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Structural snapshots of human HDAC8 provide insights into the class I histone deacetylases.
Modulation of the acetylation state of histones plays a pivotal role in the regulation of gene expression. Histone deacetylases (HDACs) catalyze the removal of acetyl groups from lysines near the N… Expand
Structural and kinetic analysis of Escherichia coli GDP-mannose 4,6 dehydratase provides insights into the enzyme's catalytic mechanism and regulation by GDP-fucose.
BACKGROUND GDP-mannose 4,6 dehydratase (GMD) catalyzes the conversion of GDP-(D)-mannose to GDP-4-keto, 6-deoxy-(D)-mannose. This is the first and regulatory step in the de novo biosynthesis of… Expand
Visualizing ATP-dependent RNA translocation by the NS3 helicase from HCV.
- T. Appleby, R. Anderson, +5 authors J. R. Somoza
- Biology, Medicine
- Journal of molecular biology
- 4 February 2011
The structural mechanism by which nonstructural protein 3 (NS3) from the hepatitis C virus (HCV) translocates along RNA is currently unknown. HCV NS3 is an ATP-dependent motor protein essential for… Expand
Structural, Biochemical, and Biophysical Characterization of Idelalisib Binding to Phosphoinositide 3-Kinase δ*
- J. R. Somoza, David Koditek, +11 authors M. Mcgrath
- Chemistry, Medicine
- The Journal of Biological Chemistry
- 28 January 2015
Background: Idelalisib is a PI3Kδ inhibitor used to treat hematological malignancies. Results: Idelalisib is selective, noncovalent, reversible, and ATP-competitive. Conclusion: The crystal structure… Expand
Crystal structure of the hypoxanthine-guanine-xanthine phosphoribosyltransferase from the protozoan parasite Tritrichomonas foetus.
The crystal structure of the hypoxanthine-guanine-xanthine phosphoribosyltransferase (HGXPRTase) from Tritrichomonas foetus has been determined and refined against X-ray data to 1.9 A resolution. T.… Expand
Structural basis for unique mechanisms of folding and hemoglobin binding by a malarial protease.
- S. Wang, K. Pandey, +6 authors J. McKerrow
- Biology, Medicine
- Proceedings of the National Academy of Sciences…
- 1 August 2006
Falcipain-2 (FP2), the major cysteine protease of the human malaria parasite Plasmodium falciparum, is a hemoglobinase and promising drug target. Here we report the crystal structure of FP2 in… Expand
The taste-active regions of monellin, a potently sweet protein.
Monellin, a protein found in the berries of the West African plant Dioscoreophyllum cumminsii, is one of the most potently sweet compounds known. The native three-dimensional structure of monellin is… Expand
Clinical targeting of HIV capsid protein with a long-acting small molecule
Oral antiretroviral agents provide life-saving treatments for millions of people living with HIV, and can prevent new infections via pre-exposure prophylaxis 1 – 5 . However, some people living with… Expand
Crystal structure of human cathepsin V.
Cathepsin V is a lysosomal cysteine protease that is expressed in the thymus, testis and corneal epithelium. We have determined the 1.6 A resolution crystal structure of human cathepsin V associated… Expand
Crystal structure of Tritrichomonas foetus inosine-5'-monophosphate dehydrogenase and the enzyme-product complex.
Inosine-5'-monophosphate dehydrogenase (IMPDH) is an attractive drug target for the control of parasitic infections. The enzyme catalyzes the oxidation of inosine monophosphate (IMP) to xanthosine… Expand