title: Synthetic polyamines: an overview of their multiple biological activities.
abstract: The binding of polyamines to a variety of receptors and other defined recognition sites has been widely reported. It is well-known that polyamines interact with aspartate, glutamate, and aromatic residues of a given receptor and/or enzyme mainly through the formation of ion bonds, since at physiological pH, protonation of amino groups is nearly complete. From this, the hypothesis arises that a polyamine may be a universal template able to recognize different receptor systems. This hypothesis suggests that both affinity and selectivity may be fine-tuned by inserting appropriate substituents onto the amine functions and by varying the methylene chain lengths between them on the polyamine backbone. In this paper, we detail several application of this design strategy aimed at discovering potent and selective polyamines able to bind neurotransmitter receptors and enzymes, such as muscarinic receptor subtypes, muscle-type nicotinic receptors and acethylcholinesterase.
authors.affiliation: Department of Pharmaceutical Sciences, Alma Mater Studiorum, University of Bologna, Via Belmeloro 6, 40126, Bologna, Italy. anna.minarini@unibo.it
authors.forename: Anna
authors.initials: A
authors.lastname: Minarini
authors.forename: Andrea
authors.initials: A
authors.lastname: Milelli
authors.forename: Vincenzo
authors.initials: V
authors.lastname: Tumiatti
authors.forename: Michela
authors.initials: M
authors.lastname: Rosini
authors.forename: Maria Laura
authors.initials: ML
authors.lastname: Bolognesi
authors.forename: Carlo
authors.initials: C
authors.lastname: Melchiorre
mesh_terms: D000818:Animals; D004798:Enzymes / Q000737:chemistry / Q000378:metabolism; D006801:Humans; D007700:Kinetics; D015394:Molecular Structure; D011073:Polyamines / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism*; D011485:Protein Binding; D017981:Receptors, Neurotransmitter / Q000737:chemistry / Q000378:metabolism
chemical_list: D004798:Enzymes; D011073:Polyamines; D017981:Receptors, Neurotransmitter