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Biomolecules, Volume 10, Issue 5

May 2020 - 148 articles

Cover Story: β-Lactamase inhibitors (BLIs) are used in combination with existing β-lactam antibiotics to overcome β-lactamase-mediated antibiotic resistance. Boronic acid transition state analog inhibitors (BATSIs) are promising BLIs that form a reversible dative bond with the active site serine and mimic the tetrahedral transition state. Here, we report microbiological, biochemical, and structural studies of four BATSIs with a class C cephamycinase, FOX-4. X-ray crystal structures reveal that the compound, SM23, adopts different binding modes across class C β-lactamases. Comparison of the FOX-4/SM23 and FOX-4/cefoxitin complexes provides a rationale for the rapid turnover of cephamycins by FOX-4. Our analyses suggest new opportunities for the design of novel transition-state analogs of class C enzymes to be used as BLIs. View this paper.
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Articles (148)

  • Article
  • Open Access
8 Citations
3,524 Views
13 Pages

Matrix metalloproteinase-9 is upregulated in inflammatory bowel disease. Barbiturate nitrate hybrid compounds have been designed to inhibit MMP secretion and enzyme activity. In this study, we investigated the mechanism of action of barbiturate-nitra...

  • Article
  • Open Access
7 Citations
5,176 Views
18 Pages

Reduced Reverse Cholesterol Transport Efficacy in Healthy Men with Undesirable Postprandial Triglyceride Response

  • Alexandre Motte,
  • Julie Gall,
  • Joe-Elie Salem,
  • Eric Dasque,
  • Martine Lebot,
  • Eric Frisdal,
  • Sophie Galier,
  • Elise F. Villard,
  • Elodie Bouaziz-Amar and
  • Jean-Marc Lacorte
  • + 4 authors

Elevation of nonfasting triglyceride (TG) levels above 1.8 g/L (2 mmol/L) is associated with increased risk of cardiovascular diseases. Exacerbated postprandial hypertriglyceridemia (PP–HTG) and metabolic context both modulate the overall effic...

  • Article
  • Open Access
20 Citations
4,945 Views
16 Pages

Streptococcus mutans has been considered as the major etiological agent of dental caries, mostly due to its arsenal of virulence factors, including strong biofilm formation, exopolysaccharides production, and high acid production. Here, we present th...

  • Article
  • Open Access
3 Citations
3,391 Views
11 Pages

TGF-β is a critical cytokine to regulate multiple pathophysiological functions. For tumor development and progression, TGF-β was reported to play dual functions as a tumor suppressor and epithelial-mesenchymal transition (EMT) inducer. The...

  • Article
  • Open Access
57 Citations
4,611 Views
11 Pages

During the course of our search for novel biologically active metabolites from tropical fungi, we are using chemotaxonomic and taxonomic methodology for the preselection of interesting materials. Recently, three previously undescribed benzo[j]fluoran...

  • Article
  • Open Access
7 Citations
3,517 Views
16 Pages

Enhanced Biomass Yield of and Saccharification in Transgenic Tobacco Over-Expressing β-Glucosidase

  • Eun Jin Cho,
  • Quynh Anh Nguyen,
  • Yoon Gyo Lee,
  • Younho Song,
  • Bok Jae Park and
  • Hyeun-Jong Bae

Here, we report an increase in biomass yield and saccharification in transgenic tobacco plants (Nicotiana tabacum L.) overexpressing thermostable β-glucosidase from Thermotoga maritima, BglB, targeted to the chloroplasts and vacuoles. The transg...

  • Article
  • Open Access
29 Citations
5,977 Views
17 Pages

Amaryllidaceae Alkaloids of Belladine-Type from Narcissus pseudonarcissus cv. Carlton as New Selective Inhibitors of Butyrylcholinesterase

  • Abdullah Al Mamun,
  • Jana Maříková,
  • Daniela Hulcová,
  • Jiří Janoušek,
  • Marcela Šafratová,
  • Lucie Nováková,
  • Tomáš Kučera,
  • Martina Hrabinová,
  • Jiří Kuneš and
  • Jan Korábečný
  • + 1 author

Thirteen known (1–12 and 16) and three previously undescribed Amaryllidaceae alkaloids of belladine structural type, named carltonine A-C (13–15), were isolated from bulbs of Narcissus pseudonarcissus cv. Carlton (Amaryllidaceae) by stand...

  • Article
  • Open Access
80 Citations
12,220 Views
16 Pages

Effects of Chronic Cannabidiol Treatment in the Rat Chronic Unpredictable Mild Stress Model of Depression

  • Zsolt Gáll,
  • Szidónia Farkas,
  • Ákos Albert,
  • Elek Ferencz,
  • Szende Vancea,
  • Melinda Urkon and
  • Melinda Kolcsár

Several neuropharmacological actions of cannabidiol (CBD) due to the modulation of the endocannabinoid system as well as direct serotonergic and gamma-aminobutyric acidergic actions have recently been identified. The current study aimed to reveal the...

  • Article
  • Open Access
13 Citations
5,399 Views
17 Pages

Effect of Erufosine on Membrane Lipid Order in Breast Cancer Cell Models

  • Rumiana Tzoneva,
  • Tihomira Stoyanova,
  • Annett Petrich,
  • Desislava Popova,
  • Veselina Uzunova,
  • Albena Momchilova and
  • Salvatore Chiantia

Alkylphospholipids are a novel class of antineoplastic drugs showing remarkable therapeutic potential. Among them, erufosine (EPC3) is a promising drug for the treatment of several types of tumors. While EPC3 is supposed to exert its function by inte...

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Biomolecules - ISSN 2218-273X