title: Structure-based optimization of benzoic acids as inhibitors of protein tyrosine phosphatase 1B and low molecular weight protein tyrosine phosphatase.
abstract: We have optimized previously discovered benzoic acids 1, which are active as inhibitors of PTP1B and LMW-PTP, two protein tyrosine phosphatases that have emerged as attractive targets for the development of novel therapeutic agents for the treatment of diabetes, obesity, and cancer. Our efforts led to the identification of new and more potent analogues with appreciable selectivity toward human PTP1B and the IF1 isoform of human LMW-PTP.
authors.affiliation: Dipartimento Farmaco-chimico, Università di Messina, Polo Universitario Annunziata, 98168 Messina, Italy. rmaccari@pharma.unime.it
authors.forename: Rosanna
authors.initials: R
authors.lastname: Maccari
authors.forename: Rosaria
authors.initials: R
authors.lastname: Ottanà
authors.forename: Rosella
authors.initials: R
authors.lastname: Ciurleo
authors.forename: Paolo
authors.initials: P
authors.lastname: Paoli
authors.forename: Giampaolo
authors.initials: G
authors.lastname: Manao
authors.forename: Guido
authors.initials: G
authors.lastname: Camici
authors.forename: Christian
authors.initials: C
authors.lastname: Laggner
authors.forename: Thierry
authors.initials: T
authors.lastname: Langer
mesh_terms: D001565:Benzoates / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D020134:Catalytic Domain; D003198:Computer Simulation; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D020033:Protein Isoforms / Q000037:antagonists & inhibitors / Q000378:metabolism; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D017027:Protein Tyrosine Phosphatases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011518:Proto-Oncogene Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D001565:Benzoates; D004791:Enzyme Inhibitors; D020033:Protein Isoforms; D011518:Proto-Oncogene Proteins; C490429:ACP1 protein, human; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1; D017027:Protein Tyrosine Phosphatases