• Journal of the Society of Cosmetic Scientists of Korea
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• v.30 no.3 s.47
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• pp.405-408
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• 2004

Several hydroxamic acid derivatives are synthesized to observe retinoidal effect and transactivation potential for $RAR{\alpha}/{\gamma]$ is screened. Among the synthesized compounds, N-(4-N-hydroxycarbamoyl )phenyl) [4-(tert-butyl )phenyl] carboxamide (2f) showed the best compatibility for potent $RAR{\alpha}/{\gamma].$ The acidic hydroxy of hydroxamic acid was easily deprotonated to form an enolate. A formed enolate has a similar role like that of all-trans-retinoic acid. This is the first example of the hydroxamic acid derivative with retinoidal activity. The retinoidal activity of 2f was further confirmed by enhancing activity for the expression of retinoid-responsive genes. To evaluate the possibility for anti.-aging agent, effect on the expression of MMP-1 was measured comparing with all-trans-retinoic acid and retinol. At 10 uM treatment, compound 2f inhibited the expression of MMP-1. These results suggest that new hydroxamic acid derivative 2f could be used as a promising anti-aging agent.

• Nuclear Medicine and Molecular Imaging
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• v.41 no.5
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• pp.343-349
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• 2007

Radioiodide transport has been extensively and successfully used in the evaluation and management of thyroid disease. The molecular characterization of the sodium/iodide symporter (NIS) and cloning of the NIS gene has led to the recent expansion of the use of radioiodide to cancers of the breast and other nonthyroidal tissues exogenously transduced with the NIS gene. More recently, discoveries regarding the functional analysis and regulatory processes of the NIS molecule are opening up exciting opportunities for new research and applications for NIS and radio iodide. The success of NIS based cancer therapy is dependent on achievement of maximal radioiodide transport sufficient to allow delivery of effective radiation doses. This in turn relies on high transcription rates of the NIS gene. However, newer discoveries indicate that nontranscriptional processes that regulate NIS trafficking to cell membrane are also critical determinants of radioiodide uptake. In this review, molecular mechanisms that underlie regulation of NIS transcription and stimuli that augment membrane trafficking and functional activation of NIS molecules will be discussed. A better understanding of how the expression and cell surface targeting of NIS proteins is controlled will hopefully aid in optimizing NIS gene based cancer treatment as well as NIS based reporter-gene imaging strategies.