title: Regioselective enzymatic acylation of complex natural products: expanding molecular diversity.
abstract: Enzymatic catalysis has become a common tool in both academia and industrial chemistry. The efforts of chemists over recent decades have led to the rationalization of the mechanism of action of biocatalysts, which have been routinely incorporated into many synthetic sequences. Nowadays, a further step consists in expanding the application of enzymes to the modification of complex molecular scaffolds common to many pharmaceutical leads isolated from nature. Regioselective enzymatic acylation is a process which has been profitably applied for this purpose in recent times, leading to new drugs with improved activity, stability and pharmacokinetic properties. This tutorial review provides an overview of this subject employing two classes of enzymes, hydrolases and acyltransferases, in the recently concluded decade although some representative older studies are commented upon, if required. We shall place special emphasis on those examples in which the novel acylated derivatives have improved the activity or properties of the parental molecules.
authors.affiliation: Entrechem, SL, Edificio Científico-Tecnológico, Campus del Cristo, 33006 Oviedo, Spain. jgsabin@entrechem.com
authors.forename: Javier
authors.initials: J
authors.lastname: González-Sabín
authors.forename: Roberto
authors.initials: R
authors.lastname: Morán-Ramallal
authors.forename: Francisca
authors.initials: F
authors.lastname: Rebolledo
mesh_terms: D000217:Acyltransferases / Q000737:chemistry / Q000378:metabolism; D055162:Biocatalysis; D001688:Biological Products / Q000737:chemistry / Q000378:metabolism*; D004798:Enzymes / Q000737:chemistry / Q000378:metabolism*; D005419:Flavonoids / Q000737:chemistry / Q000378:metabolism; D006867:Hydrolases / Q000737:chemistry / Q000378:metabolism; D061065:Polyketides / Q000737:chemistry / Q000378:metabolism; D013237:Stereoisomerism; D013729:Terpenes / Q000737:chemistry / Q000378:metabolism
chemical_list: D001688:Biological Products; D004798:Enzymes; D005419:Flavonoids; D061065:Polyketides; D013729:Terpenes; D000217:Acyltransferases; D006867:Hydrolases