Farnesyl transferase inhibitors for patients with lung cancer

Clinical Cancer Research : an Official Journal of the American Association for Cancer Research
Bruce E Johnson, John V Heymach

Abstract

The ras family of genes have been identified as potential targets for therapeutic intervention because of somatic mutations in different human cancers. They are mutated in non-small cell lung cancer (NSCLC) approximately 20% of the time. The enzyme farnesyl transferase is involved in posttranslational modification of the ras proteins by covalently linking a farnesyl group to the ras protein. This permits the ras protein to be translocated to the surface membrane, allowing the protein to be involved in signaling for increased proliferation and inhibition of apoptosis. The class of farnesyl transferase inhibitors is designed to block farnesylation and prevent the mature ras signaling and thus inhibit cell proliferation and facilitate apoptosis. Multiple agents that inhibit farnesylation have been developed, and two farnesyl transferase inhibitors have been tested in patients with lung cancer in three Phase II trials. R115777 has been studied in patients with NSCLC and in patients with relapsed small cell lung cancer (SCLC) after chemotherapy. There has been a single trial of L-778,123 in patients with untreated NSCLC. No objective tumor responses in patients with stage IIIB/IV NSCLC were seen in these studies. There were also no ...Continue Reading

Citations

May 30, 2009·Journal of Computer-aided Molecular Design·Aihua XieRobert J Doerksen
Mar 15, 2005·European Journal of Cancer : Official Journal for European Organization for Research and Treatment of Cancer (EORTC) [and] European Association for Cancer Research (EACR)·David R Newell
Sep 27, 2008·Nature Genetics·Anton Berns
Sep 20, 2006·Proceedings of the National Academy of Sciences of the United States of America·Florian HohlaCelia A Kanashiro
Aug 24, 2005·International Journal of Clinical Practice·J Spicer, P Harper
Jul 23, 2011·Genes & Cancer·Rónán C O'Hagan, Joerg Heyer
Nov 16, 2007·Proceedings of the National Academy of Sciences of the United States of America·Florian HohlaGabor Halmos
Feb 28, 2014·Digestive Diseases and Sciences·Roberto GaluppoRoberto Gedaly
Mar 26, 2013·Journal of Thoracic Oncology : Official Publication of the International Association for the Study of Lung Cancer·Petra MartinFrances A Shepherd
Mar 5, 2008·Mayo Clinic Proceedings·Taimur SherAlex A Adjei
Nov 2, 2015·Revue des maladies respiratoires·N GuibertJ Mazieres
Jan 8, 2008·Surgical Oncology Clinics of North America·Volkert B Wreesmann, Bhuvanesh Singh
Jan 24, 2007·Thoracic Surgery Clinics·Philip W SmithDavid R Jones
Jan 24, 2007·Thoracic Surgery Clinics·Adam Yagui-BeltránDavid M Jablons
Jan 22, 2005·Current Opinion in Genetics & Development·Katharine Walker, Michael F Olson
Jun 17, 2005·Expert Opinion on Pharmacotherapy·Fiona BlackhallNicholas Thatcher
Oct 22, 2016·Biomedicine & Pharmacotherapy = Biomédecine & Pharmacothérapie·Sarah Fernandes TeixeiraAdilson Kleber Ferreira
Sep 22, 2005·Genes, Chromosomes & Cancer·Paola Sinibaldi-VallebonaCorrado Spadafora
Jun 29, 2018·Current Treatment Options in Oncology·Jacqueline V Aredo, Sukhmani K Padda
Feb 23, 2007·Molecular Cancer Research : MCR·Michalis V KaramouzisAthanasios G Papavassiliou
Oct 17, 2006·Molecular Cancer Therapeutics·James W Watters, Christopher J Roberts
Jun 17, 2005·Clinical Cancer Research : an Official Journal of the American Association for Cancer Research·Pavan BachireddyDean W Felsher

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