• Title/Summary/Keyword: Apicidin

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Synthesis and Evaluation of Biological activities of New Imine Derivatives of Apicidin

  • Jin, Cheng-Hua;Kim, Hyung-Kyo;Han, Jeong-Whan;Lee, Hyang-Woo;Lee, Yin-Won;Zee, Ok-Pyo;Jung, Young-Hoon
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.253.2-253.2
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    • 2002

  • Apicidin. a natural product HDAC inhibitor. is recently isolated from Fusarium sp. at Merk Research Laboratories, induces therapeutic applications as a broad spectrum antiprotozoal agent to muti-drug resistant malaria and a potential antitumor agent. The biological activity of apicidin appears to be apicocomplexan HDAC at low nanomolar concentrations. (omitted)

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Synthesis of new apicidin derivatives as Histone deacetylase(HDAC) inhibitors

  • H.O. Kang;C.H. Jin;J.W. Han;Lee, H.W.;Lee, Y.W.;Park, H.J.;O.P. Zee;Y.H. Jung
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 2001.11a
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    • pp.110-110
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    • 2001

  • Histone deacetylase(HDAC), a neuclear enzyme that regulates gene trascription and the assembly of newly synthesized chromatin, has received much attention in recent literature. The explosion of activity in this field has yielded the cloning of a mammalian gene which encodes a complementary histone acetyl trasferases. Several cyclic tetrapeptide inhibitors of HDAC has been reported to affect the hyperacetylation of mammalian and plant histones. Apicidin, a natural product HDAC inhibitor recently isolated at Merck Research Laboratories, induces therapeutic applications as a broad spectrum antiprotozoal agent to multi-drug resistant malaria and a potential antitumor agnet. The biological activity of apicidin appears to be attributable to inhibition of apicocomplexan HDAC at low nanomolar concentrations.

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Requirement of PI3K-PKC$\varepsilon$ Signaling Pathway for Apicidin Induction of p$21^{WAFl/Cip1}$

  • Kim, Yong-Kee;Cho, Eun-Jung;Lee, Hoi-Young;Han, Jeung-Whan;Lee, Hyang-Woo
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.144.1-144.1
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    • 2003

  • We previously reported that the activation of p$21^{WAFl/Cip1}$ transcription by histone deacetylase inhibitor apicidin was mediated through Spl sites and pointed to the possible participation of protein kinase C (PKC). In this study, we investigated the role and identity of the specific isoforms of PKC involved and identified phosphatidylinositol 3-kinase (PI 3-kinase) as an upstream effector in HeLa cells. Using an isoform-specific pharmacological inhibitor of PKC, a PKC$\varepsilon$ dominant-negative mutant, and antisense oligonucleotide to inhibit PKC$\varepsilon$ specifically, (omitted)

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Apicidin-induced gelsolin expression via Spl sites is mediated by PKC signaling

  • Eun, Dae-Wook;Cho, Eun-Jung;Lee, Hoi-Young;Hong, Sung-Youl;Han, Jeung-Whan;Lee, Hyang-Woo
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.150.1-150.1
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    • 2003

  • Gelsolin, a actin binding protein, has been demonstrated to be involved in controlling cell morphology, motility, signaling, and apoptosis. It's expression is frequently downregulated in cervix cancer and several types of different human cancers indicating the role of gesolin in suppression of tumorigenicity. Apicidin, a novel histone deacetylase inhibitor, has been shown to cause growth arrest and morphological change of cancer cells, resulting from the alternation of protein expression, such as p21^${WAF1/Cip1}$ and gelsolin. (omitted)

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