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Keum, Gyochang,Kang, Soon Bang,Kim, Youseung,Lee, Eun WILEY-VCH Verlag 2004 Chem Inform Vol.35 No.40
<P>For Abstract see ChemInform Abstract in Full Text.</P>
Kim, TaeHun,Keum, Gyochang,Pae, Ae Nim Informa UK, Ltd. 2013 Expert opinion on therapeutic patents Vol.23 No.8
<P><B><I>Introduction:</I></B> There has been research on anticancer strategies which focus on disrupting a single malignant protein. One of the strategies is the inhibition of one protein, heat shock protein 90 (Hsp90). There are many reasons why Hsp90 protein is targeted by anticancer agents: maintenance of cellular homeostasis in organisms involves Hsp90 and its client proteins; moreover, Hsp90 complex is involved in regulating several signal transduction pathways and plays an important role in the maturation of lots of tumor-promoting client proteins. Geldanamycin (GM), the first benzoquinone ansamycin, has shown anticancer activity by binding to Hsp90. Currently, several GM derivatives such as 17-AAG, 17-(2-dimethylaminoethyl)amino-17-demethoxygeldanamycin, IPI-493, and IPI-504 are being progressively developed toward clinical application.</P><P><B><I>Areas covered:</I></B> Several research groups have studied GM and its derivatives to develop novel and potent Hsp90 inhibitors for the treatment of cancer. The crystal structure of Hsp90 was utilized to undergo structural optimization of GM derivatives. A wide variety of structural modifications were performed and some of the derivatives are now in clinical studies. The aim of this review was to summarize and analyze the structure-activity relationships of GM derivatives and the focus is on patented novel and pharmaceutically efficacious derivatives published from 1971 to 2012.</P><P><B><I>Expert opinion:</I></B> Hsp90 inhibitors offer an effective therapeutic approach for treatment of cancer. To date, the clinical results of 17-AAG, IPI-493, and IPI-504 suggest that these GM derivatives could be used either alone or in combination with other marketed medications for the treatment of cancer patients. As there are not any marketed Hsp90 inhibitors, inhibiting Hsp90 chaperone function remains as a promising strategy that still requires further research.</P>
Huang Tianqi,Zhao Dong,Lee Sangbin,Keum Gyochang,Yang Hyun Ok 한국응용약물학회 2023 Biomolecules & Therapeutics(구 응용약물학회지) Vol.31 No.3
Sinapic acid (SA) is a phenolic acid that is widely distributed in fruits and vegetables, which has various bioactivities, such as antidiabetic, anticancer and anti-inflammatory functions. Over-activated microglial is involved in the development progress of neurodegenerative diseases, such as Parkinson’s disease and Alzheimer’s disease. The objective of this study was to investigate the effect of SA in microglia neuroinflammation models. Our results demonstrated that SA inhibited secretion of the nitric oxide (NO) and interleukin (IL)-6, reduced the expression of inducible nitric oxide synthase (iNOS) and enhanced the release of IL-10 in a dose-dependent manner. Besides, our further investigation revealed that SA attenuated the phosphorylation of AKT and MAPK cascades in LPS-induced microglia. Consistently, oral administration of SA in mouse regulated the production of inflammationrelated cytokines and also suppressed the phosphorylation of MAPK cascades and AKT in the mouse cerebral cortex. These results suggested that SA may be a possible therapy candidate for anti-inflammatory activity by targeting the AKT/MAPK signaling pathway.
Hong, Jin Ri,Choi, Young Jin,Keum, Gyochang,Nam, Ghilsoo Pergamon 2017 Bioorganic & medicinal chemistry Vol.25 No.17
<P><B>Abstract</B></P> <P>A novel series of fused-benzensulfonamide 2-<I>N</I>-(pyrazol-3-yl)methylbenzo[<I>d</I>]isothiazole-1,1-dioxide derivatives was designed and synthesized as metabolically stable T-type calcium channel inhibitors. Several compounds, <B>9</B>, <B>10</B>, and <B>17</B>, displayed potent T-type channel inhibitory activity. Among them, compounds <B>10</B> and <B>17</B> showed good metabolic stability in human liver microsomes, and low hERG channel and CYP450 inhibition. Compound <B>10</B> exhibited diabetic neuropathic pain-alleviating effects in a streptozotocin-induced peripheral diabetic neuropathy (PDN) model. The maximum efficacy of compound <B>10</B>, which was 3-fold more potent than gabapentin, was observed at 1h after administration, and co-administration of compound <B>10</B> with gabapentin showed a considerable synergic effect.</P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>