Lonafarnib - CAS 193275-84-2
Catalog number:
193275-84-2
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
COA:
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Targets:
Farnesyl Transferase
Description:
Lonafarnib is a farnesyl transferase inhibitor. Structurely,  it is also a synthetic tricyclic derivative of carboxamide with antineoplastic properties. Lonarfanib binds to and inhibits farnesyl transferase, an enzyme involved in the post-translational modification and activation of Ras proteins. Ras proteins participate in numerous signalling pathways (proliferation, cytoskeletal organization), and play an important role in oncogenesis. Mutated ras proteins have been found in a wide range of human cancers.
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Appearance:
white solid powder
Synonyms:
SCH 66336, SCH66336, SCH-66336.
MSDS:
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Current Developer:
Schering-Plough Corporation.
1.Oral prenylation inhibition with lonafarnib in chronic hepatitis D infection: a proof-of-concept randomised, double-blind, placebo-controlled phase 2A trial.
Koh C1, Canini L2, Dahari H3, Zhao X4, Uprichard SL5, Haynes-Williams V6, Winters MA7, Subramanya G5, Cooper SL8, Pinto P9, Wolff EF10, Bishop R11, Ai Thanda Han M6, Cotler SJ5, Kleiner DE12, Keskin O13, Idilman R13, Yurdaydin C13, Glenn JS7, Heller T14. Lancet Infect Dis. 2015 Oct;15(10):1167-74. doi: 10.1016/S1473-3099(15)00074-2. Epub 2015 Jul 16.
BACKGROUND: Therapies for chronic hepatitis delta virus (HDV) infection are unsatisfactory. Prenylation is essential for HDV and inhibition abrogates HDV production in experimental models. In a proof-of-concept study, we aimed to assess the effect on HDV RNA levels, safety, and tolerability of the prenylation inhibitor lonafarnib in patients with chronic delta hepatitis.
2.Progeria: a rare genetic premature ageing disorder.
Sinha JK, Ghosh S, Raghunath M1. Indian J Med Res. 2014 May;139(5):667-74.
Progeria is characterized by clinical features that mimic premature ageing. Although the mutation responsible for this syndrome has been deciphered, the mechanism of its action remains elusive. Progeria research has gained momentum particularly in the last two decades because of the possibility of revealing evidences about the ageing process in normal and other pathophysiological conditions. Various experimental models, both in vivo and in vitro, have been developed in an effort to understand the cellular and molecular basis of a number of clinically heterogeneous rare genetic disorders that come under the umbrella of progeroid syndromes (PSs). As per the latest clinical trial reports, Lonafarnib, a farnesyltranferase inhibitor, is a potent 'drug of hope' for Hutchinson-Gilford progeria syndrome (HGPS) and has been successful in facilitating weight gain and improving cardiovascular and skeletal pathologies in progeroid children. This can be considered as the dawn of a new era in progeria research and thus, an apt time to review the research developments in this area highlighting the molecular aspects, experimental models, promising drugs in trial and their implications to gain a better understanding of PSs.
3.2-Deoxy-D-glucose Sensitizes Cancer Cells to Barasertib and Everolimus by ROS-independent Mechanism(s).
Zhelev Z1, Ivanova D2, Aoki I3, Saga T3, Bakalova R4. Anticancer Res. 2015 Dec;35(12):6623-32.
The aim of the present study was to investigate: (i) the possibility of sensitizing cancer cells to anticancer drugs using the redox modulator 2-deoxy-D-glucose (2-DDG); (ii) to find such combinations with synergistic cytotoxic effect; (iii) and to clarify the role of reactive oxygen species (ROS) for induction of apoptosis and cytotoxicity through these combinations. The study covers 15 anticancer drugs--both conventional and new-generation. Four parameters were analyzed simultaneously in Jurkat leukemia cells, treated by drugs or 2-DDG (separately or in combination): cell viability, induction of apoptosis, levels of ROS, and level of protein-carbonyl products. Very well-expressed synergistic cytotoxic effects were found after 48-h treatment of Jurkat cells with 2-DDG in combination with: palbociclib, everolimus, lonafarnib, bortezomib, and barasertib. The synergistic cytotoxic effect of everolimus with 2-DDG was accompanied by very strong induction of apoptosis in cells, but a very strong reduction of ROS level.
4.Lonafarnib is a potential inhibitor for neovascularization.
Sun L1, Xie S2, Peng G2, Wang J2, Li Y2, Qin J2, Zhong D3. PLoS One. 2015 Apr 8;10(4):e0122830. doi: 10.1371/journal.pone.0122830. eCollection 2015.
Atherosclerosis is a common cardiovascular disease that involves the build-up of plaque on the inner walls of the arteries. Intraplaque neovacularization has been shown to be essential in the pathogenesis of atherosclerosis. Previous studies showed that small-molecule compounds targeting farnesyl transferase have the ability to prevent atherosclerosis in apolipoprotein E-deficient mice, but the underlying mechanism remains to be elucidated. In this study, we found that lonafarnib, a specific inhibitor of farnesyl transferase, elicits inhibitory effect on vascular endothelial capillary assembly in vitro in a dose-dependent manner. In addition, we showed that lonafarnib treatment led to a dose-dependent decrease in scratch wound closure in vitro, whereas it had little effect on endothelial cell proliferation. These data indicate that lonafarnib inhibits neovascularization via directly targeting endothelial cells and disturbing their motility.
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