scholarly journals Farnesyl Transferase Inhibitors: Mechanism of Action, Translational Studies and Clinical Evaluation

2003 ◽  
Vol 2 (sup1) ◽  
pp. 95-103 ◽  
Author(s):  
W. Robert Bishop ◽  
Paul Kirschmeier ◽  
Charles Baum
Keyword(s):  
Clinical Evaluation ◽  
Mechanism Of Action ◽  
Farnesyl Transferase ◽  
Translational Studies ◽  
Farnesyl Transferase Inhibitors

Biological Effects and Mechanism of Action of Farnesyl Transferase Inhibitors

2000 ◽  
Vol 13 (10) ◽  
pp. 949-952 ◽  
Author(s):  
Hena R. Ashar ◽  
Lydia Armstrong ◽  
Linda J. James ◽  
Donna M. Carr ◽  
Kimberley Gray ◽  
...  
Keyword(s):  
Mechanism Of Action ◽  
Biological Effects ◽  
Farnesyl Transferase ◽  
Farnesyl Transferase Inhibitors

A rapid and simple HPLC-UV method for the determination of inhibition characteristics of farnesyl transferase inhibitors

2006 ◽  
Vol 20 (2) ◽  
pp. 161-165 ◽  
Author(s):  
Natalie M. G. M. Appels ◽  
Kien-On Tung ◽  
Hilde Rosing ◽  
Jan H. M. Schellens ◽  
Jos H. Beijnen
Keyword(s):  
Farnesyl Transferase ◽  
Farnesyl Transferase Inhibitors

2P-0527 Farnesyl transferase inhibitors, by RAS P21 inactivation, induce stroke protection

2003 ◽  
Vol 4 (2) ◽  
pp. 155
Author(s):  
R. Patern ◽  
A. Ruocco ◽  
M.R. Santillo ◽  
R. Ser ◽  
G. Cuda ◽  
...  
Keyword(s):  
Farnesyl Transferase ◽  
Ras P21 ◽  
Farnesyl Transferase Inhibitors

scholarly journals Farnesyl transferase inhibitors induce extended remissions in transgenic mice with mature B cell lymphomas

2008 ◽  
Vol 7 (1) ◽  
pp. 39 ◽  
Author(s):  
Kenneth A Field ◽  
Soratree Charoenthongtrakul ◽  
J Michael Bishop ◽  
Yosef Refaeli
Keyword(s):  
Transgenic Mice ◽  
B Cell ◽  
B Cell Lymphomas ◽  
Farnesyl Transferase ◽  
Farnesyl Transferase Inhibitors

Controlled Exploration of Structural Databases: The Case of Farnesyl Transferase Inhibitors

2009 ◽  
Vol 5 (3) ◽  
pp. 208-215 ◽  
Author(s):  
A. Tizot ◽  
G. Tucker ◽  
A. Pierre ◽  
J. Hickman ◽  
S. Goldstein
Keyword(s):  
Farnesyl Transferase ◽  
Farnesyl Transferase Inhibitors ◽  
Structural Databases

scholarly journals K-Ras prenylation as a potential anticancer target

2020 ◽  
Vol 39 (4) ◽  
pp. 1127-1141 ◽  
Author(s):  
Marcell Baranyi ◽  
László Buday ◽  
Balázs Hegedűs
Keyword(s):  
Critical Evaluation ◽  
Current Data ◽  
Proper Function ◽  
Kras Mutations ◽  
Farnesyl Transferase ◽  
Factors Affecting ◽  
Mutational Status ◽  
Farnesyl Transferase Inhibitors ◽  
Potential Strategy ◽  
Sensitivity Data

AbstractKRAS is one of the most commonly mutated oncogene and a negative predictive factor for a number of targeted therapies. Therefore, the development of targeting strategies against mutant KRAS is urgently needed. One potential strategy involves disruption of K-Ras membrane localization, which is necessary for its proper function. In this review, we summarize the current data about the importance of membrane-anchorage of K-Ras and provide a critical evaluation of this targeting paradigm focusing mainly on prenylation inhibition. Additionally, we performed a RAS mutation-specific analysis of prenylation-related drug sensitivity data from a publicly available database (https://depmap.org/repurposing/) of three classes of prenylation inhibitors: statins, N-bisphosphonates, and farnesyl-transferase inhibitors. We observed significant differences in sensitivity to N-bisphosphonates and farnesyl-transferase inhibitors depending on KRAS mutational status and tissue of origin. These observations emphasize the importance of factors affecting efficacy of prenylation inhibition, like distinct features of different KRAS mutations, tissue-specific mutational patterns, K-Ras turnover, and changes in regulation of prenylation process. Finally, we enlist the factors that might be responsible for the large discrepancy between the outcomes in preclinical and clinical studies including methodological pitfalls, the incomplete understanding of K-Ras protein turnover, and the variation of KRAS dependency in KRAS mutant tumors.

Farnesyl Transferase Inhibitors in Cancer

2007 ◽  
pp. 85-102
Author(s):  
Laura Fanucchi ◽  
Michael Fanucchi ◽  
Fadlo Khuri
Keyword(s):  
Farnesyl Transferase ◽  
Farnesyl Transferase Inhibitors
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