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Flexibility of the NSAID binding site in the structure of human cyclooxygenase-2
The first crystal structure of human cyclooxygenase-2, in the presence of a selective inhibitor, is similar to that of cyclooxygenase-1. The structure of the NSAID binding site is also wellExpand
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The structure of mammalian 15-lipoxygenase reveals similarity to the lipases and the determinants of substrate specificity
Here we report the first structure of a mammalian 15-lipoxygenase. The protein is composed of two domains; a catalytic domain and a previously unrecognized β-barrel domain. The N-terminal β-barrelExpand
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Cutting Edge: IL-1 Receptor-Associated Kinase 4 Structures Reveal Novel Features and Multiple Conformations
IL-1R-associated kinase (IRAK)4 plays a central role in innate and adaptive immunity, and is a crucial component in IL-1/TLR signaling. We have determined the crystal structures of the apo andExpand
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Crystal structures of MMP-1 and -13 reveal the structural basis for selectivity of collagenase inhibitors
The X-ray crystal structures of the catalytic domain of human collagenase-3 (MMP-13) and collagenase-1 (MMP-1) with bound inhibitors provides a basis for understanding the selectivity profile of aExpand
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Expression of the catalytic subunit of phosphorylase phosphatase (protein phosphatase-1) in Escherichia coli.
The catalytic subunit of rabbit skeletal muscle protein phosphatase-1 was expressed in Escherichia coli. Expression of phosphatase-1 in the pET3a vector, which is based on the use of the T7 promoter,Expand
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Shape and Specificity in Mammalian 15-Lipoxygenase Active Site
Previous mutagenesis studies along with molecular modeling using the x-ray coordinates of the rabbit 15-lipoxygenase have led to the suggestion that the size of the substrate binding pocket may playExpand
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Human muscle glycogen synthase cDNA sequence: a negatively charged protein with an asymmetric charge distribution.
The cDNA for human muscle glycogen synthase encodes a protein of 737 amino acids. The primary structure of glycogen synthase is not related either to bacterial glycogen synthase or to any glycogenExpand
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Selection and Characterization of Replicon Variants Dually Resistant to Thumb- and Palm-Binding Nonnucleoside Polymerase Inhibitors of the Hepatitis C Virus
ABSTRACT Multiple nonnucleoside inhibitor binding sites have been identified within the hepatitis C virus (HCV) polymerase, including in the palm and thumb domains. After a single treatment with aExpand
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Surface plasmon resonance based assay for the detection and characterization of promiscuous inhibitors.
Promiscuous binders achieve enzyme inhibition using a nonspecific aggregation-type binding mechanism to proteins. These compounds are a source of false-positive hits in biochemical inhibition assaysExpand
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Temperature-sensitive production of rabbit muscle glycogen phosphorylase in Escherichia coli.
In order to understand how allosteric switches regulate both the catalytic activity and molecular interactions of glycogen phosphorylase, it is necessary to design and analyze variant proteins thatExpand
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