Structural Mechanism for Statin Inhibition of HMG-CoA Reductase

By E. Istvan, J. Deisenhofer. Science, 2001

1,617 citations recorded by the source corpus.

Subfields: Computational Theory and Mathematics, Molecular Biology, Surgery

View Paper: https://www.semanticscholar.org/paper/c933788edcd1d03d14f2e31a899fb6703fba96b8

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Citations in the corpus

Human T Cell Receptor γδ Cells Recognize Endogenous Mevalonate Metabolites in Tumor Cells (2003, background): “To test the role of HMGR in generating TCR- stimulatory ligands, both Daudi and YMB-1 cells were treated with mevastatin, an inhibitor of the HMGR catalytic site (16).”
Generative Adversarial Networks for Electronic Health Records: A Framework for Exploring and Evaluating Methods for Predicting Drug-Induced Laboratory Test Trajectories (2017, methodology): “To this end, we decided to study the effect of HMG-CoA reductase inhibitors, or statins, on cholesterol laboratory measurements they are designed to decrease [8].”
Fluorine in medicinal chemistry. (2015, background): “As highlighted in section 7 a survey of PDB structures has shown this as a common favourable fluorine interaction [10], one other notable example being in the structure of atorvastatin (LipitorTM) (Figure 55) [94].”
Structure-based maximal affinity model predicts small-molecule druggability (2007, background): “This is likely due to underestimation of the contribution of electrostatic interactions, as statins have a conserved glutaminyl group that makes numerous hydrogen-bond and ion-pair interactions to the protei”
Anti-Inflammatory Effects of Statins: Clinical Evidence and Basic Mechanisms (2005, background): “Crystal-structure studies demonstrated that this inhibitory effect occurs by virtue of the ability of statins to occupy a portion of the HMGR binding site, thereby blocking access of this substrate to the enzyme's active sit”
Pleiotropic Effects of Statins on the Cardiovascular System (2017, background): “Statins decrease cholesterol biosynthesis and decrease serum LDL-C and triglyceride levels.(4) Landmark”
Pleiotropic effects of statins. (2005, background): “Recently, the structure of the catalytic portion of human HMG-CoA reductase complexed with different statins was determined (22).”