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Structural and biophysical studies of PCSK9 and its mutants linked to familial hypercholesterolemia
Proprotein convertase subtilisin kexin type 9 (PCSK9) lowers the abundance of surface low-density lipoprotein (LDL) receptor through an undefined mechanism. The structure of human PCSK9 shows theExpand
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Crystal Structure of the Herpes Simplex Virus 1 DNA Polymerase*
Herpesviruses are the second leading cause of human viral diseases. Herpes Simplex Virus types 1 and 2 and Varicella-zoster virus produce neurotropic infections such as cutaneous and genital herpes,Expand
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Open Access
Structural basis of transfer between lipoproteins by cholesteryl ester transfer protein.
Human cholesteryl ester transfer protein (CETP) mediates the net transfer of cholesteryl ester mass from atheroprotective high-density lipoproteins to atherogenic low-density lipoproteins by anExpand
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Open Access
Refined structures of beta-ketoacyl-acyl carrier protein synthase III.
beta-Ketoacyl-acyl carrier protein synthase III (FabH) is a condensing enzyme that plays central roles in fatty acid biosynthesis. Three-dimensional structures of E. coli FabH in the presence andExpand
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Crystal structure and substrate specificity of the β‐ketoacyl‐acyl carrier protein synthase III (FabH) from Staphylococcus aureus
β‐Ketoacyl‐ACP synthase III (FabH), an essential enzyme for bacterial viability, catalyzes the initiation of fatty acid elongation by condensing malonyl‐ACP with acetyl‐CoA. We have determined theExpand
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Structural basis for allosteric, substrate-dependent stimulation of SIRT1 activity by resveratrol.
Sirtuins with an extended N-terminal domain (NTD), represented by yeast Sir2 and human SIRT1, harbor intrinsic mechanisms for regulation of their NAD-dependent deacetylase activities. Elucidation ofExpand
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Indole naphthyridinones as inhibitors of bacterial enoyl-ACP reductases FabI and FabK.
Bacterial enoyl-ACP reductase (FabI) is responsible for catalyzing the final step of bacterial fatty acid biosynthesis and is an attractive target for the development of novel antibacterial agents.Expand
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Delineating the role of cooperativity in the design of potent PROTACs for BTK
Significance Proteolysis targeting chimera (PROTAC)-based protein degradation is an emerging field that holds significant promise for targeting the “undruggable” proteome: the vast majority of theExpand
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First X-ray cocrystal structure of a bacterial FabH condensing enzyme and a small molecule inhibitor achieved using rational design and homology modeling.
The first cocrystal structure of a bacterial FabH condensing enzyme and a small molecule inhibitor is reported. The inhibitor was obtained by rational modification of a high throughput screening leadExpand
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Crystal Structures of Cholesteryl Ester Transfer Protein in Complex with Inhibitors
  • S. Liu, A. Mistry, +6 authors X. Qiu
  • Chemistry, Medicine
  • The Journal of Biological Chemistry
  • 7 September 2012
Background: Human cholesteryl ester transfer protein (CETP) transfers cholesteryl esters from high-density to low-density lipoprotein particles. Results: Crystallographic, mutagenesis, andExpand
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