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JMJD C is another JmjC
2021-12-27

JMJD1C is another JmjC domain protein discovered as a putative oncogene in shRNA screens in MLL-AF9-, HOXA9-, and AML1-ETO-driven AML 40, 41, 42. Depletion of JMJD1C decreased the frequency of LICs by inducing their differentiation and impaired the growth and establishment of leukemia in serial tran
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The following are the supplementary data related to this art
2021-12-27

The following are the supplementary data related to this article. Transparency document Introduction Hypoxia is a pathological process that causes abnormal changes in metabolism, function and morphological structure of tissue because of insufficient oxygen supply. It's reported that hypoxia w
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br Conflict of interest statement br Introduction
2021-12-27

Conflict of interest statement Introduction The Hedgehog (Hh) family of secreted protein signals patterns many tissues and structures during embryogenesis (Chiang et al., 1996, Dessaud et al., 2008, Ingham, 1993) and, post-embryonically, governs tissue homeostasis and regeneration by regulatin
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Further SAR was explored with the imidazole series
2021-12-27

Further SAR was explored with the imidazole series to achieve better enzyme inhibition activity (). In comparison to published earlier, replacing the amide with sulfonamide and reverse sulfonamide maintained the GSNOR inhibitory activity. It is clear that exchanging the phenyl ring (, and ) by thien
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G protein coupled receptors GPCRs constitute a
2021-12-27

G-protein coupled receptors (GPCRs) constitute a large family of 7 trans-membrane-spanning proteins that activate internal signal transduction cascades through binding to different ligands including neurotransmitters, peptides, and lipids [7]. This family of receptors has therapeutic potentials in t
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To date no studies have
2021-12-27

To date, no studies have demonstrated any effect of obesity or inflammation on GPR109A expression in adipose tissue. Our findings demonstrate that HFD-induced obesity decreases adipose tissue GPR109A gene expression. Contradictory to our findings in adipose tissue in vivo, Digby et al. report that e
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br FFA GPR was deorphanised as the second
2021-12-27

FFA4 GPR120 was deorphanised as the second receptor for long-chain fatty acids in 2005 [5]. Initial focus highlighted expression in the lower gut, the capacity of unsaturated fatty acids to promote release of the incretin glucagon-like peptide-1 (GLP-1) from the enteroendocrine cell line STC-1, a
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LDE225 Diphosphate Despite having potent activity and good s
2021-12-27

Despite having potent activity and good solubility, showed inhibitory activities against cytochrome P450 (CYP) 2C8, 2C9, and 2C19 with an IC value of less than 10 μM. In general, the specificity of the compound to the target should improve and the off-target risk such as CYP inhibitory activity shou
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br Materials and methods br
2021-12-27

Materials and methods Results Discussion A synoptic review of these cases will be given. In Case 1 the process presented in a photodistributed fashion in a 79-year-old woman; while the infiltrate was atypical, it was non-effacing with polyclonal molecular studies. The disease eventually res
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Next we designed substituents of the position
2021-12-27

Next, we designed substituents of the 6-position. Edge-to-face aromatic interaction between aromatic ring of ligand and Phe162B needed to be retained because the interaction seems to be important for tight binding. 3′-Position of the 6-phenyl group of directs to a hydrophilic space where W1 exists.
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Glial cells have emerged as important protagonists of
2021-12-27

Glial cells have emerged as important protagonists of the central nervous system (CNS) physiology (Chen and Swanson, 2003; Kettenmann and Verkhratsky, 2008; Parpura and Verkhratsky, 2012). As widely described in the literature, astrocytes regulate glutamatergic synapses by clearance of glutamate in
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One effective approach to fine tuning the lipophilicity prof
2021-12-24

One effective approach to fine-tuning the lipophilicity profile of FFA1 agonists is to ‘decorate’ the 3-phenylpropahoic quetiapine mechanism of action scaffold with polar heterocyclic moieties. Alternatively, this scaffold could be replaced with heterocyclic isosteres (as in Takeda’s compounds 1,2
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GPR which is also known as FFA receptor FFAR
2021-12-24

GPR40, which is also known as FFA receptor 1 (FFAR1 or FFA1), was identified as an orphan receptor in the search for novel human galanin receptor (GALR) subtypes in 1997. Using reverse pharmacology approaches measuring calcium transients, GPR40 were deorphanized and characterized as being activated
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Fatty acid amide hydrolase FAAH is a membrane bound enzyme
2021-12-24

Fatty methysergide amide hydrolase (FAAH) is a membrane-bound enzyme which releases arachidonic acid and ethanolamine by breaking amide bond of AEA. It also controls the cellular uptake of AEA, by creating and maintaining an inward concentration gradient leading to AEA-facilitated diffusion via a s
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Here we examined Meckel s cartilage
2021-12-24

Here, we examined Meckel's cartilage of mice where Setdb1 was knocked out only in neural crest derived Pam3CSK4 with the purpose of investigating the roles of Setdb1 in Meckel's cartilage, a supportive tissue for mandible formation. We observed enlarged Meckel's cartilage that was a result of incre
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