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#33652491   2021/03/02 To Up

Questions and Controversies in the Clinical Application of Tyrosine Kinase Inhibitors to Treat Patients with Radioiodine-Refractory Differentiated Thyroid Carcinoma: Expert Perspectives.

Notwithstanding regulatory approval of lenvatinib and sorafenib to treat radioiodine-refractory differentiated thyroid carcinoma (RAI-R DTC), important questions and controversies persist regarding this use of these tyrosine kinase inhibitors (TKIs). RAI-R DTC experts from German tertiary referral centers convened to identify and explore such issues; this paper summarizes their discussions. One challenge is determining when to start TKI therapy. Decision-making should be shared between patients and multidisciplinary caregivers, and should consider tumor size/burden, growth rate, and site(s), the key drivers of RAI-R DTC morbidity and mortality, along with current and projected tumor-related symptomatology, co-morbidities, and performance status. Another question involves choice of first-line TKIs. Currently, lenvatinib is generally preferred, due to greater increase in progression-free survival versus placebo treatment and higher response rate in its pivotal trial versus that of sorafenib; additionally, in those studies, lenvatinib but not sorafenib showed overall survival benefit in subgroup analysis. Whether recommended maximum or lower TKI starting doses better balance anti-tumor effects versus tolerability is also unresolved. Exploratory analyses of lenvatinib pivotal study data suggest dose-response effects, possibly favoring higher dosing; however, results are awaited of a prospective comparison of lenvatinib starting regimens. Some controversy surrounds determination of net therapeutic benefit, the key criterion for continuing TKI therapy: if tolerability is acceptable, overall disease control may justify further treatment despite limited but manageable progression. Future research should assess potential guideposts for starting TKIs; fine-tune dosing strategies and further characterize antitumor efficacy; and evaluate interventions to prevent and/or treat TKI toxicity, particularly palmar-plantar erythrodysesthesia and fatigue.
Frederik A Verburg, Holger Amthauer, Ina Binse, Ingo Brink, Andreas Buck, Andreas Darr, Christine Dierks, Christine Koch, Ute König, Michael C Kreissl, Markus Luster, Christoph Reuter, Klemens Scheidhauer, Holger Sven Willenberg, Andreas Zielke, Matthias Schott

2980 related Products with: Questions and Controversies in the Clinical Application of Tyrosine Kinase Inhibitors to Treat Patients with Radioiodine-Refractory Differentiated Thyroid Carcinoma: Expert Perspectives.

8 inhibitors5 inhibitors2 Pieces/Box

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#33652438   2021/03/02 To Up

Alternative Flicker Glass: a New Anti-suppression Approach to the Treatment of Anisometropic Amblyopia.

Amlyopia always presents with monocular and binocular dysfunction. In this study, we aim to investage the efficacy of alternative occlusion using liquid crystal glasses versus continuous occlusion therapy using traditional patches for treating amblyopia.
Ying Yuan, Chengcheng Zhu, Peng Wang, Xiaojun Hu, Wenbo Yao, Xinhui Huang, Bilian Ke

2661 related Products with: Alternative Flicker Glass: a New Anti-suppression Approach to the Treatment of Anisometropic Amblyopia.

100.00 ul0.2 mg100 0.1 mg100 μg100 1 mL0.1 mg

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#33652358   2021/02/12 To Up

Quality markers based on phytochemical analysis and anti-inflammatory screening: An integrated strategy for the quality control of Dalbergia odorifera by UHPLC-Q-Orbitrap HRMS.

Quality control, key for the clinical application of traditional Chinese medicines (TCMs), should be connected to the authentication and efficacy of TCMs. The heartwood of Dalbergia odorifera has been widely used to treat inflammation-related diseases. However, in the Chinese pharmacopeia, only the total volatile oil, which does not sufficiently reflect the clinical efficacy, is used as a quality control indicator.
Kang Sun, Chaonan Su, Wenjing Li, Zhao Gong, Chunjie Sha, Rongxia Liu

1632 related Products with: Quality markers based on phytochemical analysis and anti-inflammatory screening: An integrated strategy for the quality control of Dalbergia odorifera by UHPLC-Q-Orbitrap HRMS.

0.2 mg0.1 mg100ug100ug100ug100ug100 TESTS500 100 TESTS1 ml

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#33652352   2021/02/09 To Up

Discovery of pyrazolo-thieno[3,2-d]pyrimidinylamino-phenyl acetamides as type-II pan-tropomyosin receptor kinase (TRK) inhibitors: Design, synthesis, and biological evaluation.

Tropomyosin receptor kinase (TRK) represents an attractive oncology target for cancer therapy related to its critical role in cancer formation and progression. NTRK fusions are found to occur in 3.3% of lung cancers, 2.2% of colorectal cancers, 16.7% of thyroid cancers, 2.5% of glioblastomas, and 7.1% of pediatric gliomas. In this paper, we described the discovery of the type-II pan-TRK inhibitor 4c through the structure-based drug design strategy from the original hits 1b and 2b. Compound 4c exhibited excellent in vitro TRKA, TRKB, and TRKC kinase inhibitory activity and anti-proliferative activity against human colorectal carcinoma derived cell line KM12. In the NCI-60 human cancer cell lines screen, compound 4g demonstrated nearly 80% of growth inhibition for KM12, while only minimal inhibitory activity was observed for the remaining 59 cancer cell lines. Western blot analysis demonstrated that 4c and its urea cousin 4k suppressed the TPM3-TRKA autophosphorylation at the concentrations of 100 nM and 10 nM, respectively. The work presented that 2-(4-(thieno[3,2-d]pyrimidin-4-ylamino)phenyl)acetamides could serve as a novel scaffold for the discovery and development of type-II pan-TRK inhibitors for the treatment of TRK driven cancers.
Wei Yan, Lingtian Zhang, Fengping Lv, Marialuisa Moccia, Francesca Carlomagno, Christophe Landry, Massimo Santoro, Fabien Gosselet, Brendan Frett, Hong-Yu Li

1583 related Products with: Discovery of pyrazolo-thieno[3,2-d]pyrimidinylamino-phenyl acetamides as type-II pan-tropomyosin receptor kinase (TRK) inhibitors: Design, synthesis, and biological evaluation.

8 inhibitors5 Inhibitors5 inhibitors400Tests50 ug 50μl40 assays

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#33652342   2021/02/19 To Up

Design and synthesis of novel glycyrrhetin ureas as anti-inflammatory agents for the treatment of acute kidney injury.

To develop new anti-inflammatory drugs for the prevention and treatment of acute kidney injury, a series of novel glycyrrhetic ureas were designed, synthesized and evaluated for anti-inflammatory activity using RAW264.7 cells. Compounds 5r-5u (2.04, 2.50, 3.25 and 2.48 μM, respectively) with acidic or neutral amino acid showed potent anti-inflammatory activity (IC = 2-3 μM for NO inhibition), amongst them, compound 5r also inhibited tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6) in a dose-dependent manner. In cisplatin-induced AKI mice model, compound 5r significantly reduced the level of pro-inflammatory factors, ameliorated the pathological damage of kidney tissue, and maintained the normal metabolic capacity.
Hongbo Wang, Jiawei Zuo, Liang Zha, Xia Jiang, Caixia Wu, Yong-An Yang, Wenjian Tang, Tianlu Shi

2656 related Products with: Design and synthesis of novel glycyrrhetin ureas as anti-inflammatory agents for the treatment of acute kidney injury.

100ug Lyophilized100μl100ug Lyophilized100.00 ul100ug Lyophilized100ug100μl

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#33652341   2021/02/19 To Up

In-vitro and in-vivo monitoring of gold(III) ions from intermediate metabolite of sodium aurothiomalate through water-soluble ruthenium (II) complex-based luminescent probe.

Real-time monitoring of drug metabolism in vivo is of great significance to drug development and toxicology research. The purpose of this study is to establish a rapid and visual in vivo detection method for the detection of an intermediate metabolite of the gold (I) drug. Gold (I) drugs such as sodium aurothiomalate (AuTM) have anti-inflammatory effects in the treatment of rheumatoid arthritis. Gold(III) ions (Au) are the intermediate metabolite of gold medicine, and they are also the leading factor of side effects in the treatment of patients. However, the rapid reduction of Au to Au by thiol proteins in organisms limits the in-depth study of metabolism of gold drugs in vivo. Here we describe a luminescence Au probe (RA) based on ruthenium (II) complex for detecting Au in vitro and in vivo. RA with large Stokes shift, good water solubility and biocompatibility was successfully applied to detect Au in living cells and vivo by luminescence imaging, and to trap the fluctuation of Au level produced by gold (I) medicine. More importantly, the luminescent probe was used to the detection of the intermediate metabolites of gold (I) drugs for the first time. Overall, this work offers a new detection tool/method for a deeper study of gold (I) drugs metabolite.
Zhenzhen Xie, Jia Wen, Shaowei Sun, Jing Zhang, Xiling Deng, Shichao Han, Lixia Wang, Bo Zhang, Chenglin Hong, Shiguo Sun

1990 related Products with: In-vitro and in-vivo monitoring of gold(III) ions from intermediate metabolite of sodium aurothiomalate through water-soluble ruthenium (II) complex-based luminescent probe.

1L250ML 5 G

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#33652305   2021/02/10 To Up

In vitro synergy of ticarcillin/clavulanate in combination with aztreonam and ceftolozane/tazobactam against SPM-1-producing Pseudomonas aeruginosa strains.

Minimal inhibitory concentrations (MICs) of ticarcillin/clavulanic acid (TLc), ceftolozane/tazobactam (C/T), and aztreonam (AT) were determined for 6 SPM-1-producing Pseudomonas aeruginosa (PSA) using Etest® strips and the synergistic effect of such antimicrobials against was evaluated by gradient diffusion strip crossing (GDSC) test. The fraction inhibitory concentration indexes (FICI) were calculated and showed a synergistic (n = 3) and additive (n = 2) effects of TLc + AT against SPM-1 producers, while TLc + C/T combination caused no effect. Average MIC reduction of TLc and AT by GDSC was 3-fold and 2-fold dilutions, respectively. Thus, TLc + AT might be a candidate as a combination therapy to treat SPM-1-producing PSA infections.
Gerlan Rocha-Santos, Gabriel T Cuba, Rodrigo Cayô, Ana Paula Streling, Carolina S Nodari, Ana C Gales, Antonio C C Pignatari, David P Nicolau, Carlos R V Kiffer

2600 related Products with: In vitro synergy of ticarcillin/clavulanate in combination with aztreonam and ceftolozane/tazobactam against SPM-1-producing Pseudomonas aeruginosa strains.

0.1ml0.1ml0.1ml96 tests50 ug1mg10mg5mg

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#33652183   2021/02/11 To Up

Does the treatment of dried herbs with ozone as a fungal decontaminating agent affect the active constituents?

Herbs and spices are food crops susceptible to contamination by toxigenic fungi. Ozone, as a decontamination approach in the industry, has attractive benefits over traditional food preservation practices. A contribution to the studying of ozone as an antifungal and anti-mycotoxigenic agent in herbs and spices storage processes is achieved in this research. Nine powdered sun-dried herbs and spices were analyzed for their fungal contamination. The results indicate that licorice root and peppermint leaves were found to have the highest population of fungi while black cumin and fennel record the lowest population. The most dominant fungal genera are Aspergillus, Penicillium, Fusarium, and Rhizopus. Ozone treatment was performed at a concentration of 3 ppm applied for exposure times of 0, 30, 90, 150, 210, and 280 min. After 280 min of exposure to ozone, the reduction of fungal count ranged from 96.39 to 98.26%. The maximum reduction in spore production was achieved in the case of A. humicola and Trichderma viride exposed for 210 min ozone gas. There was a remarkable reduction in the production of the total mycotoxin, reaching 24.15% in aflatoxins for the 150 min-treated inoculum in the case of A. flavus. The total volume of essential oil of chamomile and peppermint was reduced by 57.14 and 26.67%, respectively, when exposed to 3 ppm. For 280 min. In conclusion, fumigation with ozone gas can be used as a suitable method for achieving sanitation and decreasing microbial load in herbs and spices. Still, it is crucial to provide precautions on ozone's effect on major active constituents before recommending this method for industrial application.
Salama A Ouf, Enas M Ali

2510 related Products with: Does the treatment of dried herbs with ozone as a fungal decontaminating agent affect the active constituents?

25 assays25 assays1 ml100 assays1 kit(96 Wells)25 assays0.1 mg100 assays100 assays1 ml

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#33651821   2021/03/02 To Up

IL-6 promotes MYC-induced B cell lymphomagenesis independent of STAT3.

The inflammatory cytokine IL-6 is known to play a causal role in the promotion of cancer, although the underlying mechanisms remain to be completely understood. Interplay between endogenous and environmental cues determines the fate of cancer development. The Eμ-myc transgenic mouse expresses elevated levels of c-Myc in the B cell lineage and develops B cell lymphomas with associated mutations in p53 or other genes linked to apoptosis. We generated Eμ-myc mice that either lacked the IL-6 gene, or lacked the STAT3 gene specifically in B cells to determine the role of the IL-6/JAK/STAT3 pathway in tumor development. Using the Eμ-myc lymphoma mouse model, we demonstrate that IL-6 is a critical tumor promoter during early stages of B cell lymphomagenesis. IL-6 is shown to inhibit the expression of tumor suppressors, notably BIM and PTEN, and this may contribute to advancing MYC-driven B cell tumorigenesis. Several miRNAs known to target BIM and PTEN are upregulated by IL-6 and likely lead to the stable suppression of pro-apoptotic pathways early during the tumorigenic process. STAT3, a classical downstream effector of IL-6, appears dispensable for Eμ-myc driven lymphomagenesis. We conclude that the growth-promoting and anti-apoptotic mechanisms activated by IL-6 are critically involved in Eμ-myc driven tumor initiation and progression, but the B cell intrinsic expression of STAT3 is not required.
Oleksi Petrenko, Jinyu Li, Velasco Cimica, Patricio Mena-Taboada, Ha Youn Shin, Stephen D'Amico, Nancy C Reich

1009 related Products with: IL-6 promotes MYC-induced B cell lymphomagenesis independent of STAT3.

100ul1 g25 ml.100ml25 mg1 mg100 tests100ug Lyophilized2.5 mg1 g5 g

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