ATP Non-Competitive Ser/Thr Kinase Inhibitors as Potential Anticancer Agents

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)

Volume 17, 14 Issues, 2017

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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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Michelle Prudhomme
Institut de Chimie de Clermont-Ferrand
Université Clermont Auvergne

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ATP Non-Competitive Ser/Thr Kinase Inhibitors as Potential Anticancer Agents

Anti-Cancer Agents in Medicinal Chemistry, 9(7): 778-786.

Author(s): Giorgio Cozza, Andrea Bortolato, Ernesto Menta, Ennio Cavalletti, Silvano Spinelli and Stefano Moro.

Affiliation: Molecular Modeling Section (MMS), Dipartimento di Scienze Farmaceutiche, Universita di Padova, Via Marzolo 5, I-35131 Padova, Italy.


Protein kinases are one of the largest known families of enzyme characterized by having a well conserved ATP binding pocket. Most of the synthetic kinase inhibitors are ATP-competitive, but display some potential problems, like selectivity, discrepancy between the in vitro and in vivo inhibition assays and an high risk of developing mutation inside the ATP-binding pocket. Recently some new inhibitors with a non-competitive mechanism of action were reported, with intresting results both in vitro and in vivo.


Ser/Thr kinase inhibitors, ATP non-competitive, anticancer drugs, drug discovery.

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Article Details

Volume: 9
Issue Number: 7
First Page: 778
Last Page: 786
Page Count: 9
DOI: 10.2174/187152009789056930
Price: $58
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