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Structural evidence of N6-isopentenyladenosine as a new ligand of farnesyl pyrophosphate synthase.

Abstract：

:N6-isopentenyladenosine (i6A), a modified nucleoside belonging to the cytokinin family, has shown in humans many biological actions, including antitumoral effects through the modulation of the farnesyl pyrophosphate synthase (FPPS) activity. To investigate the relationship between i6A and FPPS, we undertook an inverse virtual screening computational target searching, testing i6A on a large panel of 3D protein structures involved in cancer processes. Experimentally, we performed an NMR investigation of i6A in the presence of FPPS protein. Both inverse virtual screening and saturation transfer difference (STD) NMR outcomes provided evidence of the structural interaction between i6A and FPPS, pointing to i6A as a valuable lead compound in the search of new ligands endowed with antitumoral potential and targeting FPPS protein.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Scrima M,Lauro G,Grimaldi M,Di Marino S,Tosco A,Picardi P,Gazzerro P,Riccio R,Novellino E,Bifulco M,Bifulco G,D'Ursi AM

doi

10.1021/jm500869x

subject

Has Abstract

pub_date

2014-09-25 00:00:00

pages

7798-803

issue

18

eissn

0022-2623

issn

1520-4804

journal_volume

57

pub_type

杂志文章

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