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Issue 18, 2017, Issue in Progress
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Chemical approaches to inhibitors of isoprenoid biosynthesis: targeting farnesyl and geranylgeranyl pyrophosphate synthases

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Abstract

Post-translational lipid modifications farnesylation and geranylgeranylation of proteins (protein prenylation) have been identified to mediate critical events in cancer, cardiovascular disorders, malaria and bone disorders like osteoporosis. To date eight compounds are commercialized for the treatment of bone disorders, and there are considerable efforts to develop selective small molecules that inhibit protein prenylation. This review summarizes the approaches currently employed to synthesize new inhibitors of isoprenoid biosynthesis. Bisphosphonates are mainly prepared through reaction of carboxylic acids with phosphorus reagents, Michael addition to tetraethylvinylidenebisphosphonate and alkylation of tetralkylmethyl bisphosphonate. Approaches to non-bisphosphonate derivatives include a variety of methodologies depending on the structure of the target compound.

Graphical abstract: Chemical approaches to inhibitors of isoprenoid biosynthesis: targeting farnesyl and geranylgeranyl pyrophosphate synthases

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Publication details

The article was received on 16 Dec 2016, accepted on 07 Feb 2017 and first published on 10 Feb 2017


Article type: Review Article
DOI: 10.1039/C6RA28316K
Citation: RSC Adv., 2017,7, 10947-10967
  • Open access: Creative Commons BY-NC license
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    Chemical approaches to inhibitors of isoprenoid biosynthesis: targeting farnesyl and geranylgeranyl pyrophosphate synthases

    P. Merino, L. Maiuolo, I. Delso, V. Algieri, A. De Nino and T. Tejero, RSC Adv., 2017, 7, 10947
    DOI: 10.1039/C6RA28316K

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