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Structural and Chemical Profiling of the Human Cytosolic Sulfotransferases
The human cytosolic sulfotransfases (hSULTs) comprise a family of 12 phase II enzymes involved in the metabolism of drugs and hormones, the bioactivation of carcinogens, and the detoxification ofExpand
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A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells.
Protein lysine methyltransferases G9a and GLP modulate the transcriptional repression of a variety of genes via dimethylation of Lys9 on histone H3 (H3K9me2) as well as dimethylation of non-histoneExpand
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Recognition and Specificity Determinants of the Human Cbx Chromodomains*
The eight mammalian Cbx proteins are chromodomain-containing proteins involved in regulation of heterochromatin, gene expression, and developmental programs. They are evolutionarily related to theExpand
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Structures of apicomplexan calcium-dependent protein kinases reveal mechanism of activation by calcium
Calcium-dependent protein kinases (CDPKs) have pivotal roles in the calcium-signaling pathway in plants, ciliates and apicomplexan parasites and comprise a calmodulin-dependent kinase (CaMK)-likeExpand
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L3MBTL1 recognition of mono- and dimethylated histones
Crystal structures of the L3MBTL1 MBT repeats in complex with histone H4 peptides dimethylated on Lys20 (H4K20me2) show that only the second of the three MBT repeats can bind mono- and dimethylatedExpand
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Chemical screening methods to identify ligands that promote protein stability, protein crystallization, and structure determination
The 3D structures of human therapeutic targets are enabling for drug discovery. However, their purification and crystallization remain rate determining. In individual cases, ligands have been used toExpand
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Genome-scale protein expression and structural biology of Plasmodium falciparum and related Apicomplexan organisms.
Parasites from the protozoan phylum Apicomplexa are responsible for diseases, such as malaria, toxoplasmosis and cryptosporidiosis, all of which have significantly higher rates of mortality andExpand
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The Structure of (3R)-Hydroxyacyl-Acyl Carrier Protein Dehydratase (FabZ) from Pseudomonas aeruginosa*
Type II fatty acid biosynthesis systems are essential for membrane formation in bacteria, making the constituent proteins of this pathway attractive targets for antibacterial drug discovery. TheExpand
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Pharmacological targeting of the Wdr5-MLL interaction in C/EBPα N-terminal leukemia
The CEBPA gene is mutated in 9% of patients with acute myeloid leukemia (AML). Selective expression of a short 30 kDa C/EBPα translational isoform, termed p30, represents the most common type ofExpand
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Structural basis of inhibition of the human NAD+-dependent deacetylase SIRT5 by suramin.
Sirtuins are NAD(+)-dependent protein deacetylases and are emerging as molecular targets for the development of pharmaceuticals to treat human metabolic and neurological diseases and cancer. To date,Expand
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