title: A perspective on rational drug design with cyclopentenone: targeting the proteome with the cyclopentenone chemical moiety.
abstract: The biological activity of cyclopentenone prostaglandins, of members of clavulones, and of other natural and synthetic compounds is strongly related to the presence of a conjugate cylcopentenone (CP) chemical moiety in their structure. CP reactivity is specifically directed toward the proteome, to covalent binding of crucial sulphydril groups on targeted proteins. In the literature it has been shown that directing this special CP biochemical reactivity by means of additional orienting constituents is a feasible strategy for inactivating specific enzymes in a cell. The introduction of a CP moiety into anticancer molecules, such as jasmonates and chalcones, has been shown to greatly boost their activity, probably due to the stable covalent chemical interaction with their targets. In general, similar strategies could lead to the development of a novel repertoire of therapeutic molecules targeted against specific pathogenetic anomalies of the proteome of diseased cells.
authors.affiliation: Laboratory of Clinical Pharmacology and Toxicology, Ospedale S. Maria delle Croci - v.le Randi, 5, 48100, Ravenna, Italy +39 0544285797 ; +39 0544285797 ; matteoconti@alice.it.
authors.forename: Matteo
authors.initials: M
authors.lastname: Conti