Enhancing FTS (Salirasib) efficiency via combinatorial treatment
Identifieur interne : 000F58 ( Main/Exploration ); précédent : 000F57; suivant : 000F59Enhancing FTS (Salirasib) efficiency via combinatorial treatment
Auteurs : Eya Wolfson [Israël] ; Eran Schmukler [Israël] ; Sari Trangle Schokoroy [Israël] ; Yoel Kloog [Israël] ; Ronit Pinkas-Kramarski [Israël]Source :
- Biology of the Cell [ 0248-4900 ] ; 2015-05.
Abstract
The Ras oncogene transmits signals, which regulate various cellular processes including cell motility, differentiation, growth and death. Since Ras signalling is abnormally activated in more than 30% of human cancers, Ras and its downstream signalling pathways are considered good targets for therapeutic interference. Ras is post‐translationally modified by the addition of a farnesyl group, which permits its attachment to the plasma membrane. Exploiting this knowledge, a synthetic Ras inhibitor, S‐trans, trans‐farnesylthiosalicylic acid (FTS; Salirasib), was developed. FTS resembles the farnesylcysteine group of Ras, and acts as an effective Ras antagonist. In the present review, the effect of FTS in combination with various other drugs, as tested in vitro and in vivo, and its therapeutic potential are discussed. As reviewed, FTS cooperates with diverse therapeutic agents, which significantly improves treatment outcome. Therefore, combinations of FTS with other agents have a potential to serve as anti‐cancer or anti‐inflammatory therapies.
The small G‐protein Ras transmits signals regulating proliferation and is activated in more than 30% of human cancers. The present review describes studies on the effects of the synthetic Ras inhibitor, S‐trans, trans‐farnesylthiosalicylic acid (FTS), in combination with various other drugs and the therapeutic potential of these combined treatments. As discussed, combinations of FTS with other agents are significantly more effective and therefore have a therapeutic potential.
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DOI: 10.1111/boc.201400087
Affiliations:
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<front><div type="abstract">The Ras oncogene transmits signals, which regulate various cellular processes including cell motility, differentiation, growth and death. Since Ras signalling is abnormally activated in more than 30% of human cancers, Ras and its downstream signalling pathways are considered good targets for therapeutic interference. Ras is post‐translationally modified by the addition of a farnesyl group, which permits its attachment to the plasma membrane. Exploiting this knowledge, a synthetic Ras inhibitor, S‐trans, trans‐farnesylthiosalicylic acid (FTS; Salirasib), was developed. FTS resembles the farnesylcysteine group of Ras, and acts as an effective Ras antagonist. In the present review, the effect of FTS in combination with various other drugs, as tested in vitro and in vivo, and its therapeutic potential are discussed. As reviewed, FTS cooperates with diverse therapeutic agents, which significantly improves treatment outcome. Therefore, combinations of FTS with other agents have a potential to serve as anti‐cancer or anti‐inflammatory therapies.</div>
<div type="abstract" xml:lang="en">The small G‐protein Ras transmits signals regulating proliferation and is activated in more than 30% of human cancers. The present review describes studies on the effects of the synthetic Ras inhibitor, S‐trans, trans‐farnesylthiosalicylic acid (FTS), in combination with various other drugs and the therapeutic potential of these combined treatments. As discussed, combinations of FTS with other agents are significantly more effective and therefore have a therapeutic potential.</div>
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