Detail of "183506-66-3"

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PKCe is essential for gelsolin expression by histone deacetylase inhibitor apicidin in human cervix cancer cells

All Rights Reserved. PKCe is essential for gelsolin expression by histone deacetylase inhibitor apicidin in human cervix cancer cells. 488850-98-2 and 183506-66-3 are also occured in this study. Eun, Dae-Wook; Ahn, Seong Hoon; You, Jeong Soo; Park, Jong Woo; Lee, Eun Kyung; Lee, Hyun Nah; Kang, Gil Myoung; Lee, Jae Cheol; Choi, Wahn Soo; Seo, Dong-Wan; Han, Jeung-Whan (College of Pharmacy, Sungkyunkwan University, Suwon 440-746, S. Korea). Biochemical and Biophysical Research Communications, 354(3), 769-775 (English) 2007 Elsevier. CODEN: BBRCA9. ISSN: 0006-291X. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Down-regulation of gelsolin expression is assocd. with cellular transformation and induction of gelsolin exerts antitumorigenic effects. In this study, we show that protein kinase C (PKC) signaling pathway is required for the induction of gelsolin by the histone deacetylase inhibitor apicidin in HeLa cells. Apicidin induces gelsolin mRNA independently of the de novo protein synthesis. Inhibitor study has revealed that the PKC signaling pathway is involved in the gelsolin expression. Furthermore, inhibition of PKCe by either siRNA or dominant-neg. mutant completely abrogates the expression of gelsolin by apicidin, indicating that PKCe is the major isoform for this process. In parallel, apicidin induction of gelsolin is antagonized by the inhibition of Sp1 using dominant-neg. Sp1 or specific Sp1 inhibitor mithramycin, and inhibition of PKC leads to suppression of Sp1 promoter activity. Our results provide mechanistic insights into mol. mechanisms of gelsolin induction by apicidin. .

Preparation of apicidin derivatives with inhibiting histone deacetylase activity and cancer metastasis, pharmaceutical compositions

Preparation of apicidin derivatives with inhibiting histone deacetylase activity and cancer metastasis, pharmaceutical compositions. Moon, Aree (S. Korea ). Repub. Korean Kongkae Taeho Kongbo KR 2002045821 A 20 Jun 2002,No pp. given (Korean). (Korea, Republic Of). CODEN: KRXXA7. CLASS: ICM: C07D419-14. APPLICATION: KR 2000-75223 11 Dec 2000. DOCUMENT TYPE: Patent CA Section: 34 (Amino Acids, Peptides, and Proteins) Section cross-reference(s): 63 Provided are Apicidin derivs. which inhibit cell growth selectively, histone deacetylase(HDAC) activity concn. dependently and MMP-2 activity effectively. 183506-66-3 is also in the experiment. And, provided are pharmaceutical compns. contg. them and their use for the inhibition of HDAC and cancer metastasis. Apicidin deriv. is represented by the formula(1), wherein R is methoxy group; hydroxy group; C2-C6 dialkylamino group; C2-C6 linear or branched hydroxyalkyl; C3-C6 linear or branched dihydroxyalkyl group; C3-C6 alkoxyalkyl group; and substituted or unsubstituted 5 or 6 membered hetero cyclic compd. including 1-3 of hetero atoms selected among unsubstituted or C1-C3 alkyl group substituted N, O, and S. .