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  • inhibitors
  • Introduction of an a-hydroxyl group in the alkynyl side chain caused a greater increase in antiaggregatory activity than either NECA or HE-NECA, resulting in the most potent inhibitors of platelet aggregation so far known in the nucleoside series. (unicam.it)
  • Lota, Rupinder K. , Olusanjo, Moniola S. , Dhanani, Sachin , Owen, Caroline P. and Ahmed, Sabbir (2008) Synthesis, biochemical evaluation and rationalisation of the inhibitory activity of a range of 4-hydroxyphenyl ketones as potent and specific inhibitors of the type 3 of 17[beta]-hydroxysteroid dehydrogenase (17[beta]-HSD3). (kingston.ac.uk)
  • Li S, Yao H, Xu J, Jiang S. Synthetic Routes and Biological Evaluation of Largazole and Its Analogues as Potent Histone Deacetylase Inhibitors. (mdpi.com)
  • We have investigated the common spice, turmeric, and have identified three curcuminoids, curcumin, demthoxycurcumin and bisdemethoxycurcumin, which were found to be potent inhibitors of sortase A. It is believed that sortase A inhibitors act as anti-infective agents and disrupt the pathogenesis of bacterial infections without affecting microbial viability. (usda.gov)
  • Identification of ponatinib and other known kinase inhibitors with potent MEKK2 inhibitory activity. (semanticscholar.org)
  • vivo
  • In vivo, RXDX-105 displays potent and dose dependent anti-tumor activity with significant tumor growth regressions in several patient derived xenograft models harboring RET-rearrangements. (aacrjournals.org)
  • Compounds having an appropriate balance between vasorelaxation and antiplatelet activity, if confirmed in vivo, deserve further development for the treatments of cardiovascular disorders. (unicam.it)
  • Here, we utilized bone marrow/liver/thymus humanized mice to evaluate the in vivo HIV-inhibitory activity of breast milk obtained from HIV-positive transmitting and nontransmitting mothers. (asm.org)
  • kinase
  • It increases levels of AMP-activated protein kinase (AMPK) phosphorylation, reduces activity of MAP kinases and decreases production of proinflammatory cytokines and chemokines. (selleckchem.com)
  • assays
  • The hydrophobicity index (k') of the new nucleosides barely correlated with the binding data, whereas high k' values were associated with increased A2 vs A1 selectivity but with reduced activity in all unctional assays. (unicam.it)
  • receptor
  • At the molecular level, insulin signaling activity was improved with an elevation in insulin-stimulated phosphorylation of insulin receptor substrate (IRS-1), Akt and GSK-3β. (frontiersin.org)
  • derivatives
  • From functional experiments the 4-hydroxy-l-butynyl(6) and the 4-(2-tetrahydro-2H-pyranyloxy)-l-butynyl (16) derivatives appear to be very potent in inducing vasorelaxation without appreciable effect on heart rate. (unicam.it)
  • Staphylococcus
  • The inhibitory activity of Curcuma longa L. (turmeric) rhizome constituents against sortase A, a bacterial surface protein anchoring transpeptidase, from Staphylococcus aureus ATCC 6538p was evaluated. (usda.gov)
  • phosphorylation
  • Similarly, in a mouse model of diet-induced obesity, ETC-1002 restores adipose AMPK activity, reduces JNK phosphorylation, and diminishes expression of macrophage-specific marker 4F/80 . (selleckchem.com)
  • lung
  • In addition, nintedanib has shown consistent anti-fibrotic and anti-inflammatory activity in animal models of lung fibrosis. (ersjournals.com)
  • greater
  • Fractionation of the supernatant by size and ion exchange chromatography demonstrated activity in the complete absence of RANTES as well as interferons-alpha, beta, and gamma and in a size range of less than 10 kD and greater than 3 kD. (duke.edu)
  • plant
  • To extract and analyze information on plant usage in such sources - which are largely unedited texts and so far have not been translated - we investigate (i) the relationship of the iatrosophia to Dioscorides' De Materia Medica as well as historic pharmaceutical books or standard texts on modern phytotherapy and (ii) the validity of the remedies by comparing them to modern scientific data on reported biological activities. (frontiersin.org)
  • herb
  • Matrine, one of the main components extracted from a traditional Chinese herb, Sophora flavescens has anti-cancer activity in an experimental model of metastatic breast cancer in mice. (greenmedinfo.com)
  • positive
  • In addition, while significant differences in breast milk composition between transmitting and nontransmitting HIV-positive mothers have been correlated with transmission risk, the HIV-inhibitory activity of their breast milk has not been compared. (asm.org)
  • Among the tested molecules, compound 18 exhibited potent inhibitory activity when compared to the Bavistine (Positive control). (omicsonline.org)