Literature DB >> 17692026

Recent advances of MEK inhibitors and their clinical progress.

John Yuan Wang1, Keith M Wilcoxen, Kenichi Nomoto, Sara Wu.   

Abstract

The RAS/RAF/MEK/ERK signaling pathway has been a major clinical focus in oncology research in recent years. A clearer association of B-RAF mutations to cancers such as melanoma, papillary thyroid cancer and others has brought an increasing interest in chemotherapeutics that target this cellular signaling pathway. In this review, the authors summarize the current understanding of science and therapeutic use of the MEK inhibitors targeting the RAS/RAF/ MEK/ERK pathway. Clinical progresses of PD0325901 and AZD6244 are highlighted in addition to developments of new MEK inhibitors. Recently disclosed MEK inhibitors in two sub-divided classes, ATP noncompetitive and ATP competitive inhibitors are discussed.

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Year:  2007        PMID: 17692026     DOI: 10.2174/156802607781696837

Source DB:  PubMed          Journal:  Curr Top Med Chem        ISSN: 1568-0266            Impact factor:   3.295


  29 in total

Review 1.  Targeting the MAPK pathway in melanoma: why some approaches succeed and other fail.

Authors:  Gajanan S Inamdar; SubbaRao V Madhunapantula; Gavin P Robertson
Journal:  Biochem Pharmacol       Date:  2010-05-09       Impact factor: 5.858

Review 2.  Targeting cancer with small molecule kinase inhibitors.

Authors:  Jianming Zhang; Priscilla L Yang; Nathanael S Gray
Journal:  Nat Rev Cancer       Date:  2009-01       Impact factor: 60.716

3.  Activation of multiple signaling pathways causes developmental defects in mice with a Noonan syndrome–associated Sos1 mutation.

Authors:  Peng-Chieh Chen; Hiroko Wakimoto; David Conner; Toshiyuki Araki; Tao Yuan; Amy Roberts; Christine E Seidman; Roderick Bronson; Benjamin G Neel; Jonathan G Seidman; Raju Kucherlapati
Journal:  J Clin Invest       Date:  2010-12       Impact factor: 14.808

4.  Fluorescent cascade and direct assays for characterization of RAF signaling pathway inhibitors.

Authors:  Kevin R Kupcho; Rica Bruinsma; Tina M Hallis; David A Lasky; Richard L Somberg; Tammy Turek-Etienne; Kurt W Vogel; Kristin G Huwiler
Journal:  Curr Chem Genomics       Date:  2008-02-25

5.  The serine protease inhibitor serpinE2 is a novel target of ERK signaling involved in human colorectal tumorigenesis.

Authors:  Sébastien Bergeron; Etienne Lemieux; Véronique Durand; Sébastien Cagnol; Julie C Carrier; Jacques G Lussier; Marie-Josée Boucher; Nathalie Rivard
Journal:  Mol Cancer       Date:  2010-10-13       Impact factor: 27.401

6.  CInQ-03, a novel allosteric MEK inhibitor, suppresses cancer growth in vitro and in vivo.

Authors:  Dong Joon Kim; Mee-Hyun Lee; Kanamata Reddy; Yani Li; Do Young Lim; Hua Xie; Sung-Young Lee; Young Il Yeom; Ann M Bode; Zigang Dong
Journal:  Carcinogenesis       Date:  2013-01-25       Impact factor: 4.944

7.  IL-4 protein expression and basal activation of Erk in vivo in follicular lymphoma.

Authors:  Katherine R Calvo; Bhavana Dabir; Alexandra Kovach; Christopher Devor; Russell Bandle; Amelia Bond; Joanna H Shih; Elaine S Jaffe
Journal:  Blood       Date:  2008-08-05       Impact factor: 22.113

8.  MEK inhibitors potentiate dexamethasone lethality in acute lymphoblastic leukemia cells through the pro-apoptotic molecule BIM.

Authors:  A A Rambal; Z L G Panaguiton; L Kramer; S Grant; H Harada
Journal:  Leukemia       Date:  2009-04-30       Impact factor: 11.528

9.  Transcriptional profiling of the dose response: a more powerful approach for characterizing drug activities.

Authors:  Rui-Ru Ji; Heshani de Silva; Yisheng Jin; Robert E Bruccoleri; Jian Cao; Aiqing He; Wenjun Huang; Paul S Kayne; Isaac M Neuhaus; Karl-Heinz Ott; Becky Penhallow; Mark I Cockett; Michael G Neubauer; Nathan O Siemers; Petra Ross-Macdonald
Journal:  PLoS Comput Biol       Date:  2009-09-18       Impact factor: 4.475

10.  Protein and lipid kinase inhibitors as targeted anticancer agents of the Ras/Raf/MEK and PI3K/PKB pathways.

Authors:  Carlos García-Echeverría
Journal:  Purinergic Signal       Date:  2008-06-04       Impact factor: 3.765

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