2009
DOI: 10.3892/ijmm_00000274
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Novel synthetic inhibitors of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase activity that inhibit tumor cell proliferation and are structurally unrelated to existing statins

Abstract: Abstract. Pilot-scale libraries of eight-membered medium ring lactams (MRLs) and related tricyclic compounds (either seven-membered lactams, thiolactams or amines) were screened for their ability to inhibit the catalytic activity of human recombinant 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase in vitro. A dozen of the synthetic compounds mimic the inhibition of purified HMG-CoA reductase activity caused by pravastatin, fluvastatin and sodium salts of lovastatin, mevastatin and simvastatin in this… Show more

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Cited by 20 publications
(17 citation statements)
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References 41 publications
(47 reference statements)
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“…For the standardization of the protocol, preliminary screening of pravastatin was done against HMG-COA reductase activity and observed 50% inhibition at 70.25 nM, which was in concordance with other studies [43]. From the data presented in Table 2 and Figure 3(a), it is evident that FPBA (IC 50 = 9.1 ± 0.61  μ g/mL), FPLE (IC 50 = 27 ± 1.21  μ g/mL), FPBD (IC 50 = 30 ± 1.51  μ g/mL), FPBE (IC 50 = 35 ± 1.84  μ g/mL), FPLH (IC 50 = 38 ± 1.86  μ g/mL), FPBM (IC 50 = 45 ± 2.13  μ g/mL), FPLD (IC 50 = 58 ± 3.21  μ g/mL), and FPLM (IC 50 = 65 ± 3.42  μ g/mL) extracts exhibited significant inhibition of HMG-CoA reductase activity, while other extracts were found to be nonsignificant.…”
Section: Resultssupporting
confidence: 88%
“…For the standardization of the protocol, preliminary screening of pravastatin was done against HMG-COA reductase activity and observed 50% inhibition at 70.25 nM, which was in concordance with other studies [43]. From the data presented in Table 2 and Figure 3(a), it is evident that FPBA (IC 50 = 9.1 ± 0.61  μ g/mL), FPLE (IC 50 = 27 ± 1.21  μ g/mL), FPBD (IC 50 = 30 ± 1.51  μ g/mL), FPBE (IC 50 = 35 ± 1.84  μ g/mL), FPLH (IC 50 = 38 ± 1.86  μ g/mL), FPBM (IC 50 = 45 ± 2.13  μ g/mL), FPLD (IC 50 = 58 ± 3.21  μ g/mL), and FPLM (IC 50 = 65 ± 3.42  μ g/mL) extracts exhibited significant inhibition of HMG-CoA reductase activity, while other extracts were found to be nonsignificant.…”
Section: Resultssupporting
confidence: 88%
“…Currently, generic statins offer several cost benefits. These inhibitors of the posttranscriptional lipid modifications of RAS are likely to be effective, because they have been shown to exert antitumoral action in different cancer cells with mutations on RAS (125,126). Indeed, statins reduced cardiac hypertrophy in a transgenic model of HCM (127,128).…”
Section: Future Directions For Therapymentioning
confidence: 99%
“…Many researches focused on the ability of MVN and other statins to sensitize tumor cells for conventional chemotherapeutics 11 . Some experimental reports manifested a potential anti-cancer activity of MVN and other HMGCo-A reductase inhibitors per se 12 . However, the exact signaling mechanism of MVNinduced cell death remain controversial.…”
Section: Introductionmentioning
confidence: 99%