Literature DB >> 17964172

Novel cholesterol biosynthesis inhibitors targeting human lanosterol 14alpha-demethylase (CYP51).

Tina Korosec1, Jure Acimovic, Matej Seliskar, Darko Kocjan, Klementina Fon Tacer, Damjana Rozman, Uros Urleb.   

Abstract

Novel cholesterol biosynthesis inhibitors, a group of pyridylethanol(phenylethyl)amine derivatives, were synthesized. Sterol profiling assay in the human hepatoma HepG2 cells revealed that compounds target human lanosterol 14alpha-demethylase (CYP51). Structure-activity relationship study of the binding with the overexpressed human CYP51 indicates that the pyridine binds within the heme binding pocket in an analogy with the azoles.

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Year:  2007        PMID: 17964172     DOI: 10.1016/j.bmc.2007.10.001

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  4 in total

1.  Azole affinity of sterol 14α-demethylase (CYP51) enzymes from Candida albicans and Homo sapiens.

Authors:  Andrew G Warrilow; Josie E Parker; Diane E Kelly; Steven L Kelly
Journal:  Antimicrob Agents Chemother       Date:  2012-12-28       Impact factor: 5.191

Review 2.  Resistance to antifungals that target CYP51.

Authors:  Josie E Parker; Andrew G S Warrilow; Claire L Price; Jonathan G L Mullins; Diane E Kelly; Steven L Kelly
Journal:  J Chem Biol       Date:  2014-08-27

3.  Potential Mechanism of Action of Cyclosporin A in Human Dermal Fibroblasts-Transcriptomic Analysis of CYPs.

Authors:  Grażyna Janikowska; Alina Pyka-Pająk; Tomasz Janikowski; Jolanta Adamska; Urszula Mazurek; Przemysław Jędrusik
Journal:  Molecules       Date:  2018-07-05       Impact factor: 4.411

4.  Human Lanosterol 14-Alpha Demethylase (CYP51A1) Is a Putative Target for Natural Flavonoid Luteolin 7,3'-Disulfate.

Authors:  Leonid Kaluzhskiy; Pavel Ershov; Evgeniy Yablokov; Tatsiana Shkel; Irina Grabovec; Yuri Mezentsev; Oksana Gnedenko; Sergey Usanov; Polina Shabunya; Sviatlana Fatykhava; Alexander Popov; Aleksandr Artyukov; Olga Styshova; Andrei Gilep; Natallia Strushkevich; Alexis Ivanov
Journal:  Molecules       Date:  2021-04-13       Impact factor: 4.411

  4 in total

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