Stereoselective synthesis of allele-specific BET inhibitors
نویسندگان
چکیده
منابع مشابه
Design of allele-specific protein methyltransferase inhibitors.
Protein arginine methyltransferases, which catalyze the transfer of methyl groups from S-adenosylmethionine (SAM) to arginine side chains in target proteins, regulate transcription, RNA processing, and receptor-mediated signaling. To specifically address the functional role of the individual members of this family, we took a "bump-and-hole" approach and designed a series of N(6)-substituted S-a...
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Members of the kinesin superfamily are force-generating ATPases that drive movement and influence cytoskeleton organization in cells. Often, more than one kinesin is implicated in a cellular process, and many kinesins are proposed to have overlapping functions. By using conventional kinesin as a model system, we have developed an approach to activate or inhibit a specific kinesin allele in the ...
متن کاملDesign of allele-specific inhibitors to probe protein kinase signaling
BACKGROUND Deconvoluting protein kinase signaling pathways using conventional genetic and biochemical approaches has been difficult because of the overwhelming number of closely related kinases. If cell-permeable inhibitors of individual kinases could be designed, the role of each kinase could be systematically assessed. RESULTS We have devised an approach combining chemistry and genetics to ...
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(-)-Spicigerolide was stereoselectively synthesized from a protected (S)-lactaldehyde. The synthesis of the polyacetylated framework relied on two Zn-mediated stereoselective additions of alkynes to aldehydes as well as a regiocontrolled [3,3]-sigmatropic rearrangement of an allylic acetate. The pyranone moiety was constructed via ring-closing metathesis.
متن کاملStereoselective synthesis of Z-alkenes.
This chapter offers a general review of the evolvement of methods for the stereoselective synthesis of Z-alkenes, with a focus on the development of catalytic systems towards this goal in recent years.
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ژورنال
عنوان ژورنال: Organic & Biomolecular Chemistry
سال: 2020
ISSN: 1477-0520,1477-0539
DOI: 10.1039/d0ob01165g