180851-50-7Relevant articles and documents
Structure of a complex formed by a protein and a helical aromatic oligoamide foldamer at 2.1 ? resolution
Buratto, Jérémie,Colombo, Cinzia,Stupfel, Marine,Dawson, Simon J.,Dolain, Christel,Langlois D'Estaintot, Béatrice,Fischer, Lucile,Granier, Thierry,Laguerre, Michel,Gallois, Bernard,Huc, Ivan
, p. 883 - 887 (2014)
In the search of molecules that could recognize sizeable areas of protein surfaces, a series of ten helical aromatic oligoamide foldamers was synthesized on solid phase. The foldamers comprise three to five monomers carrying various proteinogenic side chains, and exist as racemic mixtures of interconverting right-handed and left-handed helices. Functionalization of the foldamers by a nanomolar ligand of human carbonic anhydrase II (HCA) ensured that they would be held in close proximity to the protein surface. Foldamer-protein interactions were screened by circular dichroism (CD). One foldamer displayed intense CD bands indicating that a preferred helix handedness is induced upon interacting with the protein surface. The crystal structure of the complex between this foldamer and HCA could be resolved at 2.1 ? resolution and revealed a number of unanticipated protein-foldamer, foldamer-foldamer, and protein-protein interactions. To design a foldamer that binds to a protein surface, a strategy is proposed that uses a known protein ligand to tether the foldamer to the protein surface. Candidates are first screened for induced circular dichroism in presence of the protein. Then, structural information about foldamer-protein interactions is collected before strong binding is established. The crystal structure of human carbonic anhydrase (A, B chains) with helical aromatic amide foldamers (stick models) is shown. Copyright
177. Electrospray-ionization mass spectrometry part 2: Neighboring-group participation in the mass-spectral decomposition of 4-hydroxycinnamoyl-spermidines
Hu, Wenqing,Reder, Elke,Hesse, Manfred
, p. 2137 - 2151 (1996)
The three mono substituted N-[(E)-3-(4-hydroxyphenyl)prop-2-enoyl]spermidines 1-3 have been studied by positive-ion electrospray-ionization tandem mass spectrometry (ESI-MS/MS). Because of the neighboring-group participation, the MS/MS of [1 + H]+/s
COMPOUNDS AND USES THEREOF
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Page/Page column 137; 144, (2021/10/15)
The present disclosure features compounds useful for the treatment of BAF complex-related disorders.
Target protein degradation inducing compound, preparation method thereof and pharmaceutical composition for preventing or treating targeted protein related diseases containing the same as an active ingredient
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Paragraph 1061; 1067-1069, (2020/05/01)
The present invention relates to a degraducer for inducing the decomposition of target protein, a producing method thereof, and a pharmaceutical composition for preventing or treating target protein-related diseases by containing the degraducer as an active ingredient. A novel compound represented by chemical formula 1, ULB-L-PTM, by the present invention, as a degraducer compound inducing the decomposition of target protein using cereblon E3 ubiquitin ligase, is able to significantly achieve a target protein degradation-inducing activity with an excellent binding activity of a cereblon E3 ubiquitin ligase binder thereby, being able to achieve an excellent protein degradation activity by targeting protein or polypeptide related to various diseases. The bromodomain-containing pharmaceutical composition for preventing or treating protein-related diseases or conditions contains the novel compound represented by chemical formula 1 as an active ingredient and has a useful effect of providing a health functional food composition for prevention or improvement.(AA) Example 22 (nM, 24h)COPYRIGHT KIPO 2020