- Useful synthesis of 2,3,6-tri- and 2,3,5,6-tetrasubstitutedpyridine derivatives from aspartic acid
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New synthetic methods for 2,3,6-tri- and 2,3,5,6-tetrasubstituted pyridineskeletons, which are the essential main central segments of thiostrepton-type macrocyclic antibiotics, were developed from l-α-aspartic acid (Asp) via the Asp-derived α-dehydroamino
- Yonezawa, Yasuchika,Konn, Akihito,Shin, Chung-gi
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p. 2735 - 2746
(2007/10/03)
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- Design and application of an α-helix-mimetic scaffold based on an oligoamide-foldamer strategy: Antagonism of the Bak BH3/Bcl-xL complex
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The prevention of cell death by the antiapoptotic protein Bcl-xL has been linked to a number of cancers. Bcl-xl binds to the BH3 domain of the proapoptotic protein Bak, thus preventing programmed cell death. A competitive assay and docking studies have shown that the polyamide scaffold 1, which was synthesized based on a rational structure-based design, interferes with the Bak BH3/Bcl-xl complexation.
- Ernst, Justin T.,Becerril, Jorge,Park, Hyung Soon,Yin, Hang,Hamilton, Andrew D.
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p. 535 - 539
(2007/10/03)
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- Proteomimetic compounds and methods
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The present invention relates to compounds and pharmaceutical compositions which are proteomimetic and to methods for inhibiting the interaction of an alpha-helical protein with another protein or binding site. Methods for treating diseases or conditions which are modulated through interactions between alpha helical proteins and their binding sites are other aspects of the invention.
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