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Drug design from the cryptic inhibitor envelope
Conformational dynamics plays an important role in enzyme catalysis, allosteric regulation of protein functions and assembly of macromolecular complexes. Despite these well-established roles, such… Expand
Species-specific and inhibitor-dependent conformations of LpxC: implications for antibiotic design.
LpxC is an essential enzyme in the lipid A biosynthetic pathway in gram-negative bacteria. Several promising antimicrobial lead compounds targeting LpxC have been reported, though they typically… Expand
Structural basis of the promiscuous inhibitor susceptibility of Escherichia coli LpxC.
The LpxC enzyme in the lipid A biosynthetic pathway is one of the most promising and clinically unexploited antibiotic targets for treatment of multidrug-resistant Gram-negative infections. Progress… Expand
High susceptibility of MDR and XDR Gram-negative pathogens to biphenyl-diacetylene-based difluoromethyl-allo-threonyl-hydroxamate LpxC inhibitors.
- M. Titécat, Xiaofei Liang, +9 authors N. Lemaître
- Biology, Medicine
- The Journal of antimicrobial chemotherapy
- 20 June 2016
OBJECTIVES Inhibitors of uridine diphosphate-3-O-(R-3-hydroxymyristoyl)-N-acetylglucosamine deacetylase (LpxC, which catalyses the first, irreversible step in lipid A biosynthesis) are a promising… Expand
Curative Treatment of Severe Gram-Negative Bacterial Infections by a New Class of Antibiotics Targeting LpxC
ABSTRACT The infectious diseases caused by multidrug-resistant bacteria pose serious threats to humankind. It has been suggested that an antibiotic targeting LpxC of the lipid A biosynthetic pathway… Expand
A Scalable Synthesis of the Difluoromethyl-allo-threonyl Hydroxamate-Based LpxC Inhibitor LPC-058.
- Xiaofei Liang, Ramesh Gopalaswamy, F. Navas, E. Toone, P. Zhou
- Chemistry, Medicine
- The Journal of organic chemistry
- 6 May 2016
The difluoromethyl-allo-threonyl hydroxamate-based compound LPC-058 is a potent inhibitor of UDP-3-O-(R-3-hydroxymyristoyl)-N-acetylglucosamine deacetylase (LpxC) in Gram-negative bacteria. A… Expand
Chemical constituents from the roots and rhizomes of Silene tatarinowii Regel
Abstract Chemical investigation of the root and rhizome of Silene tatarinowii Regel led to the isolation of nine ecdysteroids (1–9) and one sterol (10). All the compounds were determined on the basis… Expand
TBIO-03. CONSTRUCTION AND PRELIMINARY CLINICAL APPLICATION OF A HIGH-SENSITIVITY AND MULTISITE IMMUNOMAGNETIC LIPOSOME-FLUORESCENCE CTC SYSTEM FOR CTC CAPTURING IN PEDIATRIC BRAIN TUMOR
A New Lignan Glycoside from the Roots of Silene tatarinowii Regel
A new lignan glycoside, siletatoside A (1), and three known lignans, (+)-isolariciresinol (2), balanophonin (3), and (+)-lariciresinol (4), were isolated from the roots of Silene tatarinowii Regel.… Expand