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Search for "CYP51" in Full Text gives 3 result(s) in Beilstein Journal of Organic Chemistry.

Synthesis and antimycotic activity of new derivatives of imidazo[1,2-a]pyrimidines

  • Dmitriy Yu. Vandyshev,
  • Daria A. Mangusheva,
  • Khidmet S. Shikhaliev,
  • Kirill A. Scherbakov,
  • Oleg N. Burov,
  • Alexander D. Zagrebaev,
  • Tatiana N. Khmelevskaya,
  • Alexey S. Trenin and
  • Fedor I. Zubkov

Beilstein J. Org. Chem. 2024, 20, 2806–2817, doi:10.3762/bjoc.20.236

Graphical Abstract
  • this work was a preliminary evaluation of the potential bioactivity of the obtained compounds. In particular, a molecular docking experiment to investigate the binding mechanisms to the CYP51 enzyme and an evaluation of the antifungal activity of imidazo[1,2-a]pyrimidines against Candida albicans were
  • -spectrum antifungal agents. Among the many drugs and hits, the azole-based systems (including triazoles and imidazoles) are of particular importance in this context. Their mechanism of action is the inhibition of the activity of the enzyme lanosterol 14α-demethylase (CYP51), which is encoded by the CYP51
  • /ERG11 gene. This enzyme contains a haem-like prosthetic group in its active center and is a member of the cytochrome P450 family, which plays a key role in the biosynthesis of sterols. Sterols in turn are integral components of the fungal cell membrane, making inhibition of CYP51 [43] an effective
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Published 05 Nov 2024

Cytochrome P450 monooxygenase-mediated tailoring of triterpenoids and steroids in plants

  • Karan Malhotra and
  • Jakob Franke

Beilstein J. Org. Chem. 2022, 18, 1289–1310, doi:10.3762/bjoc.18.135

Graphical Abstract
  • clans, families, and subfamilies. The broadest hierarchy level is represented by clans, which comprise one or multiple families. An example CYP name is CYP51G1; here, “CYP51” designates the family, “G” refers to the subfamily within the CYP51 family, and “1” represents the isoform of CYPs in this
  • other families of the CYP85 clan such as CYP87, CYP85, or CYP90 contain mostly triterpene-modifying CYPs to date. The small clans CYP51 and CYP710 are other important examples of groups with a high preference for triterpenoid substrates. The highly diverse CYP71 clan, in contrast, only contains a few
  • four CYPs could produce stigmasterol from β-sitosterol (2) in enzyme assays performed in vitro. However, Arabidopsis CYP710A2 showed substrate flexibility towards campesterol (1) epimers and could also produce brassicasterol from 24-epicampesterol in vitro. Enzymes of the CYP51G subfamily (CYP51 clan
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Published 21 Sep 2022

Chemical–biological characterization of a cruzain inhibitor reveals a second target and a mammalian off-target

  • Jonathan W. Choy,
  • Clifford Bryant,
  • Claudia M. Calvet,
  • Patricia S. Doyle,
  • Shamila S. Gunatilleke,
  • Siegfried S. F. Leung,
  • Kenny K. H. Ang,
  • Steven Chen,
  • Jiri Gut,
  • Juan A. Oses-Prieto,
  • Jonathan B. Johnston,
  • Michelle R. Arkin,
  • Alma L. Burlingame,
  • Jack Taunton,
  • Matthew P. Jacobson,
  • James M. McKerrow,
  • Larissa M. Podust and
  • Adam R. Renslo

Beilstein J. Org. Chem. 2013, 9, 15–25, doi:10.3762/bjoc.9.3

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  • of this new class of inhibitors. Keywords: activity-based probes; Chagas’ disease; cruzain; CYP51; 14-α-demethylase; hybrid drugs; Trypanosoma cruzi; Introduction The kinetoplastid protozoan Trypanosoma cruzi is the causative agent of Chagas’ disease, a leading cause of heart failure in endemic
  • investigated are cruzain [7][8][9][10], the major cysteine protease active in the parasite, and T. cruzi CYP51 (TcCYP51), a 14-α-demethylase enzyme of the cytochrome P450 family required for ergosterol biosynthesis [11][12][13][14]. TcCYP51 is analogous to the fungal enzyme targeted by the azole class of
  • performed concurrently with other CYP51 inhibitors described recently [33] and, thus, the spectra for the controls shown above are reproduced from the earlier report. Spectra of lipid extracts from parasites treated with 3, 6, 7, and 8 are provided in Supporting Information File 1. Uninfected host cell
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Published 04 Jan 2013
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