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#32454443   2020/05/23 To Up

A Dodecapeptide Selected by Phage Display as a Potential Theranostic Probe for Colon Cancers.

Colon cancer is one of the leading causes of cancer-related mortality. However, specific biomarkers for its diagnosis or treatment are not established well.
Moon Hwa Kwak, Gawon Yi, Seung Mok Yang, Younghee Choe, Sangkee Choi, Hye-Soo Lee, Eunha Kim, Yong-Beom Lim, Kun Na, Myung-Gyu Choi, Heebeom Koo, Jae Myung Park

2210 related Products with: A Dodecapeptide Selected by Phage Display as a Potential Theranostic Probe for Colon Cancers.

1 kit100 assays100 plates100 plates1 kit10 plates10 plates50 assays1 kit96 Tests100 plates

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#32453578   2020/05/26 To Up

The balance between the hemostatic effect and immune response of hyaluronan conjugated with different chain lengths of inorganic polyphosphate.

Inorganic polyphosphate (PolyP) is a potential hemostatic material. However, the effect of PolyP chain length on the immune response and hemostatic function remains to be established. We have developed PolyP-conjugated hyaluronans (HA-PolyPs) with three different short-chain PolyPs (n = 13, 40, and 100 phosphate units). All short-chain PolyP showed biocompatibility in the cell viability and inflammatory cytokine secretion test in vitro and in vivo, wherein shorter PolyPs showed milder response in some cases. We then produced HA-PolyP hydrogels (HAX-PolyPs) with three different short-chain PolyPs as hemostats. Interestingly, in vivo biocompatibility and hemostatic activity of HAX-PolyP was not significantly affected by the length of conjugated PolyPs. HAX-PolyP with all chain length significantly decreased the amount of bleeding in a novel mouse liver bleeding model. These results indicated that the shortest PolyP (n = 13) induced milder acute inflammation and had an efficient hemostatic effect when conjugated to hyaluronic acid. The present study provides key insights into the design of PolyP-based biomaterials and bioconjugates, which are expected to grow in importance for various medical applications.
Masashi Okawa, Megumu Sakoda, Seiichi Ohta, Kiyoshi Hasegawa, Yutaka Yatomi, Taichi Ito

1117 related Products with: The balance between the hemostatic effect and immune response of hyaluronan conjugated with different chain lengths of inorganic polyphosphate.

2000 IU1100ug Lyophilized100.00 ul100ug Lyophilized500 Units100ug Lyophilized10

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#32453319   2020/05/26 To Up

Mitochondria-targeted artesunate conjugated cyclometalated iridium(iii) complexes as potent anti-HepG2 hepatocellular carcinoma agents.

Hepatocellular carcinoma (HCC) poses a serious threat to people's health worldwide. Artesunate (ART), one of the classical antimalarial drugs, has recently been shown to exert significant cytotoxicity in various cancers, but its bioavailability is low. Cyclometalated iridium(iii) complexes have emerged as a promising class of anticancer therapeutic agents. Herein, through conjugation of two of them, three novel Ir(iii)-ART conjugates, [Ir(C-N)2(bpy-ART)](PF6) (bpy = 2,2'-bipyridine, C-N = 2-phenylpyridine (ppy, Ir-ART-1), 2-(2-thienyl)pyridine (thpy, Ir-ART-2), and 2-(2,4-difluorophenyl)pyridine (dfppy, Ir-ART-3)) have been synthesized, and their potential as anti-HCC agents was evaluated. We demonstrate that Ir-ART-1-3 display higher cytotoxicity against HCC cell lines than normal liver cells, and they can especially locate to mitochondria of HepG2 cells and induce a series of mitochondria-mediated apoptosis events. Moreover, Ir-ART-1-3 can regulate the cell cycle and inhibit metastasis of HepG2 cells. Finally, in vivo antitumor evaluation also demonstrates the inhibitory activity of Ir-ART-1 on tumor growth. Taken together, these Ir(iii)-ART conjugates have the potential to become drug candidates for future anti-HCC treatments.
Rui-Rong Ye, Wan Peng, Bi-Chun Chen, Ning Jiang, Xuan-Qin Chen, Zong-Wan Mao, Rong-Tao Li

1086 related Products with: Mitochondria-targeted artesunate conjugated cyclometalated iridium(iii) complexes as potent anti-HepG2 hepatocellular carcinoma agents.

100ug Lyophilized100ug100ug Lyophilized100 μl100ug Lyophilized100ug100ug Lyophilized100ug Lyophilized100ug Lyophilized100ug Lyophilized100ug Lyophilized100ug Lyophilized

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#32452650   2020/05/26 To Up

Design and synthesis of fluorescent-methylphenidate analogues for FRET-based assay of Synapsin III binding.

We previously described Synapsin III (Syn III) as a synaptic phosphoprotein that controls dopamine release in cooperation with alpha-synuclein (aSyn). Moreover, we found that in Parkinson's disease (PD), Syn III also participates in alpha-synuclein (aSyn) aggregation and toxicity. Our recent observations point to threo -methylphenidate (MPH), a monoamine reuptake inhibitor that efficiently counteracts the freezing gait characteristic of advanced PD, as a ligand for Syn III. Here, we designed and synthesized two different fluorescently-labelled MPH derivatives, one with Rhodamine Red (RHOD) and one with 5-Carboxytetramethylrhodamine (TAMRA), to be used for assessing MPH binding to Syn III by fluorescence resonance energy transfer (FRET). TAMRA-MPH exhibited the ideal characteristics to be used as a FRET acceptor, as it was able to enter into the SK-N-SH cells and could interact specifically with human green fluorescent protein (GFP)-tagged Syn III but not with GFP alone. Moreover, uptake of TAMRA-MPH and co-localization with Syn III was also observed in primary mesencephalic neurons. These findings support that MPH is a Syn III ligand and that TAMRA-conjugated drug molecules may represent valuable tools to study drug-ligand interactions by FRET or to detect Syn III in cytological and histological samples.
Andrea Casiraghi, Francesca Longhena, Valentina Straniero, Gaia Faustini, Amy H Newman, Arianna Bellucci, Ermanno Valoti

1259 related Products with: Design and synthesis of fluorescent-methylphenidate analogues for FRET-based assay of Synapsin III binding.

25 Tests100Tests96 assays 25 Tests1 kit25 Tests100 tests

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#32452579   2020/05/26 To Up

Enhancing the Activity of Drugs by Conjugation to Organometallic Fragments.

Resistance to chemotherapy is a current clinical problem, especially in the treatment of microbial infections and cancer. One strategy to overcome this is to make new derivatives of existing drugs by conjugation to organometallic fragments, either by an appropriate linker, or by direct coordination of the drug to a metal. We illustrate this with examples of conjugated organometallic metallocene sandwich and half-sandwich complexes, Ru and Os arene, and Rh and Ir cyclopentadienyl half-sandwich complexes. Ferrocene conjugates are particularly promising. The ferrocene-chloroquine conjugate ferroquine is in clinical trials for malaria treatment, and a ferrocene-tamoxifen derivative (a ferrocifen) seems likely to enter anticancer trails soon. Several other examples illustrate that organometallic conjugation can restore the activity of drugs to which resistance has developed.
Prinessa Chellan, Peter J Sadler

1105 related Products with: Enhancing the Activity of Drugs by Conjugation to Organometallic Fragments.

1 kit1 kit100ug Lyophilized100.00 ug1mg96 wells 96 Tests 100

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#32452474   2020/05/26 To Up

Comparative study of α-helical and β-sheet self-assembled peptide nanofiber vaccine platforms: influence of integrated T-cell epitopes.

Several different self-assembling peptide systems that form nanofibers have been investigated as vaccine platforms, but design principles for adjusting the character of the immune responses they raise have yet to be well articulated. Here we compared the immune responses raised by two structurally dissimilar peptide nanofibers, one a β-sheet fibrillar system (Q11), and one an α-helical nanofiber system (Coil29), hypothesizing that integrated T-cell epitopes within the latter would promote T follicular helper (Tfh) cell engagement and lead to improved antibody titers and quality. Despite significantly different internal structures, nanofibers of the two peptides exhibited surprisingly similar nanoscale morphologies, and both were capable of raising strong antibody responses to conjugated peptide epitopes in mice without adjuvant. Both were minimally inflammatory, but as hypothesized Coil29 nanofibers elicited antibody responses with higher titers and avidities against a conjugated model epitope (OVA323-339) and a candidate peptide epitope for vaccination against S. aureus. Subsequent investigation indicated that Coil29 nanofibers possessed internal CD4+ T cell epitopes: whereas Q11 nanofibers required co-assembly of additional CD4+ T cell epitopes to be immunogenic, Coil29 nanofibers did not. Coil29 nanofibers also raised stronger germinal center B cell responses and follicular helper T cell (Tfh) responses relative to Q11 nanofibers, likely facilitating the improvement of the antibody response. These findings illustrate design strategies for improving humoral responses raised by self-assembled peptide nanofibers.
Yaoying Wu, Sean H Kelly, Luis Sanchez-Perez, John H Sampson, Joel H Collier

2587 related Products with: Comparative study of α-helical and β-sheet self-assembled peptide nanofiber vaccine platforms: influence of integrated T-cell epitopes.

10 ug96 tests1 mg 5 G1 mg5 mg96 assays1.00 flask50 ug

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#32452101   2020/05/25 To Up

Molecular spring-like triple-helix coordination polymers as dual stress and thermally responsive crystalline metal-organic materials.

Herein we present a new kind of elastic metal-organic materials (MOMs) that are capable of multiple stimuli-responsiveness based on dual stress and thermally responsive triple-helix coordination polymers. The strong metal-coordination linkage in combination with the flexibility of organic linkers in these MOMs,  rather than the '4 Å' stacking interactions observed in organic crystals, renders the helical chain to be act like a molecular spring and thus accounts for their intriguing macroscopic elasticity. Moreover, the thermosalient effect of elastic MOMs is reported for the first time here. Crystal structure analyses at different temperatures reveal that this thermo-responsiveness is achieved through adaptive regulation of the triple-helix chains via fine-tuning of opening angle of flexible 'V'-shaped organic linkers as well as rotation of its lateral conjugated groups so as to resist the possible expansion, thus demonstrating the vital role of adaptive reorganization of triple-helix metal-organic chain as a molecular spring-like motif in crystal jumping.
Lei Mei, Shu-Wen An, Kong-Qiu Hu, Lin Wang, Ji-Pan Yu, Zhi-Wei Huang, Xiang-He Kong, Chuan-Qin Xia, Zhi-Fang Chai, Wei-Qun Shi

1285 related Products with: Molecular spring-like triple-helix coordination polymers as dual stress and thermally responsive crystalline metal-organic materials.

1 kit1100 tests400 assays510ml 100 G1 kit1 kit96 reactions96

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