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Based on shared structural motifs DGK isoforms in multicellu
2020-08-03
Based on shared structural motifs, DGK isoforms in multicellular organisms are classified into five subtypes. Because most of these organisms express at least one DGK ortholog of each subtype, the five DGK subtypes appear to have distinct functions. Nine mammalian DGK isoforms have been identified (
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We examined the effects of H R
2020-07-31
We examined the effects of H1R, H2R and H3R agonists on MdHCLs. Although THA, an H1R agonist, was the most potent partial agonist of MdHCLB receptors among the three tested agonists, structural modifications resulted in drastic decreases in potency (Fig. 2). Biogenic amines, such as 5-HT, DA, OA and
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thip br Introduction Chemokine receptors interact with a gro
2020-07-31
Introduction Chemokine receptors interact with a group of peptide ligands of 8–10kDa and are indispensable for coordination of cell migration in diverse physiological processes such as development, angiogenesis, immune defence and neuroendocrine regulation. They belong to the largest rhodopsin fa
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Despite the evidence accumulated on the involvement of ETs a
2020-07-31
Despite the evidence accumulated on the involvement of ETs and their receptors in many pain states, their potential contribution to nociception following SCI has not yet been investigated. Hence, the present study was designed to assess the roles exerted by ETAR and ETBR in neuropathic pain after SC
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In our case series eyes with
2020-07-31
In our case series, eyes with retinal degeneration or normal fundus unexceptionally demonstrated structural and functional photoreceptor abnormalities corresponding to the funduscopic and/or perimetric lesions, even though the RPE layer was intact (Figure 5). By stark contrast to eyes with multiple
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Simultaneous to the deorphanization of EBI we provided a cha
2020-07-31
Simultaneous to the deorphanization of EBI2, we provided a characterization of a non-peptide inverse agonist (coined GSK682753A) that suppressed the apparent constitutive activity of the receptor [16]. Here we investigate the antagonistic properties of this compound and find that it potently suppres
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Osteoporosis or porous bone is the common metabolic bone
2020-07-31
Osteoporosis or porous bone is the common metabolic bone disorder. It has characterized by a systemic reduction of bone mineral, bone volume, and strength [8]. Osteoporosis is a bone disease in which bones become fragile by a systemic reduction of bone mass and strength and also is controlled by an
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br Acknowledgments This work was
2020-07-31
Acknowledgments This work was financially supported through grantsfrom National Natural Science Foundation of China (No. 21402105), and Shenzhen Municipal government SZSITIC (JCYJ20160301153753269). Introduction Due to their unique physical, electrical, and optical properties, ultrasmall fluo
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Fmoc-Ser(tBu)-OH Chemogenomic profiling reviewed in Nijman i
2020-07-31
Chemogenomic profiling (reviewed in Nijman, 2015) is another way to identify drug MoA that have been neglected for the study of antimalarials. In a narrow sense, this approach entails perturbing the activities of different Fmoc-Ser(tBu)-OH using forward or reverse genetic methods. The cell lines wi
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Atazanavir Here we have explored the mechanisms
2020-07-31
Here, we have explored the mechanisms of Emi2 inhibition by Cdk1 (as well as Emi2 upregulation by Mos) using Xenopus egg extracts. Our results show that multiple distinct kinases, including Atazanavir B1-Cdk1 itself, bind to the N-terminal Cdk1 sites of Emi2 and phosphorylate other critical sites to
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A flexible synthetic route was employed in the synthesis of
2020-07-30
A flexible synthetic route () was employed in the synthesis of these series of compounds. Thus, synthesis of intermediate was carried out by methylation of 2-hydroxy-5-nitrobenzoic glucokinase , subsequent reduction of the nitro group to give the corresponding aniline and coupling of this aniline wi
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We show here that Shp binds to phosphotyrosine
2020-07-30
We show here that Shp-2 binds to phosphotyrosine-740 in the cytoplasmic domain of DDR1 in a collagen-dependent manner (Figs. 3A and 4A). The peptide sequence ISpYPML neighboring tyrosine 740 matches well with the immuno-receptor tyrosine-based inhibitory motif (ITIM)-consensus sequence [I/V/L]XpYXX[
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br Conflict of interest statement br Renal
2020-07-30
Conflict of interest statement Renal cell carcinoma is the third most common urogenital tumor disease with an estimated incidence of 51,000 cases per year in the United States. Although RCC appears to be curable at nonadvanced stage, locally advanced or lymph node positive tumors are likely to
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Henderson et al have demonstrated that montelukast blockade
2020-07-30
Henderson et al. have demonstrated that montelukast blockade of CysLT1 receptors improves airway remodeling, including airway goblet cell metaplasia, smooth muscle cell layer thickening, and subepithelial fibrosis in a mouse model of asthma. The histological findings of this study revealed a thicken
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what is c2 With an intention to develop a
2020-07-30
With an intention to develop a persuasive model for the screening of potent molecules as Cyclin dependent kinase inhibitors, 2D QSAR studies using CANVAS and 3D QSAR studies were carried out on 230 CDK4 inhibitor molecules with pyrido [2,3-d]pyrimidine moiety. By using CANVAS, several statistical an
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