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Open AccessJournal ArticleDOI

BD750, a benzothiazole derivative, inhibits T cell proliferation by affecting the JAK3/STAT5 signalling pathway.

TLDR
A series of benzothiazole derivatives were screened for Immunosuppressive activity and BD750 was found to be the most effective immunosuppressant.
Abstract
Background and Purpose A series of benzothiazole derivatives were screened for immunosuppressive activity; of these compounds BD750 was found to be the most effective immunosuppressant. The purpose of the current study was to determine the immunosuppressive activity of BD750 on T cell proliferation and its potential mode of action.

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Scopariusicides, Novel Unsymmetrical Cyclobutanes: Structural Elucidation and Concise Synthesis by a Combination of Intermolecular [2 + 2] Cycloaddition and C-H Functionalization

TL;DR: A concise stereocontrolled synthesis of scopariusicide A and its analogues with enhanced biological activities was efficiently achieved using the main diterpenoid isolated from this plant as a readily available starting material.
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Scopariusic acid, a new meroditerpenoid with a unique cyclobutane ring isolated from Isodon scoparius.

TL;DR: Scopariusic acid, a new ent-clerodane-based meroditerpenoid with a unique cyclobutane ring and an unusual 1-octen-3-ol substituent, together with its biosynthetic related compound 2, were isolated from the aerial parts of Isodon scoparius.
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Nitrogen-Containing Dihydro-β-agarofuran Derivatives from Tripterygium wilfordii

TL;DR: Tripterygiumine Q (26) exhibited immunosuppressive activity against human peripheral mononuclear cells with an IC50 value of 8.67 μM and showed no cytotoxicity, even at 100 μM, indicating that 26 may represent a novel scaffold for the development of new Immunosuppressants.
Journal ArticleDOI

Benwamycins A–G, Trialkyl-Substituted Benzene Derivatives from a Soil-Derived Streptomyces

TL;DR: Seven new trialkyl-substituted benzene derivatives named benwamycins A-G (1-7), together with three known congeners, 8-10, were isolated from culture broth of the soil-derived Streptomyces sp.
Journal ArticleDOI

K313, a novel benzoxazole derivative, exhibits anti-inflammatory properties via inhibiting GSK3β activity in LPS-induced RAW264.7 macrophages.

TL;DR: Investigation of the anti‐inflammatory properties and the underlying molecular mechanism of K313 in lipopolysaccharide (LPS)‐induced RAW264.7 macrophages indicated that K313 exhibited anti‐ inflammation properties and revealed the potential mechanism.
References
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Journal ArticleDOI

Calcineurin is a common target of cyclophilin-cyclosporin A and FKBP-FK506 complexes

TL;DR: The results suggest that calcineurin is involved in a common step associated with T cell receptor and IgE receptor signaling pathways and that cyclophilin and FKBP mediate the actions of CsA and Fk506 by forming drug-dependent complexes with and altering the activity of calcineURin-calmodulin.
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A mammalian protein targeted by G1-arresting rapamycin–receptor complex

TL;DR: A mammalian FKBP–rapamycin-associated protein (FRAP) is isolate whose binding to structural variants of rapamycin complexed to FK BP12 correlates with the ability of these ligands to inhibit cell-cycle progression.
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Animal Research: Reporting in vivo Experiments—The ARRIVE Guidelines:

TL;DR: The following guidelines are excerpted (as permitted under the Creative Commons Attribution License (CCAL), with the knowledge and approval of PLoS Biology and the authors) from Kilkenny et al.
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Guidelines for reporting experiments involving animals: the ARRIVE guidelines

TL;DR: An editorial summarizes the background to the ‘ARRIVE’ guidelines, gives the view of their significance, considers aspects of specific relevance to pharmacology, re‐states BJP's guidelines for authors on animal experiments and indicates the commitment to carrying on discussion of this important topic.
Journal ArticleDOI

Fibroblast-like synoviocytes: key effector cells in rheumatoid arthritis

TL;DR: Rheumatoid FLS develop a unique aggressive phenotype that increases invasiveness into the extracellular matrix and further exacerbates joint damage, and new agents that target FLS could potentially complement the current therapies without major deleterious effect on adaptive immune responses.
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