Bokt.nl

Cookie2222 schreef:

Hier is het artikel in z’n geheel waar het plaatje naar refereert :
https://zero.sci-hub.se/427/99af191ba4b ... nload=true

Met dank aan sokje voor de Doi

Citaat:

In an earlier study, several linear peptides with overlapping sequences of IL-l proteins were prepared as a part
of a general strategy to elucidate the functional regions. All of these linear peptides were found to lack bindiig
to the IL1 receptor.7 Next we turned to the preparation of constrained cyclic peptides that would mimic various
loops present in the protein. Standard methods of constraining loops involve, for example, introduction of
cysteine residues into the sequence to form disulfide bridges, side-chain to side-chain cyclixations involving
glutamic acid or aspartic acid with lysine residues, or end-to-end cyclixations. The cyclic peptides obtained
when this approach is applied to large f2 loops, such as the one present in ILla, are highly flexible, and cannot
necessarily be expected to adopt a conformation analogous to that in the protein. Because of these implications
and also the possibility that the 41-48 f2-loop in IL-la may be involved in receptor recognition, we chose to
design a spacer molecule that would span the intrachain distance and also constrain it enough to maintain the
excised loop in a conformation which is similar to the one observed in IL-la 7%~ paper describes the design,
synthesis, three-dimensional structural characterization of this loop mimetic and the comparison of its structure
with the corresponding loop in IL-la

Grainey schreef:

Leuk artikel, precies de hoek wat ik gestudeerd heb, ik vind dit soort onderzoek echt geweldig Goed onderbouwd met NMR studies, ben wel benieuwd hoeveel spacers ze hebben geprobeerd voordat het precies paste om de omega loop kunstmatig precies te kunnen repliceren. In dat artikel is het 'slechts' een manier om omega loops te kunnen synthetiseren, een proof of concept dus, of het molecuul zelf verder een actieve functie heeft ben ik wel benieuwd naar. Knap gevonden dat molecuul!

MacavityL schreef:

Femke_Tweety schreef:

Of als interleukine zelf? Is me niet helemaal duidelijk nog, of het om de antagonist gaat of de eigenlijke stof

In het eerste artikel halen ze het aan als soort antagonist.

“peptides generally do not make good drug candidates, especially as orally administered drugs, because they are rapidly proteolyzed in the GI tract and serum, and they are poorly bioavailable and rapidly excreted. In addition, many peptides can bind to multiple receptors, especially, to multiple members of the same receptor family. What is needed is a compound that mimics or blocks the biological effect of a peptide by interacting with its receptor or enzyme, but does not have the undesirable characteristics of peptides. This is a peptidomimetic.”