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91.
Ho Shin Kim Van-Hai Hoang Mannkyu Hong Kyung Chul Kim Jihyae Ann Cong-Truong Nguyen Ji Hae Seo Hoon Choi Jun Yong Kim Kyu-Won Kim Woong Sub Byun Sangkook Lee Seungbeom Lee Young-Ger Suh Jie Chen Hyun-Ju Park Tae-Min Cho Ji Young Kim Jeewoo Lee 《Bioorganic & medicinal chemistry》2019,27(7):1370-1381
On the basis of deguelin, a series of the B,C-ring truncated surrogates with N-substituted amide linkers were investigated as HSP90 inhibitors. The structure activity relationship of the template was studied by incorporating various substitutions on the nitrogen of the amide linker and examining their HIF-1α inhibition. Among them, compound 57 showed potent HIF-1α inhibition and cytotoxicity in triple-negative breast cancer lines in a dose-dependent manner. Compound 57 downregulated expression and phosphorylation of major client proteins of HSP90 including AKT, ERK and STAT3, indicating that its antitumor activity was derived from the inhibition of HSP90 function. The molecular modeling of 57 demonstrated that 57 bound well to the C-terminal ATP-binding pocket in the open conformation of the hHSP90 homodimer with hydrogen bonding and pi-cation interactions. Overall, compound 57 is a potential antitumor agent for triple-negative breast cancer as a HSP90 C-terminal inhibitor. 相似文献
92.
Song Mei Ling Kim Keun Tae Motamedi Gholam K. Cho Yong Won 《Sleep and biological rhythms》2019,17(4):447-454
Sleep and Biological Rhythms - Narcoleptics tend to have a low quality of life (QoL). Few studies have compared QoL in narcolepsy against other sleep disorders. The purpose of this study was to... 相似文献
93.
Li Yingnan Song Youngkeun Cho Donggil Han Zhen 《Landscape and Ecological Engineering》2019,15(3):265-276
Landscape and Ecological Engineering - Microclimates in urban areas arise through the interaction between prevailing weather conditions and landscape design parameters. A well-arranged landscape... 相似文献
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Mesenchymal stem cells (MSCs) have been shown to down-regulate T-cell responses. However, the mechanisms underlying remain unknown. In this study, we report that BALB/c bone marrow-derived MSCs inhibit the proliferation of allogeneic T-cells in mixed lymphocyte reactions (MLR), This inhibition is dependent on cell-cell contact, and do not induce apoptosis. Furthermore, cell-cycle analyses reveal that T-cells, in the presence of MSCs, are arrested in the G0/G1 phase through. The blockage of phosphorylation of retinoblastoma protein (Rb), mediated by the p16(INK4A)-cyclin D1/cdk4 complex and p21(waf1), p27(kip1)-cyclin E/cdk2 complex pathway. Our results suggest that MSCs may perform a crucial function in the maintenance of immune homeostasis, via direct regulation of the clonal expansion of activated T-cells. The novel T-cell regulatory mechanism exhibited by MSCs may prove useful in a variety of therapeutic applications. 相似文献
97.
XNP/ATRX, a causative gene of X-linked alpha-thalassemia/mental retardation syndrome, encodes an SNF2 family ATPase/helicase protein. To better understand the role of XNP/ATRX in development, we isolated and characterized a Drosophila XNP/ATRX homolog, dXNP, which contains highly conserved SNF2 and helicase domains. Ectopically expressed dXNP induced strong apoptosis in the developing eye and wing, but did not affect cell cycle progression or the expression of wingless and engrailed, essential regulators of development. The dXNP-induced apoptosis was strongly suppressed by DJNKK/hemipterous mutation, and dXNP increased JNK activity. Taken together, these results suggest that dXNP regulates apoptosis via JNK activation. 相似文献
98.
Winslow R. Briggs Tong-Seung Tseng Hae-Young Cho Trevor E. Swartz Stuart Sullivan Roberto A. Bogomolni Eirini Kaiserli John M. Christie 《植物学报(英文版)》2007,49(1):4-10
The phototropins phot1 and phot2 are plant blue-light receptors that mediate phototropism, chloroplast movements, stomatal opening, leaf expansion, the rapid Inhibition of hypocotyl growth in etiolated seedlings, and possibly solar tracking by leaves in those species in which It occurs. The phototroplns are plasma membrane-associated hydrophilic proteins with two chromophore domains (designated LOV1 and LOV2 for their resemblance to domains In other signaling proteins that detect light, oxygen, or voltage) in their Nterminal half and a classic serine/threonlne kinase domain in their C-terminal half. Both chromophore domains bind flavin mononucleotide (FMN) and both undergo light-activated formation of a covalent bond between a nearby cystelne and the C(4a) carbon of the FMN to form the signaling state. LOV2-cystelnyl adduct formation leads to the release downstream of a tightly bound amphlpathlc α-helix, a step required for activation of the klnase function. This cysteinyl adduct then slowly decays over a matter of seconds or minutes to return the photoreceptor chromophore modules to their ground state. Functional LOV2 is required for light-activated phosphorylation and for various blue-light responses mediated by the phototroplns. The function of LOV1 is still unknown, although It may serve to modulate the signal generated by LOV2. The LOV domain Is an ancient chromophore module found In a wide range of otherwise unrelated proteins In fungi and prokaryotes, the latter Including cyanobacterla, eubacterla, and archaea. Further general reviews on the phototropins are those by Celaya and Liscum (2005) and Christie and Briggs (2005). 相似文献
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High Performance Proteomics: 7th HUPO Brain Proteome Project Workshop March 7-9, 2007 Wellcome Trust Conference Centre, Hinxton, UK 总被引:1,自引:0,他引:1
Hamacher M Stephan C Eisenacher M Lewczuk P Wiltfang J Martens L Vizcaíno JA Kwon KH Yoo JS Park YM Beckers J Horsch M de Angelis MH Cho ZH Apweiler R Meyer HE 《Proteomics》2007,7(15):2490-2496
The Wellcome Trust Conference Centre at Hinxton, UK, was the meeting place of the 7th HUPO Brain Proteome Project Workshop entitled "High Performance Proteomics". It started on Wednesday, March 7, 2007 with a steering committee meeting followed by a two days series of talks dealing with the standardization and handling of tissues, body fluids as well as of proteomics data. The presentation and accompanying vivid discussions created a picture of actual strategies and standards in recent proteomics. 相似文献