Design, synthesis, and preliminary pharmacological evaluation of a set of small molecules that directly activate Gi proteins

…, L Di Cesare Mannelli, S Dei, N Galeotti…

Index: Manetti, Dina; Mannelli, Lorenzo Di Cesare; Dei, Silvia; Galeotti, Nicoletta; Ghelardini, Carla; Romanelli, Maria Novella; Scapecchi, Serena; Teodori, Elisabetta; Pacini, Alessandra; Bartolini, Alessandro; Gualtieri, Fulvio Journal of Medicinal Chemistry, 2005 , vol. 48, # 20 p. 6491 - 6503

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Citation Number: 5

Abstract

Heterotrimeric G proteins play a pivotal role in the communication of cells with the environment. G proteins are stimulated by cell surface receptors (GPCR) that catalyze the exchange of GDP, bound to Gα subunit, with GTP and can per se be the target of drugs. Based on the structure of two nonpeptidic modulators of Gi proteins, a series of new molecules characterized by a long hydrophobic chain and at least two nitrogen atoms ...