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Why is protein cyclisation desirable?

Biology Asked on December 7, 2020

There are a number of methods to "cyclize" an existing peptide:

Why would the "cyclization" of a protein be a desirable goal?

One Answer

As described in the abstract of Synthetic Cross-linking of Peptides: Molecular Linchpins for Peptide Cyclization by Derda et al., protein cyclization improves:

resistance to proteolytic degradation and conformational stability. The latter property leads to an increase in binding potency and increased bioavailability due to increased permeation through biological membranes.

In simpler terms, a protein that is cyclized is less likely to:

  1. Fold into an unhelpful shape.
  2. Be broken up by an enzyme.

Thus, they are more likely to:

  1. Act as better binders for a given target
  2. Make it across a cell membrane

Answered by Seanny123 on December 7, 2020

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