Poznań, Poland


Poznań, Poland
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Belter A.,Polish Academy of Sciences | Belter A.,BioInfoBank Institute | Skupinska M.,Polish Academy of Sciences | Skupinska M.,BioInfoBank Institute | And 4 more authors.
Biological Chemistry | Year: 2011

Squalene monooxygenase catalyzes the epoxidation of C-C double bond of squalene to yield 2,3-oxidosqualene, the key step of sterol biosynthesis pathways in eukaryotes. Sterols are essential compounds of these organisms and squalene epoxidation is an important regulatory point in their synthesis. Squalene monooxygenase downregulation in vertebrates and fungi decreases synthesis of cholesterol and ergosterol, respectively, which makes squalene monooxygenase a potent and attractive target of hypercholesterolemia and antifungal therapies. Currently some fungal squalene monooxygenase inhibitors (terbinafine, naftifine, butenafine) are in clinical use, whereas mammalian enzymes' inhibitors are still under investigation. Research on new squalene monooxygenase inhibitors is important due to the prevalence of hypercholesterolemia and the lack of both sufficient and safe remedies. In this paper we (i) review data on activity and the structure of squalene monooxygenase, (ii) present its inhibitors, (iii) compare current strategies of lowering cholesterol level in blood with some of the most promising strategies, (iv) underline advantages of squalene monooxygenase as a target for hypercholesterolemia therapy, and (v) discuss safety concerns about hypercholesterolemia therapy based on inhibition of cellular cholesterol biosynthesis and potential usage of squalene monooxygenase inhibitors in clinical practice. After many years of use of statins there is some clinical evidence for their adverse effects and only partial effectiveness. Currently they are drugs of choice but are used with many restrictions, especially in case of children, elderly patients and women of childbearing potential. Certainly, for the next few years, statins will continue to be a suitable tool for cost-effective cardiovascular prevention; however research on new hypolipidemic drugs is highly desirable. We suggest that squalene monooxygenase inhibitors could become the hypocholesterolemic agents of the future. © 2011 by Walter de Gruyter Berlin Boston 2011.

Bendzinska-Berus W.,Adam Mickiewicz University | Kaik-King M.,AdvaChemLab | King G.,AdvaChemLab | Rychlewska U.,Adam Mickiewicz University
Acta Crystallographica Section C: Structural Chemistry | Year: 2014

In connection with a research program involving the synthesis, structure determination, reactivity and ability to coordinate to metal centres of chiral bisphosphine ligands, we have synthesized and structurally characterized, by means of single-crystal X-ray diffraction analysis, the title compound {systematic name: (S,S)-(ethane-1,2-diyl)bis[(2-methylphenyl)phenylphosphane], abbreviated as o-tolyl-DiPAMP}, C28H28P2. So far, neither the free bisphosphine (DiPAMP) nor analogues that incorporate the ethylenebisphosphine frame have had their crystal structures reported. The investigated compound forms crystals which are isostructural with the bisphosphine dioxide analogue [King et al. (2007). Acta Cryst. E63, o3278], despite the involvement of the dioxide in C - H⋯O(=P) hydrogen bonds and the lack of similar hydrogen bonds in the investigated crystal structure. In both molecules, the P - C - C - P chain is in a trans conformation, extended further at both ends by one of the two P - Cipso bonds. The planes of the phenyl and o-tolyl rings attached to the same P atom are nearly perpendicular to one another. Both crystal structures are mainly stabilized by dispersive interactions. © 2014 International Union of Crystallography.

Szudkowska-Fratczak J.,Adam Mickiewicz University | Zaranek M.,Adam Mickiewicz University | Hreczycho G.,Adam Mickiewicz University | Kubicki M.,Adam Mickiewicz University | And 2 more authors.
Applied Organometallic Chemistry | Year: 2015

(E)-β-Iodoenamides and (E)-β-iodoenimides can be easily obtained from N-vinyl derivatives (N-vinylamides and N-vinylimides) by stereoselective ruthenium-catalysed silylative coupling with vinyltrimethylsilane (Marciniec coupling) and subsequent stereospecific silicon-iodine exchange. Bromodesilylation of (E)-β-silylenimides affords (E)-β-bromoenimides, while the analogous reactions involving (E)-β-silylenamides lead to decomposition of substrates. N-Halosuccinimides have been found as the most effective halogenating agents in the desilylation step under mild conditions. The ruthenium-catalysed silylation/halodesilylation sequence can be performed in a one-pot procedure. Copyright © 2015 John Wiley & Sons, Ltd.

Adamski A.,Adam Mickiewicz University | Kubicki M.,Adam Mickiewicz University | Pawluc P.,Adam Mickiewicz University | Grabarkiewicz T.,AdvaChemLab | Patroniak V.,Adam Mickiewicz University
Catalysis Communications | Year: 2013

The reaction of ligand L with PtCl2 leads to a novel structural motif of octahedral ortho-metalated complex of formula [Pt(L-H) Cl3] 1. This result is a consequence of drastic conditions of reaction and preferred Pt(IV) octahedral coordination geometry. The new compound has been characterised on the basis of the spectroscopic data in solution, and its structure confirmed in the solid state by X-ray crystallography (1a - [Pt(L-H)Cl3]·MeOH, 1b - [Pt(L-H)Cl 3]·C6H5CH3). This article reports organoplatinum (IV) complex 1 as effective and highly selective catalyst precursor in the hydrosilylation of styrene and terminal alkynes. © 2013 Elsevier B.V.

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