crucial for the messengers of intracellular receptors?

The messengers need to be hydrophobic to pass the cell membrane.

What happens after binding an intracellular receptor?

Binding results in dimerization and the formation of a transcription factor complex that binds to a specific nucleotide sequence on DNA.

Wat zijn voorbeelden van monoamines als liganden van GPCR's?

  • Dopamine
  • Histamine
  • Noradrenaline
  • Acetylcholine

Welke twee subfamilies heb je binnen GPCR's?

  • Rhodopsine-achtige familie van receptoren
  • Adrenerge receptoren

Zijn verschillende adrenerge receptortypes en subtypes gelijk verdeeld over weefsels?

Nee

Herkennen verschillende adrenerge receptortypes en subtypes hetzelfde ligand?

Ja

Waar leidt doelselectiviteit tot bij adrenerge receptoren?

Weefselselectiviteit

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