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Benzothiazinones Kill Mycobacterium tuberculosis by Blocking Arabinan Synthesis
Makarov, V.,Manina, G.,Mikusova, K.,Mollmann, U.,Ryabova, O.,Saint-Joanis, B.,Dhar, N.,Pasca, M. R.,Buroni, S.,Lucarelli, A. P.,Milano, A.,De Rossi, E.,Belanova, M.,Bobovska, A.,Dianiskova, P.,Kordula American Association for the Advancement of Scienc 2009 Science Vol.324 No.5928
<P>New drugs are required to counter the tuberculosis (TB) pandemic. Here, we describe the synthesis and characterization of 1,3-benzothiazin-4-ones (BTZs), a new class of antimycobacterial agents that kill Mycobacterium tuberculosis in vitro, ex vivo, and in mouse models of TB. Using genetics and biochemistry, we identified the enzyme decaprenylphosphoryl-beta-d-ribose 2'-epimerase as a major BTZ target. Inhibition of this enzymatic activity abolishes the formation of decaprenylphosphoryl arabinose, a key precursor that is required for the synthesis of the cell-wall arabinans, thus provoking cell lysis and bacterial death. The most advanced compound, BTZ043, is a candidate for inclusion in combination therapies for both drug-sensitive and extensively drug-resistant TB.</P>
Neu, V,Schulze, C,Faustini, M,Lee, J,Makarov, D,Suess, D,Kim, S-K,Grosso, D,Schultz, L,Albrecht, M IOP Pub 2013 Nanotechnology Vol.24 No.14
<P>Magnetization reversal processes in Co/Pt multilayers prepared on nanoperforated templates are probed by magnetization relaxation measurements. The signature of pinning controlled domain wall movement as expected for percolated media is identified. This contrasts with the nucleation-type reversal mechanism of a Co/Pt reference film prepared on a smooth substrate. A zero field energy barrier of 93<I>k</I><SUB>B</SUB><I>T</I> is determined by fluctuation field measurements and is elucidated by micromagnetic calculations using the nudged elastic band method. This value is sufficiently large to qualify the material as a promising percolated medium.</P>
S.K. Ryndevich,A.A. Prokin,K.V. Makarov,Yu.N. Sundukov 국립중앙과학관 2021 Journal of Asia-Pacific Biodiversity Vol.14 No.4
The fauna of Kunashir Island and the islands of the Lesser Kuril Chain contains 47 species from 18 generaof Georissidae, Helophoridae, Hydrophilidae, Hydraenidae, and Elmidae. Two species (Enochrus vilis(Sharp, 1884) and Ochthebius inermis Sharp, 1884) are recorded for Russia for the first time. Fifteenspecies are new to the fauna of Kunashir Island and the Lesser Kurils. The article contains an annotatedlist of species, including the studied material and published records. The article is illustrated by photographsof habitats and species, maps of their distribution in Kunashir. The relationships between thespecies richness on an island area and the features of the fauna of Kunashir in comparison with Hokkaidoare discussed. The species richness of the studied Polyphaga families in Kunashir is almost 2/3 of thefauna of Hokkaido, while the island’s area is 55 times smaller. The reason for the absence of large speciesof the genera Hydrochara and Hydrophilus in Kunashir is hypothesized to be a restriction of the northernrange species boundaries by the July isotherm of þ16 S.