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#34118790   2021/06/10 To Up

Characteristics and outcomes of cancer patients with covid-19 at a safety-net hospital.

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Muhammet Ozer, Suleyman Yasin Goksu, Mohammed Mahdi, Neel Gandhi

1569 related Products with: Characteristics and outcomes of cancer patients with covid-19 at a safety-net hospital.

5 mg5 g50 mg1 g100ul100ug

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#34118738   2021/04/01 To Up

How lockdown measures, during COVID-19 pandemic, matter on psoriatic patient's perception: Study on 600 patients on biologic therapy.

The outbreak of coronavirus disease-2019 (COVID-19) is a public health crisis of global proportion. In psoriatic patients treated with biologic agents, evidence is not yet available on susceptibility to infection with the novel SARS-CoV-2 coronavirus, and data about the perception of COVID-19 and its impact on these patients are lacking.
N Bernardini, N Skroza, A Spagnoli, A Marchesiello, V Balduzzi, E Tolino, A Mambrin, S Michelini, P Maddalena, S Volpe, I Proietti, A Vestri, C Potenza

1514 related Products with: How lockdown measures, during COVID-19 pandemic, matter on psoriatic patient's perception: Study on 600 patients on biologic therapy.

100ul100.00 ug 6 ml Ready-to-use 25 ml 1 g 2 ml 1 mg 25 ml Ready-to-use 6 ml 25 MG 2 ml

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#34118727   2021/05/23 To Up

Just "one of so many"? The pathologist Theodor Fahr (1877-1945) and his ambivalent relationship to National Socialism.

Theodor Fahr is well known as a pioneer in renal pathology and the eponym of "Fahr's disease". While his professional merits are undisputed, his relationship to National Socialism remains unclear. On the one hand, he signed the public "oath of allegiance" of German professors to Adolf Hitler, on the other hand, he appeared as a mentor to his Jewish colleague Paul Kimmelstiel. In 1945, Fahr committed suicide after being dismissed by the Allied military government for political reasons. However, he left behind memoirs in which he outlined himself as a determined opponent of National Socialism. It is precisely these ambiguities that form the starting point of this study. The aim is to reconstruct Fahr's personal and professional career and to outline his political stance in the Third Reich. In addition, it will be clarified how Fahr's life and work were received after 1945 and whether (or how) his relationship to National Socialism was addressed. This study is based on different types of sources: Various archival documents on Fahr and Kimmelstiel are compared and contrasted with Fahr's unpublished autobiography and the available secondary literature on Fahr and his work. The analysis shows that Fahr's relationship to National Socialism became more distanced over time. However, he did not emerge as a critic of Nazi ideology during the Third Reich - even though he claimed in his memoirs that he had consistently despised Hitler. While Fahr is not to be considered an ardent National Socialist, he held to the stereotype of the "unscrupulous" Jew. The study concludes that Fahr was a politically ambivalent character with a distinctly anti-Semitic disposition, which he tried to soften by emphasizing his relationships with individual Jewish colleagues such as Kimmelstiel.
Mila J Evers, Dominik Gross, Stephanie Kaiser

2020 related Products with: Just "one of so many"? The pathologist Theodor Fahr (1877-1945) and his ambivalent relationship to National Socialism.

100ul200 units 125 ml 100ul100 extractions 5 mg

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#34118724   2021/05/30 To Up

Improved SARS-CoV-2 M inhibitors based on feline antiviral drug GC376: Structural enhancements, increased solubility, and micellar studies.

Replication of SARS-CoV-2, the coronavirus causing COVID-19, requires a main protease (M) to cleave viral proteins. Consequently, M is a target for antiviral agents. We and others previously demonstrated that GC376, a bisulfite prodrug with efficacy as an anti-coronaviral agent in animals, is an effective inhibitor of M in SARS-CoV-2. Here, we report structure-activity studies of improved GC376 derivatives with nanomolar affinities and therapeutic indices >200. Crystallographic structures of inhibitor-M complexes reveal that an alternative binding pocket in M, S4, accommodates the P3 position. Alternative binding is induced by polar P3 groups or a nearby methyl. NMR and solubility studies with GC376 show that it exists as a mixture of stereoisomers and forms colloids in aqueous media at higher concentrations, a property not previously reported. Replacement of its Na counter ion with choline greatly increases solubility. The physical, biochemical, crystallographic, and cellular data reveal new avenues for M inhibitor design.
Wayne Vuong, Conrad Fischer, Muhammad Bashir Khan, Marco J van Belkum, Tess Lamer, Kurtis D Willoughby, Jimmy Lu, Elena Arutyunova, Michael A Joyce, Holly A Saffran, Justin A Shields, Howard S Young, James A Nieman, D Lorne Tyrrell, M Joanne Lemieux, John C Vederas

1025 related Products with: Improved SARS-CoV-2 M inhibitors based on feline antiviral drug GC376: Structural enhancements, increased solubility, and micellar studies.

100ug4X1.25ml; 200 reactions (100ug Lyophilized250ul200ul500 MG250ul100 25 TESTS/0.25ml1 g

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#34118723   2021/05/24 To Up

Design, synthesis, and biological evaluation of novel sulindac derivatives as partial agonists of PPARγ with potential anti-diabetic efficacy.

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Fengyu Huang, Zhiping Zeng, Weidong Zhang, Zhiqiang Yan, Jiayun Chen, Liangfa Yu, Qian Yang, Yihuan Li, Hongyu Yu, Junjie Chen, Caisheng Wu, Xiao-Kun Zhang, Ying Su, Hu Zhou

2648 related Products with: Design, synthesis, and biological evaluation of novel sulindac derivatives as partial agonists of PPARγ with potential anti-diabetic efficacy.

100μl100ug100ug Lyophilized100ug Lyophilized100ul100ug Lyophilized100ug100 ul

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#34118719   2021/06/02 To Up

The Mur Enzymes Chink in the Armour of Mycobacterium tuberculosis cell wall.

TUBERCULOSIS: (TB) transmitted by Mycobacterium tuberculosis (Mtb) is one of the top 10 causes of death globally. Currently, the widespread occurrence of resistance toward Mtb strains is becoming a significant concern to public health. This scenario exaggerated the need for the discovery of novel targets and their inhibitors. Targeting the "Mtb cell wall peptidoglycan synthesis" is an attractive strategy to overcome drug resistance. Mur enzymes (MurA-MurF) play essential roles in the peptidoglycan synthesis by catalyzing the ligation of key amino acid residues to the stem peptide. These enzymes are unique and confined to the eubacteria and are absent in humans, representing potential targets for anti-tubercular drug discovery. Mtb Mur ligases with the same catalytic mechanism share conserved amino acid regions and structural features that can conceivably exploit for the designing of the inhibitors, which can simultaneously target more than one isoforms (MurC-MurF) of the enzyme. In light of these findings in the current review, we have discussed the recent advances in medicinal chemistry of Mtb Mur enzymes (MurA-MurF) and their inhibitors, offering attractive multi-targeted strategies to combat the problem of drug-resistant in M. tuberculosis.
Yashodeep Shinde, Iqrar Ahmad, Sanjay Surana, Harun Patel

1084 related Products with: The Mur Enzymes Chink in the Armour of Mycobacterium tuberculosis cell wall.

1100ug Lyophilized

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#34118718   2021/06/02 To Up

Design, synthesis, and biological evaluation of furosemide analogs as therapeutics for the proteopathy and immunopathy of Alzheimer's disease.

β-Amyloid (Aβ) triggered proteopathic and immunopathic processes are a postulated cause of Alzheimer's disease (AD). Monomeric Aβ is derived from amyloid precursor protein, whereupon it aggregates into various assemblies, including oligomers and fibrils, which disrupt neuronal membrane integrity and induce cellular damage. Aβ is directly neurotoxic/synaptotoxic, but may also induce neuroinflammation through the concomitant activation of microglia. Previously, we have shown that furosemide is a known anthranilate-based drug with the capacity to downregulate the proinflammatory microglial M1 phenotype and upregulate the anti-inflammatory M2 phenotype. To further explore the pharmacologic effects of furosemide, this study reports a series of furosemide analogs that target both Aβ aggregation and neuroinflammation, thereby addressing the combined proteopathic-immunopathic pathogenesis of AD. Forty compounds were synthesized and evaluated. Compounds 3c, 3g, and 20 inhibited Aβ oligomerization; 33 and 34 inhibited Aβ fibrillization. 3g and 34 inhibited the production of TNF-α, IL-6, and nitric oxide, downregulated the expression of COX-2 and iNOS, and promoted microglial phagocytotic activity, suggesting dual activity against Aβ aggregation and neuroinflammation. Our data demonstrate the potential therapeutic utility of the furosemide-like anthranilate platform in the development of drug-like molecules targeting both the proteopathy and immunopathy of AD.
Zhiyu Wang, Yanfei Wang, Jagadeesh Prasad Pasangulapati, Kurt R Stover, Xiaojing Liu, Stephanie Wohnig Schier, Donald F Weaver

1918 related Products with: Design, synthesis, and biological evaluation of furosemide analogs as therapeutics for the proteopathy and immunopathy of Alzheimer's disease.

100ug96 tests50 ug 50 ug 1,000 tests100ug96 tests96T50 ug

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#34118715   2021/05/21 To Up

Experiences of stigma among individuals in recovery from opioid use disorder in a rural setting: A qualitative analysis.

Stigma is a barrier to accessing treatment and support services for individuals with substance use disorder. Stigma is negatively associated with completion of treatment for substance use disorder and management of recovery.
Amanda Burgess, Emily Bauer, Shane Gallagher, Brianne Karstens, LeeAnna Lavoie, Katherine Ahrens, Alane O'Connor

1091 related Products with: Experiences of stigma among individuals in recovery from opioid use disorder in a rural setting: A qualitative analysis.

1 mg100 μg100ug Lyophilized100 μg100ug100 μg100ug100 μg100ug Lyophilized 1 G1 Set

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#34118691   2021/06/09 To Up

Anti-tumor effects of rigosertib in high-risk neuroblastoma.

High-risk neuroblastoma has a poor prognosis despite intense treatment, demonstrating the need for new therapeutic strategies. Here we evaluated the effects of rigosertib (ON-01910.Na) in preclinical models of high-risk neuroblastoma. Among several hundred cancer cell lines representing 24 tumor types, neuroblastoma was the most sensitive to rigosertib. Treatment of MYCN-amplified neuroblastoma organoids resulted in organoid disintegration, decreased cell viability, and increased apoptotic cell death. Neuroblastoma response to rigosertib involved G2M cell cycle arrest and decreased phosphorylation of AKT (Ser473) and ERK1/2 (Thr202/Tyr204). Rigosertib delayed tumor growth and prolonged survival of mice carrying neuroblastoma MYCN-amplified PDX tumors (median survival: 31 days, treated; 22 days, vehicle) accompanied with increased apoptosis in treated tumors. We further identified vincristine and rigosertib as a potential promising drug combination treatment. Our results show that rigosertib might be a useful therapeutic agent for MYCN-amplified neuroblastomas, especially in combination with existing agents.
Katarzyna Radke, Karin Hansson, Jonas Sjölund, Magdalena Wolska, Jenny Karlsson, Javanshir Esfandyari, Kristian Pietras, Kristina Aaltonen, David Gisselsson, Daniel Bexell

1711 related Products with: Anti-tumor effects of rigosertib in high-risk neuroblastoma.



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