Sökning: WFRF:(Wieske Lianne H. E. 1994 ) >
MicroED as a Powerf...
MicroED as a Powerful Tool for Structure Determination of Macrocyclic Drug Compounds Directly from Their Powder Formulations
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- Danelius, Emma (författare)
- Univ Calif Los Angeles, Howard Hughes Med Inst, Los Angeles, CA 90095 USA.;Univ Calif Los Angeles, Dept Biol Chem, Los Angeles, CA 90095 USA.
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- Bu, Guanhong (författare)
- Univ Calif Los Angeles, Dept Biol Chem, Los Angeles, CA 90095 USA.
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- Wieske, Lianne H. E., 1994- (författare)
- Uppsala universitet,Organisk kemi
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- Gonen, Tamir (författare)
- Univ Calif Los Angeles, Howard Hughes Med Inst, Los Angeles, CA 90095 USA.;Univ Calif Los Angeles, Dept Biol Chem, Los Angeles, CA 90095 USA.;Univ Calif Los Angeles, Dept Physiol, Los Angeles, CA 90095 USA.
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Univ Calif Los Angeles, Howard Hughes Med Inst, Los Angeles, CA 90095 USA;Univ Calif Los Angeles, Dept Biol Chem, Los Angeles, CA 90095 USA. Univ Calif Los Angeles, Dept Biol Chem, Los Angeles, CA 90095 USA. (creator_code:org_t)
- American Chemical Society (ACS), 2023
- 2023
- Engelska.
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Ingår i: ACS Chemical Biology. - : American Chemical Society (ACS). - 1554-8929 .- 1554-8937. ; 18:12, s. 2582-2589
- Relaterad länk:
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https://doi.org/10.1...
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https://uu.diva-port... (primary) (Raw object)
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https://urn.kb.se/re...
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https://doi.org/10.1...
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Abstract
Ämnesord
Stäng
- Macrocycles are important drug leads with many advantages including the ability to target flat and featureless binding sites as well as to act as molecular chameleons and thereby reach intracellular targets. However, due to their complex structures and inherent flexibility, macrocycles are difficult to study structurally, and there are limited structural data available. Herein, we use the cryo-EM method MicroED to determine the novel atomic structures of several macrocycles that have previously resisted structural determination. We show that structures of similar complexity can now be obtained rapidly from nanograms of material and that different conformations of flexible compounds can be derived from the same experiment. These results will have an impact on contemporary drug discovery as well as natural product exploration.
Ämnesord
- NATURVETENSKAP -- Kemi -- Organisk kemi (hsv//swe)
- NATURAL SCIENCES -- Chemical Sciences -- Organic Chemistry (hsv//eng)
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