CHEM 3050 Lecture Notes - Lecture 56: Intrinsically Disordered Proteins, Insulin Receptor, Peptide
3 May 2018
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CHEM 3050
Lecture 56
Receptor Tyrosine Kinases
- It is the common mechanism for hormone
response
- Most are monomers that dimerize upon ligand binding
- Example: Insulin receptor
o 4 polypeptide segments held together by S-S
bonds (exception – ligand-dimerization rule)
o Binding of one insulin molecule pulls 2 alpha
subunits together and only 1 insulin bound per
receptor
o Ligand binding induces conformation
changes
o 2 Tyr-kinase domains brought together and
physphorylates each other (autophosphorylation
on 3 Tyr residues)
o Removes activation loop from active site so the
substrate can bind
- Interacts Indirectly with G-protein
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