4EGI-1 - Binding Site Specifics and Effects of Use

Binding Site Specifics and Effects of Use

4EGI-1, like 4E-BP polypeptides, displaces eIF4G by associating with a binding site on E. Not only does the synthetic molecule prevent the association between the two initiation factors, but by binding to a different portion of E via the same motif, it has been shown to actually increase the binding affinity of E for endogenous (originating within an organism) 4E-BP1.1 The Harvard research group leading the study screened 16,000 compounds, looking for one that would displace a fluorescein-labeled peptide derived from the G sequence that binds to the E form at the same site. Eventually they turned up 4EGI-1, which displaced eIF4G by binding to a smaller subset of its binding site (on E). The newly found molecule had the added advantage of enhancing 4E-BP1 binding, a surprise given that this molecule is also believed to bind eIF4E via the same motif. It appears that by displacing the G sequence without blocking the entire binding interface of E, 4EGI-1 is able to clear the “docking site” of the endogenous regulator.

Read more about this topic:  4EGI-1

Famous quotes containing the words binding, site and/or effects:

    “[Government’s] true strength consists in leaving individuals and states as much as possible to themselves—in making itself felt, not in its power, but in its beneficence, not in its control, but in its protection, not in binding the states more closely to the center, but leaving each to move unobstructed in its proper orbit.”
    —Andrew Jackson (1767–1845)

    “The site of the true bottomless financial pit is the toy store. It’s amazing how much a few pieces of plastic and paper will sell for if the purchasers are parents or grandparent, especially when the manufacturers claim their product improves a child’s intellectual or physical development.”
    —Lawrence Kutner (20th century)

    “I am fearful that the paper system ... will ruin the state. Its demoralizing effects are already seen and spoken of everywhere ... I therefore protest against receiving any of that trash.”
    —Andrew Jackson (1767–1845)