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provides coniferyl ferulate(CAS#:28097-03-2) MSDS, density, melting point, boiling point, structure, formula, molecular weight etc. Articles of coniferyl ferulate are included as well.>> amp version: coniferyl ferulate
Background: Latent HIV-1 is a major hurdle in obtaining HIV-1 sustained virological remission (SVR). Here we explored histone deacetylation inhibition property of nicotinamide (NAM; n=17) for the first time in comparison to a combination of methyltransferase inhibitors (MTIs; Chaetocin and BIX01294; n=25) to reactivate latent HIV ex vivo in CD8-depleted PBMCs from antiretroviral treated aviremic individuals.
Results: NAM reactivated HIV-1 from 13/17 (76.4%) samples compared to 20/25 (80.0%) using MTIs with mean viral load (VLs) of 4.32 and 3.22 log10 RNA copies/mL, respectively (p=0.004). Mean purging time after NAM and MTIs stimulation was 5.1 and 6.75 days, respectively (p=0.73). Viral purging in autologous cultures exhibited blunted HIV recovery with fluctuating VLs followed by a complete viral extinction when expanded in allogenic system. Electron microscopy from five supernatants revealed anomalous viral particles, with lack of complete viral genomes when characterized by ultradeep sequencing through metagenomics approach (n=4).
Conclusion: NAM alone was more potent HIV-1 activator than combination of MTIs, with potential of clinical use.
BIX01294; Chaetocin; Histone deacetylases inhibitor; Latency reversal agents; Methyltransferase inhibitors; Nicotinamide.
Nicotinamide activates latent HIV-1 ex vivo in ART suppressed individuals, revealing higher potency than the association of two methyltransferase inhibitors, chaetocin and BIX01294
Sadia Samer 1, Muhammad Shoaib Arif 2, Leila Bertoni Giron 3, Jean Paulo Lopes Zukurov 4, James Hunter 5, Bruna Teresa Santillo 6, Gislene Namiyama 7, Juliana Galinskas 5, Shirley Vasconcelos Komninakis 5, Telma Miyuki Oshiro 6, Maria Cecilia Sucupira 5, Luiz Mario Janini 4, Ricardo Sobhie Diaz 8
Chaetocin is a fungal metabolite that possesses a potential anti-inflammatory activity. Acute gout is a self-limiting inflammatory response to monosodium urate (MSU) crystals. However, the effect of cheatocin on gout has not been elucidated. In the study, we found that chaetocin could decrease MSU induced IL-1β secretion in bone marrow derived macrophages by several mechanisms, including inhibiting the activation of NLRP3 inflammasome. Chaetocin negatively regulated apoptosis-associated speck-like protein with a CARD domain oligomerization, and caspase-1 processing, key events during inflammasome activation. Furthermore, chaetocin restrain expressions of Hypoxia-inducible factor-1α and Hexokinase 2, mediators of glycolysis, which necessary for synthesis of pro-IL-1β during inflammasome priming. In vivo, chaetocin ameliorate MSU-induced arthritis, which showed as reduced local swelling and inflammatory cell infiltration. In MSU-induced peritonitis model, the peritoneal macrophages of chaetocin-pretreated mice showed significantly decreased mRNA levels of HIF-1α and NLRP3 related genes. These findings suggested that chaetocin has a potent anti-inflammatory effect against gout. More importantly, it is proposed that the inhibiting of glycolysis pathway would be a new avenue for the treatment of gout flare and other IL-1β related diseases.
Chaetocin; Gout; HIF-1α; IL-1β; Macrophage; NLRP3.
Chaetocin attenuates gout in mice through inhibiting HIF-1α and NLRP3 inflammasome-dependent IL-1β secretion in macrophages
Mian Wu 1, Mingliang Zhang 1, Yiwen Ma 1, Fengjing Liu 1, Si Chen 1, Junxi Lu 1, Haibing Chen 2
2019 Jul 30;
Physiological regulatory mechanisms of protein, RNA, and DNA functions include small chemical modifications, such as methylation, which are introduced or removed in a highly chemo-, regio-, and site-selective manner by methyltransferases and demethylases, respectively. However, mimicking or controlling these modifications by using labeling reagents and inhibitors remains challenging. In this Personal Account, we introduce our nascent interdisciplinary collaboration between chemists and biologists aimed at developing a basic strategy to analyse and control the methylation reactions regulated by protein methyltransferases (PMTs). We focus in particular on the structural development of chaetocin and S-adenosylmethionine to obtain PMT inhibitors and PMT substrate detectors.
detector; epidithiodiketopiperazine; inhibitor; protein methylation; proteomics.
Development of Chaetocin and S-Adenosylmethionine Analogues as Tools for Studying Protein Methylation
Yoshihiro Sohtome 1 2 3, Mikiko Sodeoka 1 2 3