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Genomic studies have afforded new insight into the
2022-07-01

Genomic studies have afforded new insight into the influence of 2-Deoxyadenosine 5-diphosphate structure on GR binding. An important clue came from genome-wide mapping of chromatin structure using DNase I hypersensitive site sequencing (DNase-seq), and comparing the locations of open chromatin to G
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br Conclusion br Conflict of
2022-07-01

Conclusion Conflict-of-Interest JJH has collaborated with several different pharmaceutical companies during the last 30 years; is currently receiving speaker honoraria from NovoNordisk and MSD and is on advisory boards for NovoNordisk. The author is currently supported by an independent grant
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To evaluate the role of increased FPPS expression in paclita
2022-06-30

To evaluate the role of increased FPPS expression in paclitaxel-treated cells, we investigated the effects of FPPS on PHA-665752 progression. DNA content analysis showed that the number of cells accumulating in the G/M phase increased in a dose-dependent manner in paclitaxel-treated cells (A and B)
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br Rationale The present study
2022-06-30

Rationale The present study was motivated to get further insight into the molecular recognition processes of 2-alkyl(amino)ethyl-1,1-bisphosphonates taking compounds 12–14 as reference structures. We have recently demonstrated that TcFPPS inhibitors 12 and 13 bind to the allylic site of the enzym
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The proposed contributory role of endogenous histamine via a
2022-06-30

The proposed contributory role of endogenous histamine via activation of H1 receptor in the locomotor sensitization induced by caffeine was further ratified by H1 receptor antagonism during the induction phase and subsequently its effect on expression to locomotor sensitization induced by caffeine.
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H R antagonism can prevent seizure development
2022-06-30

H3R antagonism can prevent seizure development and improve working memory through the activation of histaminergic neurons (Huang et al., 2004, Zhang et al., 2003). In addition, we have recently found that H3R antagonism protects against ischemia-reperfusion injury via histamine-independent mechanism
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Introduction Histamine Imidazolyl ethylamine is an important
2022-06-30

Introduction Histamine [2-(4-Imidazolyl)-ethylamine] is an important mediator of many physiological and pathological processes including inflammation, gastric NECA secretion, neuromodulation, regulation of immune function, cell proliferation and differentiation, among others. Histamine exerts its
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GSK dimethylpiperidin yl butoxy phenyl piperidine carbonyl
2022-06-30

GSK-835726 (3-[4-[4-[4-[4-(3,3-dimethylpiperidin-1-yl)butoxy]phenyl]piperidine-1-carbonyl]naphthalen-1-yl]propanoic acid) is a dual H1/H3 receptor antagonist with the potential to be used in allergic rhinitis. Likewise GSK-1004723, the drug-likeness criteria have not been passed by this drug candida
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Based on pharmacophore modeling a good HDAC inhibitor
2022-06-30

Based on pharmacophore modeling, a good HDAC inhibitor has at least three sides/regions: the attachment side of the Zn2+ cofactor/HDAC active site (Zn2+ binding group/ZBG), hydrophobic cap (CAP) and linker containing connecting unit (CU) with electronegative groups (Mohan et al., 2011, Rossi et al.,
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The prevalence of hepatitis C virus HCV infection in p
2022-06-30

The prevalence of hepatitis C virus (HCV) infection in p.C282Y homozygotes in North America is unknown. We determined the prevalence of anti-HCV antibody and HFE genotype and serum ferritin (SF) associations in non-Hispanic white participants in the Hemochromatosis and Iron Overload Screening (HEIRS
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The mD gene obtained from Dr Dimiter
2022-06-29

The mD1.2 gene obtained from Dr. Dimiter S. Dimitrov was inserted into a pComb3X vector. The transcription and translation of pComb3X plasmid in cells is inhibited by rifampicin, which binds to bacterial DNA-dependent RNA polymerase. However, in the strain BL21 (DE3) expression system, there is over
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Moreover there is a third
2022-06-29

Moreover, there is a third possible GnRH agonist target – the endometrium. The human endometrium has been shown to express high levels of both GnRH and GnRH receptors (Maggi et al., 2016), and GnRH agonists affect the function of the urokinase-type plasminogen activator/plasminogen activator inhibit
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To confirm that these were
2022-06-29

To confirm that these were bona fide interactions, we investigated whether the potassium channel subunits or Tmem263 formed complexes with GLT-1 or DAT after immunoprecipitation. Lysates of HEK-293 cells previously cotransfected with HA-GLT-1 or HA-DAT, and either YFP-Kv7.3, YFP-Kv7.2 or YFP-Kv7.5 w
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br Introduction As is now well known obesity is major
2022-06-29

Introduction As is now well known, obesity is major risk factor for various diseases such as nonalcoholic fatty liver disease, cardiovascular disease, some cancers (McWilliams and Petersen, 2009), type-2 diabetes mellitus (Jakobsen et al., 2007), and hypertension (Aneja et al., 2004), among othe
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Up to now the research about the effect of PAs
2022-06-29

Up to now, the research about the effect of PAs on inhibiting carbohydrase activity in vitro or reducing blood sugar level in vivo was mainly reported in PAs from grape seeds, Lepisanthes alata (Malay cherry) leaves, sorghum, pomegranate, cranberry and persimmon (Banerji and Banerjee, 2016, Barrett
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