The Traditional Approach to the Synthesis of Enzyme Inhibitors

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The Traditional Approach to the Synthesis of Enzyme Inhibitors
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Prof. Meggers talks about the traditional approach for synthesizing an organic compound for the use as an enzyme inhibitor and the inherent problems.
Keywords Vortrag Organik
Enzyme inhibitor Enzyme Radioactive decay Man page
Gene product DNS-Synthese Substitutionsreaktion Binding energy Gene Chemistry Electronic cigarette Molecule Lead Enzyme Functional group Cell (biology) Transcription (genetics) Protein Exciter (effect) Translation <Genetik> Base (chemistry) Factor XIII Pharmacy Cell membrane Biomolecular structure Process (computing)
Naturstoff Functional group Solution
Waterfall Complication (medicine) Stickstoffatom Binding energy Ice sheet Molecule Combine harvester Tiermodell Water Functional group N-terminus Chemical compound Cell (biology) Explosion Active site Highly sensitive person Chemical structure Cobaltoxide Pharmacy
Molecule Functional group
Molecule Benzene Musk Organische Verbindungen
where a man the greetings from
the from the makers group and I would like to and did you know a brief overview of of the research Michael this doing and that is a very exciting time for chemist and we have a sequence the human gene known we know all the energy products apology known and uh and now of course it Brentwood goal is to work to understand and to control the function of each gene product and that's the chemistry really can have an impact of for example we can make small molecules that can interfere with supporting prudent actions we can make ,comma points that can interfere with the transcription and translation of as of genetic processes such as small motors that bind to DNA or to our name or we can make small monarch sets that bind to and summoning inhibitors and knock out the function of the functions of these enzymes and um but but think about it I mean what does this mean that means you want to make the molecule that really just interviews for example was the function of a single ends up 1
enzyme out of 25 thousand proteins together with all the DNA we have in the cells that are in the membrane compartments and so on so this is an enormous challenge of Monica recognition and claim and I think a lot of people agreed with me that the typical :colon smaller organic molecules can actually not fulfill this task so if you think about it the typical bioactive organic moieties hit the psychic component that has substitutions on the periphery and um and the promise it can adopt would the confirmation the 1 confirmation it binds the one-time in another confirmation by another tied so this time this promise could promiscuity of of confirmation base the leads to this on selective binding and the
question is how can we solve this problem that's what Mike was really excited about this problem of Monica recognition and if you if you think about solutions that you can look to nature nature actually found ways to deal with this problem you probably know that complicated natural products they have very specific biological
functions they sometimes by just 1 particular target and in order to understand how the letter products do that it's actually may be important to to to have an example into 2 to learn about Jose interact with their respective targets and a half years 1 flight that shows the Net-a-Porter from get my shown here on the left it's already
fairly complicated microsecond component would be functional groups wanted its their centers back quite difficult to synthesize and this Kompong actually binds to the selectively to the N-terminal ATP binding site of the reporting 19 HSP 19 and it does so by adopting this sea shape in this shape binds to this very grilled without deep pockets and when you look at the space-filling model of this compound Howard binds to the pocket is basically like a gorilla shape with functional groups David presented on the sofa and that's what it comes down to we have basically find ways to make the
final group without structure that have function was presented on the periphery in a very practical away and nature that by paying the designed this complicated molecules in which basically the guest forward in combination with all the functional groups and the stairs and just basically in a way colt fall as three-dimensional and so and we don't of course we synthetic chemists at least my group we basically hesitate to make things complicated moniker because as a synthetic challenge is enormous and it's difficult to make many kilogram quantities of such a compost sold out we were thinking about other ways how to basically make composite had that our group will have a very defined shape and and because of this can then buy 1st selectively put target because you have to keep in
mind that an active side is global it's typically a pocket so you want to design global molecules that are kind of Richard's wife a
defined shape and and complement the shape of it and the function of the presentation of
and you if you think about organic chemistry if you just have a benzene molecule the heater cycle recital accidentally put subsistence honored the score points are not Richard cannot look without that
basically flat this morning and they have flexible on and if you wanna make something that is global and has defined shape you typically need to use strings together have Bridges doesn't have to introduce um stairs centers other functional and so on and so forth the the good news news was


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