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My name is Reinhard Grisshammer.
I am at the National Cancer Institute,
at the National Institutes of Health in Bethesda, Maryland.
The title of my talk is
structural and mechanistic insights into the neurotensin receptor.
The outline of my talk is as follows;
I will give a brief introduction into GPCRs,
G protein-coupled receptors and the neurotensin NTSR1.
Then, I will talk about conformational thermostabilization,
which is a technique to make proteins more amenable for crystallization.
Then, I will present four neurotensin receptors structures.
The first one is called NTSR1-GW5,
which has an active-like conformation and
provides insight into the neurotensin peptide binding mode.
Two more structures called NTSR1-ELF and LF
provide insight into the structural prerequisites of G protein activation.
The last structure is of a construct called EL which shows constitutive activity,
where we can learn about the structural features of a constitutively active receptor.
In the end, I will summarize constitutive and
agonist-induced signaling of the neurotensin receptor NTSR1.