Karin Schmidtkunz

TL;DR: High-resolution structures of human Sirt2 in complex with highly selective drug-like inhibitors that show a unique inhibitory mechanism are presented and structural insights into this unique mechanism of selective sirtuin inhibition provide the basis for further inhibitor development and selective tools for sIRTuin biology.

TL;DR: The biological and structural findings define the framework for the rational design of small-molecule inhibitors specifically interfering with schistosome epigenetic mechanisms, and further support an anti-parasitic epigenome targeting strategy to treat neglected diseases caused by eukaryotic pathogens.

TL;DR: BRD4 has been characterized as a key determinant in acute myeloid leukemia, multiple myeloma, Burkitt s lymphoma, NUT midline carcinoma, colon cancer, and inflammatory disease, and small molecules that inhibit BRD4 have potential as antiinflammatory, antiviral, and anticancer agents.

TL;DR: It is shown that HDAC8-selective inhibitors adopt a L-shaped conformation required for their binding to a HDAC 8-specific pocket formed by HDAC9 catalytic tyrosine and HDAC7 L1 and L6 loops.

TL;DR: Preparation and systematic variation of phenothiazines and their analogues containing a benzhydroxamic acid moiety as the zinc-binding group results in increased potency and selectivity for HDAC6, as rationalized by molecular modeling and docking studies.