What happens to peptide ligands after detaching from binding site of receptor (for reversible reactions) - are they getting free and, let's say swim away or are they metabolized together with receptor itself? Found no explanation on this subject.
Hello Dauren,
The answer is never a simple yes or no. The fate of peptides, post receptor activation, can be dependent on the receptor itself. Some receptors will internalize upon activation, with ligand still attached, causing signalling while en route to recycling. And some peptide ligands will simply activate then "swim away" to activate another receptor ligand. This is dependent on how tightly the ligand binds to the receptor. Non-specific interactions may fall into this realm. If it is a tight binding ligand, both receptor and ligand may be sent to a liposome for degradation. Hope this helps.
Hi Dauren,
As Charles said, it depends on the particular interaction between the ligand and receptor. Endothelin, for example, has an interaction half-life with the ETa receptor of ≤77 hours and therefore binds ligand very tightly.
My own research concerns calcitonin gene-related peptide and its receptor and we know that receptors can release the peptide for another binding event but they can also internalise to endosomes with the ligand still bound. The fate of ligand/receptor is very much dependent on the condition you're interested in (experimental, or otherwise...)
So, I guess the answer is "depends on what you're looking at!"
Thank you guys! What about VEGF binded to VEGFR-2 in rat experimental model of partial hepatectomy? Do you have any info on that matter? Maybe you could refer me to some resource? I could not find anything on this process' molecular dynamics... Thanks anyways!
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